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Pacijentica u dobi od 54 godine bila je primljena s jakim bolovima u gingivi i obraznim sluznicama. Oralnim pregledom uočene su plamenocrvene desni i ulcerirane lezije s bijelim strijama prekrivene pseudomembranama na objema obraznim sluznicama. Bolovala je od hipertenzije, dislipidemije, subkliničkog hipotiroidizma i artritisa. Bila je pod terapijom atorvastatina, hidroklorotijazida, valsartana, levotiroksina i nesteroidnih protuupalnih lijekova (NSAID). Oralne lezije pacijentice blago su se smanjile nakon terapije kremom s pimekrolimusom, 0,1-postotnim triamkinolon-acetonidom u orabazi i injekcijama. Nakon što je Diclofenac zamijenjen Tenoxicamom i oralne lezije tretirane različitim steroidima, stanje se znatno poboljšalo. Na temelju biopsije bukalne sluznice dijagnosticiran je lihen planus. Patch-test pokazao je pozitivnu reakciju na živu, zlatni natrijev tiosulfat i platinu. Nakon godinu dana na lijevoj obraznoj sluznici pojavila se crvena, okrugla papilomatozna lezija. Patohistološkim nalazom potvrđeno je da je riječ o nespecifičnom ulkusu s kroničnom upalom. Lezije su buknule nakon zamjene amalgamskih ispuna u zubima krunama. Nakon terapije ugljično-dioksidnim laserom, lezije su se donekle smanjile. Direktna i indirektna imunofluorescencija lezija bila je negativna. Ovaj prvi prikaz slučaja pokazuje da tijekom palijativne terapije refraktorne oralne lihenoidne lezije snažnim topikalnim steroidima sedam godina nije bilo nuspojava. U ovom slučaju CO2-laser može biti alternativna terapija., A 54-year-old female presented with severe pain on the gingiva and buccal mucosa. Oral findings revealed generalized fiery red gingiva, ulcerative with white striae covered by pseudo-membranes on both buccal mucosae. She had hypertension, dyslipidemia, subclinical hypothyroidism and arthritis. She was treated with atorvastatin, hydrochlorothiazide, valsartan, levothyroxine and non-steroidal anti-inflammatory drug (NSAIDs). Her oral lesions were a slight improvement from a previous treatment with pimecrolimus cream, triamcinolone acetonide 0.1% orabase and injection. After diclofenac was replaced with tenoxicam and oral lesions were treated with various topical steroids, the lesions showed marked improvement. The biopsy from the buccal mucosa revealed oral lichen planus. Patch test showed positivity to mercury, gold sodium thiosulfate and palladium. One year later the left buccal mucosa showed red, round papillomatous-like lesions. The histopathological report showed a non-specific ulcer with chronic inflammation. The lesions flared up after replacing amalgam with crowns. After CO2 laser treatment, the lesions showed some improvement. Direct and indirect immunofluorescence of the lesions proved to be negative. This first case report showed that the palliative treatment of refractory oral lichenoid lesions with potent topical steroids for 7 years had no side-effects. CO2 laser can be an alternative treatment of refractory lesion in this case.

In this work it is shown that when a carbon paste electrode, CPE, is modified with a β-cyclodextrin polymer, the tenoxicam oxidation becomes an adsorption controlled process due to formation of a surface inclusion complex with the β-CD molecules comprising the surface of the polymer. It was found that such surface inclusion complex can be formed independently of the tenoxicam predominant species, Tenox’, in the aqueous solution namely: H 2 Tenox + , HTenox or Tenox − , depending on the solution pH. The electrochemical quantification of the thermodynamic constant of the equilibrium Tenox’ + β-CD (polymer) = Tenox’-β-CD (polymer) was estimated as log K incl. = 4.26 ± 0.01. Furthermore, from the analyses of the experimental voltammograms according with Laviron's equation for an irreversible surface reaction [E. Laviron, J. Electroanal. Chem. 52 (1974) 355-393] it is shown that the surface concentration, Γ R , of tenoxicam increases as its concentration in solution does, reaching a maximum value of 1.51 × 10 −10 mol cm −2 at 64 μM.

Temporomandibular joint disorders affect a big portion of the population. There are a variety of treatment methods currently in use. Conservative treatment modalities are followed by more invasive approaches like arthrocentesis or arthroscopy. The aim of the study is to compare the effects of intra-articular tenoxicam injection and arthrocentesis plus viscosupplementation on patients in which a previous arthrocentesis plus viscosupplementation has failed to relieve pain and restore function. The study group consists of 18 TMJs in 16 patients (15 female and 1 male) and the patients were randomly divided into two groups as the arthrocentesis plus viscosupplementation group (n: 8) and tenoxicam injection (n: 10). 20 mg of tenoxicam was injected to the upper compartments of 10 joints without arthrocentesis. The other 8 joints were treated with a second arthrocentesis and sodium hyaluronate injection. VAS scores and maximum mouth opening with and without assistance were recorded in the post operative first week, first month and third month. The results show that there is little benefit in using relatively conservative methods once an arthrocentesis together with viscosupplementation has failed to relieve the patients pain. It is concluded that more invasive procedures should be considered for the patients who do not benefit from arthrocentesis.

In the present study efforts have been made to prepare sustained release matrix tablets of Lornoxicam. Matrix tablets were prepared by direct compression method by using Hydroxypropyl methyl cellulose K15 (HPMC- K15), Ethyl cellulose (EC) and Sodium carboxy methyl cellulose (Na-CMC) as polymers in different concentrations. A 3-factor 3- level Box-Behnken statistical design was used as an optimization tool having total of 17 experimental runs with 5 central points. All three polymers were selected as independent variables while %age drug release at various time intervals and hardness were used as dependant variables. In vivo studies were conducted on human plasma using Tenoxicam as internal standered. All the detections were made on SYKNM HPLC. Foriour Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetery (DSC) studies were conducted and no chemical interaction was found between drug and polymers. The drug release mechanism was mainly governed by non-fickian (anomalous) diffusion and zero-order (case II) transport diffusion. Regression analysis was performed on dissolution data obtained with the selected response variables and polynomial models were constructed. Polynomial models were further validated using one way ANOVA and results indicated that all the polymers used have significant effect on selected response (p>0.05). Contour plots and three dimensional response surface curves were drawn. In- vivo studies were conducted on two tablet formulation indicating slow and sustained release of the drug from matrix. From Behnken design it is possible to successfully formulate and optimize Lornoxicam sustained release matrix tablets with three polymers (HPMC- K15, EC and Na-CMC) in combination.

The objective of this study was to improve the dissolution and subsequently the therapeutic efficacy of poorly water soluble BCS class-II drugs meloxicam and tenoxicam, by lipid semi solid matrix (SSM) systems filled in hard gelatin capsules by liquid fill technology. The present research involved preparation of SSM formulations using Gelucire 44/14 as a carrier due to its self emulsifying, wetting and hydrophilic properties. The SSM capsules were characterized by assay, in vitro dissolution studies, moisture uptake, FTIR and DSC. The optimized formulations were also evaluated for their in vivo anti inflammatory activity in rat model. Six to ten fold enhancement in vitro drug release, in both acidic and basic media, was obtained with formulations containing drug to carrier in 1:6 ratio. The absence of drug peak in DSC scans indicated complete dissolution of the drug in carrier, while IR revealed no chemical interaction of pure drug and Gelucire 44/14. The optimized SSM formulations of meloxicam and tenoxicam showed a rapid decrease in paw edema with a significant increase in anti-inflammatory activity. The SSM formulations were successful in providing rapid release of drugs with improved dissolution and in vivo anti-inflammatory activity by liquid fill technology in hard gelatin capsules.

Aim. Postoperative pain is a major problem in patients who have undergone surgery of the shoulder joint. We retrospectively evaluated 26 patients in whom a subacromial catheter had been placed for postoperative pain management following shoulder surgery. Method. Infusion of local anesthetics and/or opioids through a subacromial catheter, placed at the end of the procedure, was started after surgery. This catheter was kept in place for 24 hours. The patients’ pain was evaluated by using a visual analog scale (VAS). Patients with a VAS score greater than 7 were given meperidine, 0.5 mg/kg i.v., those with a score of 5-7 received tenoxicam, 20 mg i.v., and patients who continued to have a score of >5 at the end of 30 minutes were given paracetamol, 1 g i.v. as an additional analgesic injection. Results. None of the patients had a need for meperidine after 24 hours of surveillance. Seven patients with a VAS score of 5-7 were given tenoxicam, while seven patients, all female, who had continuing pain, received paracetamol. Conclusion. A subacromial catheter, which does not cause adverse effects or complications, is easy to apply and allows effective analgesia, can be used with confidence in the postoperative pain management of patients undergoing shoulder surgery. The need for supplementary analgesia in women only is significant, indicating the role of the patient’s sex in pain perception.

Summary Esophageal stricture, one of the important complications of corrosive esophagus, develops following edema and granulation tissue that forms during and after the inflammatory reactions. Tenoxicam, a non-steroid anti-inflammatory drug with a long half-life, prevents various leukocyte functions including phagocyte and histamine secretion by inhibiting prostaglandin synthesis and removes various oxygen radicals in the region of inflammation. We designed this as a histopathological study using tenoxicam in rats for which we created a corrosive esophagus model. After necessary authorizations were obtained, the study was performed in Canakkale 18 Mart University experimental animal laboratory. Twenty-four Wistar albino rats, weighing 220–240 g, were used for the experiment. Experimental animals were randomized into three groups: tenoxicam group (group T, n:8), control group (group C, n:8), and sham group (group S, n:8). Tenoxicam 0.5 mg/kg/day was administered to animals in group T, where esophageal burn was developed experimentally, 5 mg/kg 0.9% NaCL was administered i.p. to rats in group C for 15 days, once in 24 hours. No procedure was applied to rats in group S. After 15 days, all animals were sacrificed under general anesthesia and their esophagi were extracted. As a result of histopathological evaluation, inflammation and fibroblast proliferation was not observed in rats in the sham group (group S). Intense inflammation was observed in six rats (6+/2−) in the control group, and fibroblast proliferation was observed as 5+/3−. And in treatment groups, inflammation was evaluated as 3+/5−, and fibroblast proliferation as 3+/5−. In our study, histopathologic damage score was higher in the control group (P < 0.005). We deduce that tenoxicam can be useful in the treatment of caustic esophageal injuries in the acute phase, but think that these drugs require further researches and clinical studies before routine clinical use.

Background/Aims: The present study investigates the effects of pregabalin (PGB), acetaminophen (ACET) and tenoxicam (TNX) administration in somatic and visceral nociception, using the tail flick test and the writhing test in mice. Methods: In the tail flick test, the substances were administered orally and the latency time response was recorded 15, 30, 60, 90 and 120 min after administration. In the writhing test, pain responses were scored every 5 min during a 30-min period after intraperitoneal injection of diluted acetic acid. Results: Our study demonstrated that oral administration of the combination PGB-ACET resulted in a stronger increase of latency reaction - statistically significant after 15 min compared to TNX and after 30 min compared to PGB in tail flick test. In the writhing test, the combination PGB-ACET, but also PGB-TNX, resulted in a stronger decrease of writhe numbers - statistically significant compared to the effects of the separate administration of each substance. This decrease was more intense in animals treated with the combination PGB-ACET than with PGB-TNX. Conclusion: These results suggest an antinociceptive activity which may be a consequence of the synergic action of the substances.

Background The aim of the present study was to compare the effects of preemptive intravenous tenoxicam and methylprednisolone administrations on extraction of impacted third molars. Material/Methods This was a placebo-controlled, randomized, double-blind, clinical trial. A total of 60 adult patients ages 18–40 years with the complaints of impacted third molar teeth were included in the study. Results The postoperative swelling ratios (p

Objectives In this study, we aimed to compare the postoperative analgesic efficiency of an ultrasound-guided fascia iliaca compartment block and a 3 in 1 block in patients who underwent hip prosthesis surgery as a result of hip fracture. Methods With approval from the local ethics committee, 70 patients, aged 20 to 80, undergoing hip prosthesis surgery under elective conditions were included in this randomized, prospective, controlled study. They were informed of the patient-controlled analgesia (PCA) device and visual analog scale (VAS). All patients were separated randomly into three groups. Anaesthesia induction was standardized for all groups. An ultrasound guidance fascia iliaca compartment block (FICB) was applied to the first group before anaesthesia induction. For the second group, a 3 in 1 block was applied, while for the control group no block was applied. After incision on all patients, 20 mg tenoxicam and 1 mg/kg tramadol were injected intravenously. Following surgery, IV tramadol PCA was begun on all patients routinely. In our study, the presence of cortisol and ACTH levels, hemodinamical parameters, nausea and sedation were determined. Results We observed a decrease in VAS values and opioid consumption, no adverse effects on nausea and sedation, and a suppression of stress hormones in both the ultrasound-guided FICB and 3 in 1 block groups. Conclusion We believe that the safe and efficient application of the ultrasound-guided 3 in 1 block and the FICB is necessary in multimodal analgesic treatment in order to enable postoperative analgesia in hip prosthesis surgery.

This study investigates potentials of solid lipid nanoparticles (SLN)-based gel for transdermal delivery of tenoxicam (TNX) and describes a pharmacokinetic-pharmacodynamic (PK-PD) modeling approach for predicting concentration-time profile in skin. A 23 factorial design was adopted to study the effect of formulation factors on SLN properties and determine the optimal formulation. SLN-gel tolerability was investigated using rabbit skin irritation test. Its anti-inflammatory activity was assessed by carrageenan-induced rat paw edema test. A published Hill model for in vitro inhibition of COX-2 enzyme was fitted to edema inhibition data. Concentration in skin was represented as a linear spline function and coefficients were estimated using non-linear regression. Uncertainty in predicted concentrations was assessed using Monte Carlo simulations. The optimized SLN was spherical vesicles (58.1 ± 3.1 nm) with adequate entrapment efficiency (69.6 ± 2.6%). The SLN-gel formulation was well-tolerated. It increased TNX activity and skin level by 40 ± 13.5, and 227 ± 116%, respectively. Average Cmax and AUC0-24 predicted by the model were 2- and 3.6-folds higher than the corresponding values computed using in vitro permeability data. SLN-gel is a safe and efficient carrier for TNX across skin in the treatment of inflammatory disorders. PK-PD modeling is a promising approach for indirect quantitation of skin deposition from PD activity data.

From experimental (spectro-electrochemical) and theoretical (DFT) studies, the mechanisms of tenoxicam deprotonation and electrochemical oxidation were assessed. From these studies, new insights on the nature of the ampholitic species involved during tenoxicam's deprotonation in aqueous solution are presented; see scheme A. Moreover, it is shown that, after the analysis of two different reaction schemes that involve up to 10 different molecules and 12 reaction paths, the electrochemical oxidation of tenoxicam, yields two non-electroactive products that are predominately formed by its fragmentation, after the loss of two electrons. The nature of these fragments was further confirmed by a chromatography study.

In patients who are hospitalized for surgery, anxiety disorders are frequently observed. Anxiety affects the patient’s perception of postoperative pain and has a negative impact on recovery from anesthesia. This study attempted to compare the effect of preoperative anxiety on postoperative pain control and recovery from anesthesia in patients undergoing laparoscopic cholecystectomy. A total of 80 patients were enrolled who were undergoing laparoscopic cholecystectomy. Demographic characteristics of the patients were recorded. Beck’s anxiety inventory (BAI) was administered to the patients: patients with anxiety were included in the high-anxious patient group (group H) and patients without anxiety were enrolled in the low-anxious group (group L). Duration of surgery, duration of anesthesia, extubation time, and adverse effects were recorded. During the postoperative period, patient-controlled analgesia with tramadol was used for pain control. Visual analog scale (VAS) scores and tramadol consumption of all patients were recorded. Among all patients, 31 (38.75 %) patients had preoperative anxiety, and significant correlation was found between the days of hospitalization and preoperative score of BAI. In group L, extubation time, the time for the modified Aldrete score to reach 9, was seen as significantly shorter and fewer postoperative side effects were determined. Also in group L, postoperative VAS score and tramadol consumption were significantly lower, and less tenoxicam was needed. A high preoperative anxiety level negatively affects recovery from anesthesia and control of postoperative pain. In this patient group, the increased need for postoperative analgesia must be adequately met.

The objective of the present study was to develop and evaluate thermoreversible in situ gelling and mucoadhesive liquid suppositories which are liquid at room temperature but forms a gel at body temperature to improve patient compliance and systemic absorption of tenoxicam which is a non-steroidal anti-inflammatory drug (NSAID), exhibited potent anti- inflammatory, analgesic, and antipyretic activity and licensed for use in rheumatic disease and other musculoskeletal disorders. The thermosensitive-mucoadhesive liquid suppositories were prepared by a cold method using poloxamers (P407 and P188) which are used for their temperature sensitive gelation property, and Hydroxy Propyl Methyl Cellulose (HPMC) which is a neutral and swellable polymer, and it was used to modulate gel strength and to impart mucoadhesive force to tenoxicam suppository bases. Sixteen formulations were prepared by the cold method using different concentrations of P407 and/or P188 with or without HPMC. The physicochemical properties of the liquid suppository bases were characterized by their gelation temperature, gel strength, mucoadhesive force, and In-vitro release rate of tenoxicam from prepared liquid suppositories was studied and compared with that from conventional suppository (Epicotil). Only seven formulations showed optimum gelation at body temperature and intermediate gel strength, so they were subjected to the dissolution test. The analgesic effect of tenoxicam-poloxamer gel system was also studied in rats. The results showed that, gelation temperature decreased upon incorporation of the mucoadhesive polymer in the poloxamer solution. Also polymer addition increase the gel strength and the mucoadhesive force of the prepared solutions. The release rate of tenoxicam from liquid suppository was higher than that from conventional suppositories. Analysis of release mechanism showed that the release of tenoxicam from the prepared suppositories was Fickian diffusion. Also the results of in-situ evaluation showed that, the suppositories had a significant analgesic effect (p < 0.05). Among the various formulations examined, the formulations (tenoxicam/P407/P188 (1/25/10 % w/w)) and (tenoxicam/P407/P188/HPMC (1/25/5/1 % w/w)) exhibited the appropriate gelation temperature, gel strength, mucoadhesive force, acceptable drug release and prolonging the latency of the nociceptive response in rats. These results suggested that in situ gelling liquid suppository with tenoxicam, poloxamers and mucoadhesive polymer (HPMC) was a physically safe, convenient, and effective rectal dosage form.

Tenoxicam is one of the potent non-steroidal anti-inflammatory drugs (NSAIDs), which is used clinically in the treatment of rheumatoid arthritis. Like other NSAIDs, Tenoxicam also suffers from the drawback of being associated with gastrointestinal side effects. Further, transdermal penetration of this drug is very poor, which circumvents the use of transdermal route. The main objective of this study is to exploit the concept of ultradeformable vesicles to increase the transport of Tenoxicam through transdermal route, and also to present it as a possible replacement for the oral NSAID therapy for rheumatoid arthritis. Three concentrations (5%, 15% and 25%) of three different surfactants (Tween-80, Span-80 and sodium desoxycholate) were used along with soya lecithin to prepare the ultradeformable vesicles. Among nine different types of vesicles, T3 vesicles (with 25% Tween-80) were found to have shown the smallest size (82.80 ± 0.74 nm), highest release in 24 h (98.01 ± 0.33%) and highest deformability (31....

Inhibition performance of Lornoxicam & Tenoxicam against corrosion of carbon steel in 1 MH 2 SO 4 solutions was investigated by weight loss, potentiodynamic polarization and electrochemicalimpedance spectroscopy (EIS) measurements. The inhibition efficiency increased with increasinginhibitor’s concentration, but decreased with increase in temperature. Potentiodynamic polarizationcurves showed that, the inhibitors were of mixed type. The apparent activation energy ( ) andother thermodynamic parameters for the corrosion process have also been calculated and discussed.The inhibition of carbon steel corrosion is due to the adsorption of the inhibitor molecules on thesurface, which follows Temkin adsorption isotherm. The mechanism of inhibition was discussed inthe light of the chemical structure of the undertaken inhibitors.Keywords: Acid corrosion, Carbon steel, EIS, Polarization Received March 11, 2013 : Accepted April 8, 2013 1. Introduction Acid solutions are widely used in various industrialprocesses such as oil well acidification, the petro-chemical processes, acid pickling and acidic clean-ing

Amac: Bu calismada septoplasti sonrasi agri yonetiminde intravenoz parasetamol ve tenoksikamin etkinligi karsilastirildi. Hastalar ve Yontemler: Bu randomize kontrollu calismaya Mayis 2008 Ocak 2009 tarihleri arasinda klinigimizde septoplasti yapilan 40 eriskin erkek hasta (ort. yas 21.7 yil; dagilim 19-24 yil) dahil edildi. Hastalar her bir grupta 20 kisi olacak sekilde rastgele iki gruba ayrildi. Ameliyat sonrasi analjezi, birinci grupta (parasetamol grubu) her alti saatte bir intravenoz 1 gr parasetamol ile; ikinci grupta (tenoksikam grubu) ise, ilk 24 saatte intravenoz tek doz 20 mg tenoksikam ile saglandi. Gorsel analog olcegi (GAO), ameliyat sirasinda ve ameliyat sonrasi 30. dakikada, 1, 2, 6, 12. ve 24. saatlerde agri duzeyini degerlendirmek icin kullanildi. Ameliyat sonrasi komplikasyonlar her iki grupta da kaydedildi. Bulgular: Gruplar arasinda ameliyat sirasi agri skorlari acisindan anlamli fark yoktu (p=0.47). Gorsel analog olcegi skoru parasetamol grubunda 30. dakika (p=0.018), 1, 2. ve 6. saatlerde tenoksikam grubundan anlamli olarak daha dusuktu (sirasiyla p=0.0001; p=0.001; p=0.04). Sonuc: Septoplasti ameliyati sonrasi erken donemde, orta duzey agri mevcuttur. Bu durum ise analjeziklerle onlenebilmektedir. Anahtar Sozcukler: Lokal; parasetamol; ameliyat sonrasi agri; septoplasti; tenoksikam. Objectives: This study aims to compare the efficacy of intravenous paracetamol and tenoxicam in the management of postoperative pain following septoplasty. Patients and Methods: Between May 2008 and January 2009, 40 male adults (mean age 21.7 years; range 19 to 24 years) who underwent septoplasty in our clinic were included in this randomized controlled study. Patients were randomly divided into two groups, including 20 in each group. Analgesia was achieved through intravenous paracetamol 1 g every six hours in the first group (paracetamol group) and intravenous tenoxicam 20 mg at a single dose within the first 24 hours in the second group (tenoxicam group). Visual analog scale (VAS) was used to assess the pain severity preoperatively and at 30 minutes, 1, 2, 6, 12 and 24 hours postoperatively. Postoperative complications for both groups were also recorded. Results: There was no significant difference in intraoperative pain scores between the groups (p=0.47). The VAS scores at 30 minutes (p=0.018), 1, 2 and 6 hours were significantly lower in paracetamol group, compared to tenoxicam group (p=0.0001; p=0.001; p=0.04, respectively). Conclusion: Early postoperative moderate pain is accompanied following septoplasty. This can be prevented by using analgesics.

Objective To detect the effect of intra-peritoneal instillation of local anesthetic with or without NSAIDs on pain relief after gynecological laparoscopy. Methods Seventy five patients scheduled for laparoscopy were included in the study and randomly divided into three groups. At the end of the laparoscopic procedure, 100 mL normal saline in the first group, or 100 mL normal saline contains 200 mg lidocaine in the second group, or 100 mL normal slaine containing 200 mg lidocaine and 20 mg tenoxicam in the third group were splashed into the pelvis by the surgeon. Post-operative pain were monitored and compared. Results The incidence and severity of immediate postoperative shoulder pain reduced from 44% of patients scoring 2-5 in saline group to 16% scoring 2-3 in lidocaine group and 8% scoring 2-3 in lidocaine-tenoxicam group. Compared with saline group, abdominal pain scores were significantly lower in lidocaine group and lidocaine-tenoxicam group over 24 hours after surgery. At 12 and 24 hours after surgery, abdominal pain scores were significantly reduced in lidocaine-tenoxicam group compared with lidocaine group. No pain on deep respiration was reported in 84%, and 68% in lidocaine-tenoxicam and lidocaine groups respectively compared to 12% in those in the saline group. The mean time to first request for analgesia was increased from (2.3 ±1.9) hours in saline group to (4.4 ± 2.4) hours in lidocaine group and to (8.3 ± 10.2) hours in lidocaine-tenoxicam group. Conclusion Intraperitoneal balanced analgesia (local anesthetics ± NSAIDS) is a simple and safe technique for analgesia following gynaecological Laparoscopy.

Niosomes are now widely studied as an alternative to liposomes because they alleviate the disadvantages of liposomes, such as chemical instability, variable purity of phospholipids and high cost. The aim of this work is to formulate and evaluate niosomes as carriers for topical delivery of Tenoxicam, as an anti-inflammatory drug, test their stability and improve their anti-inflammatory effect through niosomal encapsulation with objectives of prolonging its action and avoiding its most side effects. Incorporation of Tenoxicam - entrapped niosomes into gelling agents and increasing their concentrations resulted in a marked decrease in amount of drug permeated from the gel through cellulose membrane and rabbit skin. Polymers used as gelling agents are Carbopol 934 and Carboxy Methyl Cellulose sodium (CMC Na). It was found that permeated amount of Tenoxicam decreased with increasing either concentration of Carbopol 934 from 1% to 2% or concentration of CMC Na from 2% to 4%. Amount of Tenoxicam permeated from cellulose membrane are significantly high compared to the amounts permeated across the skin (p

a b s t r a c t Purpose: The purpose of this work was to assess the colloidal stability of novel milk-based formulations. Methods: Milk-based formulations were prepared in situ by adding into milk alkaline- or ethanolic-drug solutions containing an array of drugs namely; ketoprofen, tolfenamic acid, meloxicam, tenoxicam and nimesulide, mefenamic acid, cyclosporine A, danazol and clopidogrel besylate. The produced formulations were characterized by means of dynamic lightscattering, � -potential studies, atomic force microscopy, fluorescence spectroscopy, Raman spectroscopy complemented with ab initio calculations and stability studies. Results: The presence of the drugs did not induce significant changes in most cases to the particle size and � -potential values of the emulsions pointing to the colloidal stability of these formulations. Raman spectroscopy studies revealed interactions of the drugs and the milk at the intermolecular level. Comple- mentary analysis with ab initio calculations confirmed the experimental observations obtained by Raman spectroscopy. Finally the produced drug containing alkaline/ethanolic solutions exhibited stability over a period of up to 12 months. Conclusions: The current data demonstrate that milk is a promising drug carrier. © 2013 Elsevier B.V. All rights reserved.

Aim. To study coagulation and vascular-platelet haemostasis in patients with rheumatoid arthritis (RA) and coronary heart disease (CHD), who receive various non-steroidal anti-inflammatory drugs (NSAID) in combination with low doses of aspirin. Material and methods. The study included 79 patients (59 women and 20 men; mean age 61,0 years; mean disease duration 8,5 years) with confirmed RA diagnosis. All participants received disease-modifying anti-inflammatory therapy and NSAID, as well as standard pharmacological CHD therapy. The parameters of coagulation and vascular-platelet haemostasis were compared by the type of administered NSAID (diclofenac, tenoxicam, nimesulide, or meloxicam). In total, 40 patients with increased platelet aggregation but no previous antiaggregant therapy were administered aspirin (100 mg/day). Platelet aggregation was reassessed at Day 7–8 of aspirin therapy. The control group included 25 untreated healthy men (mean age 55 years). Results. Activated coagulation haemostasis was observed in 58,2% of patients with RA and CHD, as manifested in increased levels of fibrinogen, soluble fibrin monomer complexes (SFMC), factor XII-dependent fibrinolysis, and von Willebrand factor, compared to controls. The therapy with most NSAID was linked to similar changes in coagulation haemostasis. The patients receiving diclofenac, nimesulide, and meloxicam demonstrated an activation of vascular-platelet haemostasis, as manifested in a significant increase of spontaneous platelet aggregation and ADPinduced platelet aggregation, compared to controls. Among patients receiving tenoxicam, there was a tendency towards a reduction in ADP-induced platelet aggregation (aspirin-like effect). Among patients already receiving diclofenac, nimesulide, or meloxicam, aspirin administration typically resulted in reduced platelet aggregation. In total, 42,4% of the patients did not respond to aspirin therapy. Conclusion. Patients with RA and CHD who receive NSAID are also in need of antiaggregant therapy. The latter should be administered under control of vascularplatelet haemostasis, as in a substantial proportion of these patients (42,4%), aspirin effectiveness is not adequate.

Background: Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID) licensed for use in rheumatic disease and other musculoskeletal disorders in the UK, and is widely available in other countries worldwide. This review sought to evaluate the efficacy and safety of oral tenoxicam in acute postoperative pain, using clinical studies of patients with established pain, and with outcomes measured primarily over 6 hours using standard methods. This type of study has been used for many decades to establish that drugs have analgesic properties. Objectives: To assess the efficacy of single dose oral tenoxicam in acute postoperative pain, and any associated adverse events. Search strategy: We searched The Cochrane Library (Issue 1, 2009), MEDLINE (March 2009); EMBASE via Ovid (March 2009); the Oxford Pain Relief Database. Selection criteria: Randomised, double-blind, placebo-controlled clinical trials of oral tenoxicam for relief of acute postoperative pain in adults. Data collection and analysis: Two review authors independently assessed trial quality and extracted data. The area under the "pain relief versus time" curve was used to derive the proportion of participants with tenoxicam experiencing least 50% pain relief over 4 to 6 hours, using validated equations. The number needed to treat to benefit (NNT) was calculated using 95% confidence intervals (CI). The proportion of participants using rescue analgesia over a specified time period, and time to use of rescue analgesia, were sought as additional measures of efficacy. Information on adverse events and withdrawals was also collected. Main results: Not one of sixteen studies identified by the searches and examined in detail studied oral tenoxicam in patients with established postoperative pain and therefore no results are available. Authors' conclusions: In the absence of evidence of efficacy for oral tenoxicam in acute postoperative pain, its use in this indication is not justified at present. Because trials clearly demonstrating analgesic efficacy in the most basic of acute pain studies is lacking, use in other indications should be evaluated carefully. Given the large number of available drugs of this and similar classes which are effective, there is no urgent research agenda for this particular drug. Copyright © 2009 The Cochrane Collaboration. Published by John Wiley and Sons, Ltd.

Nonsteroid (steroid olmayan) antienflamatuvar ilaçlar (NSAEİ'ler) aspirin ailesindeki ilaçları da kapsayan çok geniş bir ilaç grubudur. Çeşitli artrit türlerinde inflamasyonu azaltmak ve ağrı, şişlik ve katılığı kontrol altına almak için reçete edilirler. Narkotik olmayan analjeziklere göre bu grup ilaçların farmakolojik etki profiline uygun düşen bir adla non-steroidal (steroid olmayan) antienflamatuvar ilaçlar (NSAEİ'ler) veya kısaca antienflamatuvar analjezikler denilmektedir. Nonsteroid antienflamatuar ilaçların özellikle de oksikamların iyonlaşma sabitlerinin birkaç uygun yöntem ile tam olarak tayini, etki mekanizmalarının anlaşılmasında ve biyoyararlanabilirlikleri açısından oldukça önemlidir. Farmakolojik açıdan bu kadar önemli olan bu ilaç grubunun, iyonlaşma sabitlerinin doğru ve hassas bir şekilde tayin edilmesi de büyük bir önem arz etmektedir. Bu tez kapsamında öncelikle NSAEİ'lerin organik çözücü-su ortamlarında florimetrik parametreleri (uyarma ve emisyon dalga boyu, floresans şiddeti) belirlenmiştir. Florimetrik parametrelerin belirlenmesi için, öncelikle saf asetonitril, metanol, DMF, THF ve su içerisinde, daha sonra %10 - %50 organik çözücü su karışımlarında ilaç etken maddelerinin uygun derişimlerdeki çözeltileri hazırlanarak, uyarma dalga boyları 10' ar nm aralıklarla değiştirilip emisyon spektrumları alınmış ve her bir ilaç etken maddesinin, her bir organik çözücü-su ortamında maksimum floresans şiddetine sahip oldukları uyarma ve emisyon dalga boyları belirlenmiştir. NSAEİ'ler molekül yapılarında fenolik (-OH) ve amin (-NH) grupları gibi, asidik ve bazik fonksiyonlu gruplara sahip olduklarından, optimum koşullarda %10-40 asetonitril-su ortamlarında, bu ilaç etken maddelerinin iyonlaşma sabitleri spektroflorimetrik ve spektrofotometrik yöntemlerle hem pH-floresans şiddeti grafiklerinden hem de pKa değerlerini deney koşullarında hesaplayan bir bilgisayar programı olan STAR programıyla iyonlaşma sabitleri tayin edilmiştir. Deneysel yöntemlerle elde edilen pKa değerleri, SPARC programından (online teorik pKa hesaplama programı) hesaplanan teorik pKa değerleriyle karşılaştırılmıştır. Ancak tenoksikam dışında diğerleri (meloksikam ve piroksikam) için, spektroflorimetrik yöntem kullanılarak iyonlaşma sabitleri tam olarak belirlenememiştir., Non-steroidal antiinflammatory drugs (NSAI) is a wide group of medications which contain drugs of the aspirin family. They are prescribed for the various forms of arthritis to reduce the inflammation and control the pain, edema and rigidity. They are termed as non-steroidal antiinflammatory or shortly antiinflammatory analgesics due to their pharmacological profile compared to non-narcotic analgesics. It is important to determine the exact ionization constants of non-steroidal antiinflammory drugs especially the oxicams using several suitable methods is essential for understanding the mechanism of action and bioavailability. Also the exact and precise determination of the ionization constants of these pharmacologically important drugs is of upmost importance. For this reason in this study, the fluorimetric parameters of NSAEIs in organic solvent-water media are determined. In order to specify the fluorimetric parameters (excitation and emission wavelength, fluorescence intensity), the efficient drug components were prepared at suitable concentrations primarily in acetonitrile, methanol, DMF, THF and in pure water, and then in 10-50 % organic solvent-water mixtures. The emission spectra were obtained by changing the excitation wavelength at 10 nm intervals and the excitation and emission wavelengths were determined for every efficient drug molecule, in every organic solvent-water medium in which they had the maximum fluorescence intensity. Since NSAEIs contain acidic and basic functional groups such as phenolic (-OH) and amine (-NH) groups, under optimum conditions, 10-40 % acetonitrile-water medium, the effective drug materials' ionization constants were determined by spectrofluorimetric and spectrofluorimetric methods both from the pH-fluorecence intensity graphics and from the STAR programme which calculates the pKa values during experimental conditions. The pKa values obtained experimentally were compared to theoretic pKa values obtained from SPARC programme (online theoretic pKa calculation programme). However except tenoxicam, the ionization constants using spectrofluorimetric method could not be exactly determined for the other drugs (meloxicam and piroxicam).

Objectives Headache during migraine attack may recur during a single attack. The present study evaluated efficacy of both individual and combined use of agents from nonsteroidal anti-inflammatory drug (NSAID) and triptan groups widely used in treatment of migraine attacks. Methods A total of 201 attacks in 67 migraine patients were evaluated. Patients were divided into 3 study groups: those receiving rizatriptan 10mg, tenoxicam 20 mg, and rizatriptan + tenoxicam (combination). Patients evaluated severity of headache based on visual analogue scale (VAS) at moment of drug delivery, after 30 minutes, and after 1, 2, 4, 8 and 24 hours. Attacks were evaluated separately for each treatment alternative, and results were also compared. Results VAS values were the same at onset of attack, but were lower in rizatriptan and combination groups than in tenoxicam group at 30 minutes and onward. VAS score was above 4 at 60 minutes in tenoxicam group and mean VAS value in this group was found to be significantly higher than values in rizatriptan and combined groups. At 24 hours, VAS scores were similar in combination and tenoxicam groups, while rizatriptan group had higher mean VAS score than the other 2 groups. Conclusion When single drug use fails to provide adequate control, combined use of a rapid-acting triptan and a long-acting NSAID appears to be a suitable treatment option.

Cocrystals of tenoxicam, a non-steroidal anti-inflammatory drug, are screened, prepared, and characterized in this study. Nine tenoxicam cocrystals were identified using solvent-drop grinding (SDG) techniques. Structural characterization was performed using powder X-ray diffraction (PXRD), differential scanning calorimetry, and multinuclear solid-state NMR (SSNMR). Thermal analysis, PXRD, and 1D SSNMR are used to detect solvates and phase mixtures encountered in SDG cocrystal screening. 2D SSNMR methods are then used to confirm cocrystal formation and determine structural aspects for selected cocrystals formed with saccharin, salicylic acid, succinic acid, and glycolic acid in comparison to Forms I and III of tenoxicam. Molecular association is demonstrated using cross-polarization heteronuclear dipolar correlation (CP-HETCOR) methods involving 1 H and 13 C nuclei. Short-range 1 H– 13 C CP-HETCOR and 1 H– 1 H double-quantum interactions between atoms of interest, including those engaged in hydrogen bonding, are used to reveal local aspects of the cocrystal structure. 15 N SSNMR is used to assess ionization state and the potential for zwitterionization in the selected cocrystals. The tenoxicam saccharin cocrystal was found to be similar in structure to a previously-reported cocrystal of piroxicam and saccharin. The four selected cocrystals yielded intrinsic dissolution rates that were similar or reduced relative to tenoxicam Form III.

Objective: to study coagulative and vascular-thrombocytic hemostases in patients with rheumatoid arthritis (RA) and coronary heart disease (CHD) depending on therapy with different nonsteroidal anti-inflammatory drugs (NSAIDs) alone and in combination with low-dose aspirin. Subjects and methods. The trial enrolled 58 patients (43 women and 15 men) with a valid diagnosis of RA. The patients' mean age was 61.2 years; the disease duration averaged 10 years. All the patients received therapy with disease-modifying antirheumatic drugs (DMARDs) and NSAIDs. All had CHD; 52 of the 58 patients presented with arterial hypertension; 30 had noncoronary atherosclerosis. Cardiovascular diseases were first identified in 18 patients. All took heart medications. Coagulative and vascular-thrombocytic hemostases were studied in all the patients and the results were compared depending on to the taken NSAID (diclofenac, tenoxicam, nimesulide, meloxicam). Thirty-seven patients who had not previously received antiaggregant therapy were given aspirin in a dose of 100 mg when they were found to have platelet hyperaggregation and aggregation was restudied on aspirin therapy days 7-8. A control group consisted of 26 healthy men (mean age 55 years) who received no medications. Results. In patients with RA and CHD, activated coagulative hemostasis was identified in 65.5% of cases. The signs of hypercoagulation were observed in 35 of the 58 patients. When different NSAIDs were used, the coagulative hemostatic changes were unidirectional and no statistically significant differences were found between the groups. The patients taking diclofenac, nimesulide, or meloxicam were found to have activated vascular-thrombocytic hemostasis. Those receiving tenoxicam showed a tendency towards decreased adrenaline-induced platelet aggregation (the drug's aspirin-like effect); however, no statistical processing was made because of few cases. The use of aspirin in the patients taking diclofenac, nimesulide, or meloxicam resulted in lower platelet aggregation in the vast majority of cases despite NSAID intake. No adequate aspirin response was obtained in 32.4% of the patients. Conclusion. Aspirin is indicated in RA and CHD patients receiving NSAIDS. Antiaggregant therapy should be used under control of vascular-thrombotyc hemostasis as aspirin is insufficiently effective in one third of cases in this group.

From potentiostatic current transients and voltammetry studies, carried out under both stagnant and forced convection conditions, the tenoxicam electrochemical behavior on a bare carbon paste rotating disk electrode was assessed in an aqueous solution (pH = 0.403). It was found that tenoxicam's electrochemical oxidation is a mass transfer-controlled process where a current peak is clearly formed at around 0.74 V when the potential scan was varied in the positive direction. However, when the potential was switched to the negative direction, up to the initial potential value, no reduction peak was formed. Tenoxicam's electrochemical oxidation follows an EC mechanism where the electrodic and chemical kinetics are fast. From sample-current voltammetry both the number of electrons, n , that tenoxicam losses during its electro-oxidation and its half-wave potential, E 1/2 , were determined to be 2 and 0.770 V vs. Ag/AgCl, respectively. Moreover, from differential pulse voltammetry plots it was confirmed that effectively in this case n = 2. Considering 2 electrons and both the Randles-Sevcik and Cotrell equations, the tenoxicam's diffusion coefficient, D , was determined to be (3.745 ± 0.077) × 10 −6 and (4.116 ± 0.086) × 10 −6 cm 2 s −1 , respectively. From linear sweep voltammetry plots recorded under forced convection conditions, it was found that Levich's equation describes adequately the limiting current recorded as a function of the electrode rotation rate, from where the D value was also found to be (4.396 ± 0.058) × 10 −6 cm 2 s −1 . Therefore, the average D value was (4.09 ± 0.33) × 10 −6 cm 2 s −1 . Furthermore, from the radius of the tenoxicam molecule, previously optimized at M052X/6-31 + G(d,p) level of theory, and using the Stokes–Einstein approach, D was also estimated to be 4.54 × 10 −6 cm 2 s −1 which is similar to the experimentally estimated values, under both stagnant and forced convection hydrodynamic conditions.

Tenoxicam is a poorly water-soluble NSAID drug and dissolution plays an important role in its absorption, so the present investigation was to develop and characterize orodispersible tablets of tenoxicam using solid deposition technique on superdisintegrants in order to improve its dissolution and aqueous solubility to facilitate faster onset of action. The super-disintegrants used were crospovidone, cross-carmellose sodium, sodium starch glycolate and pregelatinised maize starch in ratios of 1:1, 1:2 and 1:4 (w/w) drug:carrier. Drug excipients compatibility study was carried out using DSC, IR spectroscopy and SEM photography. General characterization of the prepared tablets was performed, in addition to wetting time, in vitro disintegration time and in vitro dissolution studies. The formula containing cross-carmellose sodium as a carrier in a ratio of 1:2 showed highest dissolution rate and shortest disintegration time. It was subjected to stability stress testing and drug concentration was detected by stability indicating HPLC assay method and in conclusion, the results of this work suggest that stable rapid release tenoxicam orodispersible tablets can be developed by solid deposition method.

Tenoxicam (TX) solid dispersions (SDs) with hydrophilic carriers, prepared by solvent evaporation method, were characterized for their saturation solubility, dissolution rate, DSC, and X-ray diffraction patterns. TX-Nicotinamide SD (1:4) was selected to prepare seventeen buccoadhesive discs containing adhesive polymers namely, sodium alginate, chitosan, guar gum, HPMC K4M, or Carbopol 934. All discs were characterized for in vitro release, mucoadhesion, and swelling index. A selected disc was characterized for disc hydration, ex vivo permeation, anti-microbial activity, and bioavailability. All SDs showed increase in TX solubility. Permeation studies revealed that TX could permeate easily with a steady state flux of 1.738 mg/cm 2 .h. The percentage relative bioavailability compared to oral Tenocam tablet was found to be 127 % with a significant difference regarding all pharmacokinetic parameters. . The results suggest that the selected buccoadhesive disc showed a higher dissolution rate, a faster onset of action, and improved bioavailability accompanied with buccal anti-microbial activity.

The maximum cutaneous fluxes of 12 nonsteroidal anti-inflammatory drugs (NSAIDs), determined in a preceding study from the lipophilic vehicle light mineral oil in vivo on 24 healthy volunteers, were related to data concerning their intrinsic activities. From the multiplication of the relative intrinsic activities with the relative maximum fluxes, both related to indometacin (CAS 53-86-1) as standard, the percutaneous activities result as parameters for the prediction of the efficacy of cutaneous preparations with NSAIDs. According to the results of the calculations, the percutaneous activities of ibuprofen (CAS 15687-27-1) and nabumetone (CAS 42924-53-8) from lipophilic vehicles are remarkable because of their very high maximum fluxes. NSAIDs with still high percutaneous activities are ketoprofen (CAS 22071-15-4), naproxen (CAS 22204-53-1), piroxicam (CAS 36322-90-4) and diclofenac (CAS 15307-86-5). In contrast, the systemically highly effective NSAIDs indometacin and acemetacin (CAS 53164-05-9) show rather low percutaneous activities, when applied in lipophilic vehicles. Especially nabumeton and also tenoxicam (CAS 59804-37-4), both not yet commercially used cuta-neously, can be recommended for lipophilic skin preparations.

A new, simple and rapid thin-layer chromatography (TLC) method with densitometric detection for simultaneous determination of four oxicams, namely, piroxicam, meloxicam, tenoxicam and isoxicam, has been developed. The chromatographic separation was carried out on TLC F254 plates with a mobile phase consisting of ethyl acetate-ethanol-toluene 6:3:1 (v/v/v) + 2 drops of ammonia 25%. Quantitative determination was done by densitometric scanning at wavelength λ = 360 nm. The method was validated with respect to linearity (in the range from 0.05 to 0.50 mg per band), LOD and LOQ, accuracy (about 99.90%) and precision (RSD from 0.33% to 0.80%) in accordance with the International Conference of Harmonization guidelines. The method has been successfully applied to the analysis of drugs in the pharmaceutical formulations.

To evaluate the safety profile of eight oral nonsteroidal anti-inflammatory drugs (NSAIDs) available in France, using data reported through the French pharmacovigilance system. Data (from 2002 to 2006) were analysed for aceclofenac, diclofenac, ketoprofen, meloxicam, naproxen, nimesulide, piroxicam and tenoxicam, focusing on the reported rates of serious adverse drug reactions (ADRs) in the following system organ classes: gastrointestinal, hepatic, cutaneous, renal and cardiovascular. A total of 42 389 serious ADR reports were identified, and 38 506 were included in a case/noncase analysis. Ketoprofen was associated with the highest cumulative reported rate of serious ADRs (0.78 cases per million defined daily doses), followed by diclofenac (0.58), nimesulide (0.52), naproxen (0.50), piroxicam (0.47), tenoxicam (0.42), meloxicam (0.41) and aceclofenac (0.30). The most frequently reported serious ADRs were cutaneous, followed by gastrointestinal, hepatic, renal and rarely, cardiovascular events. In the case/noncase analysis, ketoprofen, piroxicam and naproxen were associated with the highest risk of serious gastrointestinal ADRs (odds ratios [ORs] of 6.87, 6.54 and 5.07, respectively). Nimesulide and aceclofenac were associated with the highest risk of liver ADRs (adjusted ORs of 4.53 and 3.67, respectively), as was meloxicam for cutaneous ADRs (adjusted OR of 3.15) and tenoxicam for renal ADRs (adjusted OR of 3.17). The most frequent serious ADRs reported with the selected oral NSAIDs are cutaneous, followed by gastrointestinal, hepatic and renal events. The highest risks for serious gastrointestinal, hepatic, cutaneous and renal adverse events were linked, respectively, with ketoprofen, nimesulide, meloxicam and tenoxicam compared with the other NSAIDs.

Aim The purpose of this study was to develop transdermal films (TFs) with the addition of different polymer ratios that incorporated 0.5% tenoxicam in order to ensure maximum controlled and sustained drug release capacity. Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID) widely used in the treatment of rheumatic diseases and characterized by its efficacy and reduced side effects in comparison to other NSAIDs. Main methods Transdermal films of tenoxicam were designed with the Eudragit L30D-55copolymer with permeation enhancers like polyethylene glycol (PEG) and propylene glycol (PG) incorporated at different concentrations using the casting evaporation technique. Evaluations of these formulae were performed through mechanical characterizations and Fourier Transform Infrared Spectroscopy [FTIR]. In-vitro release studies were performed during 24 h using diffusion cells. The film formulations with optimum in vitro-release rate have been taken up for testing of the anti-inflammatory effects and the sustaining action of tenoxicam. The in-vivo studies performed included carrageenan-induced hind paw edema and skin biopsies in Wistar rats. Key findings Formulation (F7) had the best effective combination [glycerol (0.25 g), PEG200 (0.5 g), PEG400 (1 g) and PG (10%) and 0.5% dispersed drug] among all of the tenoxicam TF formulations studied. Also, this formula had the highest release value than formula 1 (F1) that contains [glycerol (2.5 g), PEG200 (0.5 g), PEG400 (0.5 g) and 0.5% dissolved drug] or a commercially available gel after 24 h. FTIR revealed that there was an interaction between the polymer and the drug. The drug–polymer interaction occurring between tenoxicam and Eudragit L30D-55 seems to cause a drag effect, leading to a delay of the tenoxicam release from the Eudragit L film. Significance When the films were applied half an hour before the subplantar injection of carrageenan in the hind paw of Wistar rats, it was observed that formula F7 provided maximum inhibition of paw edema in rats over 24 h in contrast to both formula F1 and the marketed piroxicam gel as a reference. This was also confirmed histopathologically from skin biopsies. Thus, we show that tenoxicam can be formulated into transdermal films to sustain its release characteristics, and the polymeric composition of PEG200/PEG400 at a ratio of 1:2 and 10% PG was found to be the best choice to manufacture tenoxicam TF.

A simple, rapid and precise flow-injection–chemiluminescence (FI–CL) method is presented for the determination of tenoxicam in pharmaceutical preparations and biological samples. The method is based on the weak chemiluminescence signal arising from the reaction of cerium(IV) in a nitric acid medium with sodium hyposulphite being significantly increased by tenoxicam in the presence of sodium dodecyl benzene sulphonate. Several experimental parameters affecting the CL reaction were examined and optimized systematically. Under the optimum conditions, the CL intensity was proportional to the concentration of tenoxicam in the range 7.0 × 10–11–5.0 × 10–8 g/mL. The detection limit was 2.3 × 10–11 g/mL tenoxicam and the relative standard deviation (RSD) was 2.1% for 1.0 × 10–9 g/mL tenoxicam solution (n = 11). The proposed method was applied to the determination of tenoxicam in pharmaceutical preparations, serum and human urine, with satisfactory results. The possible mechanism of the chemiluminescence reaction is also briefly discussed. Copyright © 2011 John Wiley & Sons, Ltd.

A direct, rapid, and sensitive thin-layer chromatography (TLC) method with densitometric detection was developed and validated for the determination of tenoxicam and its degradation products. The chromatographic separation was executed on silica gel TLC 60 F254 plates. Elution was performed with ethyl acetate-toluene-butylamine (2:2:1, ν/ν/ν) as mobile phase. Quantitative analysis was carried out on the basis of the peak areas obtained from reflectance scanning densitometry performed at 288 nm. The method was validated in terms of linearity (35–1820 mg mL−1), accuracy (RSD < 1%), precision (RSD < 2%), sensitivity (LOD = 0.86 mg per band; LOQ = 2.30 mg per band), selectivity, and repeatability. Degradation products were identified by the RF values, absorption spectra, and LC-MS analysis. As the method could effectively separate the drug from its degradation products (i.e., pyridine-2-amine, tiophen), it can be employed as a method to indicate the stability of the compound. Moreover, the proposed TLC method...

Kandis, Hayati/0000-0001-9151-6050 WOS: 000293479500020 Background: Postoperative strictures, which are still serious problems of tracheal surgery, are caused by an inflammatory reaction with subsequent edema and granulation tissue formation. Taking this into consideration, we have designed a study in which tenoxicam (potent, non-steroidal, anti-inflammatory drug) was used after a tracheal surgery in rats. Methods: Fourteen female Wistar rats were randomly divided into two groups (tenoxicam and control group) with equal numbers. Ketamine-xylazine anesthesia was performed in the rats. A vertical incision on the anterior tracheal wall, including the third to fifth cartilaginous rings, was performed and closed primarily with an interrupted suture technique using 4/0 absorbable suture. The tenoxicam group was administered 0.5 mg/kg/day tenoxicam and the control group was given 0.5 cc/day 0.9% NaCl via intraperitoneal route for 10 days beginning from the operation day. After two weeks, all animals were sacrificed under general anesthesia. Tracheas were excised, and a pathologist blindly evaluated the cases. The Mann-Whitney U-test was used for statistical analysis, and a value of p

Post laminectomy arachnoiditis has been shown by experiments with rats and post operative radiological imaging in humans. The purpose of this experimental study was to determine the efficacy of tenoxicam in preventing arachnoiditis in rats. Twenty-four Wistar rats were divided into two groups, and L3 laminectomy was performed. In the tenoxicam group, 0.5 mg/kg tenoxicam was applied intraperitoneally. Normal saline was applied intraperitoneally in the control group. Later, the rats were killed at weeks 3 and 6, and the laminectomy sites were evaluated pathologically for arachnoiditis. The results showed that 6 weeks after surgery, the tenoxicam group showed lowest arachnoiditis grades. However, statistically significant difference was not found in arachnoiditis between the control group and the tenoxicam group. Based on these findings it is concluded that application of the tenoxicam after lumbar laminectomy did not effectively reduce arachnoiditis. Performing the most effective surgical technique without damage around tissue in a small surgical wound and having meticulous hemostasis in surgery seem to be the key for preventing arachnoiditis effectively.

Tenoxicam is an effective analgesic and anti-inflammatory agent for symptomatic treatment of various conditions. The purpose of this study was to evaluate clinically the effectiveness of prophylactic tenoxicam and prophylactic ibuprofen in reducing post-endodontic pain compared with placebo. A total of 48 patients consented to a double-blind, single dose, prophylactic oral administration of 20 mg of tenoxicam, 200 mg of ibuprofen, or a placebo before root canal treatment. The root canal treatment was performed in one visit. The patients registered their degree of discomfort on a 100-mm visual analog scale, immediately postoperative, and 6, 12, 24, 48 and 72 h after initiation of root canal treatment. The two-way ANOVA test and Tukey HSD post hoc test showed that in the 6-h period, both 20 mg of tenoxicam and 200 mg of ibuprofen provided significantly better pain relief than the placebo. Prophylactic administration of a single dose of 20 mg tenoxicam or 200 mg ibuprofen before RCT provides an effective reduction at 6 h (P < 0.05). Because of the advantages of tenoxicam, it may be useful as a prophylactic analgesic when post- endodontic pain is anticipated. (J Oral Sci 53, 157- 161, 2011)

The mechanism of interaction of the non-steroidal anti-inflammatory drugs, isoxicam (IXM) and tenoxicam (TXM) with bovine serum albumin (BSA) has been studied using spectroscopic techniques, viz ., spectrofluorescence, circular dichroism (CD), UV–visible absorption and FT-IR under simulative physiological conditions. Stern–Volmer analysis of fluorescence quenching data shows the presence of the static quenching mechanism. Thermodynamic parameters (negative Δ H 0 and positive Δ S 0 values obtained in the present study) revealed that the hydrophobic interactions played a major role in the interaction of these drugs with BSA. The distance, r between the donor (BSA) and acceptor (IXM/TXM) was calculated based on the Forster’s theory of non-radiation energy transfer and the values were observed to be 3.85 nm and 2.60 nm in IXM–BSA and TXM–BSA system, respectively. CD and FT-IR studies indicated that the binding of IXM/TXM to BSA induced conformational changes in BSA. The effect of common ions on the binding of IXM/TXM to BSA has been investigated.

Purpose: The present study was conducted to evaluate the effect of tenoxicam on cellular and humoral immunity.Methods: Tenoxicam (2.5 - 10mg/kg) was administered at three different doses to three groups of mice and the cellular immune responses were studied using delayed hypersensitivity response (DTH) and cyclophosphamide-induced neutropenia while the humoral immune response was evaluated using hemagglutination test and mice mortality ratio. Normal saline and cyclophosphamide were used as negative and positive controls, respectively.Results: DTH assay resulted in a significant reduction in skin thickness (p < 0.05) for tenoxicam treated groups when compared to the negative control group at 24 h, 48 h and 72 h after administration of challenging dose of dinitrochlorobenzene (DNCB). Cyclophoshamide induced neutropenia showed a significant percentage reduction in total leukocyte count (TLC) and differential leukocyte count (DLC) i.e. lymphocytes and neutrophils (p< 0.05), but an increase in monocytes in all the treatment groups in the following order: 10 mg>5 mg >2.5 mg> negative control group. A dose dependent reduction response was observed (p

Introduction To investigate the effects of subacromial tenoxicam injection during physical therapy after rotator cuff tear and subacromial decompression.

A rapid and sensitive reversed phase high performance liquid chromatographic (HPLC) method was developed and validated for the analysis of tenoxicam in raw material and its pharmaceutical formulation. The analysis was carried out on a reversed phase C18 column, using mixtures of buffer/acetonitrile (40:60, v/v) with flow rate was of 1 mL min−1. The method was validated statistically for its linearity (correlation coefficient = 0.9983), accuracy, robustness, and intermediate precision. An experimental design was used during validation to evaluate method robustness and for the determination of intermediate precision. To test robustness, four factors were considered, mainly, percentage of organic modifier in the mobile phase, pH, flow rate, and different wavelengths. An increase of the flow rate results in a decrease of the drug concentration found, while the percentage of organic modifier, pH, and wavelength have no significant effect on the response. For intermediate precision the factors examined were mul...

Background There has been a trend over recent years for combining a nonsteroidal antiinflammatory drug (NSAID) with paracetamol (acetaminophen) for pain management. However, therapeutic superiority of the combination of paracetamol and an NSAID over either drug alone remains controversial. We evaluated the efficacy of the combination of paracetamol and an NSAID versus either drug alone in various acute pain models. Methods A systematic literature search of Medline, Embase, Cumulative Index to Nursing and Allied Health Literature, and PubMed covering the period from January 1988 to June 2009 was performed to identify randomized controlled trials in humans that specifically compared combinations of paracetamol with various NSAIDs versus at least 1 of these constituent drugs. Identified studies were stratified into 2 groups: paracetamol/NSAID combinations versus paracetamol or NSAIDs. We analyzed pain intensity scores and supplemental analgesic requirements as primary outcome measures. In addition, each study was graded for quality using a validated scale. Results Twenty-one human studies enrolling 1909 patients were analyzed. The NSAIDs used were ibuprofen (n = 6), diclofenac (n = 8), ketoprofen (n = 3), ketorolac (n = 1), aspirin (n = 1), tenoxicam (n = 1), and rofecoxib (n = 1). The combination of paracetamol and NSAID was more effective than paracetamol or NSAID alone in 85% and 64% of relevant studies, respectively. The pain intensity and analgesic supplementation was 35.0% +/- 10.9% and 38.8% +/- 13.1% lesser, respectively, in the positive studies for the combination versus paracetamol group, and 37.7% +/- 26.6% and 31.3% +/- 13.4% lesser, respectively, in the positive studies for the combination versus the NSAID group. No statistical difference in median quality scores was found between experimental groups. Conclusion Current evidence suggests that a combination of paracetamol and an NSAID may offer superior analgesia compared with either drug alone.

Meloxicam, piroxicam, and tenoxicam belong to a highly potent oxicam group of nonsteroidal anti-inflammatory drugs. Whereas the structurally similar oxicams have different pharmacokinetics, treatment efficiency, and adverse effects, their common mechanism of action is the inhibition of a membrane enzyme, cyclooxygenase. Because the prerequisite for accessing the cyclooxygenase by the drugs is interaction with the membrane, the focus of the current study was a comparison of how meloxicam, piroxicam, and tenoxicam interact with lipid monolayers used as models of biological membranes. The monolayers were formed with 1,2-dipalmitoyl-sn-glycero-3-phospho-rac-(1-glycerol), 1,2-dipalmitoyl-sn-glycero-3-phospho-l-serine, 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine, 1,2-myristoyl-sn-glycero-3-phosphoethanolamine, and 1,2-dilauroyl-sn-glycero-3-phosphoethanolamine. These systems were examined via surface pressure and surface electrical potential measurements, polarization modulation infrared reflection adsorption spectra, and Brewster angle microscopy. The three oxicams are differentiated in the monolayers; meloxicam shows the highest ability to modify membrane fluidity and surface potential, followed by piroxicam and tenoxicam. The dissimilarity of the biological activity of the oxicams may be linked to different interaction with the membrane, as revealed by the present study.

In this work it is explained, by the first time, the application of programs SQUAD and HYPNMR to refine equilibrium constant values through the fit of electrophoretic mobilities determined by capillary zone electrophoresis experiments, due to the mathematical isomorphism of UV-vis absorptivity coefficients, NMR chemical shifts and electrophoretic mobilities as a function of pH. Then, the pK(a) values of tenoxicam in H(2)O/DMSO 1:4 (v/v) have been obtained from (1)H NMR chemical shifts, as well as of oxicams in aqueous solution from electrophoretic mobilities determined by CZE, at 25 degrees C. These values are in very good agreement with those reported by spectrophotometric and potentiometric measurements.

Membrane fusion is a critical step in many biological events. The fusion process is always induced by different fusogenic agents of which proteins and peptides form the largest group. The mechanistic details of the fusion process vary depending on the nature of the fusogenic agents. However, membrane fusion induced by small drug molecules at physiologically relevant concentration has not been observed. Only recently our group has shown that three painkillers, namely, meloxicam, piroxicam, and tenoxicam, belonging to the oxicam group of non-steroidal anti-inflammatory drugs (NSAIDs) share this property. In this work, we present the effect of drug concentration and temperature on the kinetics of the fusion process. Small unilameller vesicles (SUVs) formed by dimyristoylphosphatidylcholine (DMPC) with an average diameter of 50-60 nm were used as model membranes. Fluorescence assays were used to probe the time dependence of lipid mixing, content mixing, and leakage whereas transmission electron microscopy (TEM) was used to image the fusion process and to calculate the average diameter of the vesicles. The results show that, in this fusion process, lipid mixing and content mixing are two sequential events and can occur even at a very low drug to lipid ratio (D/L) of 0.018. For a D/L ratio greater than 0.045, leakage of the vesicles leading to rupture compete with the fusion thereby inhibiting it. Temperature variation in the presence of drugs gives linear Arrhenius plots and is used to calculate the activation energies for the lipid mixing and content mixing, which are less compared to that seen in SUVs with a smaller diameter of 45 nm. Thermodynamic parameters of the transition state are calculated. The fusogenic property of the drugs has been interpreted in terms of the ability of the drugs to introduce membrane perturbation even at such low D/L ratios as studied here.

Submitted by Guilherme Lemeszenski (guilherme@nead.unesp.br) on 2013-08-22T18:49:22Z No. of bitstreams: 1 S0100-46702009000400008.pdf: 1476319 bytes, checksum: 7b1b22e8ff53b51fdbc37b64c198512f (MD5) Made available in DSpace on 2013-08-22T18:49:22Z (GMT). No. of bitstreams: 1 S0100-46702009000400008.pdf: 1476319 bytes, checksum: 7b1b22e8ff53b51fdbc37b64c198512f (MD5) Previous issue date: 2009-12-01 Made available in DSpace on 2013-09-30T19:39:45Z (GMT). No. of bitstreams: 2 S0100-46702009000400008.pdf: 1476319 bytes, checksum: 7b1b22e8ff53b51fdbc37b64c198512f (MD5) S0100-46702009000400008.pdf.txt: 37641 bytes, checksum: e41e24858b9a849354e7b9ecef8324d3 (MD5) Previous issue date: 2009-12-01 Submitted by Vitor Silverio Rodrigues (vitorsrodrigues@reitoria.unesp.br) on 2014-05-20T15:10:34Z No. of bitstreams: 2 S0100-46702009000400008.pdf: 1476319 bytes, checksum: 7b1b22e8ff53b51fdbc37b64c198512f (MD5) S0100-46702009000400008.pdf.txt: 37641 bytes, checksum: e41e24858b9a849354e7b9ecef8324d3 (MD5) Made available in DSpace on 2014-05-20T15:10:34Z (GMT). No. of bitstreams: 2 S0100-46702009000400008.pdf: 1476319 bytes, checksum: 7b1b22e8ff53b51fdbc37b64c198512f (MD5) S0100-46702009000400008.pdf.txt: 37641 bytes, checksum: e41e24858b9a849354e7b9ecef8324d3 (MD5) Previous issue date: 2009-12-01 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Diferentes substâncias utilizadas como fármacos foram ensaiadas como inibidores da colagenase intersticial humana, também conhecida como metaloprotease 1 da matriz conjuntiva e pela sigla em inglês MMP-1. O estudo foi de natureza experimental e também de simulação computacional. A atividade da colagenase foi quantificada fluorimetricamente, pela reação com um substrato sintético fluorescente, cuja emissão se altera após a hidrólise. A interação colagenase-inibidor foi analisada teoricamente, mediante cálculos de docking. Três das quatro substâncias testadas apresentaram atividade inibidora moderada sobre a colagenase humana. Different common drugs (Meloxicam, Tenoxicam and Piroxicam, and sodium alendronate) were tested both experimental and theoretically as inhibitors of interstitial human collagenase, also known as matrix metalloproteinase 1 (MMP-1). The in vitro collagenase activity, alone and in the presence of inhibitors, was quantified by the reaction with a fluorescent synthetic substrate and measuring the change of emission. Collagenase-inhibitor interaction was studied theoretically by computational calculations. Three among the four tested substances showed moderate inhibiting activity against the human collagenase. UNESP Instituto de Química UNESP Instituto de Química

To compare the efficacy and safety of a combination therapy, doxazosin plus tenoxicam, and doxazosin alone for lower urinary tract symptoms (LUTS) caused by benign prostatic hyperplasia (BPH), as various combination therapies increase the efficacy of medical therapy. Alpha blocker agents have been widely used for the treatment of LUTS secondary to BPH.Fifty-seven patients complaining of LUTS secondary to BPH were enrolled in this clinical trial. Patients were randomly assigned to receive doxazosin 4 mg or doxazosin 4 mg plus tenoxicam 20 mg treatment. Patients were evaluated for BPH according to the European Association of Urology and American Urological Association clinical guidelines. In addition, patients were assessed with Overactive Bladder Symptom Score (OABSS) and International Index of Erectile Function (IIEF). Patients were reevaluated after a 6-week treatment course. The International Prostatic Symptom Score (IPSS), IPSS-Quality of Life (IPSS-QoL), maximal urinary flow rates (Q(max)), and average urinary flow rates (AFR) were determined at baseline and again at 6 weeks as efficacy parameters.The total IPSS, IPSS-QoL, and OABSS decreased significantly in both tenoxicam plus doxazosin group and doxazosin alone group compared with baseline (P.01). Also, Q(max) and AFR significantly improved in both groups (P.01). The improvements in IPSS, IPSS-QoL, and OABSS were significantly better in patients treated with combination therapy (P.05).COX-2 inhibitors in combination with an alpha blocker may increase the effectiveness of the therapy for LUTS secondary to BPH without significant effects on side effect profile.