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The purpose of the present study was to prepare inclusion complex of domperidone with hydroxylpropyl-β-cyclodextrin in order improved the solubility and hence to increase dissolution of domperidone. An effect of concentration of hydroxylpropyl-β-cyclodextrin on the aqueous solubility of domperidone was determined by phasesolubility method. The aqueous solubility of domperidone increased as a function of hydroxylpropyl-β-cyclodextrin concentration, showing AL type diagram. Solid domperidone/hydroxylpropyl-β-cyclodextrin complex was prepared in ratio 1:1 by ultrasonication and kneading method. Solid state inclusion complex was characterized by FTIR, powder X-ray diffraction and differential-scanning calorimetry techniques. FTIR studies showed intactness of drug in complex whereas powder diffraction studies showed that hydroxylpropyl-β-cyclodextrin complex was amorphous. Solubility studies showed that complexation increased domperidone solubility as compared to pure drug in 0.1M hydrochloric acid and distilled water. Drug content confirms that ultrasonication is one of the efficient methods to prepare inclusion complex. Dissolution data of inclusion complexes also indicated that there is 1.4 folds increase in dissolution as compared to pure drug and was observed in case of inclusion complexes prepared by ultrasonication. [ABSTRACT FROM AUTHOR]

Objective: To evaluate the antihyperglycemic activity of atorvastatin and hydroxychloroquine combination in alloxan-induced diabetic rats. Materials and Methods: Alloxan induced diabetic Wistar male rats were randomized into six groups of 6 rats each. (Normal rats, diabetic control, atorvastatin (ATV), hydroxychloroquine (HCQ), ATV 5 mg /kg + HCQ 100 mg/kg, and ATV 10 mg/kg + HCQ 200 mg/kg). The rats were treated for 9 days and blood samples were collected at baseline and end of therapy. These samples were analyzed for plasma glucose by autoanalyzer. Changes in body weight, water, food intakes and total protein content were also recorded. Results: Atorvastatin and hydroxychloroquine alone and in combination reported significant fall in blood glucose level from baseline. Fall in glucose level was significantly more in high dose combination of atorvastatin and hydroxychloroquine (ATV: 10 mg/kg + HCQ: 200 mg/kg) as compared to other study treatment groups (ATV: 17% Vs HCQ: 7% Vs ATV 5mg/kg + HCQ 100mg /kg: 14% Vs ATV 10mg/kg + HCQ 200mg /kg: 21%; p<0.01). ATV and HCQ individually and in combination also improved the body weight loss. The weight gain was significantly more in combination treated rats as compared to positive control group and greater than those who received atorvastatin and hydroxychloroquine alone. Rats treated with the combination also reported significant decrease in food intake and significant increase in total protein. Conclusion: Increased hypoglycemic effect in combination may be due to potentiation or synergism between HCQ and ATV. Further studies are required to demonstrate clinically significant antidiabetic effect. [ABSTRACT FROM AUTHOR]

A simple, precise, accurate and rapid high performance thin layer chromatographic method has been developed for the simultaneous estimation of ondansetron combinations in solid dosage form with omeprazole and rabeprazole, respectively. The method involved separation of components by TLC on a precoated silica gel 60 F254 using a mixture of dichloromethane:methanol (9:1) as a mobile phase. Detection of spots was carried out at 309 nm and 294 nm for ondansetron with omeprazole and ondansetron with rabeprazole combinations, respectively. The mean retardation factor for ondansetron and omeprazole were found to be 0.42±0.02, 0.54±0.03, respectively while for ondansetron and rabeprazole, 0.41±0.02 and 0.51±0.02, respectively. The linearity and range was 0.1 to 0.5 µg/ spot for three drugs. The method was validated for precision, accuracy and reproducibility. [ABSTRACT FROM AUTHOR]

Two simple, accurate and precise spectrophotometric methods have been developed for simultaneous determination of lansoprazole and domperidone in pharmaceutical dosage form. Method A involves formation of Q-absorbance equation at 256.0 nm (isoabsorptive point) and at 294.2 nm while method B is two wavelength method where 277.6 nm, 302.1 nm were selected as λ1 and λ2 for determination of lansoprazole and 231.3 nm, 292.0 nm were selected as λ1 and λ2 for determination of domperidone. Both the methods were validated statistically and recovery studies were carried out. The Beer's law limits for each drug individually and in mixture was within the concentration range of 5-50 µg/ml. Linearity of lansoprazole and domperidone were in the range of 24-36 µg/ml and 8-12 µg/ml, respectively. The proposed methods have been applied successfully to the analysis of the cited drugs either in pure form or in pharmaceutical formulations with good accuracy and precision. The method herein described can be employed for quality control and routine analysis of drugs in pharmaceutical formulations. [ABSTRACT FROM AUTHOR]

In the present study strong cation exchange resin (Amberlite IRP69) was used to improve the physicochemical properties of ranitidine hydrochloride such as taste and bulk properties and to sustain dissolution rate. Drug-resin complexes were prepared using batch method. Drug loading was done under different processing conditions such as temperature, pH, drug-resin ratio, and drug concentration to get the optimum condition for resinate preparation. Resinate prepared under optimized condition was tested for taste, bulk properties and release rate. Degree of bitterness of ranitidine was found to reduce to zero after complexation with resin. Improvement in flow properties was also observed. Angle of repose for resinate was found to be 33.21o as compared to 42.27o for ranitidine HCl. Effect of dissolution medium and particle size on in vitro release of drug from resinate was also investigated. Resinate with drug to resin ratio of 2:3 and particle size >90 µm showed about 90% of drug release within 12 h. The orodispersible tablet formulated from the resinate containing 10% croscarmellose sodium disintegrated within 35 sec in oral cavity and showed similar dissolution profile as the resinate. Tablets were found stable after stability studies with no change in dissolution profile. [ABSTRACT FROM AUTHOR]

An attempt has been made to develop buccoadhesive bilayered tablets comprising of drug containing bioadhesive layer and drug free backing layer to release the drug for extended period of time with reduction in dosing frequency. Tablets of terbutaline sulphate were prepared by direct compression method using bioadhesive polymers like Carbopol 934P, Methocel K4M, Methocel K15M and sodium carboxy methyl cellulose either alone or in combinations with backing layer of ethyl cellulose. The physical characteristics, swelling index, surface pH, in vitro bioadhesion strength, and in vitro release of formulated tablets were shown to be dependent on characteristics and composition of bioadhesive materials used. The modified in vitro assembly was used to measure and compare the bioadhesive strength of tablets with fresh porcine buccal mucosa as a model tissue. The maximum bioadhesive strength was observed in tablets formulated with Carbopol 934P alone and strength decreases with decrease in its content. The tablets were evaluated for in vitro release in pH 6.8 phosphate buffer for 10 h using a standardized dissolution apparatus. In order to determine the mode of release, the data was subjected to Korsmeyer and Peppas diffusion model. All the formulations followed non-Fickian release mechanism. Carbopol 934P and Methocel K4M in the ratio of 1:1 could be used to design effective and stable buccoadhesive tablets of terbutaline sulphate. [ABSTRACT FROM AUTHOR]

Present work reports extraction of mucilage of Eulophia campestris by multiple maceration technique using water and precipitation by acetone (36% w/w yield). Physicochemical characteristics of mucilage, such as solubility, swelling index, loss on drying, pH and viscosity, were studied and also microbial load was determined. The mucilage was evaluated for its granulating and binding properties in tablets, using paracetamol as a model drug. Mucilage was used in three different concentrations -- 6, 8 and 10% w/v. The granules were prepared by wet granulation technique. The prepared granules were evaluated for percentage of fines, average particle size, total porosity, compressibility index and flow properties. The properties were compared with starch, which was used as a standard binder at 10% w/v concentration. The tablets were prepared and evaluated for content uniformity, hardness, friability, disintegration time and in vitro dissolution profiles. The tablets had good physicochemical properties, and the drug release was more than 85% within 3 h. The tablets prepared by using 10% mucilage as binder exhibited more hardness than by using 6 and 8% concentrations. Hence, 6 and 8% concentrations can be considered as ideal concentrations for preparation of tablets. [ABSTRACT FROM AUTHOR]

Two simple, accurate, rapid and economical spectrophotometric methods have been developed for the simultaneous determination of paracetamol and metoclopramide hydrochloride from tablet dosage form. The first method developed employs formation and solving simultaneous equations using 248.6 nm and 275.6 nm as two wavelengths for formation of equations. Second method is absorbance ratio in which wavelengths selected were 265.6 nm as isoabsorptive point and 275.6 nm as λmax of paracetamol. Both the drugs and their mixtures obey Beer-Lamberts law at selected wavelengths at given concentration range. The methods have been validated statistically and by recovery studies. The results of analysis have been validated statistically and by recovery studies. [ABSTRACT FROM AUTHOR]

Vacuum dried juice extract and methanol extract of the fruits of Lagenaria siceraria Mol. have been evaluated for its diuretic activity in albino rats. Different parameters viz. total urine volume (corrected for water intake during the test period), urine concentration of electrolytes such as sodium, potassium and chloride have been evaluated. The rats treated with vacuum dried Lagenaria siceraria juice extract (LSJE) and Lagenaria siceraria methanol extract (LSME) (100-200 mg/kg; p.o.) showed higher urine volume when compared to the respective control. Both LSJE and LSME have exhibited dose-dependent increase in the excretion of electrolytes when compared to control group. The elevated diuretic potential of LSFE and LSME was statistically significant (P<0.05) and comparable to that of the standard diuretic agent furosemide (20 mg/kg; i.p.). [ABSTRACT FROM AUTHOR]

Ayurvedic eye drops preparation contains aqueous extracts of different herbs. Ethnobotanical survey shows that plants used in Ayurvedic eye drops formulation are rich source of tannin and tannin like compounds. Antioxidant and antimicrobial properties of ayurvedic eye drops are attributed to the presence of tannins and tannin like compounds. Therefore in the present study an attempt has been made to determine the tannin content in some ayurvedic eye drops, by using Folin-Denis method. A blue colored complex is formed by using phosphotungustomolybdic acid. Estimation was done on UV/Vis spectrophotometer. The tannin content of all the three brands was found to be 420, 918 and 270.49 µg/ml. The results obtained are reproducible with coefficient of variation less than 1.0%. Hence the present approach can be used as one of the parameters for the standardization of ayurvedic eye drop preparations. [ABSTRACT FROM AUTHOR]

Since solubility is the main constraint for oral bioavailability of silymarin, an attempt has been made to design tablet formulations of silymarin-HP-β-CD solid dispersion in order to improve oral bioavailability. Tablet formulations were prepared by direct compression technique using superdisintegrants such as crosscarmellose sodium, sodium starch glycolate and polyplasdone XL in different concentrations. Developed formulations were evaluated for various pharmaceutical characteristics viz. hardness, % friability, weight variation, drug content, disintegration time and in vitro dissolution profiles. Amongst different batches, formulations containing crosscarmellose sodium showed superior disintegration and dissolution profiles compared to other formulations. However all the formulations showed improved dissolution over marketed formulation reflecting vital role of HP-β-CD dispersion in promotion of silymarin oral bioavailability. Moreover, optimized formulation showed stability at varying temperature and relative humidity. [ABSTRACT FROM AUTHOR]

A simple, rapid, precise and accurate gas liquid chromatographic method was developed for the determination of ethanol in marketed preparation of abhayarishta using flame ionization detector. The separation was performed employing carbowax 20 M stainless steel column using nitrogen as a carrier gas at optimized conditions. The column was maintained at 90°, while injection port and detector were maintained at 110°. The system suitability parameters were studied throughout the study. The method has been applied successfully for the assay of ethanol in abhayarishta. The recovery values were found to be in the range of 98.14-104.54% with RSD values less then 0.800%. The proposed method can be used for the determination of generated ethanol content in abhayarishta preparation. [ABSTRACT FROM AUTHOR]

Two simple, accurate, and precise methods for simultaneous estimation of tramadol hydrochloride and chlorzoxazone in combined dosage form have been described. The first method employs formation and solving of simultaneous equations using 272.20 and 248.30 nm as two analytical wavelengths. The second method is absorption ratio method, which uses 272.20 and 257.50 nm as two analytical wavelengths. Both the methods allow the simultaneous determination of tramadol hydrochloride and chlorzoxazone in concentration ranges employed for this purpose with the standard deviation of <1.0% in the assay of tablet. [ABSTRACT FROM AUTHOR]

A simple, fast, precise and accurate RP-HPLC method was developed for the simultaneous estimation of valdecoxib and tizanidine hydrochloride in tablet formulations. The separation was achieved by C18 Intersil column and acetonitrile: 0.02 M phosphate buffer (pH 3.5) (60:40 v/v) as mobile phase, at a flow rate of 1.5 ml/min. Detection was carried out at 240 nm. The retention time of valdecoxib and tizanidine hydrochloride was found to be 4.21 and 2.16 min respectively. The validation of the proposed method was also carried out for linearity, accuracy and precision. The linear dynamic range for valdecoxib and tizanidine hydrochloride was 0-100 µg/ml and 0-20 µg/ml respectively. The mean percentage recoveries obtained for valdecoxib and tizanidine hydrochloride were 99.10 and 100.19% respectively. The developed method was found to be accurate, precise, selective and rapid, and it can also be used for routine quality control analysis of these drugs in combination tablets. [ABSTRACT FROM AUTHOR]

A simple, precise, accurate, and validated reverse phase HPLC method has been developed for the simultaneous estimation of aceclofenac and paracetamol in tablet by reverse phase C-18 column (Intersile 4.6 mmx25 cm, 10 µm) using acetonitrile: 50 mM NaH2PO4 in a ratio of 65:35 (pH adjusted to 3.0 with orthophosphoric acid) as a mobile phase at a flow rate of 1.5 ml/min and detection at 276 nm. The retention time for aceclofenac and paracetamol was found to be 1.58 and 4.01 min respectively, and recoveries from tablet were between 99 and 101%. The method can be used for estimation of combination of these drugs in tablets. [ABSTRACT FROM AUTHOR]

Ethnopharmacological Relevance: Barleria prionitis Linn. (Family: Acanthaceae), one of the important Ayurvedic medicinal plant in India, has long been used to treat variety of ailments including swellings, gout, arthritic and rheumatic disorders, nervine and skin diseases, and also acts as immunorestorative., Aim of the Study: The present study was aimed to explore in vitro and in vivo immunomodulatory activities of the iridoids fraction i.e. n-butanol fraction of methanol extract from Barleria prionitis aerial parts (IFBp)., Materials and Methods: IFBp was studied for in vitro [nitroblue tetrazolium (NBT) test and neutrophils candidacidal assay] and in vivo immunomodulatory activity on cellular and humoral immune responses to the antigenic challenge by sheep red blood cells (SRBCs) and by neutrophil adhesion test, phagocytic activity and cyclophosphamide-induced myelosuppression. The study comprised the preliminary phytochemical screening, HPTLC standardization and maximum tolerable dose determination of IFBp., Results: IFBp (50, 100 and 200μg/ml) significantly (P≤0.01) increased the intracellular killing activity of stimulated neutrophils assayed by in vitro NBT reduction test and neutrophils candidacidal assay. Pretreatment of IFBp (100 and 200mg/kg; p.o.) evoked a significant increase in percent neutrophils and neutrophils adhesion to nylon fibres. Oral administration of IFBp augmented the humoral immune response to SRBCs, evidenced by increase in antibody titres and dose dependently potentiated the delayed-type hypersensitivity reaction induced by SRBCs in mice. IFBp potentiated significantly (P≤0.01) the macrophage phagocytic activity and ameliorated the red blood cells, total white blood cells and platelets count and haemoglobin concentration, and also restored the myelosuppressive effects induced by cyclophosphamide. The content (% w/w; mean±SD, n=3) of main iridoids i.e. shanzhiside methyl ester and barlerin was found to be 21.55±2.40 and 10.03±1.69 in IFBp of BP, respectively., Conclusion: The present investigation reveals that IFBp is a potent immunostimulant, stimulating both the specific and non-specific immune mechanisms., (Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.)

Ethnopharmacological Relevance: Lagenaria siceraria Stand. (Cucurbitaceae) fruits have been used, traditionally, in the treatment of hyperlipidemia and atherosclerotic impasse and considered as cardioprotective and cardiotonic drug., Aim of the Study: The present work was undertaken to investigate the effects of methanolic extract from Lagenaria siceraria in experimentally induced hyperlipidemia in rats., Materials and Methods: Methanolic extract of Lagenaria siceraria fruits (LSFE) (100, 200 and 300 mg/kg; p.o.) was administered to the high fat-diet-induced hyperlipidemic rats for 30 days to evaluate its antihyperlipidemic activity. Atorvastatin (10mg/kg; p.o.) was used as a standard drug., Results: At the 30 th day, most significant reduction in lipid levels in the LSFE treated rats as compared to the rats fed with high-fat diet at the 0th day were: total cholesterol 290.14+/-18.42 mg/dl vs. 228.58+/-16.38 mg/dl, low-density lipoprotein cholesterol 195.14+/-8.86 mg/dl vs. 120.57+/-8.11 mg/dl, triglyceride 232.41+/-15.22 mg/dl vs. 181.79+/-15.68 mg/dl, very low-density lipoprotein cholesterol 46.48+/-3.04 mg/dl vs. 36.35+/-3.13 mg/dl (P<0.0001). Conversely, high-density lipoprotein cholesterol levels were significantly (P<0.0001) increased from 48.52+/-6.52 to 71.66+/-5.14 mg/dl. The increase in weight in rats administered with LSFE was less when compared to rats fed with high-fat diet. Moreover, LSFE also exhibited significant increase in excretion of bile acids., Conclusion: The results demonstrate that the LSFE has a definite antihyperlipidemic potential. There is also a valid scientific basis for consuming it in the treatment of coronary artery diseases in India.

Oral administration is unsuitable for drugs prone to extensive first-pass metabolism, like buspirone. Thus, in the present study an attempt has been made to develop a mucoadhesive intranasal formulation improving permeation characteristics of buspirone HCl. Nasal formulations containing different concentrations of chitosan HCl and hydroxypropyl-beta-cyclodextrins (HP-beta-CD) were prepared and compared with control buspirone HCl solution regarding permeability, in vitro duration of mucoadhesion, in vivo nasal clearance in rats and in vitro cytotoxicity on cell culture. Nearly two fold increase in buspirone permeation was observed with 1% chitosan HCl and a 3.5 fold increase with 1% chitosan HCI and 5% HP-beta-CD. Nasal clearance studies showed retention of 50% radioactivity up to about 3.5 h for formulation F7 containing 1% chitosan HCI compared to 1.5 h for control buspirone solution (F1). Results conclusively demonstrated enhancement in permeation with no cytotoxicity. Thus formulations can be used to improve bioavailability of buspirone HCl.

The ethanol and water extracts of Capparis zeylanica leaves showed dose-dependent and significant (P<0.05) increases in pain threshold in tail-immersion test. Moreover, both the extracts (100-200 mg/kg) exhibited a dose-dependent inhibition of writhing and also showed a significant (P<0.001) inhibition of both phases of the formalin pain test. The water extract (200 mg/kg) significantly (P<0.01) reversed yeast-induced fever. Preliminary phytochemical screening of the extracts showed the presence of alkaloids, flavonoids, saponins glycosides, terpenoids, tannins, proteins and carbohydrates.

The present study was undertaken to explore the immunomodulatory activity of ethanolic and water extracts of Capparis zeylanica Linn. (family: Capparidaceae) leaves on neutrophil adhesion test, humoral response to sheep red blood cells, delayed-type hypersensitivity, phagocytic activity and cyclophosphamide-induced myelosuppression. Pre-treatment of water extract (300 mg/kg, oral) of Capparis zeylanica evoked a significant increase in neutrophil adhesion to nylon fibres. The augmentation of humoral immune response to sheep red blood cells by ethanolic and water extracts (150-300 mg/kg) is evidenced by increase in antibody titres in mice. A dose-related increase in both primary and secondary antibody titre was observed. Oral administration of ethanolic and water extracts of Capparis zeylanica leaves, at doses of 150 and 300 mg/kg in mice, dose dependently potentiated the delayed-type hypersensitivity reaction induced by sheep red blood cells. Immunomodulatory activity was also assessed by serological and haematological tests. Capparis zeylanica extracts prevented myelosuppression in mice treated with cyclophosphamide drug. The study comprised the acute toxicity and preliminary phytochemical screening of the ethanol and water extracts.

Bottle gourd [(Lagenaria siceraria (Mol.) Stand.] fruit is ascribed with many therapeutic effects. The present study was undertaken to explore the antihyperlipidemic effect of four different extracts viz. petroleum ether, chloroform, alcoholic and aqueous extracts from bottle gourd in Triton-induced hyperlipidemic rats and their hypolipidemic effects in normocholesteremic rats. The study is comprised preliminary phytochemical screening of the extracts. Oral administration of the extracts, at doses of 200 and 400 mg/kg body weight in rats, dose-dependently inhibited the total cholesterol, triglycerides, low-density lipoproteins level, and significantly increased the high density lipoproteins level. However, petroleum ether extract did not show the significant effects. Both the chloroform and alcoholic extract exhibited more significant effects in lowering total cholesterol, triglycerides and low density lipoproteins along with increase in HDL as compared to the others. Preliminary phytochemical screening revealed the presence of flavonoids, sterols, cucurbitacin saponins, polyphenolics, proteins, and carbohydrates. The results obtained suggest marked antihyperlipidemic and hypolipidemic activity of the extracts.