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The technologies for fabrication of nanocrystals have an immense potential to improve solubility of a variety of the poor water-soluble drugs with subsequent enhanced bioavailability. Repaglinide (Rp) is an antihyperglycemic drug having low bioavailability due to its extensive first-pass metabolism. Microfluidics is a cutting-edge technique that provides a new approach for producing nanoparticles (NPs) with controlled properties for a variety of applications. The current study's goal was to engineer repaglinide smart nanoparticles (Rp-Nc) utilizing microfluidic technology (Dolomite Y shape), and then to perform in-vitro, in-vivo, and toxicity evaluations of them. This method effectively generated nanocrystals with average particle sizes of 71.31 ± 11 nm and a polydispersity index (PDI) of 0.072 ± 12. The fabricated Rp's crystallinity was verified by Differential scanning calorimetry (DSC) and Powder X-ray diffraction (PXRD). In comparison to the raw and commercially available tablets, the fabricated Rp's nanoparticles resulted in a higher saturation solubility and dissolving rate (p < 0.05). Rp nanocrystals had a considerably lower (p < 0.05) IC50 value than that of the raw drug and commercial tablets. Moreover, Rp nanocrystals at the 0.5 and 1 mg/kg demonstrated a significant decrease in blood glucose level (mg/dL, p < 0.001, n = 8) compared to its counterparts. Rp nanocrystals at the 0.5 mg/kg demonstrated a significant decrease (p < 0.001, n = 8) in blood glucose compared to its counterparts at a dose of 1 mg/kg. The selected animal model's histological analyses and the effect of Rp nanocrystals on several internal organs were determined to be equivalent to those of the control animal group. The findings of the present study indicated that nanocrystals of Rp with improved anti-diabetic properties and safety profiles can be successfully produced using controlled microfluidic technology, an innovative drug delivery system (DDS) approach. [ABSTRACT FROM AUTHOR]

Indomethacin a Non-steroidal anti-inflammatory drug (NSAID) demonstrates low bioavailability. To counter the problem an attempt was made by preparing indomethacin nanocrystals in a micro-channel fluid reactor using different concentrations of the polymers. Indomethacin crystals were optimized by determining the particle size of 380 nm ± 5.0 with PDI of 0.29±0.05. The crystalline nature was confirmed with the help of Powder X-Ray diffraction and Differential scanning calorimetry. A high antisolvent volume (2.0/0.5ml/min), low inlet angle (10°) and mixing time of 60 min with 15 min sonication at a high rate of stirring were the key parameters that produced Indomethacin nanocrystals with good particles size. A high anti-solvent volume (2.0/0.5ml/min), low inlet angle (10°) and mixing time of 60 min with 15 min sonication at a high rate of stirring were the key parameters that produced Indomethacin nanocrystals with good particle size. Similarly, the polymeric combination of including Polyvinylpyrrolidone k-30 (1%)- Hydroxypropyl methyl cellulose-15cps (0.5%) and Sodium lauryl sulfate (0.5%) were the appropriate concentrations. The Transmission electron microscopy and Scanning electron microscopy studies demonstrated the homogeneity with a distinct crystalline structure. The stability study displayed stability at 4°C and 25°C. The nanocrystals exhibited a dissolution rate correlated to the marketed and unprocessed drugs. [ABSTRACT FROM AUTHOR]

The antidiarrheal effect of methanolic extract of Trillium govanianum Wall. ex D. Don (Melanthiaceae alt. Trilliaceae) was studied at doses of 12.5, 25, and 50 mg/kg in different animal models of diarrhea including castor oil (6 mL/kg), magnesium sulfate (2 gm/kg), sodium picosulfate (2 mL/kg) and lactitol (0.25 mL/kg). The antispasmodic effect of T. govanianum was studied on isolated rabbit's jejunum, using acetylcholine as tissue stabiliser and verapamil as calcium channel blocker. T. govanianum attenuated the diarrhea by producing a significant decrease in the number and weight of stool, and an increase in stool latency time. T. govanianum completely inhibited both spontaneous as well as high potassium induced contractions of isolated rabbit's jejunum, which was analogous to verapamil. Moreover, T. govanianum produced a right shift in calcium concentration response curve, confirming its calcium channel blocking activity. These findings provide scientific ground to its medicinal use in diarrhea and gut spasms. [ABSTRACT FROM AUTHOR]

Moxifloxacin and gemifloxacin were tested on isolated rabbits' jejunal preparations as little is known about its effects on gastrointestinal tissues. Moxifloxacin and gemifloxacin were tested in concentrations 0.01-10µg/mL for possible effect(s) on isolated rabbits' jejunal preparations. The drugs were applied on spontaneous, on low K+ (20mM)-induced contractions and on high K+ (80mM)-induced contractions. Response was plotted as % of its respective controls. EC50 for Moxifloxacin and Gemifloxacin on spontaneous (without Glibenclamide) contractions are 2.83±0.5µg/mL and 1.11±0.2µg/mL, respectively. Moxifloxacin and Gemifloxacin relaxed the low K+ (20mM) -induced contractions, which were inhibited in presence of Glibenclamide (3µM). Our result indicates that the relaxant activity of Moxifloxacin and Gemifloxacin is mediated possibly through activation of ATP-sensitive potassium channels (KATP). The relaxant effect of Moxifloxacin and Gemifloxacin is predominantly mediated by activation of ATP-Sensitive potassium channels (KATP), which could be cause of one of relaxing mechanisms. [ABSTRACT FROM AUTHOR]

Antibiotics are key drugs which are used for the treatment of infectious disease and are among the drug that are most frequently prescribe in pediatric patients. This study was designed to assess antibiotics utilization patterns in pediatric ward of a tertiary care teaching unit, Peshawar. Study Design: A retrospective cross sectional study. Setting: Pediatric ward by evaluating antibiotics utilization patterns in pediatric ward of a tertiary care teaching unite, Peshawar. Period: January, 2017 up to March, 2017. Materials and Methods: There were 219 patients included in the study. In this study, the major medical conditions for which antibiotics were prescribed include pneumonia (23.28%). Results: The most commonly used antibiotics were ceftriaxone, 46.21%, while the most commonly prescribed multiple antibiotics were ceftriaxone plus ampicillin (21.9%) followed by Ceftriaxone & Metronidazole. The average number of antibiotics per prescription was 1.75. At least 114 (52%) patients were prescribed with single antibiotic and patients prescribed with two antibiotics were 72 (32%). There was a high rate of parental administration which account for about 92.26% of the total antibiotic prescribed. It is assessed that 26.89% of total drugs were prescribed by generic name which were extremely lesser than the medication prescribed with brand names 73.10%. Conclusion: From the result we concluded that third generation cephalosporin especially ceftriaxone was most frequently prescribed antibiotic in hospitalized children. [ABSTRACT FROM AUTHOR]

OBJECTIVES: To assess and evaluate prescription pattern and prescription errors using World Health Organization (WHO) drug use indicators in the medical ward of Leady Reading Hospital, Peshawar, Pakistan. METHODS: This retrospective study of 200 in-patient's prescriptions was conducted to investigate the WHO drug use indicators (average number of drugs prescribed per prescription, percentage of prescriptions encounter with an injection(s) prescribed, percentage of prescriptions encounter with an antibiotic(s) prescribed, percentage of drugs prescribed with generic names, percentage of drugs prescribed from the WHO's Essential Drug List (EDL), drugs prescribed from the National Essential Drug List (NEDL) and prescriptions errors. RESULTS: Drugs prescribed for 200 admitted patients were 1410 and average number of drugs prescribed per prescription were 7.05 (n=1410). Prescriptions with an injection(s) prescribed were 704/1410 (49.9%), prescriptions with an antibiotic(s) prescribed were 241/1410 (17.1%), prescriptions with drugs prescribed by generic names was none. Number of drugs prescribed from the WHO EDL were 704 (49.9%). NEDL was not available. A total of 572 (40.6%) errors in prescription writing were observed including 211/572 (36.9%) errors having absent strength of drugs, 267/572 (46.7%) contains an illegible hand writing prescriptions, 48(n=572; 8.4%) prescriptions have missing frequency of drugs and 46 (n=572; 8.04%) prescriptions had improper abbreviations. Decision errors were observed in 703 (n=1410;49.86%) cases for drug-drug interactions. CONCLUSION: Illegible hand writing, absence of strength of drugs, no mentioning of frequency of drugs and improper abbreviations were main types of prescription errors while error in drug-drug interactions was the main decision error in our study. [ABSTRACT FROM AUTHOR]

Bisthiourea derivatives were synthesized by the reaction of benzoylisothiocyanate and diamines to give 1,2- Bis(N'-benzoylthioureidobenzene (1), 1,3-di(benzoylthioureido)benzene (2) and 1,4-di(benzoylthioureido)benzene (3) in acetone. Acute toxicity study revealed that LD50 of compound (1) and (3) is 120 mg/kg body weight. Visceral pain induced by injecting i.p acetic acid in mice were strongly inhibited by all the compounds. 94.65, 95.25 and 85.54% analgesic activity were observed in compounds (1), (2) and (3) at 15 mg/kg and (2) and (3) shows 97.63 and 96.42% at 30 mg/kg body weight respectively while (1) gives 100% analgesic activity. 100% cytotoxicity was observed in compounds (2) and (3) and 96% in compound (1) at 750 ppm. The results suggest that these compounds may have potential values for treatment of cancer and painful disorders. [ABSTRACT FROM AUTHOR]

OBJECTIVE: to determine the prescription pattern of drug for hospitalized patients with diabetes mellitus (DM) attending a tertiary care hospital, Peshawar, Pakistan. METHODS: This retrospective study was conducted from January 2015 to February 2015 in the department of endocrinology of tertiary care private sector hospital, Peshawar, Pakistan. During 2 months study period, 354 prescriptions were collected and analyzed. Prescriptions written for all DM patients of any gender, socio-economic status, religion specificity and ethnicity were included. RESULTS: Out of 354 patients, 209 (59%) were female and 145 (41%) were males; majority age group was 60-69 years. Most common concurrent disease with DM was hypertension (31.63%). The maximum time spent by diabetic patients in hospitals was 3-days (27.15%). The most prescribed drugs were cardiovascular drugs (21.80% in females and 26.11% in males) followed by antibiotic (16.02% in females and 17.04% in males patients). Most common prescribed dosage form to female diabetic was tablet (46.19%) and to male diabetics was injection (45.84%). The most frequently prescribed anti-diabetic drug as a monotherapy was insulin (29.66%), two-drug combination was sitagliptin+metformin (8.47%), three-drug drug combinations were insulin+sitagliptin+metformin (5.08%) and four drug combinations were insulin+vildagliptin+metformin+pioglitazone (0.84%). The most frequently antibiotic prescribed for the management of diabetic foot was ceftriaxone (14.45%). CONCLUSION: In our study, most prescribed antihyperglycemic monotheray drug for hospitalized diabetic patient was insulin and two-drug combination drugs were sitagliptin+metformin. The most commonly drugs prescribed apart from anti-diabetic were cardiovascular drugs followed by antibiotics. [ABSTRACT FROM AUTHOR]

This study is carried out to assess the effects of rosuvastatin and simvastatin on blood vessels for possible vasorelaxant effect. The study is also translating the possible vasorelaxant effect in Wistar rats for a subsequent fall in systolic blood pressure. It is evident from the EC 50 , that rosuvastatin is more effective on relaxing N.E induced contractions, while simvastatin is more effective on relaxing KCL induced contractions. Simvastatin is equipotent when compared to effects of amlodipine on KCl induced contractions in denuded aortae. Simvastatin produced significant right shift in test concentration 1.1× 10 -6 M with its respective EC 50 -1.85logCa ++ M as compared to its respective control EC 50 -3logCa ++ M. Rosuvastatin also produced significant right shift in the EC 50 . In conclusion, it is stated that rosuvastatin and simvastatin relax the aortic strips preparations through inhibition of voltage gated calcium channels and inhibition of N.E induced contractions. Rosuvastatin and simvastatin have additive effects when used in the presence of a standard vaso-relaxant drug like amlodipine, which further confirms its additive effect on decreasing the systolic blood pressure of hypertensive rats (P<0.05).