Pharmacokinetic and bioequivalence studies of immediate release diclofenac potassium tablets (50mg) in healthy volunteers.

This study was conducted with the aim to determine the pharmacokinetic and bioequivalence of diclofenac potassium 50 mg test (F4) tablet formulation with reference product (Caflam). Present study was single dose, randomized, two phase cross over design, conducted in 12 healthy Pakistani volunteers and planned in accordance with FDA guidelines. In this study a simple, selective, sensitive and reproducible HPLC procedure was developed and validated for the estimation of diclofenac potassium in plasma. The process was validated in the range of 50 - 0.05 µg.mL-1 and used in bioequivalence trial of two products. Multiple blood samples were collected at various time points (0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12 and 14 hr after treating volunteers with test (F4) and marketed reference brand. Plasma separation and deproteination were carried out with acetonitrile; samples (20µL) were injected using the validated HPLC method. Various pharmacokinetic parameters (compartmental and noncompartmental) were estimated using KineticaTM 4.4.1 (Thermo Electron Corp. USA). Bioequivalence among the products was established by calculating the 90% CI with log and non log transformed data for Cmaxcalc, Tmaxcalc, AUC0-∞, AUCtot and AUClast using two way ANOVA and Schirmann's Two one sided t- test. No significant difference was found between log and non-log data. The 90% confidence interval values using log transformed data for AUC0-∞ (0.997-1.024), AUCtot (1.004-1.031), AUClast (0.997 -1.024), Cmaxcalc (0.994-1.007) and Tmaxcalc (0.996-1.013) for the trial and reference products were found within the FDA acceptable limits of 0.8-1.25. Results were further verified by the Schirmann's one-sided t test. Results showed the bioequivalence of test and reference formulations. Both the products were well tolerated.

Antimalarial and insecticidal activities of newly synthesized derivatives of Benzimidazole.

The bioactive benzimidazole and corresponding substituted phenacyl halides has been synthesized (11) new derivatives out of three compounds 8, 10 and 11 were found to inhibit the Plasmodium falciparum moderately after 72 hours of incubation hence acting as antimalarial agents. While these derivatives were exhibited negligible insecticidal activity too when analyzed by impregnated filter paper method.

Antidepressant effect and categorization of inhibitory activity of monoamine oxidase type A and B of ethanolic extract of seeds of Trigonella foenum graecum Linn.

Trigonella foenum- graecum Linn (Fabaceae) is an annual aromatic herb and no wit is cultivated globally like in Pakistan, Egypt, India, Middle East etc. Traditionally it was used in anorexia, as febrifuge, to soothe gastritis and gastric ulcers, as a galactagogue and as condiment, hypoglycemic agent and employed in various as nervous disorders. The study aimed to investigate the antidepressant effect of ethanolic extract of seeds of Trigonella foenum graecum and underlying mechanism of action. For assessment of antidepressant activity Forced Swimming Test (FST), Tail Suspension Test (TST), Monoamine (MAO) Assay and Locomotor Activity Test were studied. Acute toxicity, Rota Rod and Grip Strength Tests were also performed. The significant declining in immobility time as compared to control was shown in Forced swimming test as compared to tail suspension test. Considerable change was not found in open field test (OFT). EtOH extract of seeds of fenugreek represent maximum significant reduction which was 30 and 24.65% in MAO- A and B activity respectively in the rat's whole brain as compared to control animals in Monoamine oxidase (MAO) assay. All tested doses were found ineffective in impairment of muscle coordination in Rota rod and in grip strength related to muscle relaxant property. According to experimental findings it is revealed that ethanolic extract of seeds of Trigonella foenum graecum showed antidepressant effect by inhibiting the activity of MAO-A and B.

Antihyperglycemic and hypolipidemic effects of Hibiscus schizopetalus (Mast) Hook in alloxan-induced diabetic rats.

The antihyperglycemic and hypolipidemic activities of Hibiscus schizopetalus (Mast) Hook (Malvaceae) flower and leaves extracts were investigated in alloxan-induced diabetic rats. The hypoglycemic activity of both the extracts (100mg/kg, body weight) was tested in fasting normal rat, glucose loaded rats. Observation on body weight was also recorded. The extracts showed a significant (p<0.001) reduction in blood glucose level in normal fasting rats. In glucose tolerance test, significant (p<0.01) decreased observed in all glucose loaded animals. While in alloxan induced diabetic rats, the percent blood glucose reduction was 59.94% and 45.14% in extracts treated groups. The results obtained were compared with the reference standard drug Tolbutamide (100mg/kg, body weight). The diabetic rats showed sign of decreased in their body weight during the treatment period. Cholesterol and triglycerides levels were significantly decreased (p<0.001) by HFE. The results obtained demonstrated the potential hypoglycemic activity of methanolic extracts of H. schizopetalus. There is need of bioassay-directed assay of the active principles responsible for the anti-diabetic activity. The methanolic extracts showed the presence of carbohydrates, alkaloids, steroids, terpenes, saponins and glycosides.

Antidepressant activity of ethanolic extract of Hibiscus rosa sinenesis Linn.

The present study was undertaken to assess the antidepressant effect of crude ethanolic extract of floral part of Hibiscusrosa sinensis (HRS) at doses 100mg/kg, 250mg/kg and 500mg/kg using three parameters which are forced induced swimming test (FST), tail suspension test (TST) and open field test(OFT). Flouxetine (15mg/kg, body weight) was used as standard. Significant dose dependent decline in immobility time was observed in all the three doses in FST and TST while in case of OFT none of the dose of HRS exhibited effectual results. To determine MAO"A" and MAO"B" activity HRS extract was used and the results revealed that each dose of this plant exhibited marked effect on MAO"A", while on MAO"B" only 250mg/kg dose was found significant.