No abstract

Trimetazidine (CAS 5011-34-7) is an effective and well-tolerated antianginal drug that possesses protective properties against ischemia-induced heart injury. The relative bioavailability and pharmacokinetic characteristics of two modified release formulations of 35 mg trimetazidine, one as the test product (Metacard MR) and one as the reference product, were compared in healthy Bangladeshi male volunteers. The randomized, two-way crossover study was conducted in 24 healthy male volunteers after administration of a single 35 mg dose of each modified release formulation after 12-h overnight fasting, with a washout period of two weeks. Blood samples were collected at various time intervals following oral administration and analyzed for trimetazidine concentrations using a validated HPLC method. The pharmacokinetic parameters were determined by a non-compartmental method. After administering a single dose of 35 mg of each trimetazidine formulation, the obtained mean (SD) values for the test and reference products were 104.78 (29.3) and 98.57 (28.7) ng/ml for Cmax; 4.00 (1.1) and 3.54 (1.32) h for tmax; 423.81 (173.9) and 410.01 (195.87) ng ? h/ml for AUC0?12; and 472.51 (195.2) and 462.78 (225.13) ng ? h/ml for AUCo?? respectively. The mean t1/2 was found 3.69 (1.1) h and 3.45 (0.72) h for test and reference products respectively. From paired t-test, no significant differences were observed (p > 0.05) for any pharmacokinetic parameters. The 90% confidence intervals of the test/reference mean ratios of the In-transformed AUC0?12, AUC0?? and Cmax mean values were 106.19% (97.16%?116.06%), 104.74% (95.04%?115.42%) and 106.30% (95.23%?118.66%), respectively. The two formulations demonstrated similar bioavailability with respect to both the rate and extent of trimetazidine absorption.

In this study, three different self emulsifying drug delivery systems of rifampicin (SEDD-R) were made using oleic acid and different surfactants such as Tween 80, Chremophor RH 40 and Chremophor EL designated as RN-TW, RN-CRH and RN-CEL. These self-emulsifying systems were converted to rifampicin nanoemulsion by adding water under sonication. The resulting particle sizes were found to be 192. Antibacterial effect of the preparations was evaluated against S. epidermidis and S. aureus isolated from acne and showed effective results.

Abstract:Trimetazidine is an effective and well-tolerated antianginal drug. In the present study, a simple, sensitive and specific liquid chromatography (HPLC) method with UV detection was developed and validated for the quantification of trimetazidine in human serum samples using caffeine as internal standard. Protein precipitation method with methanol was employed in the extraction of trimetazidine and caffeine from biological matrix. The chromatographic separation was accomplished on Xterra C 18 Column with a mobile phase consisting 0.01 M potassium dihydrogen phosphate buffer (pH 4.16 ± 0.01 adjusted with orthophosphoric acid, with a solvent system of triethanolamine and acetonitrile (90:10) at a flow rate of 1.0 ml/min. The chromatogram was monitored at a wavelength of 207 nm. The method was validated over a linear concentration range of 5-200 ng/ml and limit of quantification (LOQ) was 5.0 ng/ml with a coefficient of correlation (r 2 ) ≥ 0.996. The intra-day and inter-day precision expressed as relative standard deviation was 3.40%-11.63% and 1.30%-10.21%, respectively. The average recovery of trimetazidine from serum was 97.44%. The method was successfully applied to a pharmacokinetic study after oral administration of modified release trimetazidine hydrochloride tablet (35 mg) in healthy Bangladeshi volunteers.