The bioequivalence of two different tablet formulations containing losartan potassium 100 mg was determined in healthy volunteers after a single oral dose in a randomized crossover study. Test and reference products were administered to 60 volunteers with 240 ml water after overnight fasting. Plasma concentrations of losartan and its active carboxylic acid metabolite were monitored over a period of 36 h after drug administration by validated LC/MS/MS analytical method. The pharmacokinetic parameters Cmax, AUC0-t, AUC0-∞, AUC0-t/AUC0-∞, tmax, Kel and t½ were determined from plasma concentration time profile of both formulations for losartan and its active metabolite losartan carboxylic acid and were found to be in good agreement. The carboxylic acid metabolite was considered for profiling purpose only. The analysis of variance did not show any significant difference between the two formulations and 90% confidence intervals for the ratio of Cmax (84.89-104.09%), AUC0-t (95.84-102.84%) and AUC0-∞ (96.43-103.25%) values for losartan between the test and reference products were within the 80-125% interval, satisfying the bioequivalence criteria of the US FDA guidelines. These results indicate that the test and the reference products of losartan potassium are bioequivalent and, thus, may be prescribed interchangeably.
Pyrazinamide is a widely used drug for the treatment of tuberculosis. A 150 mg Dispersible Tablet (DT) formulation of the drug was prepared by Micro Labs, a generic drug company. The formulation was developed for easy administration into paediatric patients. It was tested for bioequivalence in healthy adult human volunteers in fasting condition. A total of 36 subjects were enrolled in the study and all the 36 subjects completed both the two periods of the study without showing major adverse events. The pharmacokinetic parameters determined for bioequivalence were Cmax and AUC0-t. The two parameters were within the limit of bioequivalence criteria. The 150 mg DT formulation developed by Micro Labs was found to be bioequivalent to 500 mg immediate release tablet formulation of Riemser Pharma. Both the formulations were safe and well tolerated among the tested human subjects. No major adverse events were observed.
A simple, sensitive, and selective LC-MS/MS method was developed and validated for the quantification of carbocisteine in human plasma. Rosiglitazone was used as the internal standard and heparin was used as the anticoagulant. The chromatographic separation was performed by using the Waters Symmetry Shield RP 8, 150 × 3.9 mm, 5 μ column at 40°C with a mobile phase consisting of a mixture of methanol and 0.5% formic acid solution in a 40:60 proportion. The flow rate was 500 μl/min along with a 5 μl injection volume. Protein precipitation was used as the extraction method. Mass spectrometric data were detected in positive ion mode. The MRM mode of the ions for carbocisteine was 180.0 > 89.0 and for rosiglitazone it was 238.1 > 135.1. The method was validated in the concentration curve range of 50.000 ng/mL to 6000.000 ng/mL. The retention times of carbocisteine and the internal standard rosiglitazone were approximately 2.20 and 3.01 min, respectively. The overall run time was 4.50 min. This method was found suitable to analyze human plasma samples for the application in pharmacokinetic and BA/BE studies.
Levomilnacipran is a drug used to treat depression. Micro Labs is a generic drug company which had developed an extended release formulation of Levomilnacipran 120 mg capsule. Two studies were conducted to assess the safety, tolerability and bioequivalence of the extended release formulation of 120 mg Levomilnacipran capsules. A total of 42 subjects had been included for each of the fasting and fed studies. Out of them, 30 subjects completed the fasting study and 28 subjects completed the fed study. Pharmacokinetic parameters like Cmax, AUC0-t, AUC0-inf, Tmax, Kel, t1/2 and %AUCextra were calculated for Levomilnacipran in order to compare the bioavailability of the test and reference formulations. The studies were conducted in healthy human volunteers in both fasting and fed conditions as per the US regulatory requirements for conduct of bioequivalence studies. The formulations were found to be bioequivalent to each other. Vomiting was observed as a major adverse reaction.
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