Bioequivalence study of two perindopril erbumine tablet formulations in healthy volunteers
| Autor: | Arini Setiawati, Siti Hawa Deniati, Joan Aprilla Arland, Danang Agung Yunaidi, Lai Yeo Lian, Effi Setiawati, Lucia Rat Handayani, Iwan Dwi Santoso |
|---|---|
| Rok vydání: | 2011 |
| Předmět: |
Adult
Male Chemistry Pharmaceutical Cmax Angiotensin-Converting Enzyme Inhibitors Pharmacology Bioequivalence Body Mass Index Young Adult Pharmacokinetics Tandem Mass Spectrometry Drug Discovery Perindopril Erbumine Perindopril medicine Humans Single-Blind Method Chromatography High Pressure Liquid Cross-Over Studies Chemistry Middle Aged Perindoprilat Crossover study Bioavailability Therapeutic Equivalency Area Under Curve Female Algorithms Half-Life Tablets medicine.drug |
| Zdroj: | Arzneimittelforschung. 61:234-238 |
| ISSN: | 1616-7066 0004-4172 |
| DOI: | 10.1055/s-0031-1296193 |
| Popis: | The present study was performed to compare the bioavailability of two perindopril erbumine (CAS 107133-36-8) 4 mg tablet formulations (test formulation and reference formulation). This study was a randomized, single-blind, two-period, two-sequence cross-over study which included 20 healthy adult male and female subjects under fasting conditions. In this study, one subject withdrew from the study and one reserve subject did not appear at both periods. The pharmacokinetic parameters were assessed based on the concentrations of perindopril (CAS 82834-16-0) and perindoprilat (CAS 95153-31-4) because perindopril has litte pharmacologic activity until hydrolized in the liver into its active metabolite, perindoprilat. The blood samples from 18 subjects were analyzed for plasma concentrations of perindopril and perindoprilat. In each of the two study periods (separated by a washout of three weeks) a single dose of test or reference drug was administered. Plasma concentrations of the drug were determined by LC-MS/MS method. The pharmacokinetic parameters assessed in this study were area under the plasma concentration-time curve from time zero to 192 h (AUC), area under the plasma concentration-time curve from time zero to infinity (AUCinf), the peak plasma concentration of the drug (Cmax time needed to achieve the peak plasma concentration (tmax), and the elimination half-life (t(1/2)). The geometric mean ratios (90% CI) of the test drug/reference drug for perindopril and perindoprilat were 106.59% (92.97-122.20%) and 100.56% (94.11-107.46%) for AUC,, 106.64% (93.39-121.77%) and 100.88% (95.30-106.80%) for AUCinfo, and 101.23% (87.39-117.27%) and 99.30% (90.42-109.05%) for Cmax, respectively. The 90% confidence intervals calculated for AUCt and Cmax of perindopril and perindoprilat were within the standard bioequivalence range (80-125% for AUC and Cmax). It was concluded that the two perindopril erbumine tablets (test and reference drug) were bioequivalent in terms of the rate and extent of absorption. |
| Databáze: | OpenAIRE |
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