盐酸吡格列酮胶囊生物等效性研究

Studies on bioequivalence and relative bioavailability of pioglitazone hydrochloride capsule in healthy volunteers

目的 研究盐酸吡格列酮胶囊在健康人体内的药动学和相对生物利用度 ,进行生物等效性评价。方法 2 0名男性健康志愿者双周期随机交叉单剂量 po盐酸吡格列酮片剂和胶囊 30mg ,服药间隔为 1周 ,采用高效液相色谱法测定血浆中吡格列酮浓度。结果 两种制剂主要药动学参数无显著性差异 ,片剂和胶囊的cmax分别为 (1172 .4 3± 347.0 1)和 (110 8.8± 375 .5 5 )μg·L-1;tmax分别为 (2 .16± 0 .89)和 (1.79± 1.10 )h ;t1/2 分别为 (7.75± 1.79)和 (8.2 0± 2 .10 )h ;AUC0～tn分别为 (12 2 6 8.0 1± 35 4 2 .93)和 (116 2 3.17± 4 0 38.6 5 ) μg·h·L-1。盐酸吡格列酮胶囊的相对生物利用度为 (94 .4 8± 15 .78) %。结论 方差分析和双向单侧t检验结果表明两种制剂具有生物等效性。

OBJECTIVE: To evaluate the bioequivalence and relative bioavailability of pioglitazone hydrochloride capsule in healthy volunteers. METHOD: 20 healthy male volunteers were randomized into A and B groups. A single dose (30 mg) of pioglitazone hydrochloride capsules and tablets were given respectively according to an open 2-way crossover study design. The washout period was 1 week. The plasma concentrations of pioglitazone were determined by HPLC method. RESULTS: The pharmacokinetic parameters of pioglitazone hydrochloride tablets and capsules were as follows: cmax (1 172.43 ± 347.01) and (1 108.8 ± 375.55) μg&middot L-1; tmax (2.16 ± 0.89) and (1.79 ± 1.10) h; t1/2(7.75 ± 1.79) and (8.20 ± 2.10) h; AUC0∼tn(12268.01 ± 3 542.93) and (11 623.17 ± 4 038.65) μg&middoth&middotL-1, respectively. The relative bioavailability of pioglitazone hydrochloride capsule was (94.48 ± 15.78) %. CONCLUSION: The results of variance analysis and two one-side t test showed that the two formulations were of bioequivalence.