中国临床药学杂志

目的评价国产盐酸曲美他嗪胶囊和进口盐酸曲美他嗪包衣片的人体生物等效性。方法20名健康男性受试者按两制剂两周期的交叉试验设计单剂量口服20mg的参比制剂和受试制剂后,采用LC-MS法测定血浆中盐酸曲美他嗪的浓度,使用DAS1.0软件计算药动学参数并进行生物等效性统计分析。结果参比制剂和受试制剂的ρmax分别为(55.9±9.2)和(56.4±12.2)μg·L-1;tmax分别为(2.5±0.8)和(2.7±0.9)h;AUC0→24h分别为(493.8±82.8)和(489.8±108.4)μg·h·L-1;AUC0→∞分别为(513.7±88.6)和(510.1±116.8)μg·h·L-1;t21分别为(4.8±0.4)和(4.7±0.4)h。双单侧t检验结果显示受试制剂的ρmax、AUC0→24h的90%置信区间分别为参比制剂相应参数的92.0%～108.4%和91.5%～105.3%,受试制剂的相对生物利用度为(99.6±16.5)%(以AUC0→24h计算)。结论国产盐酸曲美他啶胶囊与其进口包衣片具有生物等效性。

AIM To study the relative bioavailability and bioequivalence of domestic trimetazidine hydrochloride capsules in healthy subjects.METHODS In a randomized two-period reference and test crossover study,20 healthy male volunteers were given a single oral dose of 20 mg trimetazidine hydrochloride.The concentration of trimetazidine hydrochloride in plasma were determined by LC-MS.The pharmacokinetic parameters were processed by DAS program for statistic analysis.RESULTS The pharmacokinetic parameters of the test capsules and reference tablets were as follows:ρmax were(56.4±12.2)and(55.9±9.2)μg·L-1;tmax were(2.7±0.9)and(2.5±0.8)h;AUC0→24h were(489.8±108.4)and(493.8±82.8)μg·h·L-1;AUC0→∞ were(510.1 ±116.8)and(513.7±88.6)μg·h·L-1;t12 were(4.7±0.4)and(4.8±0.4)h,respectively.The relative bioavailability of the test preparations was(99.6±16.5)%.The 90% confidential interval of ρmax and AUC0→24h was between 92.0%-108.4% and 91.5%-105.3% of those of reference tablets.CONCLUSION The domestic trimetazidine hydrochloride capsules are bioequivalent to the imported trimetazidine hydrochloride tablets.