盐酸曲普利啶的人体药代动力学及相对生物利用度

Pharmacokinetics and Relative Bioavailability of Triprolidine Hydrochloride Capsulesand Tablets in Healthy Volunteer

目的:测定盐酸曲普利啶的药代动力学及相对生物利用度。方法:18名健康男性志愿者,随机分为三组,采用三制剂、三周期的3×3拉丁方设计,单剂量口服5mg盐酸曲普利啶后,采用反相高效液相色谱法测定血浆药物浓度。结果:口服盐酸曲普利啶胶囊、片剂及对照药盐酸曲普利啶胶囊后血药浓度的达峰时间分别为1.9±0.2h,1.8±0.3和1.8±0.2h,峰浓度分别为40.3±5.6μg·L-1,40.4±4.9μg·L-1和40.6±4.6μg·L-1,药时曲线下面积分别为139.2±19.9μg·L-1,136.6±21.9μg·L-1和139.2±23.lμg·L-1。结论:结果表明盐酸曲普利啶胶囊和片剂均与对照药盐酸曲普利啶胶囊具有生物等效性,以盐酸曲普利啶胶囊为参比制剂,两药的相对生物利用度分别为101.0%±6.4%和98.4%±5.2%。

OBJECTIVE:To determine the pharmacokinetics and relative bioavailablityof triprolidine hydrochloride capsules and tab1ets. METHODS: The drugconcentrations in plasma were assayed by reverse-HPLC method following a singleoral of 5mg triprolidine hydrochloride capsule or tablet or the triprolidine contractcapsules, respectively, given to each of 18 male volunteers in a randomized cross-over test. RESULTS: The peak levels (Tmax) in plasma averaged 40.3±5.6μg.L-1,40.4±4.9μg.L-1 and 40.6±4.6μg.L-1 at l.9±0.2h, l.8±0.3h and l.8±0.2h,and the areas under the drug concentrations curves (AUC) were l39.2±9.9μg.L-l,l36.6±2l.9μg.L-1, and l39.2±23.lμg.L-1 for triprolidine hydrochloridcapsules, tablets and the triprolidine contract capsules, respectively.CONCLUTION: The results of statistical analysis showed that three formulationswere bioequivalent.