舍曲林胶囊和片剂的药动学及生物等效性

目的:研究舍曲林胶囊和片剂的药动学和相对生物利用度,评价其生物等效性。方法:健康志愿者 18名随机分3组,按三周期三交叉口服舍曲林试验胶囊和片剂与舍曲林参比制剂,剂量分别为100 mg,用高效液相色谱法测定血浆中舍曲林的浓度。计算相对生物利用度并评价试验制剂与参比制剂的生物等效性。结果:口服舍曲林胶囊、片剂和参比制剂后血浆中的舍曲林的c_(max)分别为(48±s 8),(44±8)和(46±8)μg·L-1; t_(max)分别为(4．7±1．3),(5．2±1．0)和(5．0±1．3)h;AUC_(0-120)分别为(1 372±426),(1 338±216)和(1 450± 370)μg·h·L~(-1);AUC_(0-∞)分别为(1 486±441),(1 462±216)和(1 573±391)μg·h·L~(-1)。胶囊制剂与参比制剂的相对生物利用度为(95 ±18)％,片剂与参比制剂的相对生物利用度为(96±18)％。结论:舍曲林胶囊和片剂与参比制剂具有生物等效性。

Pharmacokinetics and bioequivalence of sertraline capsules and tablets

AIM: To evaluate the bioequivalence of sertraline capsules and tablets by pharmacokinetios and relative biological availability in healthy volunteers. METHODS: A single oral doses (100 mg of capsules, tablets and reference formulation)were given separately to 18 healthy volunteers in three alternative periode for an open radomized three groups. The concentrations of sertraline in plasma were determined by HPLC, simulataneously with calculating the pharmacokinetics parameters and evaluating the bioavailability and bioequivalence of the formulations. RESULTS: After taking a single dose, the pharmacokinetics parameters for sertraline of capsules,tablets and reference formulation were as follows: c_(max) were (48±s 8), (44 ± 8) and (46± 8)μg·L~(-1); t_(max)were(4.7± 1.3), (5.2 ± 1.0) and(5.0± 1.3) h;AUC_(max) were (1 372± 426), (1 338±216) and (1 450± 370)μg·h·L~(-1);AUC_(0-x) were (1486± 441),(1 462± 216) and (1 573± 391) μg·h·L~(-1) respectively. The relative bioavailabilities of capsules to reference formulation and tablets to reference formulation were (95± 18) % and(96± 18) % respectively. CONCLUTION: The results of the statistic analysis showed that the tested sertra-line capsules and tablets were in bioequivalence with reference formulations.