噻氯匹定胶囊的药代动力学及其生物等效性评价

PHARMACOKINETICS AND BIOEQUIVALENCE ASSESSMENTOF TICLOPIDINE CAPSULE

１０名健康志愿者，随机交叉口服单剂量噻氯匹定胶囊或片剂，采用ＨＰＬＣ测得血浆中药物浓度分别在２．９４±１．０２和２．４１±０．６５ｈ达到峰值２２５３．３±６６４．１和２０５４．５±３３７．６μｇ／Ｌ。两种制剂的消除相半衰期分别为１２．６±１．５５和１２．９±２．１９ｈ；ＡＵＣ分别为１６９１８．２±２６７３．７和１７２１７．３±２８５１．７μｇ·ｈ·Ｌ－１。药时曲线符合一级吸收的二室模型。以进口噻氯匹定片为标准，算得国产噻氯匹定胶囊的相对生物利用度为９８．５±７．８２％，经双单侧ｔ检验，两种制剂具有生物等效性。

The pharmacokinetics of ticlopidine was determined following a single oral dose of 500 mg given to each 10 volunteers in an open randomized crossover study. Drug concentration in blood was assayed by HPLC method. The peak levels in blood averaged 2253.3±664.1 and 2054.5±337.6 μg/L at 2.94±1.02 and 2.41±0.65 h, and the mean terminal elimination half-lives were 12.6 ±1.55 and 12.9±2.19 h for domestic capsule and imported tablet respectively; The areas under the drug concentration curve were 16918.2±2673.7 and 17217.3±2851.7 μg·h·L-1 domestic capsule and imported tablet respectively. The concentration-time course after medication conformed to a 2-compartment open model with a first order absorption. The relative bioavailability of domestic capsule of ticlopidine was 98.5±7.82 %. The results of two one-sided tests showed that the two formulation were bioequivalent.