司巴沙星胶囊在正常人体内的药动学及生物等效性评价

Pharmacokinetics and Bioequivalence of Sparfloxacin in Healthy Subject

１２名健康志愿者，随机交叉口服单剂量（２００ｍｇ）国产司巴沙星胶囊和国外司巴沙星片，采用ＨＰＬＣ测得血浆中药物浓度分别在５．２８±１．８３，５．５６±２．３４ｈ达到峰值７１１．７±１１６．３，７５１．８±９５．９ｎｇ／ｍｌ。两种制剂的消除相半衰期分别为１４．１±４．９４，１５．２±２．１５ｈ；血药曲线下面积分别为２０５７６．９±４３９５．４，２１３７８７±３８８４２ｎｇ·ｈ／ｍｌ。药时曲线符合一级吸收的一室模型。以国外片为标准，算得国产司巴沙星胶囊的相对生物利用度为９６．１±１０．４％，经双单侧ｔ检验，两种制剂具有生物等效性。

The pharmacokinetics of sparfloxacin was determined following a single oral dose of 200 mg given to each 12 volunteers in an open randomized crossover study. Drug concentration in plasma was assayed by HPLC method. The peak levels in plasma averaged 711.7±116.3 and 751.8±95.9 ng/ml at 5.28±1.83和5.56±2.34 h, and the terminal elimination half lives were 14.1±4.94 and 15.2±2.15 h for capsule and tablet respectively, and the areas under the drug concentrationtime curves were 20576.9±4395.4 and 21378.7±3884.2 ng·h/ml。for the two formulations. The concentration-time courses after medication conformed to a 1compartment open model with a first order absorption. The pharmacokinetics of the two formulations of Sparfloxacin was similar and the result of statistical analysis showed that the two formulations were bioequivalent.