Zhou X J, Zhou-Pan X R, Favre R, Rahmani R
INSERM U278, Faculté de Pharmacie, Marseille, France.
Biopharm Drug Dispos. 1994 Oct;15(7):577-86. doi: 10.1002/bdd.2510150705.
A study was carried out in 14 cancer patients to assess the relative bioavailability of two oral formulations of navelbine. A single 130 mg oral dose of the drug was given according to a randomized two-way crossover design as two capsules: one contained the drug in powder (formulation A, reference); another contained the drug in solution (formulation B). A 7 d washout period separated each dose. Navelbine was rapidly absorbed after administration of either formulation and exhibited a biphasic concentration decay pattern. The peak plasma level was reached within 2 h of administration in most patients. Formulation B resulted in better navelbine absorption with respect to peak plasma concentration (Cmax) and area under the plasma concentration-time curves (AUC) than did formulation A as ascertained by analysis of variance (ANOVA). The relative bioavailabilities (solution versus powder) were, respectively, 286.0% and 268.0% as estimated from experimental (0-72 h) and extrapolated (0-infinity) AUC.
对14名癌症患者进行了一项研究，以评估两种口服长春瑞滨制剂的相对生物利用度。按照随机双向交叉设计，以两粒胶囊的形式给予单次130mg口服剂量的药物：一粒胶囊含有粉末状药物（制剂A，参比制剂）；另一粒胶囊含有溶液状药物（制剂B）。每次给药间隔7天的洗脱期。给予任一制剂后，长春瑞滨均迅速吸收，并呈现双相浓度衰减模式。大多数患者在给药后2小时内达到血浆峰浓度。通过方差分析（ANOVA）确定，制剂B在血浆峰浓度（Cmax）和血浆浓度-时间曲线下面积（AUC）方面的长春瑞滨吸收情况优于制剂A。根据实验（0 - 72小时）和外推（0 - 无穷大）AUC估算，相对生物利用度（溶液剂相对于粉剂）分别为286.0%和268.0%。
