奥沙普秦肠溶胶囊与片在中国健康者的药物动力学及相对生物利用度

Oxaprozin enteric capsules vs tablets on pharmacokinetics and bioavailability in Chinese healthy men

目的：了解国产奥沙普秦肠溶胶囊在人体的药物动力学及相对生物利用度。方法：采用随机交叉试验设计，１０例男性健康者单剂量口服奥沙普秦肠溶胶囊与片剂 ６００ ｍｇ，以 ＨＰＬＣ法测定血药浓度。结果：胶囊与片剂各项动力学参数为：（１）ＡＵＱＯ ——（７５７２±ｓ ６９５） ｍｇ· Ｌ－１与（８２０１± ９４９）ｍｇ．Ｌ－１．ｈ－１；（２）Ｔ １／２－（５９±７） ｈ与（５３±４ ） ｈ ，上述２参数经ｔ检验；差别无统计学意义（Ｐ＞０． ０５）；（３） Ｃｍａｘ－－（８３± １５）ｍｇ．Ｌ－１与（１２６± ２１）ｍｇ·Ｌ－１；（４） Ｔｍａｘ－（１５± ７） ｈ与（４± ３） ｈ，经方差分析，均 Ｐ＜ ０． ０５，符合肠溶制剂原有性质。胶囊的相对生物利用度为（９３± １３）％，经双向单侧 ｔ检验作统计学分析，（Ｐ＞０．０５）。结论：胶囊与片剂两者之间具有生物等效性。

AIM: To study the pharmacokinetics and relative bioavailability of oxaprozin enterosoluble capsule in Chinese healthy men. METHODS: Ten male Chinese helthy men received po 600 mg oxaprozin enterosoluble capsule or tablet in a random crossover design. Drug concentrations in serum were determined by high pressure liquid chromatography. The pharmacokinetic parameters were calculated with 3P87 software. RESULTS: Time course of serum concentrations conformed to one compartment model. The pharmacokinetic parameterss of capsule and tablet were as follows: (1) AUC (7572 +- 695) mg.L-1. h-1 and (8201+- 949) mg.L-1 .h-1. (2) T1/2 (59 +- 7) h and (53 +- 4) h. (3) Cmax(83 +- 15) mg. L-1 and (126 +-21) mg.L-1. (4)Tmax(15+-7) h and (4 +- 3) h, respectively. There was no significant differences in AUC and T1/2 between the two preparations (P > 0. 05 ). The relative bioavailability of oxaprozin enterosoluble capsule was (93 +- 13 )%. CONCLUSION: The results suggest the capsule has a equal bioavailability with tablet.