噁丙嗪胶囊剂人体药动学及生物利用度研究

Pharmacokinetic and Relative Bioavailability of Oxaprozin Capsule in Human

目的:探讨噁丙嗪胶囊剂人体药代动力学特征和相对生物利用度。方法:采用随机交叉法单次给予8名受试者噁丙嗪胶囊剂或片剂600mg后,于不同时间取血浆样本,高效液相色谱法测定受试者血浆中药物浓度,运用TopFit药动学软件的非房室模型拟合药时曲线,计算药代动力学参数及相对生物利用度。结果:统计学分析显示,两制剂的t_(1/2)、MRT、Cl和AUC_(0～∞)均无显著性差异(P>0.05)。药一时曲线呈双峰现象,可能与药物的肠肝循环有关。两制剂的达峰浓度Cp_1及Cp_2均差异显著(P<0.05)。结论:胶囊剂相对于片剂的生物利用度为121.06％,胶囊剂的吸收程度优于片剂,有利于临床治疗应用。

Aim: To investigate pharmacokinetic characteristics and relative bioavalability of oxaprozin capsule and was compared with tablet. Method: A single oral dose (600 mg) of oxaprozin capsule and table were administrated to eight healthy male volunteers according to a randomized, tow-way crossover design. The plasma concentrations of oxaprozin were determined by reverse HPLC. The concentration-time curves were fitted with TopFit pharmacokinetic program with non compartment model . The pharmacokinetic parameters and relative bioavailability were calculated. Results; The statistic analysis showed that t1/2, MRT, C1 and AUC0-∞ had no significantly different (P>0.05) between the two preparations. A double peaks was observed in the concentration-time curve. It might result from the hepatoenteral circulation. The peak concentrations Cpi or Cp2 were significantly different (P<0.05) in the two preparations. Conclusion; The relative bioavailabitity of oxaprozin capsule are 121.06% compared with oxaprozin tablet. Oxaprozin capsule seems to have a better advantage in the drug absorption than tablet. This characteristic is useful for the therapeutic application.