国产噁丙嗪颗粒剂与片剂人体生物利用度的比较研究

Comparative Study on Bioavailability of the Granules and Tablets of Oxaprozin

目的:对?丙嗪颗粒剂,以?丙嗪片剂为参比制剂,进行药代动力学和相对生物利用度的研究。方法:采用双交叉试验设计,用高效液相色谱(HPLC-UV)法测定不同时相的血药浓度。结果:10名健康志愿者口服颗粒剂及参比制剂600mg后所得的药时曲线均符合一室开放模型。?丙嗪颗粒剂与片剂的主要药代动力学参数分别为:t1/2k(h):44.04±5.76和42.14±5.31;Cmax(mg·L-1):30.09±2.78和29.81±2.63;Tmax(h):2.80±1.03和3.00±1.05;MRT(h):67.07±7.83和70.51±6.59;AUC0-∝(mg·h·L-1):1884.78±203.78和1822.67±267.64;这些参数经交叉试验下的方差分析法证明差异无显著性(P>0.05)。?丙嗪颗粒剂对片剂的相对生物利用度(F%)为:104.64±8.44。结论:两种制剂的药代动力学参数lnAUC、lnCmax、lnMRT经交叉试验下的方差分析和双单侧检验法检验证明?丙嗪颗粒剂与片剂具有生物等效性。

Objective:To compare the granulas of oxaprozin with the tablets of oxaprozin in terms of pharmacokinetics and bioavailability.Methods:A single 600 mg dose of the granules of oxaprozin or tablet of oxaprozin was administered orally to ten healthy male volunteers in a randomized crossover study. Plasma levels of oxaprozin were detected by HPLC UV method.Results:The pharmacokinetic parameters of the two formulations of oxaprozin (granules and tablets) read as follows: t1/2k(h):44.04±5.76 and 42.14±5.31;Cmax(mg·L-1):30.09±2.78 and 29.81±2.63;Tmax(h):2.80±1.03 and 3.00±1.05;MRT(h):67.07±7.83 and 70.51±6.59;AUC0-∝(mg·h·L-1):1 884.78±203.78 and 1 822.67±267.64. Conclusion:The relative bioavailability of oxaprozin granulas was 104.64±8.44. There was no significant difference between two formulations of oxaprozin in pharmacokinetic parameters(P >0.05). The granules of oxaprozin showed bioequivalence compared with the tablets by one two-sided test.