阿苯达唑自微乳化释药系统大鼠体内药代动力学的研究

Pharmacokinetics of self-microemulsifyingdrug delivery system albendazole in rat

目的:研究阿苯达唑自微乳化释药系统在大鼠体内的药代动力学。方法:通过高效液相色谱法,以阿苯达唑原料药和市售片剂做对照,对高低剂量口服阿苯达唑自微乳浓缩液进行大鼠体内相对生物利用度研究,利用DAS药动学软件对血药浓度数据进行处理。结果:血药浓度测定的方回收率均大于70%,日内、日间精密度良好;大鼠分别以38 mg/kg的剂量灌胃给予原料药、片剂和ABZ-SMEDDS后,大鼠体内血药浓度-时间曲线结果表明:SMEDDS的AUC分别是市售片剂和原料药的2倍和3倍多,且药时曲线的形状发生一定的改变。结论:自微乳系统可显著提高ABZ口服生物利用度。

Objective：The HPLC method was developed for the determination of Albendazole in mouse Plasma.pharmacokinetics of Albendazole Microemulsion in mouse after oral administration were investigated. Methods：The concentration of drug and metabolites in plasma was determined by HPLC,The rats plasma after double doses oral administration of ABZ-SMEDDS and conventional tablet,pharmaceutical product concentration and its metabolites were determined by HPLC.Compared with conventional tablet and pharmaceutical product,the Cmax,Tmax,AUC were determined by DAS pharmacokinetics software. Results：The recovery was over 70%,and the intra-day and inter-day RSD were less than 15%.The pharmacokinetic parameters of powder,conventional tablet and ABZ-SMEDDS were investigated after oral administration to rats at doses of 38mg/L and 76 mg/L.Compared with pure conventional tablet and pharmaceutical product,the relative bioavailability of SMEDDS were increased 2 and 3 times,The curve of plasma concentration versus time was changed. Conclusion：The SMEDDS resulted in a significant promote of ABZ for the oral bioavailability.