中文摘要：

目的：考察自制大黄酸肠溶缓释微丸在家兔体内的药动学过程,将其与大黄酸海藻酸钠溶液在兔体内大黄酸的药动学行为作比较,以明确该缓释制剂在体内的药动学特征,并对其相对生物利用度进行初步研究。方法：采用双周期交叉设计,按大黄酸量10只家兔单剂量口服35 mg·kg-1。自制大黄酸肠溶缓释微丸和大黄酸的海藻酸钠溶液,分别于服药前、服药后0.5,1,2,3,4,6,8,9,10,12,14,24,28,32,36 h采血,以高效液相色谱法测定大黄酸不同时间点的血浆浓度,并进行统计学处理。结果：两种制剂在家兔体内的药-时曲线中自制的大黄酸肠溶缓释微丸：tmax（9.73±0.68）h,Cmax（3.00±0.81）g·L-1,AUC0～∞（59.21±4.35）mg·L·h-1,MRT（21.12±1.12）h;参比制剂：tmax（4.17±0.12）h,Cmax（2.71±0.74）g·L-1,AUC0～∞（39.72±3.11）mg·L·h-1,MRT（9.33±2.08）与参比制剂相比,自制大黄酸肠溶缓释微丸的达峰时间更晚,峰浓度更大,两制剂间有显著性差异（P〈0.05）。结论：自制大黄酸肠溶缓释微丸生物利用度优于参比制剂。

英文摘要：

Objective：To study the pharmacokinetics and bioequivalence of self-prepared rhubarb acid enteric-coated sustained-release pellets,and compare the pharmacokinetics of rhein between rhubarb acid enteric-coated sustained-release pellets and solution,make clear the pharmacokinetic character of the sustained release preparation in vivo.Method：Ten rabbits were given a single oral dose of 35 mg·kg-1 of self-prepared rhubarb acid enteric-coated sustained-release pellets（test preparation） and the sodium alginate solution of rhein（reference preparation） in a crossover study.HPLC was applied to determine the plasma concentrations of rhein before and 0.5,1,2,3,4,6,8,9,10,12,24,28,32,36 h after administration of the medicine.The pharmacokinetic parameters were calculatedand statistically analyzed.Result：The plasma concentration curves of both the sustained-release matrix pellets and the sodium alginate solution of rhein had one peak.The main pharmacokinetic parameters of test preparation were as follows：tmax（9.73±0.68）h,Cmax（3.00±0.81） g·L-1,AUC0~∞（59.21±4.35） mg·L-1·h-1,MRT（21.12±1.12）h;and those of reference preparation were as follows：tmax（4.17±0.12）h,cmax（2.71±0.74） g·L-1,AUC0~∞（39.72±3.11） mg·L-1·h-1,MRT（9.33±2.08）h respectively.Conclusion：Compared with the sodium alginate solution of rhein,the self-prepared rhubarb acid enteric-coated sustained-release pellets have better bioavailability.