黄芩苷胶囊的人体生物等效性研究

目的:建立人血浆中黄芩苷浓度的高效液相-紫外(HPLC-UV)测定方法,测定志愿者口服黄芩苷胶囊后的血药浓度,估算其药动学参数并对供试制剂与参比制剂的生物等效性进行评价。方法:18名健康志愿者随机单剂量交叉口服黄芩苷试验胶囊和参比片750mg,血浆样品采用固相萃取法处理后,进行HPLC-UV测定。结果:受试及参比制剂中药物主要药动学参数如下:cmax分别为(91±s33)μg·L-1和(86±29)μg·L-1,tmax分别为(7.4±1.3)h和(7.4±1.0)h,AUC0~24分别为(586±233)μg·h·L-1和(579±173)μg·h·L-1,AUC0~∞分别为(616±249)μg·h·L-1和(613±180)μg·h·L-1。黄芩苷试验胶囊的相对生物利用度为(101±18)%。结论:本方法操作简单,专属性强,灵敏度高,准确性好。试验胶囊与参比片生物等效。

Bioequivalence study of baicalin capsules in healthy volunteers

AIM: To establish a HPLC-UV method for the study of pharmacokinetics and bioavailability of baicalin in human plasma. METHODS: The study was performed with 18 male volunteers according to a random 2-way cross-over design. Plasma samples of 18 male volunteers after oral administration of 750 mg baicalin test capsules and reference tablets were prepared by solid phase extraction and the concentrations of baicalin were determined by HPLC-UV method. Pharmacokinetic parameters were also estimated. RESULTS: The main pharmacokinetic parameters of baicalin test capsules and reference tablets were as follows: c_(max)(91±s 33)μg·L~(-1) and (86±29) μg·L~(-1), t_(max)(7.4±1.3) h and (7.4±1.0) h, AUC_(0-24)(586±233) μg·h·L~(-1) and(579±(173) μg·)h·L~(-1), AUC_(0-∞)(616±249) μg·h·L~(-1) and(613±180)μg·h·L~(-1), respectively. The relative bioavailability of baicalin test capsules was(101±(18) %). CONCLUSION: The HPLC-UV is proved to be simple, sensitive and rapid method showing the bio-( )equivalence of the two formulations.