摘要
目的:研究黄芪甲苷羟丙基-β-环糊精包合物在大鼠体内的相对生物利用度。方法:给大鼠口服单剂量黄芪甲苷羟丙基-β-环糊精包合物(受试制剂)和黄芪甲苷混悬液(参比制剂),用HPLC-MS法测定大鼠血浆中黄芪甲苷的浓度,并采用3P97程序计算药动学参数。结果:口服黄芪甲苷后大鼠血浆药物浓度-时间曲线符合二室模型。受试样品中黄芪甲苷的C_(max)为(250.29±25.19)ng·ml^(-1),t_(max)为(1.75±0.42)h,AUC_(0→∞)为(2 469.65±168.90)h·ng·ml^(-1),参比样品中黄芪甲苷的C_(max)为(57.83±8.02)ng·ml^(-1),t_(max)为(6.67±0.84)h,AUC_(0→∞)为(862.00±149.61)h·ng·ml^(-1)。黄芪甲苷羟丙基-β-环糊精包合物中黄芪甲苷的相对生物利用度为(293.6±28.9)%。结论:黄芪甲苷羟丙基-β-环糊精包合物的生物利用度较高。
Objective： To study the bioavailability of HP-13-cyclodextrin （HP-β-CD） inclusion compound of astragaloside 1V in rats. Method： HP-B-CD inclusion compound of astragaloside Ⅳ（＇test preparation） and astragaloside IV suspendion （reference prepara- tion） were administrated to the rats in a single oral dose of 10 mg.kg -1 . The concentrations of astragaloside IV of plasma in rats were determined by HPLC-MS and processed with 3P97 program. Result： The concentration-time curve of astragaloside IV after oral admin- istration were best fitted to the compartment model. The main pharmacokinetic parameters were as follows：the Cmax tmax ,A UCo of the test spreparation were （250. 29 ± 25. 19 ） ng. ml - 1, （ 1.75± 0. 42） h, （2 469. 65± 168.90） h. ng. ml - 1, respectively; those of the refer- ence were （ 57. 83 ± 8.02） ng. ml -1, （ 6. 67 ± 0. 84） h, （ 862. 00 ± 149. 61 ） h. ng. ml - 1, respectively. The relative bioavailability of as- tragaloside IV in test preparation was （293.60 ± 28.90） %. Conclusion： The test preparation has a higher bioavailability than the ref- erence one .
出处
《中国药师》
CAS
2010年第4期469-471,共3页
China Pharmacist
基金
福建省莆田市科技局基金资助项目(编号:2003S12)
作者简介
通讯作者：林健Tel：13626912304E—mail：linjian73@126．com
