文献类型：期刊文献

中文题名：灵芝酸单体Me肠溶胶囊制备及其兔体内生物利用度测定

英文题名：Preparation of enteric-coated capsule of ganoderic acid Me and determination of its bioavailability in rabbits

作者：陶少林[1,2];陈香[1,2];高峰[1,2];钟建江[3]

机构：[1]华东理工大学上海市功能性材料化学重点实验室,上海200237;[2]华东理工大学药学院药剂教研组,上海200237;[3]上海交通大学生命科学技术学院,上海200240

年份：2011

卷号：33

期号：6

起止页码：950

中文期刊名：中成药

外文期刊名：Chinese Traditional Patent Medicine

收录：CSTPCD;;北大核心:【北大核心2008】；CSCD:【CSCD2011_2012】；

基金：上海市"科技创新行动计划"中药现代化专项项目(08DZ1971900);111学科创新引智计划资助(B07023)

语种：中文

中文关键词：灵芝酸单体Me;β-环糊精;肠溶胶囊;药动学;高效液相色谱法;家兔

外文关键词：ganoderic acid Me; β-cyclodextrin; enteric-coated capsule; pharmacokinetics; HPLC; rabbit

摘要：目的制备灵芝酸单体Me(简称GA-Me)β-环糊精(β-CD)包合物肠溶胶囊,以提高GA-Me的溶解度和避免在胃中降解,并考察其在兔体内的生物利用度。方法采用研磨法制备GA-Me-β-CD包合物,考察不同投料摩尔比对增溶效果的影响;通过优化处方和制备工艺,制得包合物肠溶胶囊;采用高效液相色谱法,测定其体外释放及兔体内生物利用度。结果当GA-Me∶β-CD摩尔比为1∶3时,包合物的溶解度为5.28μg/mL,是原药的5倍;采用等量递加法将GA-Me-β-CD包合物与适量微晶纤维素及微粉硅胶共150 mg;GA-Me静脉给药组:t1/2α为(2.88±0.36)min,AUC0-24 h为(237.08±8.25)μg.min/mL;GA-Me口服给药组:t1/2α为(4.06±1.02)min,AUC0-24 h为(240.04±8.31)μg.min/mL,F为(21.70±0.75)%;肠溶胶囊口服给药组:t1/2α为(79.28±5.04)min,AUC0-24 h为(308.98±53.60)μg.min/mL,F为(27.93±4.84)%。结论 GA-Me-β-CD包合物改善了GA-Me的溶解度,包合物肠溶胶囊口服生物利用度为(27.93±4.84)%。
AIM To prepare the enteric-coated capsule of inclusion complex of ganoderic acid Me（GA-Me） β-cyclodextrin（β-CD） for improving its solubility and avoiding degradation in stomach,and to investigate its bioavailability in rabbits.METHODS The inclusion complex of GA-Me with β-CD was prepared by grinding method to study the different effects of mole ratio on solubility.The formulation and preparation of GA-Me-β-CD loaded capsules were studied.The in vitro release of the capsule was investigated and its bioavailability in rabbits was determined by HPLC method.RESULTS When the optimal mole ratio of GA-Me to β-CD was selected at 1∶ 3,the solubility of GA-Me-β-CD was 5.28 μg/mL,5 times higher than that of GA-Me.Capsules were prepared by mixing 150 mg of GA-Me-β-CD complex with silica powder and microcrystalline,The main pharmacokinetic parameters of i.v.group： t1/2α（2.88±0.36） min,AUC0-24 h（237.08±8.25） μg·min/mL;p.o.GA-Me group： t1/2α（4.06±1.02） min,AUC0-24 h（240.04±8.31） μg·min/mL,F（21.70±0.75）%;p.o.GA-Me-β-CD complex loaded capsules group： t1/2α（79.28±5.04） min,AUC0-24 h（308.98±53.60） μg·min/mL,F（27.93±4.84）%.CONCLUSION The results show that the inclusion complex improves the solubility of GA-Me,and oral bioavai-lability of enteric-coated capsule of GA-Me-β-CD inclusion complex is（27.93±4.84）% in rabbits.