交泰丸有效部位自微乳系统的体内外评价  

Evaluation on SMEDDS of effective parts from Jiaotai pills in vitro and in vivo

作　　者：杨丽娟[1] 刘起华[2] 黄果[1] 张瑞[1] 张玉杰[1] 

机构地区：[1]北京中医药大学中药学院,北京100102 [2]中国中医科学院广安门医院,北京100053

出　　处：《中国中药杂志》2010年第10期1246-1250,共5页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(30672585)

摘　　要：目的:对交泰丸有效部位自微乳化释药系统质量及大鼠在体肠吸收进行评价。方法:考察交泰丸有效部位自微乳液的外观、自微乳化后微乳粒径分布、外观、形态、类型、自乳化时间、药物含量及自微乳、微乳化后的稳定性;以黄连总碱为指标,运用大鼠在体肠回流模型,分析比较交泰丸有效部位制备自微乳前后对大鼠在体肠吸收的改善。结果:交泰丸有效部位自微乳化后微乳平均粒径为34.12 nm,可在3 min内基本乳化完全;自微乳液在室温下放置3个月较稳定;自微乳化后的微乳液在37℃下0.1 mol.L-1HCl溶液中放置8 h,交泰丸有效部位自微乳液与有效部位溶液剂比较,黄连总碱在体肠灌流液中的相对剩余百分含量(T)和表观吸收速率常数(Ka)值均获得明显提高(P<0.01),前者的Ka是后者的152.6%。结论:自微乳化给药系统能显著改善交泰丸有效部位中黄连总碱大鼠小肠吸收,增加肉桂油在制剂中的稳定性。适合难溶性和难吸收药物的口服吸收,提高其生物利用度,是具有良好应用前景的中药制剂新剂型。Objective： To investigate the properties of self-microemulsifying drug delivery system（SMEDDS）of effective parts from Jiaotai pills,and evaluate the character on improving intestinal absorption in rat.Method：The appearance,the morphology,the particle size,tape,the time of formulating micro emulsion,the content and the stability were investigated;Taken total alkaloid as index,the intestinal absorption were investigated by using in situ recirculation model and comparing the micro emulsion solution and reference solution,The T（relative percentage remained） and Ka（absorption rate constant）were calculated.Result：After self-microemulsified,the average diameter of microemulsion was 34.12 nm and the time of self-microemulsifying was less than 3 min.SMEDDS was stable in room temperature in 3 months.The microemulsion were stable in 0.1 mol·L-1 HCl at 37 ℃ for 8 h.T and Ka of total alkaloid in SMEDDS were much higher than in that of its reference（P0.01）,and the former Ka was 152.6% of versus reference.Conclusion：SMEDDS might significantly improve the absorption of both poorly soluble and low biological availability drugs in the intestinal tract,and increase drug stability,which will be sutiable for compound Chinese medicine.

关 键 词：交泰丸 有效部位 黄连总碱 自微乳系统 体内外评价 肠吸收 

分 类 号：R285.5[医药卫生—中药学]