黄芩苷、黄芩苷磷脂复合物与黄芩苷磷脂复合物鼻用温敏型原位凝胶的鼻黏膜渗透性研究  

Permeability of Baicalin,Baicalin Phospholipid Compound,Baicalin Phospholipid Compound Thermo-sensitive In-situ Nasal Gel Across Nasal Mucosa

作　　者：叶英杰[1] 李楠[1,2] 陈祝君[1] 向小飞[1] 黄亮[1] 邹文铨[1] 杨明[1,3] 

机构地区：[1]成都中医药大学药学院,成都市611137 [2]四川大学华西药学院,成都市610041 [3]江西中医学院中药现代制剂教育部重点实验室,南昌市330004

出　　处：《中国药房》2011年第27期2503-2506,共4页China Pharmacy

基　　金："重大新药创制"科技重大专项(2009ZX09103-353)

摘　　要：目的:研究黄芩苷、黄芩苷磷脂复合物与黄芩苷磷脂复合物鼻用温敏型原位凝胶的体外鼻黏膜渗透性,对黄芩苷磷脂复合物温敏型鼻用原位凝胶的处方进行筛选。方法:采用Franz扩散池法进行鼻黏膜渗透试验,高效液相色谱(HPLC)法测定接受池中药物累积渗透量。以单位面积累积渗透量(Q)和稳态透膜速率(Js)为标准考察黄芩苷、黄芩苷磷脂复合物与黄芩苷磷脂复合物鼻用温敏型原位凝胶的体外鼻黏膜渗透性,从而确定三者的体外释药曲线和对黄芩苷磷脂复合物鼻用温敏型原位凝胶处方的筛选结果。结果:各个供试药物的释药符合一级释放模型;与黄芩苷溶液比较,黄芩苷磷脂复合物能明显增加释药量和释药速率。处方二的Q和Js为3种鼻用原位凝胶处方中最高值。结论:黄芩苷磷脂复合物可明显提高黄芩苷的膜渗透性。黄芩苷磷脂复合物鼻用温敏型原位凝胶为处方二最佳,可用于鼻腔给药。OBJECTIVE：To investigate in vitro permeability of baicalin,baicalin phospholipid compound and baicalin phospholipid compound thermo-sensitive in-situ nasal gel,and to screen out the best prescription of baicalin phospholipid compound thermo-sensitive in-situ nasal gel.METHODS：Franz diffusion cell was adopted.Accumulative permeation amount of drug in the receptor was determined by HPLC.By taking the cumulative permeation amount and steady-state infiltration rate as evaluation standard,the permeability of baicalin,baicalin phospholipid compound and baicalin phospholipid compound thermo-sensitive in-situ nasal gel across nasal mucosa were investigated.Then in vitro release curves of them were determined and the prescription of baicalin phospholipid compound thermo-sensitive in-situ nasal gel was screened out.RESULTS：Drug release of test samples met the first order release model.Compared with baicalin solution,baicalin phospholipid compound could increase the drug release amount and release rate.The second prescription had the highest cumulative permeation amount and steady-state infiltration rate among three prescriptions.CONCLUSION：Baicalin phospholipid compound significantly increase the membrane permeability of baicalin.Baicalin phospholipid compound thermo-sensitive in-situ nasal gel is the best,and can be used for nasal administration.

关 键 词：黄芩苷 黄芩苷磷脂复合物 鼻用原位凝胶 鼻黏膜渗透性 

分 类 号：R285[医药卫生—中药学] R97[医药卫生—中医学]