辣椒碱多囊脂质体的制备及在大鼠体内的药动学研究
Preparation of Capsaicin multivesicular liposomes and its pharmacokinetics in the rats
作者：郑雪;陈丽宇;任春娟;串俊兰;张彦;龚涛;张志荣;
Author：
收稿日期： 年卷（期）页码：2011,26(05):-401-404
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：辣椒碱;多囊脂质体;药物动力学;大鼠
Key words：
基金项目：国家十一五重大新药创制计划关键技术项目(2009ZX09503-026)
中文摘要
目的制备辣椒碱多囊脂质体,并考察其包封率和在大鼠体内的药动学。方法采用复乳法制备辣椒碱多囊脂质体、单因素筛选处方,并考察大鼠sc辣椒碱多囊脂质体后的体内药动学。结果制备的辣椒碱多囊脂质体的外观圆整,大小均匀,包封率为71.9%±3.8%,平均粒径为8.1μm。大鼠sc辣椒碱多囊脂质体后,与辣椒碱溶液相比,Cmax分别为405.72±53.87、804.06±108.17 ng.mL-1;AUC0-t为16.7836±2.8541、3.7622±0.6651μg.h.mL-1;消除时间分别为32.31±2.64、3.23±0.34 h,72 h时血浆中仍可检测到药物。结论采用复乳法可成功将脂溶性药物辣椒碱载入多囊脂质体中,大鼠体内的药动学研究显示有明显的缓释特征。
英文摘要
[1]郭峰,姜晓钟,赵云富.辣椒素的作用机制及其镇痛应用[J].第二军医大学学报,2002,23(1):96-98.
[2]Long XY,Luo JB,Yan ZH,et al.Preparation and in vitro&invivo evaluations of topically applied capsaicin transfersomes[J].Pharmac Sinica,2006,41(5):461-466.
[3]Mantrip ragada S.A lipid based depot(DepoFoamtechnology)for sustained release drug delivery[J].Progr in Lip Res,2002,41:392-406.
[4]Qiang Ye,John Asherman,Mark Stevenson,et al.DepoFoamTMtechnology:a vehicle for controlled delivery of protein and peptidedrugs[J].J Contr Rel,2000,64:155-166.
[5]董新荣,王锦,刘仲华,等.辣椒素的荧光分析方法研究[J].天然产物研究与开发,2007,19:135-137.
[6]Chen X,Sun X,Ren K,et al.Enhanced aqueous solubility andbioavailability of capsaicin by the preparation of an inclusion com-plex[J].Arzneimittel for Schung,2010,60(9):571-574.
[7]Saria A,Skofitch O,Lembeck F.Distribution of capsaicin in rattissues after systemic administration[J].Pharm Pharmacol,1982,34:273-275.
【关闭】
