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卡维地洛固体自微乳化药物传递系统的应用

魏兰兰, 孙佩男, 田蕾, 唐歆, 姚婷婷, 潘卫三*   

  1. 1. 沈阳药科大学药学院, 辽宁 沈阳 110016;
    2. 复旦大学附属华山医院, 上海 200032
  • 收稿日期:2006-03-11 修回日期:2006-11-10 出版日期:2006-12-15 发布日期:2006-12-15
  • 通讯作者: 潘卫三*

Use of Solid SMEDDS in Delivery of Carvedilol

WEI Lan-lan, SUN Pei-nan, TIAN Lei, TANG Xin, YAO Ting-ting, PAN Wei-san*   

  1. 1. Shenyang Pharmaceutical University, Shenyang 110016, China;
    2. Pharmacy Department, Huashan Hospital, Fudan University, Shanghai 200032, China
  • Received:2006-03-11 Revised:2006-11-10 Online:2006-12-15 Published:2006-12-15

摘要: 目的 为了提高卡维地洛的溶解度和溶出速度, 制备了一种新型的固体自微乳化硬胶囊。方法 考察了卡维地洛在各种基质中的溶解度, 绘制三元相图用来确定Gelucire 44/14-Lutrol F68-Transcutol PTefose 63-Lutrol F68-Transcutol P两种三元系统的有效自乳化和自微乳化区域。优选Gelucire 44/14-Lutrol F68-Transcutol P系统制备了自微乳化硬胶囊,对其粒径分布, ζ-电位及体外溶出特征进行了评价。结果 自制自微乳化硬胶囊能够显著地提高药物的体外溶出速率。结论 自制卡维地洛固体自微乳化硬胶囊有希望提高药物的生物利用度。

关键词: 自微乳化, 自微乳化, 自微乳化, 卡维地洛, 卡维地洛, 卡维地洛, 粒径分布, 粒径分布, 粒径分布, ζ-电位, ζ-电位, ζ-电位, 溶出, 溶出, 溶出

Abstract: Aim A new solid SMEDDS (self-microemulsifying drug delivery system) capsule has been developed to increase the solubility and dissolution rate. Methods The solubilities of carvedilol in various bases were investigated. Ternary phase diagrams were used to evaluate the self-emulsification and self-microemulsfication domains. The particle size distribution and ζ-potential were determined. The mean diameter of the three formulae decreased with an increase of Lutrol F68. Results The in vitro dissolution rate of carvedilol from solid SMEDDS capsule was significantly increased, compared with that from commercially available tablets. Conclusion The solid self-microemulsifying capsule showed the potential of improving the bioavailability of carvedilol.

Key words: self-microemulsification, self-microemulsification, carvedilol, carvedilol, particle size distribution, particle size distribution, ζ-potential, ζ-potential, dissolution, dissolution

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Supporting: *Corresponding author. Tel.: 86-24-23953241