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 P及Tefose 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。
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 ...
关键词
自微乳化
卡维地洛
粒径分布
ζ-电位
溶出
self-microemulsification
carvedilol
particle size distribution
ζ-potential
dissolution