表面活性剂对疏水片面润湿性的调节及其对崩解和药物释放的影响  

Regulation of surfactant on the wettability of hydrophobic tablet and its effect on the disintegration and drug release

作　　者：丛佳亮 杨白雪[1] 马一楠 宫艳畅 黄宇豪 李三鸣[1] CONG Jialiang;YANG Baixue;MA Yinan;GONG Yanchang;HUANG Yuhao;LI Sanming(Shool of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2020年第2期106-112,共7页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81473161).

摘　　要：目的表面活性剂对疏水片面润湿性的调节及其对崩解和药物释放的影响。方法采用静态液滴法测定其液滴在辅料表面或混有表面活性剂的辅料表面上的接触角。结果离子型表面活性剂与泊洛沙姆系列溶液均可提高疏水性辅料的润湿性;混有表面活性剂的疏水辅料片的接触角较无表面活性剂时小,润湿性得到改善,同时润湿性的改善可有效缩短崩解时间,提高药物的溶出度。F68与F127对辅料片润湿性质改善能力仅次于SDS。并初步建立了辅料润湿、片崩解时间、药物释放百分率之间的关系。结论在片剂润湿、崩解、药物释放过程中,泊洛沙姆系列表面活性剂可部分替代离子型表面活性剂作为润湿调节剂,研究结果对制剂的处方设计及筛选具有指导意义。Objective Abstract:Objective:To study the regulation of surfactant on the wettability of hydrophobic tablet and its effect on disintegration time and drug release.Methods The contact angles of the droplets on the surface of excipient tablets with or without surfactants were determined by sessile droplet technique.Results The results showed that both ionic surfactant and poloxamer solutions could improve the wettability of hydrophobic excipients.The contact angles of hydrophobic excipient tablets with surfactants were smaller than those without surfactants,which indicated that the wettability of hydrophobic excipient was also improved by adding surfactants in solid firm.Moreover,the better wettability of excipients lead to the reduction of tablet disintegration time and the increase of accumulative release of the drug.For SDS,its ability to improve the wettability of excipients was better than that of F68 and F127.The relationship between wettability of excipients and the tablet disintegration time or the accumulative release of the drug was preliminarily established.Conclusion As wetting regulator,poloxamer can be utilized to replace some ionic surfactants in the preparation.The results of the study can be an important guidance for the formulation design.

关 键 词：表面活性剂 辅料 润湿性 崩解 释放速率 

分 类 号：R943[医药卫生—药剂学]