摘要
目的优选得到具有温敏性和直肠滞留黏附性的苦参碱原位温敏凝胶。方法通过冷法制备,以胶凝温度为指标,采用星点设计-效应面法(CCD-RSM),对泊洛沙姆407(P407)、泊洛沙姆188(P188)以及羧甲基纤维素钠(CMC-Na)的用量进行优选,采用质构仪测定制剂的凝胶强度、黏附力,通过大鼠直肠给药考察其直肠滞留情况,并以改良桨法考察体外释放度。结果确定的苦参碱原位温敏凝胶最优处方为苦参碱2%、CMC-Na 1.0%、P188 1.3%、P407 16.5%、苯扎溴铵0.02%。该处方凝胶在大鼠直肠给药后不会出现泄漏,且能在体内滞留6 h以上,其体外释放符合Weibull模型。结论优选得到符合直肠给药需求的苦参碱原位温敏凝胶。
Objective Optimize to obtain the in situ gel of matrine with thermosensitivity and rectal retention of bioadhesion rectum. Methods Thermosensitive gel was prepared by cold method, and then using gelation temperature as an indicator, central combination design-response surface method（CCD-RSM） was used to optimize the dosage of P407, P188, and CMC-Na. Texture Analyzer was used to measure the gel strength and adhesion of prescription, the rectal retention was investigated by rectal administration, and the release rate was explored by modified paddle method. Results The optimal prescription was matrine 2%, CMC-Na 1.0%, P188 1.3%, P407 16.5%, and benzalkonium bromide 0.02%. The prescription gel did not leak after rectal administration in rats, which can remain in the body for more than 6 h, in vitro release in line with Weibull model. Conclusion The optimized matrine-loaded thermosensitive in situ gel could meet the requirement of rectal administration.
作者
薛棱芬
殷雅卓
谢兴亮
邹维
陈林
XUE Ling-fen, YIN Ya-zhuo, XIE Xing-liang, ZOU Wei, CHEN Lin(School of pharmacy, Chengdu Medical College, Chengdu 610500, Chin)
出处
《中草药》
CAS
CSCD
北大核心
2018年第6期1311-1316,共6页
Chinese Traditional and Herbal Drugs
基金
四川省科技创新苗子工程培育项目(2016072)
国家级大学生创新创业训练计划项目(201513705027)
成都医学院应用开发与成果转化培育项目(CYCG16-02)
作者简介
薛棱芬，女，硕士研究生，从事药物制剂研究。Tel：15828152390E-mail：781856389@qq．com;通信作者谢兴亮，男，博士，教授，研究方向为中药学与中药新制剂。Tel：（028）62739515E-mail：421733038@qq.com
