伊曲康唑自乳化释药系统处方研究.docVIP

伊曲康唑自乳化释药系统的处方研究 陈鹰1, 郑庆玲1, 2, 刘宏1, 辛华雯1（1广州军区武汉总医院药剂科, 武汉 430070； 2咸宁学院药学院, 咸宁 437000） 摘 要 目的：研究伊曲康唑自乳化给药系统（ITZ—SEDDS）的处方工艺。方法：通过溶解度试验﹑处方配伍和伪三相图的绘制，筛选油相﹑表面活性剂﹑ 助表面活性剂及最佳配比。并对ITZ－SEDDS的理化性质和体外溶出度进行了测定。结果：伊曲康唑自乳化最终优化处方为：Maisine 35－1：Cremophor EL ：Transcutol P = 25：30：45 ITZ—SEDDS的粒径为162.5nm，ITZ—SEDDS在人工肠液中2h累积溶出百分率为90.9%，是原药（0.52%）的174.8倍，市售胶囊（10.1%）的9.0倍。结论：所制备的TIZ—SEDDS为ITZ的新制剂开发提供了实验依据。 关键词： 伊曲康唑；自乳化释药系统；处方研究；体外溶出度 Study on Formulation of Self-emulsifying Drug Delivery System of Itraconazole CHEN Ying1, Zheng Qing-ling1, 2, Liu Hong1, Xin Hua-wen1 ( 1.Department of pharmacy, Wuhan General Hospital of Guangzhou Command, Wuhan 430070, China; 2. The pharmacy school of Xianning University, Xianning 437000, China ) ABSTRACT OBJECTIVE: To develop the formulation of self- emulsifying drug delivery system for Itraconazole ( ITZ-SEDDS ). METHODS：The optimum formulations of ITZ-SEDDS were screened by solubility experiments, compatibility tests and pseudo-ternary phase diagrams. And the physic-chemical characters and dissolution in vitro of ITZ-SEDDS were also determined. RESULTS The optimum self- emulsifying drug delivery system was composed of Maisine 35-1（25%）,Cremophor EL （30%） and Transcutol P（45%）.The particle diameter was 162.5nm. The percent of accumulated dissolution of Itraconazole in SEDDS in simulated intenstinal fluid was up to 90.9% at 2 h, which was 174.8 times as much as that of ITZ raw powder, and 9.0 times as much as that of ITZ capsules. CONCLUSION: The study of ITZ-SEDDS provide reference for the new dosage form of Itraconazole. KEY WORDS: Itraconazole；Self-emulsifying drug delivery system；Formulation design；Dissolution in vitro *作者简介：陈鹰，女，博士，副主任药师，Tel: 027 E-mail:cy9262005@ 地址：武汉武珞路627号?（广州军区武汉总医院药剂科）邮编430070Itraconazole， ITZ）为临床上常用的抗真菌类药物，但由于其水溶性差，造成口服吸收和血浆浓度的不稳定性，个体差异大，且受食物影响大，进餐时服用较空腹时的生物利用度增高31%-163%[1]，而空腹服用的吸收率和临床疗效低，甚至导致治疗失败。为此，国内外采用了环糊精包合等方法来增加其溶解度和生物利用度[2，3]，但也存在环湖精的胃肠道刺激等不良反应，使用时不便于携带等问题。 自乳化释药系统（Self-emulsifyi