缬沙坦自微乳化药物传递系统的处方筛选与体外评价.doc

缬沙坦自微乳化药物传递系统的处方筛选与体外评价 袁悦，李三鸣，王艳娇，赵明沂，刘洪卓，姚慧敏 （沈阳药科大学 药学院，辽宁 沈阳 110016） 摘要：目的 选择适宜比例的油、表面活性剂和助表面活性剂，筛选缬沙坦自微乳化药物传递系统的处方并进行体外评价。方法 考察了在不同油相通过绘制三元相图制剂粒径考察处方选用为油相,温80为表面活性剂, Transcutol P为助表面活性剂。所得3个处方乳化后的粒径及分布分别为(46.71.6)、(57.0±2.4)、( 86.3±1.5) nm。结论 通过处方研究确定%和关键词：；； 中图分类号：R943.4 文献标识码:A of self-microemulsifying drug delivery systems for Valsartan YUAN Yue, LI Sanming, WANG Yanjiao, ZHAO Mingyi, LIU Hongzhuo, YAO Huimin (School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China) ABSTRACT: OBJECTIVE In order to screen formula and to evaluate in vitro of self-microemulsifying drug delivery systems for Valsartan, the self-microemulsion formula containing Valsartan was prepared by using appropriate proportion of oil, surfactant and cosurfactant. METHODS The solubilities of Valsartan in various bases were investigated. According to the self-emulsification domains basing on the ternary phase diagrams and the mean diameter of three formulas, the optimum formula was screened initially. RESULTS The results showed that oil, surfactant and cosurfactant were ethyl oleate, Tween 80 and Transcutol P?, respectively. Droplet size and distribution of three SMEDDS formulations were (46.7±1.6)、(57.0±2.4)、(86.3±1.5) nm individually. CONCLUSION The optimized formula was 4% Valsartan, 35% oil (ethyl oleate), 45% surfactant (Tween 80) and cosurfactant (Transcutol P?). KEY WORDS: Valsartan; self-microemulsifying drug delivery systems; ternary phase diagrams; screening formula 缬沙坦是新一代非肽类血管紧张素Ⅱ受体拮抗剂，它可阻止血管紧张素Ⅱ所引起的血管收紧及醛固酮释放,对轻中度高血压病的降压效果显著。临床研究证实该药安全性好，降压平稳、疗效强、作用时间长，患者耐受性好，目前在全球已被广泛用于治疗高血压[1]。 目前上市的缬沙坦剂型主要是胶囊剂和片剂，由于缬沙坦是脂溶性很强的药物，水中几乎不溶，影响了药物在体内的吸收，口服给药的生物利用度。自乳化药物传递系统SEDDS）是由药物、油相、非离子型表面活性剂和助表面活性剂组成的液体或固体制剂在体内胃肠道蠕动下可自发乳化形成乳剂。粒径可进一步减小(粒径≤100 nm)此时称(SMEDDS)。SEDDS和SMEDDS在[2]。 本文选用为模型药物为提高缬沙坦的生物利用度，更好的满足市场需求，拟将缬沙坦制成自乳化给药系统考察在不同油相通过绘制三元相图对制剂粒径考察最优处方并进行体外评价高效液相色谱仪（SPD-10A VP 紫外-可见检测器，LC-10AT VP高效液相色谱泵，日本岛津株式会社），ZS501-A数显恒温水浴振荡器（辽阳博大科学仪器有限公司），ESJ210-4精密电子天平（沈阳龙腾电子称量仪器公司）