阿伐那非自微乳释药系统的制备与药动学评价  

Preparation and Pharmacokinetic Evaluation of Self-microemulsifying Drug Delivery System with Avanafil

作　　者：崔颖[1] 田霞[1] CUI Ying;TIAN Xia(Tianyou Hospital Affiliated to Wuhan University of Science and Technology,Wuhan 430064,China)

机构地区：[1]武汉科技大学附属天佑医院,湖北武汉430064

出　　处：《解放军药学学报》2018年第5期398-400,435,共4页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的制备阿伐那非自微乳释药系统,并进行处方筛选和药动学评价。方法以溶解度大小为指标,通过对不同配比处方性质考察和伪三元相图筛选阿伐那非自微乳释药系统,并评价阿伐那非自微乳释药系统的体外溶出度和药动学。结果自微乳释药系统处方为25%小茴香油、55%吐温-80、22%1,2-丙二醇、0.5g阿伐那非,15 min时自微乳释药系统中阿伐那非累积释放度达93.5%,最大血药浓度(C_(max))为(40.36±9.19)ng·ml^(-1),AUC0~8h是片剂的1.4倍。结论得到较好阿伐那非自微乳释药系统处方组成。Objective To prepare a self-microemulsifying drug delivery system（SMEDDS）with avanafil,optimize prescription screening and to investigate the pharmacokinetics.Methods Using the solubility as an index,the formulation rate of SMEDDS with avanafil was screened using prescriptions with drugs of different proportions and the pseudo-tertiary phase diagram.The dissolution rate and pharmacokinetics of SMEDDS with avanafil in vitro were evaluated.Results The SMEDDS formula included 25% dill oil,55% tween-80,22%1,2-propylene glycol and 0.5 g avanafil.The accumulated release rate of SMEDDS with avanafil was 93.5%in 15 min,the Cmaxwas（40.36±9.19）ng·ml^（-1）,and the 0-8 hAUC of SMEDDS was 1.4 times that of corresponding tablets.Conclusion A good SMEDDS formulation of avanafil has been made available.

关 键 词：阿伐那非 自微乳释药系统 伪三元相图 药动学 

分 类 号：R94[医药卫生—药剂学] R969.1[医药卫生—药学]