吡罗昔康自微乳化药物传递系统的处方筛选与体外评价  

Design and in vitro evaluation of self-microemulsifying drug delivery systems for piroxicam

作　　者：周晓堂[1] 王晶[1] 王颖[1] 孙佳轶[1] 聂淑芳[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《药学学报》2008年第4期415-420,共6页Acta Pharmaceutica Sinica

摘　　要：筛选吡罗昔康自微乳化药物传递系统(SMEDDS)的处方并进行体外评价。考察了吡罗昔康在不同油相和表面活性剂中的溶解度;对不同油相和表面活性剂进行初步配伍研究;通过绘制三元相图研究处方中不同油相、表面活性剂和辅助表面活性剂形成微乳的能力和区域;对制剂粒径及溶出度进行考察。处方选用肉桂醇作为吡罗昔康的溶剂,以Labrafil M1944CS为油相,Cremophor EL为表面活性剂,Transcotol P为辅助表面活性剂。所得3个处方乳化后的粒径及分布分别为(32.2±5.0)、(40.1±6.4)、(81.9±12.2)nm。制剂溶出速度快。通过处方研究确定了最优处方,研制了吡罗昔康SMEDDS。Self-microemulsifying drug delivery systems （SMEDDS） were developed to overcome the problems of delivery and administration of piroxicam, a drug with low bioavailability and gastrointestinal irritation, The in vitro properties of it were assessed. The solubility of piroxicam in several oils and surfactants was determined, and the compatibility of various oils and surfactants was investigated, Ternary phase diagrams were constructed to optimal area of microemulsion, and the influence of different oily phases, surfactants and co-surfactants was studied. The droplet size and dissolution of optimal formulation were determined to prove that the dosage form is a useful delivery system for piroxicam. In the optimized piroxicam SMEDDS, cinnamic alcohol was selected that gave the maximal solubility to piroxicam, Labrafil M 1944CS, Cremophor EL and Transcotol P were used as oils, surfactant and co-surfactant, respectively. Droplet size and distribution of three piroxicam SMEDDS formulations were （32.2± 5.0） , （40. 1 ± 6.4） , （81.9 ± 12. 2） nm individually. And the releasing of piroxicam was rapid and complete. The optimized SMEDDS for piroxicam was obtained,

关 键 词：吡罗昔康 自微乳化药物传递系统 三元相图 处方设计 体外评价 

分 类 号：R943.4[医药卫生—药剂学]