基于渗透泵的头孢曲松钠自动微输注透皮贴剂的制备和体外释放  

Preparation and release in vitro of hypodermic automicroinjection patch of ceftriaxone sodium based on the osmotic pump

作　　者：马瑞[1,2] 李志平[1] 梅兴国[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850 [2]解放军第305医院,北京100017

出　　处：《军事医学》2011年第11期854-858,共5页Military Medical Sciences

基　　金：国家科技重大专项资助项目(2008ZXJ09010-001)

摘　　要：目的制备头孢曲松钠自动微输注贴剂,对渗透泵处方进行优化并考察贴剂的体外释放。方法采用高效液相色谱法测定不同处方制剂初始释放时间、持续释放时间、累积释放率,通过体外释放对渗透泵处方进行优化。结果渗透泵系统中增渗剂的种类及用量、衣膜中致孔剂的种类及用量、增塑剂的用量以及包衣增重对贴剂的释放行为有一定程度的影响,以致孔剂用量、增塑剂用量以及包衣增重为主要因素对其进行正交试验优化,结果表明,最优处方为葡萄糖300 mg、聚乙二醇1500 1.5 g、邻苯二甲酸二乙酯0.5 ml、包衣增重为11%。结论初步体外释放研究表明,头孢曲松钠自动微输注贴剂初始释放时间为15 min,可持续释放6 h,而且体外释放呈良好的零级释放特征。Objective To prepare the osmotic pump controlled release system of ceftriaxone sodium,optimize the formulation of the osmotic pump and evaluate the in vitro release of the automicroinjection patch.Methods The initial release time,the sustained release time and the cumulative drug release of different formulated preparations were measured by HPLC method.The patch was evaluated in vitro to select the best formula.Results The type and dosage of penetration enhancers of the osmotic pump system and the component of semipermeable membrane had marked effect on drug release.The selected formula was 300 mg glucose,1.5 g PEG1500,0.5 ml DEP and 11% weight gain of coat.Conclusion The osmotic pump controlled release system of ceftriaxone sodium of selected formula releases by zero order kinetics.Furthermore,the initial release time and the sustained release time are 15 min and 6 h,respectively.

关 键 词：头孢曲松钠 自动微输注贴剂 渗透泵控释系统 皮下注射 

分 类 号：R944.9[医药卫生—药剂学]