特布他林脉冲控释微丸体外释放度影响因素的研究  

Study on Factors Involved in Release in Vitro of Terbutaline Sulphate Pulsatile Controlled release Pellets

作　　者：陈燕忠[1] 张纪兴[1] 吕竹芬[1] 张蜀[1] 

机构地区：[1]广东药学院,广州510224

出　　处：《中国药师》2004年第10期750-753,共4页China Pharmacist

基　　金：国家重点科技攻关计划专题项目(No.96-901-05-63)。

摘　　要：目的考察硫酸特布他林脉冲控释微丸释放度的影响因素。方法采用滚制法制备载药丸芯,使用水溶胀性材料为内包衣溶胀层,乙基纤维素水分散体为外包衣控释层制备脉冲控释微丸,并考察十二烷基硫酸钠(SDS)含量、溶胀层和控释层包衣增重量对药物释放的影响。结果药物通过控释层衣膜破裂而释放,内包衣层中SDS的加入与否、溶胀层和控释层厚度对脉冲控释微丸的释药时滞和释药速率均具有显著性影响。结论制备的脉冲控释微丸,在模拟人体内胃肠道pH值变化条件下达到了时滞为4.5h,时滞后1.5h累积释药80%以上的脉冲释药效果。Objective: To investigate the factors involved in the release in vitro degree of terbutaline sulphate pulsatile controlled release pellets.Method: The pulsatile controlled release pellets were prepared with the core of pellets preprared by the rolling technique, the materials that could be quickly absorbed water, had a water solubility and swelling property, get lubricious in an aqueous were used as inner swelling coating, the EAD was used as outer controlled release coat. The effects of contenting of SDS, inner swelling coating, and outer controlled release coating on the release of the pellets were also investigated.Result: terbutaline sulphate was released by the break of controlled release coating, SDS was added in inner coating or not and the thickness of swelling coating and controlled release coatings could significantly affect the release postponement and release rate.Conclusion: The accumulative pulsile release effect of more than 80% of release rate of the prepared pulsile controled release pellets could be recorded when 4.5 h of release postponement in the simulated pH variations of gastrointestinal tract in human body 1.5 h after release postponement.

关 键 词：特布他林 硫酸控释微丸 脉冲 体外释放 

分 类 号：TQ460.6[化学工程—制药化工] R965.2[医药卫生—药理学]