沙丁胺醇包合物缓释片的制备及其体外释放研究

Preparation of sustained release tablets of the inclusion compound of salbutamol-ethylated β-cyclodextrins and a study on their in vitro release

目的研究沙丁胺醇 乙基化 β 环糊精包合物缓释片的制备方法 ,并考察其体外释放 ,筛选出适宜处方。方法采用粉末直接压片法制备沙丁胺醇 乙基化 β 环糊精包合物缓释片 ,含量测定采用紫外法 ,释放度测定采用《中华人民共和国药典》2 0 0 0版二部释放度测定法中的第 3法 ,用显色法测定释放介质中沙丁胺醇的浓度。结果增加淀粉用量可使 1∶1包合物缓释片的释药加快 ,但对1∶2包合物缓释片影响较小 ;1 %～ 5 %的硬脂酸镁可明显加速缓释片的药物释放 ,3%～ 7%的滑石粉对药物释放影响较小 ;压片压力、搅拌速度、释放介质对缓释片的药物释放影响较小。结论以乙基化β 环糊精为载体制成的沙丁胺醇包合物缓释片具有较好的缓释作用。

Objective The objective of the study is to prepare the sustained release tablets of the inclusion compound of salbutamol ethylated β cyclodextrins(SRT) and investigate its in vitro release, and to select formulation of SRT by determination of the release rate. Methods SRT were prepared by the directly powder tabletting method. The release rates were acquired according to the Chinese Pharmacopoeia( 2000 ). The concentration of salbutamol in the release medium was measured by the color method. Results The time of the drug released could be accelerated as the amount of the filling agent(starch) and lubricant agent(magnesium stearate) were increased. However, less influences were observed from the release rates of the different pressures, rotating speeds and release mediums. Conclusion The results indicated ECD may be used as a hydrophobic drug carrier for the sustained release of salbutamol.