冯波,何仲贵,赵临襄,赵春顺,张秀荣,李砥晖
FENG Bo 1; HE Zhong gui 2; ZHAO Lin xiang 2; ZHAO Chun shun 2; ZHANG Xiu rong 1; LI Di hui 1 (1. Jilin Military Medical College;

• 1:第四军医大学吉林军医学院
• 2:沈阳药科大学药学院
• 3:沈阳药科大学药学院
• 4:沈阳药科大学药学院

摘要(Abstract)：

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.

关键词(KeyWords)： 沙丁胺醇;乙基化β-环糊精;包合物;释放度
salbutamol; ethylated β cyclodextrins; inclusion compound; release rate

Abstract:

Keywords:

基金项目(Foundation):

作者(Authors): 冯波,何仲贵,赵临襄,赵春顺,张秀荣,李砥晖
FENG Bo 1; HE Zhong gui 2; ZHAO Lin xiang 2; ZHAO Chun shun 2; ZHANG Xiu rong 1; LI Di hui 1 (1. Jilin Military Medical College;

参考文献(References)：

• [1]张毅兰,侯惠民.沙丁胺醇缓释双层片的研究[J].中国医药工业杂志,1997,28(7):305-307.
• [2]吕万良,屠锡德,蒋曙光,等.硫酸沙丁胺醇缓释片的制备及其在健康人体内的药动学研究[J].中国药科大学学报,1997,28(5):278-281.
• [3]吴涛,潘卫三,庄殿友,等.硫酸沙丁胺醇口服渗透泵控释片的制备及体外释放度考察[J].沈阳药科大学学报,1999,16(2):79-82.
• [4]汪新夏,徐惠南.硫酸沙丁胺醇控释微丸研究[J].中国医药工业杂志,1999,30(2):62-64.
• [5]LemesleLamacheV ,WouessidjeweD ,Ch啨ronM,etal.Studyofβ cyclodextrinandethylatedβ cyclodextrinsalbutamolcomplexes,invitroevaluationofsustaine re leasebehaviourofsalbutamol[J].IntJPharm,1996,141:117-124.
• [6]HoriuchiY ,HirayamaF ,UekamaK .Slow releasechar acteristicsofDiltiazemfromethylatedβ cyclodextrincomplexes[J].JPharmSci,1990,79(2):128131.
• [7]HirayamaF ,HirashimaN ,AbeK ,etal.Utilizationofdiethyβ cyclodextrinasasustained releasecarrierforisosorbidedenigrate[J].JPharmSci,1988,77(3):233-236.