摘要
目的制备坎地沙坦酯速释和缓释固体分散体,提高坎地沙坦酯生物利用度。方法用固体分散体技术制备坎地沙坦酯速释和缓释固体分散体,并将制备方法对体外释放度的影响进行分析。结果聚乙二醇6000、泊洛沙姆188为混合载体的速释型固体分散体与物理混合物对比,药物的溶出速率和溶出量明显提高。乙基纤维素（EC）的黏度对缓释型固体分散体有较大影响;释放调节剂PEG的使用比例影响缓释效果;药物与载体用量的比例控制在1∶4~1∶6之间缓释效果较好。结论速释和缓释固体分散体均能提高药物的溶出量,以乙基纤维素为载体的固体分散体缓释效果明显。
Objective To prepare candesartan cilexetil immediate-release and sustained release solid dispersions（SD） to improve bioavailability.Methods SD technology was used to prepare immediate-release and sustained release SD,and the effect of the preparing technology on the in vitro release was analyzed.Results The rate and amount of dissolution were improved significantly by comparison of SD using PEG6000 and Poloxamer 188 as mixed carrier with the physical mixtures.The dissolution of the sustained release SD was affected greatly by the viscosity of ethyl cellulose（EC）,and was also affected by the proportion of the sustained release modifier PEG.If the proportion of the drug and the carrier had been controlled between 1∶4 to 1∶6,the sustained release effect was satisfactory.Conclusion The immediate-release and a sustained release SD can increase the amount of drug dissolution,the SD using EC as the carrier has a good sustained-release effect.
出处
《中国医药导报》
CAS
2013年第1期126-128,134,共4页
China Medical Herald
基金
浙江省大学生科技创新活动计划(新苗人才计划)项目(项目编号:2011R460002)
关键词
坎地沙坦酯
固体分散体
速释
缓释
Candesartan Cilexetil
Solid dispersions
Immediate-release
Sustained release
