佐米曲坦缓释及速释固体分散体的制备工艺研究  

Preparation process of sustained-release and immediate-release solid dispersions of Zolmitriptan

作　　者：徐俊[1] 闫启东[1] XU Jun YAN Qidong(Pharmaceutical R＆D Center of Taizhou Vocational and Technical College, Zhejiang Province, Taizhou 318000, China)

机构地区：[1]台州职业技术学院生化制药研发中心,浙江台州318000

出　　处：《中国医药导报》2017年第1期16-19,共4页China Medical Herald

基　　金：浙江省科学技术厅省级高技能人才培养和创新活动计划项目(2013R30051)

摘　　要：目的制备佐米曲坦缓释和速释固体分散体,提高佐米曲坦生物利用度。方法采用固体分散体技术,制备佐米曲坦缓释及速释固体分散体,考察载体种类、用量等对体外释放度的影响。结果缓释固体分散体受乙基纤维素(EC)黏度、释放调节剂PEG6000用量、药物与载体用量比例的影响。选择EC(10 c P)和聚乙二醇(PEG)6000混合物为载体材料,其中PEG6000占混合载体总量的40%,控制药物与载体材料比为1∶4,缓释效果较好。采用药物、PEG6000与泊洛沙姆188比例为1∶3.7∶1制备速释固体分散体,药物溶出速率显著提高。结论缓释及速释固体分散体能提高药物溶出量,处方合理,具有良好的缓释效果。Objective To prepare Zolmitriptan sustained-release and immediate-release solid dispersions（SD） and improve bioavailability. Methods SD technology was used to prepare immediate-release and sustained release SD of Zolmitriptan, the effect of the preparing technology on the in vitro release with the type and quality of carrier material was examined. Results The viscosity of ethyl cellulose（EC） and the dosage of PEG6000 releasing moderator, and the ratio of drug and carrier could impact on the release rates in vitro. When the mixture of EC（10 c P） and PEG6000 as a carrier material to Zolmitriptan was 4∶1, and 40% of the mixed carrier as PEG6000, the sustained-release effect was satisfactory. The dissolution rate were improved significantly to the fast released solid dispersion by using drugs and PEG6000 and poloxamer 188 with a ratio of 1∶3.7∶1. Conclusion The immediate-release and sustained release SD can increase the amount of drug dissolution, the fomulation is reasonable, and the SD using EC and PEG6000 as the carrier has good and stable sustained-release effect.

关 键 词：佐米曲坦 固体分散体 缓释 速释 

分 类 号：R944.2[医药卫生—药剂学]