中国药业
中國藥業
중국약업
CHINA PHARMACEUTICALS
2014年
22期
60-62
,共3页
中空微球%达比加群酯%制备%体外释放度
中空微毬%達比加群酯%製備%體外釋放度
중공미구%체비가군지%제비%체외석방도
hollow microspheres%Dabigatran etexilate%preparation%in vitro release
目的:改变制备中空微球中所需有机溶剂的不同配比,探讨有机溶剂对中空微球形成的影响。方法采用以乙醇与二氯甲烷之比为1:1的最优配比制备达比加群酯中空微球,并测定其含量、体外释放度。结果制备的达比加群酯中空微球具有明显空腔,体外漂浮性能良好,体外释放行为符合Higuchi方程,2 h和12 h时累积释放率分别为45.3%和61.4%。结论所制备的达比加群酯中空微球具有缓释效果,有利于减少给药次数。
目的:改變製備中空微毬中所需有機溶劑的不同配比,探討有機溶劑對中空微毬形成的影響。方法採用以乙醇與二氯甲烷之比為1:1的最優配比製備達比加群酯中空微毬,併測定其含量、體外釋放度。結果製備的達比加群酯中空微毬具有明顯空腔,體外漂浮性能良好,體外釋放行為符閤Higuchi方程,2 h和12 h時纍積釋放率分彆為45.3%和61.4%。結論所製備的達比加群酯中空微毬具有緩釋效果,有利于減少給藥次數。
목적:개변제비중공미구중소수유궤용제적불동배비,탐토유궤용제대중공미구형성적영향。방법채용이을순여이록갑완지비위1:1적최우배비제비체비가군지중공미구,병측정기함량、체외석방도。결과제비적체비가군지중공미구구유명현공강,체외표부성능량호,체외석방행위부합Higuchi방정,2 h화12 h시루적석방솔분별위45.3%화61.4%。결론소제비적체비가군지중공미구구유완석효과,유리우감소급약차수。
Objective To investigate the influence of organic solvent on the hollow microspheres formation by changing different propor-tions of organic solvent required in the preparation of hollow microspheres. Methods Dabigatran etexilate hollow microspheres were pre-pared by adopting the optimal proportion of 1:1 for dichloromethane and ethanol. Its content and in vitro release were calculated. Results The prepared Dabigatran etexilate hollow microspheres had obvious cavities,good in vitro floating performance,and the in vitro release behavior conformed to the Higuchi equation,the 2 h and 12 h cumulative release rates were 45. 3% and 61. 4% respectively. Conclusion The prepared Dabigatran etexilate hollow microspheres have a sustained-release effect and help to reduce the frequency of administration.