摘要
为提高烯丙孕素的生物利用度,减少给药次数,降低猪场的养殖成本,旨在制备一种具有缓释长效性能的烯丙孕素缓释微球。以单甲氧基聚乙二醇-聚乳酸共聚物(mPEG-PLA)为载体材料,采用乳化-溶剂挥发法制备烯丙孕素缓释微球,在模拟胃肠道环境的溶出介质中测定烯丙孕素缓释微球的体外释放情况,并对烯丙孕素缓释微球的药物稳定性进行考察。结果显示,烯丙孕素缓释微球的最佳制备条件为搅拌速度1000 r/min,水相中吐温-80含量0.2%,mPEG-PLA质量浓度0.07 g/mL,油水体积比0.6,水相中明胶含量1.0%;以最佳制备条件制得的烯丙孕素缓释微球平均包封率为(95.64±0.23)%,平均载药量为(9.83±0.61)%,mPEG-PLA对烯丙孕素的包埋效果最佳。烯丙孕素缓释微球呈球形或近球形,外观圆整,平均粒径为82.3μm。烯丙孕素缓释微球能在分别含1%吐温-80,pH 1.2、pH 4.1以及pH 6.8这3种不同溶出介质中持续释放4 h以上,且释放机理符合一级动力学方程。烯丙孕素缓释微球在高湿环境中的稳定性良好,但在高温和强光照射的条件下储存10 d时,烯丙孕素的含量分别下降3.00%和11.92%。烯丙孕素缓释微球具有缓释的性能,且制备方法简单,包封率高,载药量好,易于产业化生产,可进一步推动烯丙孕素在养猪业的开发利用。
In order to improve the bioavailability of altrenogest,reduce the times of administration and reduce the breeding cost of pig farm,this experiment aimed to prepare altrenogest sustained-release microspheres with long-term performance.The altrenogest sustained-release microspheres were prepared by emulsification-solvent volatilization method using monmethoxy-polyethylene glycol polylactic acid copolymer(mPEG-PLA)as the carrier material.The release of the altrenogest sustained-release microspheres in vitro was measured in the dissolution medium simulating the gastrointestinal tract environment,and the drug stability of the altrenogest sustained-release microspheres was investigated.The results showed that the optimal preparation conditions of altrenogest sustained-release microspheres were as follows:stirring speed 1000 r/min,Tween-80 content 0.2%,mPEG-PLA concentration 0.07 g/mL,oil-water volume ratio 0.6,gelatin content 1.0%in aqueous phase.Under the optimum preparation conditions,the average encapsulation rate of altrenogest sustained-release microspheres was(95.64±0.23)%and the average drug loading was(9.83±0.61)%.mPEG-PLA had the best embedding effect on altrenogest.The altrenogest sustained-release microspheres were spherical or nearly spherical in appearance,with an average particle size of 82.3μm.Altrenogest sustained-release microspheres can be released continuously for more than 4 h in three different dissolution media containing 1%Tween-80 pH 1.2,pH 4.1 and pH 6.8,respectively,and the release mechanism conforms to the first-order kinetic equation.The stability of altrenogest sustained-release microspheres in high humidity environment was good,but when stored under high temperature and strong light exposure for 10 days,the content of altrenogest decreased by 3.00%and 11.92%respectively.Altrenogest sustained-release microspheres have the properties of sustained-release,and the preparation method is simple,the encapsulation rate is high,the drug loading is good,and it is easy to be industrialized,which can further promote the development and utilization of altrenogest in pig industry.
作者
陈沃俊
张志远
邓翔云
张妙齐
曾蔼宁
冼伟杭
陈胜锋
陈志胜
计慧琴
刘璨颖
张晖
白银山
王丙云
CHEN Wo-jun;ZHANG Zhi-yuan;DENG Xiang-yun;ZHANG Miao-qi;ZENG Ai-ning;XIAN Wei-hang;CHEN Sheng-feng;CHEN Zhi-sheng;JI Hui-qin;LIU Can-ying;ZHANG Hui;BAI Yin-shan;WANG Bing-yun(College of Life Science and Engineering,Foshan University of Science and Technology,Foshan,Guangdong 528000,China)
出处
《动物医学进展》
北大核心
2024年第5期68-74,共7页
Progress In Veterinary Medicine
基金
广东省普通高校动物干细胞工程技术研究中心项目(2021GCZX006)。
