甲氧苄啶增溶技术研究
Study on Trimethoprim Solubilisation Techniques
吴家鑫 1张国栋 1葛辛玫 1赵伯杨 1齐鹏 1肖进1
作者信息
- 1. 中牧实业股份有限公司,农业农村部兽用生物制品与化学药品重点实验室,北京市兽用多肽疫苗设计与制备工程技术研究中心,北京 100095
- 折叠
摘要
本文首先测定了甲氧苄啶在水中的溶解度,然后采用表面活性剂增溶、β环糊精包合、固体分散体等药剂学常用增溶技术对甲氧苄啶开展了溶解度提升研究.实验结果显示,甲氧苄啶在水中的溶解性为0.31 mg/mL,使用表面活性剂增溶、β环糊精包合、固体分散体三种增溶技术后,甲氧苄啶在水中的最高溶解度分别为 0.37 mg/mL、7.06 μg/mL和3.3 mg/mL.通过三种药物制剂技术的对比说明,固体分散体制备的最优方法为溶剂法,最优载体为聚维酮K30,最优冷冻时间为 2小时,制得甲氧苄啶固体分散体溶液甲氧苄啶的浓度可以达到3.3 mg/mL,与自身溶解度 0.31 mg/mL相比,浓度达到甲氧苄啶普通水溶液的10.64 倍,有效提高了甲氧苄啶在水中的溶解性.
Abstract
In this paper,the solubility of trimethoprim in water was firstly determined,and then the solubility enhancement study of trimethoprim was carried out by using surfactant solubilisation,β-cyclodextrin inclusion,solid dispersion and other solubilisation techniques commonly used in pharmaceutical science.The results showed that the solubility of trimethoprim in water was 0.31 mg/mL,and the highest solubility of trimethoprim in water was 0.37 mg/mL,7.06 μg/mL and 3.3 mg/mL after using solubilization techniques of surfactant solubilization,β-cyclodextrin inclusion and solid dispersion,respectively.The comparison of the three solubilisation techniques illustrates that the optimal method of solid dispersion preparation is the solvent method,the optimal carrier is PVP K30 and the optimal freezing time is 2 h.The concentration of trimethoprim in the solid dispersion solution can reach 3.3 mg/mL,which is 10.64 times more concentrated than the ordinary aqueous solution of trimethoprim compared to its own solubility of 0.31 mg/mL.The solubility of trimethoprim in water was improved effectively.
关键词
甲氧苄啶/溶解性/表面活性剂增溶/β环糊精包合/固体分散体Key words
Trimethoprim/solubility/surfactant solubilization/β-cyclodextrin inclusion/solid dispersion引用本文复制引用
出版年
2024
NETL
NSTL
万方数据