摘要
目的:制备难溶性药物新藤黄酸的羟丙基-β-环糊精包合物,并对包合物进行鉴定及质量控制。方法:采用冷冻干燥法制备包合物,并经差示量热扫描、红外光谱、扫描电镜、相溶解度等方法对其进行表征;高效液相色谱法测定包合物中新藤黄酸的含量。结果:新藤黄酸和羟丙基-β-环糊精形成了包合物,且形成的包合物的主客分子物质的量比为1:1,表观稳定常数为Ka=117L.mol-1;新藤黄酸线性范围为4.12～24.72μg.mL-1(r=0.9999),平均回收率为100.1%,RSD为0.48/%。结论:冷冻干燥法制备包合物方法简单可行,增加了药物的溶解度。
Objective：To study the preparation,identification and quality control of neogambogic acid hydroxypropyl-β-cyclodextrin inclusion complex （neogambogic acid-HP-β-CD）.Methods：The inclusion complex was prepared by freeze-drying technique and was identified by differential scanning calorimetry （DSC）,fourier transformation-infrared spectroscopy （FTIR）,scanning electron microscopy （SEM） and phase solubility methods,respectively.A HPLC method was established to determinate the content of neogambogic acid in the inclusion complex.Results：The identification suggested the formation of inclusion complex of 1：1 mol ratio with stability constant Ka（117 L·mol^-1）.The content determination method showed a linear range of 4.12～24.72 μg·mL^-1（r=0.999 9） and a mean recovery rate of 100.1% with a RSD of 0.48%.Conclusion：Freeze-drying method is simple and advantageous to prepare inclusion complex and it can increase the solubility of neogambogic acid.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第7期628-631,共4页
Chinese Journal of New Drugs
基金
安徽省科技厅十一五攻关项目(06013131B)
关键词
新藤黄酸
羟丙基-Β-环糊精
包合物
冷冻干燥法
高效液相色谱
neogambogic acid
hydrresuoxypropyl-β-cyclodextrin
inclusion complex
freeze-drying technique
high performance liquid chromatography（HPLC）
