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吲达帕胺-β-环糊精包合物的制备、物相鉴定及体外释放度研究
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| 篇名： | 吲达帕胺-β-环糊精包合物的制备、物相鉴定及体外释放度研究 |
| TITLE： | |
| 摘要： | 目的：建立吲达帕胺（IDP）-β-环糊精（β-CD）包合物的含量测定方法并优化其制备工艺，对所制包合物进行物相鉴定及体外释放度考察。方法：采用紫外分光光度法测定IDP-β-CD包合物中IDP的含量；采用溶液-搅拌法制备IDP-β-CD包合物，以包合率为考察指标，采用正交试验优化制备工艺；比较不同干燥法对包合率和载药率的影响；采用红外光谱分析（IR）法和差式扫描量热法（DSC）对IDP-β-CD包合物进行物相鉴定；通过体外释放度试验考察不同干燥法对IDP-β-CD包合物释放行为的影响。结果：IDP的检测质量浓度线性范围为2.0～14.0 μg/mL（r＝0.999 7）；定量限、检测限分别为0.204、0.067 μg/mL；精密度、稳定性、重复性试验的RSD均小于2％；加样回收率为98.8％～101.8％（RSD＝1.10％，n＝6）。最优制备工艺为β-CD与IDP摩尔比为3 ∶ 1，包合时间为3 h，搅拌速度为300 r/min；所得包合物的平均包合率为72.81％。IR和DSC分析结果均显示，IDP与β-CD通过物理作用形成包合物。经喷雾干燥后，IDP-β-CD包合物的包合率为（60.96±0.25）％、载药率为（4.18±0.12）％；经冷冻干燥后，其包合率为（77.31±0.51）％、载药率为（5.31±0.27）％。12 h内，IDP 原料药、IDP-β-CD包合物（分别经冷冻干燥和喷雾干燥制备）的累积释放度分别为37.2％、42.5％、81.9％；与IDP 原料药相比，喷雾干燥所得IDP-β-CD包合物的累积释放度升高更为明显。结论：所建含量测定方法简便、准确；优化的包合物制备工艺稳定、可行，成功制得IDP-β-CD包合物，且喷雾干燥法可获得释放度更高的包合物。 |
| ABSTRACT： | OBJECTIVE： To establish a method for content determination of indapamide （IDP）-β-cyclodextrin （β-CD） inclusion compound， optimize the preparation technology， carry out phase identification and in vivo release study of it. METHODS： UV spectrophotometry was used to determine the content of IDP in IDP-β-CD inclusion compound. IDP-β-CD inclusion compound was prepared by the solution-stirring method and the preparation technology was optimized by the orthogonal experiment using inclusion rate as index. The inclusion rate and drug-loading rate were compared between different drying methods. Phase identification of IDP-β-CD inclusion compound was verified by IR and DSC. The cumulative release rate of inclusion compound was tested by in vitro experiment. RESULTS： The linear range of concentration of IDP was 2.0-14.0 μg/mL （r＝0.999 7）. The quantitative limit and detection limit were 0.204， 0.067 μg/mL， respectively. RSDs of precision， stability and repeatability tests were all less than 2％. The recoveries range was 98.8％-101.8％（RSD＝1.10％，n＝6）. The optimum technology conditions were as follows the molar ratio of β-CD to IDP was 3 ∶ 1， the inclusion time was 3 h， and the stirring speed was 300 r/min. Average inclusion rate of IDP-β-CD inclusion compound was 72.81％. IR and DSC analysis showed that IDP and β-CD formed inclusion compound through physical interaction. After spray drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （60.96±0.25）％ and （4.18±0.12）％. After freeze-drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （77.31±0.51）％ and （5.31±0.27）％. Accumulative release rates of IDP， IDP-β-CD inclusion compound （by freeze-drying and spray drying） were 37.2％， 42.5％ and 81.9％ within 12 h， respectively. Compared with IDP raw material， accumulative release rate of IDP-β-CD inclusion compound increased significantly after spray drying. CONCLUSIONS： Established method is simple and accurate. The optimal preparation technology of inclusion compound is stable and feasible. IDP-β-CD inclusion compound is prepared successfully. The inclusion compound prepared by spray drying shows higher release rate. |
| 期刊： | 2019年第30卷第12期 |
| 作者： | 宋美佳，韩景田，田宝成 |
| AUTHORS： | SONG Meijia，HAN Jingtian，TIAN Baocheng |
| 关键字： | 吲达帕胺；β-环糊精；包合物；工艺优化；物相鉴定；体外释放 |
| KEYWORDS： | Indapamide； β-cyclodextrin； Inclusion compound； Technology optimization； Phase identification； in vitro release rate |
| 阅读数： | 424 次 |
| 本月下载数： | 11 次 |
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