亲水性聚合物对自乳化药物传递系统稳定性的影响
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篇名: | 亲水性聚合物对自乳化药物传递系统稳定性的影响 |
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摘要: | 目的:研究亲水性聚合物对自乳化药物传递系统(SMEDDS)稳定性的影响。方法:以非洛地平(FDP)为模型药物,采用高效液相色谱法测定FDP含量,考察不同介质种类[纯水和0.5%的共聚维酮VA64、羟丙基甲基纤维素(HPMC)E5、HPMC K100LV、HPMC K4M、聚乙烯吡咯烷酮(PVP)K30水溶液],以及不同介质浓度[0.1%、0.5%、1.0%的HPMC E5和共聚维酮VA64水溶液]对SMEDDS中剩余溶解状态FDP含量的影响。结果:SMEDDS在共聚维酮VA64、HPMC E5、HPMC K100LV、PVP K30、HPMC K4M、纯水中室温放置1 h时剩余溶解状态FDP的含量分别为 92.7%、63.6%、50.2%、46.2%、36.0%和24.0%,表明维持系统过饱和能力的顺序为共聚维酮VA64>HPMC E5>HPMC K100LV>PVP K30>HPMC K4M>纯水。SMEDDS在0.1%、0.5%、1%的共聚维酮VA64和HPMC E5水溶液中室温放置1 h时剩余溶解状态FDP的含量分别为93.2%、95.1%、96.0%和48.4%、62.1%、75.1%。结论:共聚维酮VA64和HPMC E5可显著抑制药物从SMEDDS中析出,适于作为SMEDDS的稳定剂,其中共聚维酮VA64效果更好。 |
ABSTRACT: | OBJECTIVE: To investigate the effects of hydrophilic polymers on the stability of self-microemulsifying drug delivery systems (SMEDDS). METHODS: Taking felodipine (FDP) as model drug, the content of FDP was determined by HPLC method. The effects of pure water, 0.5% Kollidon VA64, HPMC E5, HPMC K100LV, HPMC K4M, PVP K30 solution, while 0.1%, 0.5% and 1.0% HPMC E5 and Kollidon VA64 on residual content of dissolved FDP were determined in SMEDDS. RESULTS: The residual contents of dissolved FDP in SMEDDS placed in Kollidon VA64, HPMC E5, HPMC K100LV, PVP K30, HPMC K4M and pure water for 1 h were 92.7%, 63.6%, 50.2%, 46.2%, 36.0% and 24.0%, respectively. The order of maintaining the supersaturation state was Kollidon VA64>HPMC E5>HPMC K100LV>PVP K30>HPMC K4M>pure water. The residual contents of dissolved FDP in SMEDDS placed in 0.1%, 0.5%, 1% Kollidon VA64 and HPMC E5 and pure water for 1 h were 93.2%, 95.1%, 96.0% and 48.4%, 62.1%, 75.1%. CONCLUSIONS: Kollidon VA64 and HPMC E5 can significantly inhibit drug release in SMEDDS and be used as stabilizer of SMEDDS, wherein Kollidon VA64 was better. |
期刊: | 2016年第27卷第7期 |
作者: | 靖博宇,郑霞,杨瑞,赵佳,于绍军 |
AUTHORS: | JING Boyu,ZHENG Xia,YANG Rui,ZHAO Jia,YU Shaojun |
关键字: | 亲水性聚合物;过饱和;自乳化药物传递系统;非洛地平;羟丙基甲基纤维素;共聚维酮 |
KEYWORDS: | Hydrophilic polymers; Supersaturable; Self-microemulsifying drug delivery systems; Felodipine; Hydroxypropyl methylcellulose; Kollidon VA64 |
阅读数: | 389 次 |
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