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。
OBJECTIVE： To investigate the effects of hydrophilic polymers on the stability of self-microemulsifying drug delively 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 ES, 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.
出处
《中国药房》
CAS
北大核心
2016年第7期910-912,共3页
China Pharmacy
关键词
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
Hydrophilic polymers
Supersaturable
Self-microemulsifying drug delivery systems
Felodipine
Hydroxypropyl methylcellulose
Kollidon VA64
