摘要
分别制备了马来酸氟吡汀(1)速释和缓释颗粒,再混合后灌装入胶囊得到1缓释胶囊。体外释放试验表明,速释颗粒在纯化水中30 min累积释放率大于90%,而缓释颗粒则呈现明显的缓释特征;终产品缓释胶囊在0.1 mol/L盐酸、pH 4.5乙酸盐缓冲液和纯化水中均能缓慢地释放完全,但在pH 6.8磷酸盐缓冲液中24 h累积释放率约40%。以市售普通胶囊为对照进行Beagle犬体内的药动学研究。结果显示,自制的1缓释胶囊与普通速释胶囊的t_(max)分别为9.33和3.33 h,根据c_(max)和AUC数据(双单侧t检验及置信区间法)推断两种制剂间存在显著差异。自制缓释胶囊的相对生物利用度为(121.0±12.9)%(n=6)。
The rapid- and sustained-release granules of flupirtine maleate （1） were prepared respectively, then they were mixed and filled into vacant capsules to obtain the title capsules. The results of in vitro release test showed that drug release from the rapid-release granules in pure water was above 90% within 30 min, while the sustained-release granules demonstrated an obvious sustained-release behavior. The final capsules could slowly and completely release in 0.1 mol/L hydrochloric acid, pH 4.5 acetate buffer and pure water, but the cumulative release at 24 h in pH 6.8 phosphate buffer was only about 40%. The pharmacokinetic study in Beagle dogs was carried out with the commercial capsules as the control. The results showed that the tmax vaules of the self-made sustained-release capsules and the commercial capsules were 9.33 and 3.33 h. The cmax and AUC data were analyzed with two-one sided t-test and （1-2α） confidence interval method. The results showed that these two preparations had a significant difference. The relative bioavailability of the self-made capsules was （121.0±12.9）%（n=6）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2017年第1期50-54,共5页
Chinese Journal of Pharmaceuticals
关键词
马来酸氟吡汀
速释颗粒
缓释颗粒
缓释胶囊
体外释放
药动学
flupirtine maleate
rapid-release granule
sustained-release granule
sustained-release capsule
in vitrorelease
pharmacokinetics
