使用亲水性聚合物调节硝苯地平从缓释骨架片中的释放(英文)  

Modulating the nifedipine release from sustained release matrix tablets using hydrophilic polymers

作　　者：达第[1] 吕雅琪[1] 赵海伟[1] 武占楠[1] 尹莉芳[1] 唐鹤松 

机构地区：[1]中国药科大学药学院,江苏南京210009 [2]成都蓉药集团四川长威制药有限公司,四川成都614000

出　　处：《药学研究》2013年第6期314-320,共7页Journal of Pharmaceutical Research

基　　金：科技部十二五国家重大专项(2012ZX09202101-008)

摘　　要：目的根据体外释放曲线调节硝苯地平缓释片(20 mg)的药物释放特性同时评价不同羟丙甲纤维素(HPMC)作为骨架材料的作用。方法硝苯地平HPMC骨架片使用不同粘度的HPMC和其他辅料由湿法制粒后压片制得。自制制剂和参比制剂的释放曲线采用美国药典中桨法进行评价,硝苯地平药物含量采用高效液相色谱法进行测定。结果使用不同的骨架材料药物的释放具有显著性差异,通过改变HPMC的种类调节和控制硝苯地平的释放。聚合度相同,与低粘度的HPMC(K4M,K100LV,E5)相比高粘度的HPMC(K15M)会使硝苯地平释放变慢。最终的处方用10 mg K4M作为主要的骨架材料,10 mg PVP K30作为释药调节剂。结论制备硝苯地平缓释片使用骨架材料HPMC K4M和释药调节剂PVP K30;口服缓释剂型可以改善慢性治疗顺应性并且可维持有效血药浓度。Objective To modulate the drug release characteristics of extend release Nifedipine（20 mg） Tablets while evaluating the effect of different Hydroxypropyl Methylcellulose（HPMC） matrix systems in terms of in vitro release profile.Methods HPMC matrix tablets of Nifedipine using HPMC with different viscosity and others excipients were prepared by wet granulation compression process.The Nifedipine release profile of the prepared tablets was then evaluated in comparison to a selected reference using the USP paddle method.Analysis of Nifedipine was carried out by HPLC method.Results Significant differences among the drug release profiles from different matrices showed that the release of Nifedipine could be controlled and modulated by varying the HPMC.At a fixed polymer level,drug release from the higher viscosity grades（K15M） was slower as compared to the lower viscosity grades（K4M,K100LV,E5）.The final prescription was established to be using K4M as the main skeleton material with 10 mg and 10 mg of PVP K30 as modifier.Conclusion Selected HPMC K4M and modifier PVP K30 were found to be suitable for the preparation of Nifedipine sustained release tablet： hence an oral release dosage form that could improve chronic therapy compliance and maintain drug concentration in the blood was achieved.

关 键 词：硝苯地平 羟丙甲纤维素骨架片 缓释 

分 类 号：R944.9[医药卫生—药剂学]