目的 基于羟丙甲纤维素(HPMC)的压缩性质,研究HPMC粒径对硝苯地平亲水凝胶骨架缓释片释放度影响的机制。方法 测定不同粒径HPMC K4M的压缩性质,以硝苯地平为模型药物,HPMC K4M为骨架材料,制备亲水凝胶骨架缓释片。研究HPMC K4M的压缩性质对缓释片孔隙率、释放度等性质的影响。结果 随着粒径的减小,HPMC K4M的堆密度、振实密度、压缩度、抗张强度逐渐增大,弹性恢复逐渐减小,使得硝苯地平缓释片的厚度和孔隙率逐渐减小,单位体积HPMC浓度逐渐增大,导致HPMC凝胶速率加快,使得水分渗入骨架片速率减慢,骨架膨胀减慢,释放度减小。结论 不同粒径分布HPMC的压缩性质明显不同,从而显著影响硝苯地平缓释片的孔隙率和凝胶骨架的形成速率,进而影响缓释片的释放度。
Abstract
OBJECTIVE To investigate the influencing mechanism of the particle size of hydroxypropyl methylcellulose (HPMC) on the release behavior of nifedipine from a sustained-release tablet system based on the compaction properties of HPMC. METHODS The compaction properties of HPMC K4M of different particle sizes were determined. Hydrophilic matrix sustained-release tablets were prepared using nifedipine as the active ingredient and HPMC K4M as a hydrophilic matrix former. The effect of compaction properties of HPMC K4M on the porosity, release, and other properties of nifedipine hydrophilic matrix sustained-release tablets were also studied. RESULTS The decrease of the particle size of HPMC K4M resulted in higher bulk density, tap density, compressibility index, and tensile strength and smaller elastic recovery of HPMC K4M, which all led to the decrease of thickness and porosity and the increase of HPMC concentration per unit volume of nifedipine hydrophilic matrix sustained-release tablets. These factors resulted in faster gelation rate of nifedipine sustained-release tablets and decreased water ingress and polymer swelling, so the release of nifedipine from the delivery system was prolonged. CONCLUSION The obviously different compaction properties of HPMC of different particle sizes influence the porosity and gelation rate and then the release of hydrophilic matrix nifedipine sustained-release tablets.
关键词
羟丙甲纤维素 /
压缩性质 /
粒径 /
硝苯地平 /
缓释片 /
释放度
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Key words
HPMC /
compaction property /
particle size /
nifedipine /
sustained-release tablet /
release
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中图分类号：
R944
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