羟丙甲纤维素粒径对茶碱亲水凝胶骨架缓释片释放度的影响机制考察

Influence Mechanism of Particle Size of HPMC on Release of Theophylline from Hydrophilic Matrix Sustained-release Tablets

基于羟丙甲纤维素(HPMC)的压缩性质,考察了HPMC粒径对亲水凝胶骨架缓释片中药物释放的影响机制。将HPMC K100M筛分成4种不同的粒径,测定其压缩性质,并以HPMC K100M为骨架材料,茶碱(1)为模型药物制备缓释片,考察HPMC K100M压缩性质对1缓释片抗张强度、孔隙率和释放度的影响。结果表明,随着粒径的减小,HPMC K100M的堆密度、振实密度、压缩度和抗张强度逐渐增大,弹性恢复逐渐降低,导致1缓释片的厚度和孔隙率逐渐减小,单位体积HPMC浓度增加,从而使得HPMC凝胶速率加快,水分渗入骨架片的速率变慢,骨架膨胀较慢,释放度降低。

Based on the compaction property of hydroxypropyl methylcellulose （HPMC）, the influence mechanism of its particle size on the drug release behaviour from the hydrophilic matrix sustained-release tablets was investigated. HPMC KI00M was sieved into four different particle sizes, and their compaction properties were determined respectively. The hydrophilic matrix sustained-release tablets loaded with theophylline （1） were prepared with the sieved HPMC K100M as the matrix. The influence of compaction properties of HPMC K100M on the tensile strength, porosity and in vitro release of 1 sustained-release tablets were investigated. The results showed that the bulk density, tap density, compressibility, tensile strength increased with the decreasing of the particle size of HPMC K100M, while the elastic recovery decreased. All above resulted in decreases in thickness and porosity of tablets and an incerase in HPMC concentration per tablet. Then the gelation rate of 1 hydrophilic matrix sustained-release tablets was accelated and the water ingress was inhibited, which induced a slower polymer swelling rate and a lower drug release amount.