原料药粒径对盐酸普萘洛尔渗透泵片释药行为的影响

Influence of Particle Size of Propranolol Hydrochloride on Its Osmotic Pump Tablets' Release

目的:研究原料药粒径等对盐酸普萘洛尔渗透泵片释药行为的影响。方法:取不同批号盐酸普萘洛尔及同批号重结晶前、后的原料药均按相同处方制备成渗透泵片,考察药物体外释放情况及释药24h后衣膜形态;并对上述不同原料药的粒径分别以光学显微镜和激光粒度分析仪进行证实。结果:以原料药粒径较小的渗透泵片释放完毕后衣膜变形,且不能维持零级释放,原料药粒径较大的渗透泵片结果与之相反。不同原料药经仪器证实粒径确有差异。结论:原料药的粒径可影响制备的渗透泵片的释放行为,提示性状稳定的原料药的合理选择在制剂过程中不可忽视。

OBJECTIVE ： To observe the influence of particle size of propranolol hydrochloride on drug release of its osmotic pump tablets. METHODS： Same formulation was applied to prepare osmotic pump tablets with propranolol hydrochloride （different batches） and crude drug （same batches） before and after recrystallization. In vitro drug release and coat-membrane morphology after 24 h＇ s drug release were observed. The particle size of above crude drugs were detected and verified using optical microscope and LGA. RESULTS： Osmotic pump tablets made from raw materials with small particle size had film coats deformation and nonzero- order release while tablets made from raw material with big particle size presented opposite drug release. That the particle sizes were different among various raw materials was firmed by apparatus. CONCLUSIONS： The drug release of osmotic pump tablets are obviously affected by particle size of crude drug, which indicates the importance of rational choice of crude drug in preparation pocess.