氢氯噻嗪包合物微孔渗透泵片的制备

Preparation of Hydrochlorothiazide Inclusion Compound Micro-porous Osmotic Pump Tablets

关键词:  氢氯噻嗪  包合物  微孔渗透泵片  制备工艺

Key words:  hydrochlorothiazide  inclusion complex  micro-porous osmotic pump tablets ( MPOP)  preparation process

摘要:

目的 制备氢氯噻嗪-羟丙基-β-环糊精(HCTZ-HP-β-CD)包合物微孔渗透泵片。方法 采用中和法制备HCTZ-HP-β-CD包合物,并通过红外光谱法和核磁共振法对其进行表征；以累积释药百分率为指标,采用单因素法优化包衣膜处方,并对优化处方的体外释药行为进行模型拟合。结果 优化后的氢氯噻嗪包合物微孔渗透泵片12 h内符合零级释药模型,累积释放度达到90%。结论 以HCTZ-HP-β-CD包合物为中间体,可制成12 h内零级释药特征显著的微孔渗透泵片。

Abstract:

ABSTRACT: OBJECTIVE To prepare hydrochlorothiazide-hydroxypropyl-β-cyclodextrin inclusion complex micro-porous osmotic pump tablets. METHODS The HCTZ-HP-β-CD inclusion compound prepared by acid-base neutralization was characterized by infrared spectroscopy (IR) and nuclear magnetic resonance (NMR). Using accumulative drug release rate as the key index，single factor experiments were carried out to optimize such factors as the coating membrane formulation. The release in vitro of the optimized formulation was fitted to different models. RESULTS Hydrochlorothiazide inclusion compound micro-porous osmotic pump tablets obeyed the zero-order release mode in 12 hours and the cumulative release over 90%. CONCLUSION The HCTZ-HP-β-CD inclusion compound micro-porous osmotic pump tablets could deliver drug constantly for 12 h based on the intermediat of HCTZ-HP-β-CD inclusion complex.