【摘要】 目的 :以盐酸地尔硫为模型药物研制溶蚀分散型脉冲控释片并考察其体内外脉冲释药特性。方法 :以巴西棕榈蜡、蜂蜡和亲水性纤维素为主要包衣材料 ,采用干包衣法制备脉冲控释片 ;通过释放度实验考察处方及工艺因素对脉冲控释片体外释放的影响规律 ;通过溶蚀实验考察脉冲释药的机制 ;以高效液相色谱法测定 4名受试者的体内血药浓度 ,研究脉冲控释片的体内药物动力学。结果 :该制剂在体外延迟释放时间t10 为 2 .1h ,释放至最大的时间trm为 4.0h ,脉冲释放时间t10 90 为 1.7h ;其体内的延迟释放时间tlag为 5 .7h ,达峰时间tmax为 8.5h ,从开始释放到达峰的时间tpsi为 2 .6h。结论 :溶蚀分散型盐酸地尔硫脉冲控释片在体外和体内都具有脉冲释放特性更多还原

【Abstract】 To investigate the preparation of pulsatile release tablets, the release of the drug in vitro and the pharmacokinetics in vivo . Methods: Diltiazem hydrochloride(DIL) was used as model drug. The pulsatile release tablets were prepared by dry coated method with carnauba wax, bee wax and hydrophilic cellulose as coating materials. The effects of formulation and technology on the release characteristic of diltiazem hydrochloride was investigated. The mechanism of pulsatile release of the drug was proved by erosion test. The pharmacokinetic study on four human subjects was done by means of HPLC measurement. Results: In vitro , delayed release time t 10 was 2.1 h, the maximum release time t rm 4.0 h and the pulsed release time t 10 90 1.7 h. In vivo , delayed release time t lag was 5.7 h, the peak time 8.5 h and the pulsed release time 2.6 h. Conclusion: The release of drug from pulsatile released tablets of diltiazem hydrochloride was in a pulsed way both in vitro and in vivo .更多还原