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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
OBJECTIVE: To develop dissolution-dispersion type controlled-release tablets with diltiazem hydrochloride as model drug and study its in vitro and in vivo pulsatile drug release characteristics. Methods: The main coating materials of carnauba wax, beeswax and hydrophilic cellulose were prepared by dry coating method. The influence of prescription and process factors on the release of pulse controlled release tablets The mechanism of pulsed drug release was investigated by dissolution test. The in vivo plasma concentration of 4 subjects was determined by high performance liquid chromatography (HPLC) and the in vivo pharmacokinetics of pulsed controlled release tablets was investigated. RESULTS: The in vitro delayed release time t10 was 2. 1 h, the maximum release time trm was 4.0 h and the pulse release time t 10 90 was 1.7 h. The in vivo delayed release time tlag was 5.7 h, the peak time tmax Is 8.5h, the time tpsi from the beginning of the release to reach the peak is 2.6h. CONCLUSION: Dissolution-dispersed diltiazem hydrochloride pulse controlled release tablets have both pulsed release properties in vitro and in vivo