CAJ | 학술논문

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 t 10为2.1 h，释放至最大的时间 t rm为4.0 h，脉冲释放时间 t 10-90为1.7 h；其体内的延迟释放时间 t lag为5.7 h，达峰时间 t max为8.5 h，从开始释放到达峰的时间 t psi为2.6 h。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。
목적：이염산지이류위모형약물연제용식분산형맥충공석편병고찰기체내외맥충석약특성。방법：이파서종려사、봉사화친수성섬유소위주요포의재료，채용간포의법제비맥충공석편；통과석방도실험고찰처방급공예인소대맥충공석편체외석방적영향규률；통과용식실험고찰맥충석약적궤제；이고효액상색보법측정4명수시자적체내혈약농도，연구맥충공석편적체내약물동역학。결과：해제제재체외연지석방시간 t 10위2.1 h，석방지최대적시간 t rm위4.0 h，맥충석방시간 t 10-90위1.7 h；기체내적연지석방시간 t lag위5.7 h，체봉시간 t max위8.5 h，종개시석방도체봉적시간 t psi위2.6 h。결론：용식분산형염산지이류맥충공석편재체외화체내도구유맥충석방특성。
Objective: To investigate the preparation of pulsatile release tablets, the release of the drug in vitro and the pharmacokinetics in vivo . Methods: Dil tiazem hydrochloride（DIL） was used as model drug. The pulsatile release tabl e ts were prepared by dry-coated method with carnauba wax, bee wax and hydrophil i c cellulose as coating materials. The effects of formulation and technology on t he release characteri stic of diltiazem hydrochloride was investigated. The mechanism of pulsatile rel ease of the drug was proved by erosion test. The pharmacokinetic study on four h uman subjects was done by means of HPLC measurement. Results: In vitro ， delayed-release ti me t 10 was 2.1　h, the maximum release time t rm 4.0　h and t he pulsed-releas e time t 10-90 1.7　h. In vivo ， delayed-release time t la g was 5.7　h, the p eak time 8.5　h and the pulsed-release time 2.6　h. Conclusion: The rele ase of drug from pulsatile-released tablets of diltiazem hydrochloride was in a pulsed way both in vitro and in vivo .