单室模型药物血管外给药零级、一级释放药物动力学  

Pharmacokinetics of zero-order release and first-order release of mono-compar tment drugs administered by non-parenteral route

作　　者：张继稳[1] 钟大放[2] 毕殿洲[2] 

机构地区：[1]中国科学院上海药物研究所,上海201203 [2]沈阳药科大学,辽宁沈阳110015

出　　处：《中国药理学通报》2005年第2期245-248,共4页Chinese Pharmacological Bulletin

摘　　要：目的　建立单室模型药物血管外给药零级释放和一级释放的药物动力学,探讨以剂型中药物的释放动力学和活性药物固有的吸收、分布、清除动力学参数为基础的血管外给药零级释放和一级释放血药动力学。方法　以拉氏变换解微分方程和隔室模型分析等经典的药物动力学方法,分析单室模型药物血管外给药零级释放和一级释放在释放阶段和释放完成后的药物动力学。结果　得到了零级释放和一级释放在释放期间和释放结束后的血药动力学。结论　建立了单室模型药物血管外给药零级释放和一级释放的药物动力学。由于零级释放与一级释放是基本的释放模式,零级释放和一级释放药物动力学理论是建立和理解缓释、控释制剂药物动力学的基础。Aim To establish the pharmacokinetic principles of the zero-order release and the first-order release of mono-compartment drugs administered by non-parenteral route based on the release kinetics of the dosage forms and the intrinsic pharmacokinetic parameters of the active drug, such as the rate constants of the absorption and elimination, and the distribution volume of the drug. Methods By the Laplace transform and the compartmental analysis method, the pharmacokinetic behaviors of the zero-order release and the first-order release of mono-compartment drugs administered by non-parenteral routes were deduced with divisions of the dose being absorbed during the release phase and after the release has terminated. Results The pharmacokinetics of the non-parenteral administration of the zero-order release and the first-order release of mono-compartment drugs were established. Conclusion The pharmacokinetic theories of the zero-order release and the first-order release of mono-compartment drugs administered by non-parenteral route have been established. Since the zero-order release and the first-order release are the primary release patterns, the theory should be a key to explore the pharmacokinetics of the controlled/sustained release dosage forms.

关 键 词：零级释放 一级释放 单室模型 药物动力学 缓释 制剂 控释制剂 

分 类 号：R452[医药卫生—治疗学] R969.1[医药卫生—临床医学]