摘要
雷公藤甲素(TP)作为雷公藤的主要活性成分,具有抗炎、免疫抑制、抗生育、抗囊肿和抗肿瘤等作用,但其治疗窗窄,对消化系统、泌尿生殖系统和血液系统等有较大的毒副作用,因此临床开发研究受到了一定限制。本文主要针对TP药代动力学的研究进行整理和归纳,并概述了基于改善TP体内药动学特性所研发的新型TP衍生物和相关制剂,以期为TP的新药开发研究提供助益。
As a major active component of extracts derived from the medicinal plant Tripterygium wilfordii,triptolide（TP） has multiple pharmacological activities including anti-inflammatory,immunosuppressive,anti-fertility,anti-cystogenesis and antitumor activities.Nevertheless,its narrow therapeutic window and severe toxicities on digestive,genitourinary and hematopoietic systems have restricted its clinical development.This review will focus on the pharmacokinetic profiles of TP as well as new TP derivatives and formulations developed for improving TP pharmacokinetic characteristics.
出处
《药学与临床研究》
2012年第3期229-235,共7页
Pharmaceutical and Clinical Research
基金
国家自然科学基金(81173651)
中医药行业科研专项(200707008)
关键词
雷公藤甲素
药代动力学
毒性
衍生物
制剂
Triptolide
Pharmacokinetics
Toxicity
Derivatives
Formulations
