马钱子及其制剂药动学研究进展

Research progress on pharmacokinetics of Strychnos nux-vomica and its preparation

从给药剂型和给药方式的角度入手,就近年来对马钱子及其相关制剂的的药动学研究进行概述。马钱子碱ig给药的绝对生物利用度为33.0%~47.8%,注射给药绝对生物利用度为75%左右;以马钱子碱为指标,马钱子总碱ig给药后的血药浓度最高,其次是马钱子碱,马钱子粉的血药浓度最低;马钱子碱或马钱子总碱脂质体注射给药后马钱子碱生物利用度有很大提高;另外外用制剂可减少马钱子碱和士的宁在体内的量,有利于降低毒性;口服马钱子制剂可延长马钱子碱和士的宁的体内作用时间,降低峰浓度。马钱子及其相关制剂的药动学研究还较薄弱,有待继续深入探索。

From the angle of dosage form and administration mode to start, the author reviewed the pharmacokinetics of Strychnos nux-vomica and its dosage forms in recent years. The absolute bioavailability of brucine by ig administration is 33.0%—47.8%, and that by injection is about 75%; With brucine as index, strychnos alkaloid by ig administration has the highest blood drug concentration, followed by brucine and nux vomica powder being the lowest; After injecting the brucine or strychnos alkaloid with liposome as a carrier, the brucine bioavailability was improved greatly; In addition, external preparation can reduce the content of brucine and strychnine in the body, which is beneficial to reduce the toxicity; Oral compound preparation extends the action time of brucine and strychnine in vivo, with reducing the peak concentration. However, the pharmacokinetic study on S. nux-vomica and its dosage forms is relatively weak and needs further exploration.