Badiola N, Al-Angary A N, Halbert G W
Pharmacy Department, School of Pharmacy and Pharmacology, Strathclyde University, Glasgow, UK.
J Pharm Pharmacol. 1992 Apr;44(4):366-8. doi: 10.1111/j.2042-7158.1992.tb03624.x.
The effect of intravenous pre-treatment with empty small liposomes on the pharmacokinetics and metabolism of antipyrine in rabbits has been investigated. The measured half-life of antipyrine was 104 min and the volume of distribution was 830 mL kg-1. The excretion of metabolites in a 24 h urine sample was measured, the main metabolite 4-hydroxyantipyrine was excreted to a level of 10% with the free drug accounting for 4%. The norantipyrine and 3-hydroxymethylantipyrine metabolites were excreted to a level of 8 and 7%, respectively. The intravenous administration of liposomes at a dose equivalent to 8 mg of egg yolk phosphatidylcholine daily for one week, had no significant effect on any of the measured pharmacokinetic parameters. The half-life after liposome treatment was 110 min and the volume of distribution was 790 mL kg-1, the metabolic pattern in the urine was also unaltered. The results suggest that the repeated administration of low doses of liposomes do not affect the pharmacokinetics and metabolism of antipyrine.
已研究了用空的小脂质体进行静脉预处理对兔体内安替比林药代动力学和代谢的影响。测得安替比林的半衰期为104分钟，分布容积为830 mL·kg-1。测定了24小时尿液样本中代谢物的排泄情况，主要代谢物4-羟基安替比林的排泄量为10%，游离药物占4%。去甲安替比林和3-羟甲基安替比林代谢物的排泄量分别为8%和7%。以相当于每日8 mg蛋黄卵磷脂的剂量静脉注射脂质体，持续一周，对任何测得的药代动力学参数均无显著影响。脂质体处理后的半衰期为110分钟，分布容积为790 mL·kg-1，尿液中的代谢模式也未改变。结果表明，重复给予低剂量脂质体不会影响安替比林的药代动力学和代谢。
