炔诺酮与异烟肼对小型猪口服联合给药后的相互作用。

Interaction of norethindrone and isoniazid following their oral co-administration to the minipig.

作者信息

Loo J C, Jordan N, Menzies J A, Watanabe H

出版信息

Biopharm Drug Dispos. 1983 Apr-Jun;4(2):145-50. doi: 10.1002/bdd.2510040206.

Abstract

Following the oral co-administration of isonicotinic acid hydrazide and norethindrone to minipigs, the hydrazone of norethindrone was detected in plasma as its p-methoxybenzaldehyde derivative, using a high performance liquid chromatographic technique. The suspected precursor of the hydrazone of norethindrone was isonicotinyl hydrazone of norethindrone, a reaction product probably formed between norethindrone and isonicotinic acid hydrazide in the acid environment of the stomach. An in vitro liver metabolite of isonicotinyl hydrazone of norethindrone was isolated following derivatization with p-methoxybenzaldehyde and characterized by high resolution mass spectrometric and radiochemical techniques. The results demonstrated that the hydrazone of norethindrone is a metabolite of isonicotinyl hydrazone of norethindrone.

摘要

对小型猪口服异烟肼和炔诺酮后，采用高效液相色谱技术在血浆中检测到炔诺酮腙的对甲氧基苯甲醛衍生物。炔诺酮腙的疑似前体是炔诺酮异烟酰腙，它可能是炔诺酮与异烟肼在胃的酸性环境中反应生成的产物。对炔诺酮异烟酰腙进行对甲氧基苯甲醛衍生化后，分离出其体外肝脏代谢物，并通过高分辨质谱和放射化学技术对其进行了表征。结果表明，炔诺酮腙是炔诺酮异烟酰腙的代谢产物。