[~3H]α-萜品烯醇在豚鼠体内的吸收、分布和排泄

α-萜品烯醇为艾叶油中的平喘成分,本文以inhal,po与iv[~3H]α-萜品烯醇研究其在豚鼠体内的吸收,分布和排泄。结果表明inhal,po后吸收快,但inhal时有大部分药物进入胃肠道;分布广、除细胞内、外间液外,还可能与血浆蛋白结合;在气管平滑肌,肺脏与心肌中有较高的浓度;消除速度快,inhal,po与iv的t_(1/2)β分别为5.92,8.45与13.33h,主要以原形由尿排泄。

Kinetic aspects of absorption,distribution and excretion of [~3 H] α-terpineol in guinea pigs

α-Terpineol is one of the antiasthmatic principles of essential oil of Artemisia argyi. The present paper reports the pharmaco kinetic studies of α-terpineol in guinea pig by isotope technique. On the basis of α-terpineol blood levels following administrations of [3H] α-terpineol by different routes, the pharmacokinetic parameters were calculated by one-compartment and two-compartment kinetic analysis. The results showed that the absorption rates of crterpineol by aerosolinhalation and oral administration were rapid, but a lot of aerosol were swallowed into gastrointestinal tract. The distribution rates of a-terpineol by orai or intravenous administration were also rapid, the drug was distributed widely in vivo. Except distribution in the intracellular and extracellular space, it might probably bind to plasma proteins. Radioactivity was found in trachcal smooth muscle, lung, heart, liver and kidney with rather high concentrations. The elimination rate of crterpineol was fast, its biological half-lives were 5.92 and 8.45 hours for inhalation and oral administration, respectively. α-Terpineol mainly excreted in urine as unchanged form.