[The pharmacokinetic study of 3H-alpha-2-butylhydroxybenzyl alcohol in rabbits].

A derivative of Gastrodigenin, alpha-2-butylhydroxybenzyl alcohol, has shown a high distribution in the mice brain and stronger pharmacologic effects than its parent compounds. With 3H-alpha-2-butylhydroxybenzyl alcohol as radioactive tracer, pharmacokinetic data were obtained after the intravenous administration of a single dose alpha-2-butylhydroxybenzyl alcohol to rabbits, according to a cross-over design. Then, serial plasma samples were taken from 1 min to 480 min and measured by liquid scintillation counter. The data were analyzed by IBMPC computer for the estimation of pharmacokinetic parameters and the judgement of compartment model with a program recently developed by ourselves. The results suggested that the pharmacokinetics of alpha-2-butylhydroxybenzyl alcohol accords with the two compartment open model based on either the comparison of the calculated theoretic value with measured concentration or F test for the model judgement, and that the process of distribution was quite rapid, and the elimination half-life (T1/2 beta) was 12 h, indicating a slow elimination process.

[The distribution of 3H-alpha-sec-butyl-p hydroxybenzyl alcohol in mice].

alpha-sec-butyl-p-hydroxybenzyl alcohol is a derivative of gastrodigenin. It dissolves in lipid and passes through the blood-brain barrier more easily than gastrodin does. The distribution experiment has demonstrated that 3H-alpha-sec-butyl-p-hydroxybenzyl alcohol in the brain of mice is higher than in other organs, such as the liver, kidney and intestines. Radioactivity of brain tissue rises to the highest peak in about 1/2-2 min after intravenous injection. Each gram of the brain tissue takes up 21.89% radioactivity of the total dose administered. The sedative effect of alpha-sec-butyl-p-hydroxybenzyl alcohol on the center is rapid and short. It has been proved by the reactions in mice, results indicated by the electrocorticogram obtained from the mice after giving alpha-sec-butyl-p-hydroxybenzyl alcohol, and the correspondence with the distribution of alpha-sec-butyl-p-hydroxybenzyl alcohol in the mouse brain.