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M Hanano

Publications and source records attributed to M Hanano.

At least 235 records · Page 13Linked to original sources

Significance of 17-hydroxycorticosteroid glucuronide in urine as an index of salicylamide glucuronidation in guinea pigs.

The glucuronidation of 17-hydroxycorticosteroids (17-OHCS) and its effectiveness as an index of salicylamide (SAM) glucuronidation were examined in guinea pigs, the same cortisol type animals as man, treated with carbon tetrachloride (CCl4), D-galactosamine, phenobarbital, D,L-ethionine and alloxan. There was not a statistically significant correlation between the plasma clearance of SAM glucuronidation (CLglu) and the urinary excretion ratio of 17-OHCS glucuronide to total 17-OHCS in the intact, and CCl4, D-galactosamine, alloxan and D,L-ethionine treated guinea pigs (r = 0.158). However, there was a statistically significant correlation between the CLglu and the clearance of 17-OHCS glucuronidation obtained as urinary 17-OHCS glucuronide/plasma cortisol concentration (r = 0.738, p less than 0.1). It was proposed that the clearance of 17-OHCS glucuronide metabolized from endogenous cortisol could be used as an index to assess the drug glucuronidation activity.

17-Hydroxycorticosteroids↗

The study on the biological fate of paraben at the dose of practical usage in rat. II. The pharmacokinetic study on the blood concentration after the administration of ethyl paraben or p-hydroxybenzoic acid.

The biological fates of ethyl paraben and p-hydroxybenzoic acid in rat were investigated after intravenous and intraduodenal administrations at the dose of 2 mg/kg. The blood concentrations were measured in detail from 3 min after the administration at appropriate time intervals until 90 min. Areas under the blood concentration curves and clearances were calculated from these time course data. Ethyl paraben was little detected in blood after intraduodenal administration. It is suggested that the intestinal metabolism and the first pass effect in liver greatly contribute to the hydrolysis of ethyl paraben. Total radio activity after intraduodenal administration did not show the maximum peak and decreased rapidly. The maximum peak was not observed also in the time course of p-hydroxyhippuric acid after intravenous administration. It shows that not only the rate of hydrolysis but also absorption and conjugation are very rapid. The differences of the areas under the blood concentration curves of p-hydroxybenzoic acid or p-hydroxyhippuric acid was found between the routes or chemical forms of administration. The complex kinetic mechanisms were assumed in the biological fates of these compounds as follows: Conjugation to p-hydroxyhippuric acid is excellent in ethyl paraben administration than p-hydroxybenzoic acid, and in intraduodenal administration than intravenous administration. These phenomenon can not be explained by the conventional kinetic model which is constructed with the connected blood compartments in series. The kinetic models including the assumed routes conjugating directly ethyl paraben in blood or intestine to p-hydroxyhippuric acid were presented, and the least square curve fitting analyses were carried out on these kinetic models.

Animals↗

Effect of heparin injection on plasma protein binding of 1-anilino-8-naphthalenesulfonate and salicylate in rats.

After intravenous injection of heparin, the plasma protein binding of 1-anilino-8-naphthalenesulfonate (ANS) was remarkably decreased in rats. This effect occurred within one min after the injection of 1000 units/kg of heparin and lasted for about 30 min. The change in the binding of ANS was closely related to the plasma concentration of free acids (FFA), which was suggested as one of the heparin-induced inhibitors. The free fatty fraction of salicylate in plasma after the intravenous injection of heparin, has a pronounced variation, and also had a statistically significantly correlation with the plasma free fraction of ANS. It was suggested that ANS might be useful for the prediction of the heparin-induced changes in the plasma protein binding of acidic drugs.

Anilino Naphthalenesulfonates↗

Correlation between in vitro and in vivo drug metabolism rate: oxidation of ethoxybenzamide in rat.

In vitro and in vivo correlations of the microsomal oxidation of drugs were examined, using ethoxybenzamide as a model drug. Ethoxybenzamide disappearance time course from rat plasma in vivo was analyzed by a two-compartment model assuming a Michaelis-Menten type elimination process. Ethoxybenazmide oxidation in vitro was measured by the appearance rate of salicylamide in rat liver microsomal suspension. Parameters obtained were Vmax = 3.46 and 3.77 mumoles/min/kg body weight and Km = 0.378 and 0.192 mM, in vitro and in vivo, respectively.

Animals↗