Methanesulfonic Acid Derivative of p, p′-Diaminodiphenylsulfone. II. Pharmacokinetics and Availability of Parental Drug in Rabbit

Abstract

Pharmacokinetic studies on various methanesulfonic acid derivatives of p,p'diamino- diphenylsulfone (Da) were carried out on rabbit and the liberation of parental Da was pursued. The general formula of the studied derivatives is [formula omitted], where R are H-, CH3-, HOCH2(CHOH)4-(promin) and C6H5-. The time courses of the blood concentration for all the derivatives and parental Da administered intravenously were represented in biexponential equations. The elimination rates of the water-soluble derivatives were about 10-fold larger than that of parental Da. The distribution volume of central compartment for Da was larger than those of the derivatives. No detectable amount of Da was found in blood after the i.v. administrations of promin and the derivative of R=H. From the viewpoint of drug availability, the area under liberated Da vs. time curve was compared to that of intact Da and deconvolution calculation was also carried out. © 1974, The Pharmaceutical Society of Japan. All rights reserved.