E. V. Kompantseva, M. V. Gavrilin, I. I. Monastyreva
Mar 1, 2000
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Journal
Pharmaceutical Chemistry Journal
Abstract
Diazoline (mebhydrolin) is used as an antihistamine free o f both sedative (calming) and hypnotic effects, which is administered in cases when any suppressing action upon the central nervous system is undesirable [1]. The drug is available in the form of 50 and 100 mg dragee produced in Russia and Ukraine [2, 3]. It was reported that the biological accessibility of diazoline in these forms amounts to 28 30% relative to the parent substance [4]. Moreover, diazoline dragee administered perorally produced strong irritation of the mucous membrane of the stomach, leading to discomfort in patients upon multiply repeated drug administration. One way of solving this problem is to develop diazoline tablets with zinc sulfate containing 200 and 400 mg of the parent substance [5]. Administration of these large doses increases the diazoline concentration in the blood. We have also developed 50 and 100 mg diazoline tablets based on the products o f diazoline reaction with 13-cyclodextrin. Pharmacological investigations indicated a 30% increase in the bioaccessibility of diazoline in tablets as compared to that in dragee and showed the absence of local irritation effects [6]. The purpose of this work was to elaborate the methods for analysis and standardization of diazoline tablets and to determine the shelf life o f the drug.