Study of structural and mechanical properties of suppositories with bifonazole

Abstract

Currently, candidal vulvovaginitis is one of the most common infectious lesions of the mucous membrane of the vulva and vagina. The prevalence of this infection is one of the main reasons for impaired reproductive function and the development of pregnancy complications. In addition, this pathology is an important medical and social problem both for the healthcare system and for society, as it significantly reduces the quality of life of patients due to the manifestation of characteristic adverse symptoms. Treatment of candidal vulvovaginitis should be not only etiotropic, considering the species of the causative agent, but also pathogenetic. In addition, this pathology is an important medical and social problem both for the healthcare system and for society. As it significantly reduces the quality of life of patients due to the manifestation of characteristic adverse symptoms. Treatment of candidal vulvovaginitis should be not only etiotropic, considering the species of the causative agent, but also pathogenetic. One of the promising biologically active substances is bifonazole, which is an antifungal compound of the azole group with a wide spectrum of action. Based on complex physico-chemical, microbiological and biopharmaceutical research, the Department of Medicines Technology of the Zaporizhzhia State Medical and Pharmaceutical University developed a rational composition of the soft vaginal dosage form of bifonazole – suppositories containing 0.3 g of the active substance on a hydrophobic carrier.

The aim of this work is to study the rheological characteristics of the vaginal dosage form of bifonazole, depending on the temperature regime of the production process for the suppositories manufacture.

Materials and methods. The study of the structural and mechanical characteristics of the suppository mass with bifonazole based on cocoa oil with the addition of 5 % emulsifier No. 1 was carried out using a rotary viscometer “Reotest-2” with a cylindrical device at a human body temperature of +37 °С and the temperature of the technological process of manufacturing the dosage form.

Results. They indicate the existence of a present structure in the suppository composition, that is evidenced by the decrease in effective viscosity simultaneously with the increase in deformation forces. The obtained data enable us to analyze the strength characteristics of the suppository mass and to calculate the main parameters of structural and mechanical studies, which allow us to conduct an objective assessment of the consistency studies of the system.

Conclusions. The consistent properties of the suppository mass with bifonazole based on cocoa oil with the addition of 5 % emulsifier No. 1 at human body temperature were studied. It was established, that it is a structured system with pronounced thixotropic properties, in which there is a uniform distribution of biologically active and auxiliary substances both at the time of manufacture and during use and long-term storage. It was found, that increasing the temperature of the suppository mass to +50 °С does not lead to a significant change in its structural and mechanical properties and transformation into a Newtonian system. Considering the obtained data, it was established, that the temperature regime for the manufacture of vaginal suppositories with bifonazole on a lipophilic basis (mixing, homogenization, pouring into molds) in the range of +50–55 °С creates sufficient fluidity of the mass for the unhindered implementation of the technological process and thixotropy of the suppositories, distribution of active and auxiliary substances in this dosage form.