The study and selection of excipients for formulation of antimycobacterial capsules with propiltiodiazolochinazolin one

Abstract

Introduction: Tuberculosis is a bacterial infection, endemic and contagious disease, caused by Mycobacterium tuberculosis, which affects, according to statistics of the World Health Organization year 2014, 9.6 million of population, including new cases of illness 6 million and 480 thousands multidrug-resistant TB. The studies of TB drugs in our country and from the world, have demonstrate that the efficiency of treatment is increasingly smaller. So, our goal is the formulation of capsules with propiltiodiazolochinazolin-one, a new original compound antimycobacterial.

Materials and methods:We studed the bibliographic advanced nomenclature of excipients used most often in solid formulations with antimycobacterial therapeutic effect, depending on the structure of active substances and physico-chemical properties. We selected the following auxiliary substances: anhydrous lactose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyvinylpyrrolidone, sodium starch gluconate, polyethyleneglycol 4000, 6000.

Results and discussion: Propiltiodiazolochinazolin-one is a microcrystalline substance, insoluble in water, which allow us to choose excipients which can be used in gels, to obtain granules and excipients with a certain concentration of water, to obtain powders. In the base of the list of selected excipients, were elaborate six formulation of capsules, for which subsequently will be determinated the physico-chemical and technology properties of powders and granulates.

Conclusion: The selected excipients, according to the physico-chemical characteristics, the structure and the therapeutic effects of the active substance, allow the formulation of the antimycobacterial capsules with propiltiodiazolochinazolin-one.