The widespread distribution of Mycobacterium tuberculosis strains with not only multiple but also broad drug resistance stimulates the development of new effective anti-tuberculosis drugs. The antimycobacterial activity of new furoxan sulfonamides against the international reference strain Mycobacterium tuberculosis H37Rv was studied in vitro. A clear inhibitory effect was shown by substances 4d and 4f (MIC = 3.02 ± 0.07 and 6.31 ± 1.32 μg/ml respectively). The results obtained in the present study demonstrate the potential of new furoxan derivatives as anti-tuberculosis agents.
This article describes the application of a technological approach to increasing solubility consisting of obtaining model mixtures of the active pharmaceutical ingredient (API) N-benzyl-N-methyl-1-phenylpyrrolo-[1,2-a]pyrazine-3-carboxamide (GML-1) with polymers with solubilizing properties, by codissolution in 96
This article presents results obtained during the development of the composition and technology for producing tablets of a sedative drug containing a dry extract from a mixture of stinging nettle, lemon balm, and motherwort. The work examined seven compositions differing in terms of the presence and nature of excipients prepared by direct pressing and wet granulation. The technical properties and quality indicators of the compressed masses of the seven tablet compositions of the sedative drug were studied. The results led to selection of a composition prepared by wet granulation with the following composition: active ingredient: dry extract 0.25 g; excipients: lactose 0.063 g, potato starch 0.034 g, and calcium stearate 0.003 g. The wet granulation technology developed here ensured production of tablets meeting the requirements of the State Pharmacopoeia of the Russian Federation, XV edition (SP RF XV). Studies of the acute toxicity parameters of this sedative drug in the form of tablet granules given intragastrically at doses of 30, 40, 50 g/kg showed that no symptoms of acute poisoning were found in any of the experimental animals (mice) and that there was no mortality. The drug was shown to belong to toxicity class IV, low-toxicity substances: LD50 was 50 g/kg.
A composition and technology for producing syrups based on a dry extract from the herb of Melissa officinalis L. have been developed using the excipients sucrose (64 wt
