期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 24, 期 15, 页码 -出版社
MDPI
DOI: 10.3390/ijms241512215
关键词
amorphous solid dispersions; composite; solubility; bioavailability; anxiolytics; antidepressants
This study aimed to develop a water-soluble, high-release active pharmaceutical ingredient (API) composite based on the practically water-insoluble API N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3), which has antidepressant and anxiolytic action, to ensure the bioavailability of the medicinal product. Composites obtained by creating amorphous solid dispersions using polyvinylpyrrolidone (PVP) or Soluplus® as a polymer were studied for crystallinity, stability, and API release into purified water. The results showed that the composites achieved amorphous state at 1:15 API:PVP ratio and 1:5 Soluplus® ratio, ensuring the solubility of GML-3 in purified water and maintaining the supercritical state in solution.
This work aimed to develop and characterize a water-soluble, high-release active pharmaceutical ingredient (API) composite based on the practically water-insoluble API N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3), a substance with antidepressant and anxiolytic action. This allows to ensure the bioavailability of the medicinal product of combined action. Composites obtained by the method of creating amorphous solid dispersions, where polyvinylpyrrolidone (PVP) or Soluplus(& REG;) was used as a polymer, were studied for crystallinity, stability and the release of API from the composite into purified water. The resulting differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), and dissolution test data indicate that the resulting composites are amorphous at 1:15 API: polymer ratios for PVP and 1:5 for Soluplus(& REG;), which ensures the solubility of GML-3 in purified water and maintaining the supercritical state in solution.
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