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Abstract <p><i>N</i>-Butyl-<i>N</i>-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) is a compound with both anxiolytic and antidepressant activity. Like most compounds developed as active pharmaceutical ingredients (APIs), it is virtually insoluble in water, which can negatively impact its bioavailability and complicate the development of tablets based on it. According to the Noyes–Whitney equation, the solubilization of poorly soluble APIs in water is possible by increasing the contact area with the aqueous medium or by achieving a supersaturated state in the solution. The surface area of APIs can be increased by micronization using a method such as rapid expansion of a supercritical solution (RESS). The solubility of GML-3 in CO<sub>2</sub> enables its micronization by the RESS method and the development of tablets with the micronized API.</p>

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Study of the Influence of Micronization of N-Butyl-N-Methyl-1-Phenylpyrrolo[1,2-a]Pyrazine-3-Carboxamide by Rapid Expansion of Supercritical Fluid on the Kinetics of Dissolution from Tablets

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • V. B. Markeev,
  • A. M. Vorobei,
  • S. V. Tishkov,
  • E. V. Blynskaya,
  • O. O. Parenago,
  • V. L. Dorofeev

摘要

Abstract

N-Butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3) is a compound with both anxiolytic and antidepressant activity. Like most compounds developed as active pharmaceutical ingredients (APIs), it is virtually insoluble in water, which can negatively impact its bioavailability and complicate the development of tablets based on it. According to the Noyes–Whitney equation, the solubilization of poorly soluble APIs in water is possible by increasing the contact area with the aqueous medium or by achieving a supersaturated state in the solution. The surface area of APIs can be increased by micronization using a method such as rapid expansion of a supercritical solution (RESS). The solubility of GML-3 in CO2 enables its micronization by the RESS method and the development of tablets with the micronized API.