Kazan Federal University’s A. M. Butlerov Chemical Institute has developed a novel method for producing a metastable crystalline form of phenylbutazone, a widely used nonsteroidal anti-inflammatory drug. Phenylbutazone, known under various brand names, remains a common medicinal substance due to its affordability, well-documented side effects, and the absence of royalty payments required for manufacturing.
According to the institute’s press service, current methods for producing this form of phenylbutazone have a major drawback: they cause partial oxidation of the substance by atmospheric oxygen, compromising the product’s safety. The new method developed by Kazan chemists eliminates this oxidation and does not require the use of an inert atmosphere.
The development eliminates the need for solution preparation by using solid-phase processes, where a stable crystalline form of the substance is saturated with vapors of two solvents, one after another, explained Valery Gorbachuk, Professor of the Department of Physical Chemistry at Kazan Federal University’s Chemical Institute.
The first solvent creates a solvate, a crystalline compound containing both phenylbutazone and the solvent, which is then displaced by vapors of a second solvent to form a metastable form free of oxidation products. According to Gorbachuk, this metastable form allows for reduced drug dosages while maintaining or enhancing therapeutic effects and minimizing side effects.
The research was conducted as part of a government assignment, with the application for the invention submitted under the support of the Priority 2030 program.
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