Research of pharmacotechnological properties, anti-inflammatory activity and stability of centrifugally formed solid dispersed system of nimesulide
DOI:
https://doi.org/10.30857/2786-5371.2026.2.7Keywords:
solid dispersion system, nimesulide, anti-inflammatory properties, active pharmaceutical ingredient, pharmaco-technological indicators, stabilityAbstract
Purpose. The purpose of the work is to study the pharmaco-technological properties, anti-inflammatory activity and stability of a solid dispersed system (SDS) of nimesulide obtained by centrifugal fiber formation.
Methodology. The study of the pharmaco-technological properties of a SDS of nimesulide based on polyvinylpyrrolidone (PVP) K-17 and mannitol obtained by the method of centrifugal fiber formation was carried out in accordance with the requirements of the State Pharmacopoeia of Ukraine. Anti-inflammatory activity was determined in vitro using a competitive enzyme-linked immunosorbent assay by inhibiting recombinant cyclooxygenase-2 (COX-2) with subsequent spectrophotometric detection of the reaction product at λ=405 nm and the half-maximal inhibition concentration (IC50) was calculated. Stability studies were performed on three experimental laboratory series under accelerated test conditions for 6 months, recording changes in the FTIR spectra of the test sample and the quantitative content of nimesulide in SDS.
Findings. It was established that the centrifugally formed SDS with the composition of nimesulide:PVP K-17:mannitol (5%:85%:10%, respectively) is characterized by optimal pharmaco-technological indicators, which indicates the possibility of developing medicinal products based on it in powder form without the need to add excipients. It was established for the first time that the developed TDS retains a pronounced inhibitory activity against COX-2: the IC50 value for the composition is 25.2 ± 3.5 μM, which is statistically comparable to the indicator of the native substance (26.5 ± 1.4 μM). It was confirmed that the developed SDS is stable under accelerated testing conditions, and its predicted shelf life is 2 years.
Originality. For the first time, the pharmaco-technological indicators, anti-inflammatory properties and stability of a solid dispersion system of nimesulide obtained by the method of centrifugal fiber formation have been comprehensively characterized.
Practical value. A highly soluble centrifugally formed solid dispersed system of nimesulide can be used as an active pharmaceutical ingredient (API) for the development of effective anti-inflammatory drugs with increased bioavailability.
Keywords: solid dispersion system; nimesulide; anti-inflammatory properties; active pharmaceutical ingredient; pharmaco-technological indicators; stability.
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