DEVELOPMENT AND CHARACTERIZATION OF POLYMERIC SOLID DISPERSED SYSTEMS OF NIMESULIDE OBTAINED BY SPRAY DRYING

Authors

DOI:

https://doi.org/10.11603/2312-0967.2024.4.15055

Keywords:

nimesulide, solid dispersed system, spray drying, solubility improvement, polymer carrier, spectrophotometry, active pharmaceutical ingredient

Abstract

The aim of the work - development of polymeric solid dispersed systems (SDS) of nimesulide by spray drying, study of their physicochemical characteristics and kinetics of release of the active pharmaceutical ingredient (API) from the obtained composites in vitro.

Materials and Methods. Solid dispersed systems of nimesulide based on pharmaceutically acceptable polymeric carrier polyvinylpyrrolidone (PVP) of different molecular weights (PVP K-12, PVP K-17, PVP K-25) were obtained using a Mini Spray Dryer B-290 (Büchi Labortechnik AG, Switzerland). The physicochemical characteristics of the developed solid dispersed systems were studied by Fourier transform infrared  (FTIR) spectroscopy using a Nicolet IS50 FTIR spectrometer with an ATR diamond crystal (Thermo Fisher Scientific, USA), as well as by differential scanning calorimetry using a DSC Q2000 device (TA Instruments, USA). The release kinetics of nimesulide from SDS was studied according to the dissolution test method for solid dosage forms in accordance with the requirements of the State Pharmacopoeia of Ukraine using a Vankel Varian VK 7000 dissolution tester with an external water heater VK 750D (Vankel, USA).

Results and Discussion. It has been established that the molecular weight of PVP affects both the degree of improvement of the water solubility of nimesulide in solid dispersed systems and the yield of the resulting composites. It was proved that the solubility of nimesulide in SDS based on PVP obtained by spray drying increases directly proportionally with a decrease in the molecular weight of the polymer. Among the studied samples, the solid dispersed system based on PVP K-12 is characterized by the highest percentage yield of SDS (82%) and the best indicator of increasing the solubility of nimesulide in water (5.84 times).

The results of differential scanning calorimetry confirmed the amorphization of nimesulide in the composition of solid dispersed systems obtained by spray drying. Using FTIR spectroscopy, it was proved that the interaction of nimesulide with polyvinylpyrrolide K-12 in the obtained SDS is carried out through the formation of intermolecular hydrogen bonds.

In vitro release kinetics studies using the “Dissolution” test showed that in all buffer media used (pH=6.8, 7.4 and 7.8) the degree of dissolution of the API in the composition of the spray-dried SDS is better compared to the original drug product “Aulin”, granules for oral suspension 100 mg/2g. Thus, in a buffered medium with pH=6.8, after 30 minutes of the test, the degree of dissolution of nimesulide in solid dispersed systems was about 14%, while the comparison drug “Aulin” showed only 8% dissolution of the API.

Conclusions. The spray drying method is an effective technological process for obtaining solid dispersed systems of nimesulide with increased solubility. This approach opens up new opportunities for the development of anti-inflammatory drugs based on nimesulide SDS with improved pharmacokinetic characteristics.

Author Biographies

V. G. Kostiuk, Kyiv National University of Technologies and Design

Postgraduate-student of Department of Industrial Pharmacy

V. I. Bessarabov, Kyiv National University of Technologies and Design; L. M. Litvinenko Institute of Physical-Organic Chemistry and Coal Chemistry of the National Academy of Sciences of Ukraine

DSc (Technical Sciences), Professor, Professor of Department of Industrial Pharmacy

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Published

2024-12-30

How to Cite

Kostiuk, V. G., & Bessarabov, V. I. (2024). DEVELOPMENT AND CHARACTERIZATION OF POLYMERIC SOLID DISPERSED SYSTEMS OF NIMESULIDE OBTAINED BY SPRAY DRYING. Pharmaceutical Review Farmacevtičnij časopis, (4), 39–48. https://doi.org/10.11603/2312-0967.2024.4.15055

Issue

No. 4 (2024)

Section

Pharmaceutical technology, biopharmacy, homeopathy, biotechnology

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