Description:
Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in
vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability
due to its low aqueous solubility. The objective of this work was to enhance the dissolution
of cilostazol with the aim of formulating fast dissolving tablets for geriatrics and those of
swallowing difficulties.
Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted.
Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste
improving agents. The obtained products were investigated regarding differential scanning
calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction,
scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets
were prepared and evaluated.
Results: Thermal behavior of the developed products reflected reduced crystallinity, it also
suggested possible existence of new crystalline species with sucralose. Eutexia was also
suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated
size reduction with the deposition of the drug as submicron particles over the excipient surface.
Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The
optimized formulations were successively formulated into fast disintegrating tablets.
Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a
platform for the formulation of easy to use tablets with optimum drug release.
URL:
http://103.158.96.210:88/web_repository/uploads/no_data.jpg
Type:
Journal
Document:
Diploma III Farmasi
Date:
23-06-2024
Author:
Alaa Y. Bazeed