Abstract
EFFECT OF THE ADDED EXCIPIENTS ON THE RELEASE CHARACTERISTICS OF ACECLOFENAC FROM ALGINATE MICROCAPSULES

Osamah Al Rikabi*, Esmat Zein Eldein and Mohamed Osman

ABSTRACT

Aceclofenac is analog of the potent non-steroidal anti-inflammatory drug Diclofenac with low gastric damage. It belongs to class II according to the Biopharmaceutical classification system (BCS) that has poor aqueous solubility. The aim of this study was to investigate the potential of microcapsule of Aceclofenac with different polymers, to enhance dissolution rate of the drug and minimize gastric release. Alginate based micro-pellets were prepared to contain Aceclofenac in addition to other polymers to impart enteric effect. The selected polymers were Eudragit L100-55, Eudragit S100 and polyvinylpyrrolidone K90 (PVP) at different drug:alginate:polymer ratios. Microcapsules were prepared using ionotropic gelation method where the polymer was dispersed in sodium alginate solution. This liquid was then added drop wise to a solution containing divalent cations (calcium chloride solution). The resultant beads were separated, washed and dried. Before monitoring the dissolution pattern, the obtained beads were characterized using Fourier–transform infrared spectroscopy (FTIR) spectroscopic, X-ray diffraction and differential scanning calorimetry (DSC). The dissolution studies were conducted in acidic and alkaline media. Physical state characterization reflected no interaction between the drug and excipients with possible reduction in the drug crystalline nature. The release of Aceclofenac from the polymeric matrices was considerably reduced in the gastric phase. While the modified crystalline state was associated with a considerable enhancement in the dissolution rate in the intestinal phase, therefore, this technique is considered simple and promising eco-friendly strategy to enhance the dissolution rate of the drug with expected reduction in its deleterious effect on gastric mucosa.

Keywords: Aceclofenac, ionotropic gelation, enhance dissolution, Eudragit S100.


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