European Journal of Biomedical and Pharmaceutical Sciences

ENHANCEMENT OF IRBESARTAN DISSOLUTION VIA CONTROLLED PRECIPITATION: PREPARATION OF ORALLY DISPERSIBLE COMPACTS

Khaleel M. Abuleid*, Ebtessam A. Essa and Gamal M. El Maghraby

ABSTRACT

Irbesartan is an antihypertensive angiotensin II receptor antagonist. It suffers poor aqueous solubility. Therefore, the aim of this work was to investigate the potential use of controlled precipitation over solid carrier technique to enhance irbesartan dissolution rate. Hydrophilic polymers were used to increase the hydrophilicity of the prepared crystals. The selected polymers were polyvinylpyrrolidone 40T (PVP), hydroxypropylmethyl cellulose E5 (HPMC) and polyethylene glycol 4000 (PEG). The work was extended to develop fast disintegrated compacts. Aerosil 200 was dispersed in ethanolic solution of irbesartan in presence hydrophilic polymers. Distilled water was added as antisolvent to precipitate the drug over Aerosil 200. Unprocessed and drug liberated from its ethanolic solution were used as negative and positive control, respectively. The resultant precipitate were centrifuged and dried at ambient temperature. The recovered microparticles were subjected to FTIR spectroscopic, X-ray diffraction, thermal analyses and dissolution studies. The FTIR spectroscopy excluded any interaction between irbesartan and excipients. The thermal analysis reflected possible reduction in crystal size after controlled precipitation in the presence of hydrophilic polymers. This was further confirmed by X-ray diffraction. These changes was associated with a significant enhancement irbesartan dissolution rate. The recovered microcrystals were successfully formulated as rapidly disintegrating compacts with subsequent fast drug liberation. Precipitation over large solid surface area in presence of hydrophilic polymers during precipitation process is a simple promising technique for improving dissolution of slowly dissolving drugs with high scaling up potential.

Keywords: Irbesartan, controlled precipitation, Aerosil, fast disintegrating tablets.