Romanian Society of Pharmaceutical Sciences

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IRBESARTAN DISSOLUTION ENHANCEMENT USING PEG-BASED SOLID DISPERSIONS: THE EFFECT OF PEG MOLECULAR WEIGHTS

NOUSHIN BOLOURCHIAN *, FATEMEH MIRZAYEH FASHAMI, SEYED MOHSEN FOROUTAN

Department of Pharmaceutics and Pharmaceutical Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran

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The aim of the present study was to enhance the dissolution of irbesartan (IBS), a poorly soluble drug, using solid dispersion (SD) with different molecular weights of polyethylene glycol (PEG). Irbesartan loaded SDs and PMs (physical mixtures) were prepared with different drug: carrier ratios using PEG 6000, 10000 and 20000. Dissolution behaviour, physical state of formulations as well as solubility were studied on the formulations. Based on the results, the dissolution rate was remarkably increased in all formulations compared to the intact IBS. However, the dissolution improvement in SDs was more than related PMs. The PEG molecular weight was an effective factor on the results. The highest dissolution efficiency (DE60 = 95.47%) was obtained for IBS:PEG 10000 ratio of 1:5. Saturation solubility of IBS was also increased significantly due to the presence of hydrophilic carrier as well as reduced drug particle size. The negative values of Gibbs free energy revealed the spontaneous process of drug solubilisation in aqueous polymer environment. The results confirmed no polymorphic changes during sample preparation.