Abstract

ORAL INTESTINAL PERMEABILITY AND PHARMACOKINETIC EVALUATION OF OLMESARTAN MEDOXOMIL COMPLEXES IN ALBINO MALE RABBITS

G. Sandhyarani*, Naga Soumya P. and M. Sarangapani

ABSTRACT

For poorly soluble drugs, solubility is one of the rate limiting parameters to achieve their desired concentration in systemic circulation for pharmacological response. The solubility of these drugs can be solved by different technological approaches during the pharmaceutical product development such as: solid dispersion, Micronization, Salt formation, inclusion complexation etc. Olmesartan medoxomil (OLM) is an angiotensin II receptor antagonist used in the treatment of hypertension. The absolute bioavailability is about 26%, it is bound to plasma proteins to an extent of about 99 %. So there is strong need to enhance aqueous solubility of hydrophobic drug by different methods like solid dispersion, inclusion complexation etc. Hence the study aimed to develop inclusion complexes of the model drug (olmesartan medoxomil) and evaluate the physicochemical parameters of the inclusion complexes, in-vitro intestinal permeability studies and in-vivo pharmacokinetic studies and revealing that naringin (P-glycoprotein inhibitor) can be used a pharmaceutical excipient for inclusion complex to increase in intestinal permeability and in-vivo pharmacokinetic performance of olmesartan. However, further studies are required for comprehensive, systematic, multi-disciplinary evaluation of various claims to make effective use of these products.

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