Enhancement of dissolution and bioavailability of poorly soluble Telmisartan:Designing modified cyclodextrin inclusion complexes

Thirupati Ajmeera, Sonia Gera,

Abstract

Present work investigated the ability of modified Cyclodextrin such as sulphobutyl ether 7β - cyclodextrin (SBE7β - CD) to form an inclusion complex with telmisartan (TEL) , a poorly soluble drug and its related effects on dissolution rate and relative bioavailability. The binary systems of drug with modified cyclodextrin were prepared by different techniques like simple mixing, kneading and lyophiliza tion. Molecular modelling studies (docking) were carried out to understand and demonstrate significant interactions between SBE7β - CD and telmisartan. Resulting complexes were characterized by differential scanning calorimetry, x - ray powder diffractometry ( XRD), proton nuclear magnetic spectroscopy and infrared spectroscopy. The analytical studies authenticated the formation of an inclusion complex between telmisartan and sulfobutyl ether7β - cyclodextrin whereas XRD studies revealed an amorphous nature of the inclusion complex. Inclusion complexes displayed improved dissolution rate when compared to pure drug. Pharmacokinetic profile of complexes had shown a significant enhancement in the relative bioavailability of selected drug. Therefore, SBE7β - CD can be su ccessfully used as a carrier for the oral administration of telmisartan with enhanced bioavailability and industrial applicability in terms of scale up.

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