Background:Olmesartan medoxomil (OLM), an anti-hypertensive agent administered orally has absolute bioavailability of only 26% due to the poor aqueous solubility (<7.75 μg/ml). The present investigation aimed at enhancing the oral bioavailability of OLM by improving its solubility and dissolution rate by preparing nanosuspensions.Materials and methods:The nanosuspensions of OLM were prepared using media milling technique followed by its lyophilization using mannitol as a cryoprotectant. Various formulation as well as process parameters were optimized in order to achieve desirable size and saturation solubility. Characterization of the prepared nanosuspension was done with respect to particle size, zeta potential, saturation solubility, dissolution rate, morphology study (TEM), in-vitro and exvivo drug diffusion study. Evaluation of the crystalline state before and after particle size reduction was done by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD).Results:The results indicated that the initial crystalline state is preserved following particle size reduction and that the saturation solubility, dissolution velocity and diffusion rate of the drug from the nanosuspension is significantly higher than that of the plain drug suspension as well as from the marketed tablet formulation.Conclusion:Nanosuspension seems to be a promising approach for bioavailability enhancement because of the simple method of its preparation and its universal applicability.
Background: Olmesartan medoxomil (OLM), an anti-hypertensive agent administered orally, has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). Inclusion complexation with cyclodextrins (CD) has been reported to increase the aqueous solubility of various compounds. Aim: The present investigation aimed to enhancing the oral bioavailability of OLM by inclusion complexation with 2-hydroxypropylβ-cyclodextrin (HP-β-CD). Materials and Methods: The inclusion complexes with HP-β-CD were prepared using two different methods, viz., physical mixture and kneading. The prepared complexes were characterized for various parameters such as drug content, aqueous solubility, dissolution study, in vitro diffusion, intestinal permeability and stability study. The formation of the inclusion complex was confirmed by differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy. Results: The solubility, dissolution, diffusion rate, and intestinal permeability of the prepared complexes were found to be significantly higher than that of the plain drug. Among the two methods used for formation of inclusion complex, KN method gave higher solubility rates and hence is a better method when compared with PM. Conclusion: The approach seems to be promising in improving the oral bioavailability of OLM.
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