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Published on:August 2016
Indian Journal of Pharmaceutical Education and Research, 2016; 50(3s):S209-S217
Original Article | doi:10.5530/ijper.50.3.31

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods


Authors and affiliation (s):

Pankaj Vijay Dangre*, Mangesh Dinanath Godbole, Priyanka Vijay Ingale, Debarshi Kar Mahapatra

Department of Pharmaceutics, Kamla Nehru College of Pharmacy, Nagpur, Maharashtra, INDIA.

Abstract:

Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

Key words: Eprosartan mesylate, Solid dispersion, Dissolution, Bioavailability, Characterization.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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