AAPS PharmSciTech

, Volume 10, Issue 1, pp 276–281 | Cite as

Preformulation Study of the Inclusion Complex Irbesartan-β-Cyclodextrin

Research Article

Abstract

The aim of the present work was to improve the solubility and dissolution profile of Irbesartan (IRB), a poorly water-soluble drug by formation of inclusion complex with β-cyclodextrin (βCD). Phase solubility studies revealed increase in solubility of the drug upon cyclodextrin addition, showing AL—type of graph with slope less than one indicating formation of 1:1 stoichiometry inclusion complex. The stability constant (K s) was found to be 104.39 M−1. IRB–βCD binary systems were prepared by cogrinding, kneading using alcohol, kneading using aqueous alcohol, and coevaporation methods. Characterization of the binary systems were carried out by differential scanning calorimetry, Fourier transform infrared spectroscopy, scanning electron microscopy, X-ray diffraction, and proton nuclear magnetic resonance. The dissolution profiles of inclusion complexes were determined and compared with those of IRB alone and physical mixture. Among the various methods, coevaporation was the best in which the solubility was increased and dissolution rate of the drug was the highest. The study indicated the usefulness of cyclodextrin technology to overcome the solubility problem of IRB.

Key words

β-cyclodextrin dissolution inclusion complex Irbesartan solubility 

Abbreviations

βCD

beta-cyclodextrins

CE

coevaporation

CG

cogrinding

DSC

differential scanning calorimetry

FTIR

Fourier transform infra-red spectroscopy

1H NMR

nuclear magnetic resonance

HCl

hydrochloric acid

IRB

Irbesartan

Ks

apparent stability constant

K

kneading

PM

physical mixture

SEM

scanning electron microscopy

TMS

tetramethylsilane

XRD

X-ray diffraction

Notes

Acknowledgment

We would like to thank Dr. Vikram Jagtap, Aarti Drugs Ltd, India for kindly supplying the drug, Irbesartan, and Dr. M.R. Vora, Signet, India for kindly supplying β-cyclodextrin.

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Copyright information

© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  1. 1.Department of PharmaceuticsBharati Vidyapeeth’s College of PharmacyNavi MumbaiIndia

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