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Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility

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Abstract

The effect of complexation of irbesartan (IRB), a practically water-insoluble drug, with cyclodextrins in presence of different concentrations of water-soluble polymers (PEG 4000 and PVP K-90) on the dissolution rate of the drug has been investigated. Phase solubility studies were carried out to evaluate the solubilizing power of βCD in association with water-soluble polymers towards IRB and to determine the apparent stability constant (K S) of the complexes. Improvement in K S value for ternary complexes (IRB–βCD–polymers) clearly proved the benefit on the addition of water-soluble polymer to increase complexation efficiency. The dissolution rate of the drug from ternary systems containing PEG 4000 and PVP K-90 was higher as compared to the binary system. An optimum increase in the dissolution rate of the drug was observed at a polymer concentration of 5% w/w for PVP K-90 and 10% w/w for PEG 4000. DSC, FTIR, SEM, and XRD studies were carried out to characterize the complexes.

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Abbreviations

IRB:

irbesartan

βCD:

beta-cyclodextrins

DSC:

differential scanning calorimetry

FTIR:

Fourier transform infrared spectroscopy

XRD:

X-ray diffraction

SEM:

scanning electron microscopy

K S :

apparent stability constant

CE:

co-evaporation

HCl:

hydrochloric acid

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Authors and Affiliations

  1. Department of Pharmaceutics, Bharati Vidyapeeth’s College of Pharmacy, Sec-8, CBD Belapur, Navi Mumbai, 400 614, Maharashtra, India

    Rajashree S. Hirlekar, Suneeta N. Sonawane & Vilasrao J. Kadam

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  1. Rajashree S. Hirlekar
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  2. Suneeta N. Sonawane
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  3. Vilasrao J. Kadam
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Correspondence to Rajashree S. Hirlekar.

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Hirlekar, R.S., Sonawane, S.N. & Kadam, V.J. Studies on the Effect of Water-Soluble Polymers on Drug–Cyclodextrin Complex Solubility. AAPS PharmSciTech 10, 858–863 (2009). https://doi.org/10.1208/s12249-009-9274-6

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