Studies on the effect of water-soluble polymers on drug-cyclodextrin complex solubility.
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 betaCD 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-betaCD-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.
Hirlekar
Rajashree S
RS
Department of Pharmaceutics, Bharati Vidyapeeth's College of Pharmacy, Sec-8, CBD Belapur, Navi Mumbai 400 614, Maharashtra, India. rshirlekar@rediffmail.com
Sonawane
Suneeta N
SN
Kadam
Vilasrao J
VJ
D047228:Angiotensin II Type 1 Receptor Blockers / Q000008:administration & dosage / Q000737:chemistry; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D003505:Cyclodextrins / Q000737:chemistry*; D000077405:Irbesartan; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013777:Tetrazoles / Q000008:administration & dosage / Q000737:chemistry; D014961:X-Ray Diffraction
D047228:Angiotensin II Type 1 Receptor Blockers; D001713:Biphenyl Compounds; D003505:Cyclodextrins; D004364:Pharmaceutical Preparations; D011108:Polymers; D013777:Tetrazoles; D000077405:Irbesartan