Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers
| Autor: | Om Prakash Katare, Naveen Ahuja, Bhupinder Singh |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Chemistry
Pharmaceutical Pharmaceutical Science Excipient Polyethylene glycol Crystallography X-Ray Diffusion Lactones chemistry.chemical_compound Spectroscopy Fourier Transform Infrared medicine Organic chemistry Sulfones Solubility Dissolution Drug Carriers Aqueous solution Calorimetry Differential Scanning Chemistry Hydrotrope technology industry and agriculture Water General Medicine Models Theoretical Poloxamer Kinetics Models Chemical Chemical engineering Microscopy Electron Scanning Thermodynamics Citric acid Biotechnology medicine.drug |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 65:26-38 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2006.07.007 |
| Popis: | Role of various water-soluble carriers was studied for dissolution enhancement of a poorly soluble model drug, rofecoxib, using solid dispersion approach. Diverse carriers viz. polyethylene glycols (PEG 4000 and 6000), polyglycolized fatty acid ester (Gelucire® 44/14), polyvinylpyrollidone K25 (PVP), poloxamers (Lutrol® F127 and F68), polyols (mannitol, sorbitol), organic acid (citric acid) and hydrotropes (urea, nicotinamide) were investigated for the purpose. Phase-solubility studies revealed AL type of curves for each carrier, indicating linear increase in drug solubility with carrier concentration. The sign and magnitude of the thermodynamic parameter, Gibbs free energy of transfer, indicated spontaneity of solubilization process. All the solid dispersions showed dissolution improvement vis-a-vis pure drug to varying degrees, with citric acid, PVP and poloxamers as the most promising carriers. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer–Peppas model and the drug release kinetics primarily as Fickian diffusion. Solid state characterization of the drug–poloxamer binary system using XRD, FTIR, DSC and SEM techniques revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement in dissolution rate. |
| Databáze: | OpenAIRE |
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