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Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers.
Eur J Pharm Biopharm. 2007 Jan; 65(1):26-38.EJ

Abstract

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-à-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.

Authors+Show Affiliations

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16962750

Citation

Ahuja, Naveen, et al. "Studies On Dissolution Enhancement and Mathematical Modeling of Drug Release of a Poorly Water-soluble Drug Using Water-soluble Carriers." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 65, no. 1, 2007, pp. 26-38.
Ahuja N, Katare OP, Singh B. Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur J Pharm Biopharm. 2007;65(1):26-38.
Ahuja, N., Katare, O. P., & Singh, B. (2007). Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 65(1), 26-38.
Ahuja N, Katare OP, Singh B. Studies On Dissolution Enhancement and Mathematical Modeling of Drug Release of a Poorly Water-soluble Drug Using Water-soluble Carriers. Eur J Pharm Biopharm. 2007;65(1):26-38. PubMed PMID: 16962750.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. AU - Ahuja,Naveen, AU - Katare,Om Prakash, AU - Singh,Bhupinder, Y1 - 2006/07/20/ PY - 2006/03/11/received PY - 2006/06/14/revised PY - 2006/07/13/accepted PY - 2006/9/12/pubmed PY - 2007/2/3/medline PY - 2006/9/12/entrez SP - 26 EP - 38 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 65 IS - 1 N2 - 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-à-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. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/16962750/Studies_on_dissolution_enhancement_and_mathematical_modeling_of_drug_release_of_a_poorly_water_soluble_drug_using_water_soluble_carriers_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(06)00190-1 DB - PRIME DP - Unbound Medicine ER -