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To enhance dissolution rate of poorly water-soluble drugs: glucosamine hydrochloride as a potential carrier in solid dispersion formulations.
Colloids Surf B Biointerfaces. 2010 Mar 01; 76(1):170-8.CS

Abstract

The solid dispersion technique is the most effective method for improving the dissolution rate of poorly water-soluble drugs, however this is reliant on a suitable carrier and solvent being selected. The work presented explores D-glucosamine HCl (G-HCl) as a potential hydrophilic carrier to improve dissolution rate of a poorly water-soluble drug, carbamazepine (CBZ), from physical mixtures and solid dispersion formulations. The effect of different solvents in the preparation of solid dispersion formulations was also investigated. Solid dispersions of the drug and G-HCl were prepared using different ratios by the conventional solvent evaporation method. Different solvents (ethanol, acetone and water) were used as second variable in the preparation of solid dispersions. Physical mixtures of CBZ and G-HCl were also prepared for comparison. The properties of all solid dispersions and physical mixtures were studied using a dissolution tester, FT-IR, SEM and DSC. These results showed that the presence of glucosamine can increase dissolution rate of CBZ compared to pure CBZ. All solid dispersions of CBZ-G-HCl showed considerably a higher dissolution rate than the corresponding physical mixtures. The presence of water during preparation of the solid dispersions reduced the dissolution rate of CBZ due to formation of carbamazepine dihydrate during the preparation of solid dispersion, as proved by DSC and FT-IR studies. To facilitate comparison, the dissolution efficiency was calculated for solid dispersions prepared with different solvents and the dissolution efficiency can generally be ranked as follows: ethanol>acetone>ethanol-water>acetone-water when the ratios of drug to carrier were 4:1 and 2:1. It has thus been shown that the use of G-HCl in solid dispersion formulations can significantly enhance the dissolution rate of poorly water-soluble drugs such as carbamazepine. This amino sugar could be used as a new carrier in solid dispersion formulations and would have significant commercial potential.

Authors+Show Affiliations

Medway School of Pharmacy, University of Kent, Kent, UK.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

19945828

Citation

Al-Hamidi, Hiba, et al. "To Enhance Dissolution Rate of Poorly Water-soluble Drugs: Glucosamine Hydrochloride as a Potential Carrier in Solid Dispersion Formulations." Colloids and Surfaces. B, Biointerfaces, vol. 76, no. 1, 2010, pp. 170-8.
Al-Hamidi H, Edwards AA, Mohammad MA, et al. To enhance dissolution rate of poorly water-soluble drugs: glucosamine hydrochloride as a potential carrier in solid dispersion formulations. Colloids Surf B Biointerfaces. 2010;76(1):170-8.
Al-Hamidi, H., Edwards, A. A., Mohammad, M. A., & Nokhodchi, A. (2010). To enhance dissolution rate of poorly water-soluble drugs: glucosamine hydrochloride as a potential carrier in solid dispersion formulations. Colloids and Surfaces. B, Biointerfaces, 76(1), 170-8. https://doi.org/10.1016/j.colsurfb.2009.10.030
Al-Hamidi H, et al. To Enhance Dissolution Rate of Poorly Water-soluble Drugs: Glucosamine Hydrochloride as a Potential Carrier in Solid Dispersion Formulations. Colloids Surf B Biointerfaces. 2010 Mar 1;76(1):170-8. PubMed PMID: 19945828.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - To enhance dissolution rate of poorly water-soluble drugs: glucosamine hydrochloride as a potential carrier in solid dispersion formulations. AU - Al-Hamidi,Hiba, AU - Edwards,Alison A, AU - Mohammad,Mohammad A, AU - Nokhodchi,Ali, Y1 - 2009/11/11/ PY - 2009/07/10/received PY - 2009/09/22/revised PY - 2009/10/19/accepted PY - 2009/12/1/entrez PY - 2009/12/1/pubmed PY - 2010/5/11/medline SP - 170 EP - 8 JF - Colloids and surfaces. B, Biointerfaces JO - Colloids Surf B Biointerfaces VL - 76 IS - 1 N2 - The solid dispersion technique is the most effective method for improving the dissolution rate of poorly water-soluble drugs, however this is reliant on a suitable carrier and solvent being selected. The work presented explores D-glucosamine HCl (G-HCl) as a potential hydrophilic carrier to improve dissolution rate of a poorly water-soluble drug, carbamazepine (CBZ), from physical mixtures and solid dispersion formulations. The effect of different solvents in the preparation of solid dispersion formulations was also investigated. Solid dispersions of the drug and G-HCl were prepared using different ratios by the conventional solvent evaporation method. Different solvents (ethanol, acetone and water) were used as second variable in the preparation of solid dispersions. Physical mixtures of CBZ and G-HCl were also prepared for comparison. The properties of all solid dispersions and physical mixtures were studied using a dissolution tester, FT-IR, SEM and DSC. These results showed that the presence of glucosamine can increase dissolution rate of CBZ compared to pure CBZ. All solid dispersions of CBZ-G-HCl showed considerably a higher dissolution rate than the corresponding physical mixtures. The presence of water during preparation of the solid dispersions reduced the dissolution rate of CBZ due to formation of carbamazepine dihydrate during the preparation of solid dispersion, as proved by DSC and FT-IR studies. To facilitate comparison, the dissolution efficiency was calculated for solid dispersions prepared with different solvents and the dissolution efficiency can generally be ranked as follows: ethanol>acetone>ethanol-water>acetone-water when the ratios of drug to carrier were 4:1 and 2:1. It has thus been shown that the use of G-HCl in solid dispersion formulations can significantly enhance the dissolution rate of poorly water-soluble drugs such as carbamazepine. This amino sugar could be used as a new carrier in solid dispersion formulations and would have significant commercial potential. SN - 1873-4367 UR - https://www.unboundmedicine.com/medline/citation/19945828/To_enhance_dissolution_rate_of_poorly_water_soluble_drugs:_glucosamine_hydrochloride_as_a_potential_carrier_in_solid_dispersion_formulations_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0927-7765(09)00524-4 DB - PRIME DP - Unbound Medicine ER -