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A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution.
Arch Pharm Res. 2013 Jan; 36(1):79-85.AP

Abstract

A novel surface-attached, spray-dried solid dispersion containing poorly water-soluble carvedilol (CV) without any change in the crystallinity was prepared using water, polyvinylpyrrolidone (PVP K30) and Tween 80. The solid dispersion was optimized by investigating the effects of the weight ratios of Tween 80/PVP K30 and carrier/drug on the aqueous solubility of CV. The optimum solid dispersion consisted of a relatively low carrier to drug weight ratio: the weight ratio of CV/PVP K30/Tween 80 was 12/4/2. Unlike conventional methods of solid dispersion preparation, this method yielded CV-loaded solid dispersion with no change in the crystallinity of the drug as was evident from SEM, DSC and XRD. It was demonstrated that the solid dispersions prepared had hydrophilic carriers attached to the surface of the drug, thus changing it from a hydrophobic to a hydrophilic form without changing the crystalline form. The optimized solid dispersion improved the drug solubility and dissolution rate by about 11,500-fold and twofold, respectively. It was further suggested that this method of solid dispersion preparation is better than conventional methods in terms of environmental and industrial standpoints. Thus, it was concluded that CV-loaded solid dispersion prepared using this method would be of use for delivering poorly water-soluble CV with enhanced solubility and dissolution, but without crystalline changes.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

23328872

Citation

Lee, Sung Neung, et al. "A Novel Surface-attached Carvedilol Solid Dispersion With Enhanced Solubility and Dissolution." Archives of Pharmacal Research, vol. 36, no. 1, 2013, pp. 79-85.
Lee SN, Poudel BK, Tran TH, et al. A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution. Arch Pharm Res. 2013;36(1):79-85.
Lee, S. N., Poudel, B. K., Tran, T. H., Marasini, N., Pradhan, R., Lee, Y. I., Lee, D. W., Woo, J. S., Choi, H. G., Yong, C. S., & Kim, J. O. (2013). A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution. Archives of Pharmacal Research, 36(1), 79-85. https://doi.org/10.1007/s12272-013-0008-7
Lee SN, et al. A Novel Surface-attached Carvedilol Solid Dispersion With Enhanced Solubility and Dissolution. Arch Pharm Res. 2013;36(1):79-85. PubMed PMID: 23328872.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution. AU - Lee,Sung Neung, AU - Poudel,Bijay Kumar, AU - Tran,Tuan Hiep, AU - Marasini,Nirmal, AU - Pradhan,Roshan, AU - Lee,Young Im, AU - Lee,Dong Won, AU - Woo,Jong Soo, AU - Choi,Han-Gon, AU - Yong,Chul Soon, AU - Kim,Jong Oh, PY - 2013/1/19/entrez PY - 2013/1/19/pubmed PY - 2013/7/20/medline SP - 79 EP - 85 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 36 IS - 1 N2 - A novel surface-attached, spray-dried solid dispersion containing poorly water-soluble carvedilol (CV) without any change in the crystallinity was prepared using water, polyvinylpyrrolidone (PVP K30) and Tween 80. The solid dispersion was optimized by investigating the effects of the weight ratios of Tween 80/PVP K30 and carrier/drug on the aqueous solubility of CV. The optimum solid dispersion consisted of a relatively low carrier to drug weight ratio: the weight ratio of CV/PVP K30/Tween 80 was 12/4/2. Unlike conventional methods of solid dispersion preparation, this method yielded CV-loaded solid dispersion with no change in the crystallinity of the drug as was evident from SEM, DSC and XRD. It was demonstrated that the solid dispersions prepared had hydrophilic carriers attached to the surface of the drug, thus changing it from a hydrophobic to a hydrophilic form without changing the crystalline form. The optimized solid dispersion improved the drug solubility and dissolution rate by about 11,500-fold and twofold, respectively. It was further suggested that this method of solid dispersion preparation is better than conventional methods in terms of environmental and industrial standpoints. Thus, it was concluded that CV-loaded solid dispersion prepared using this method would be of use for delivering poorly water-soluble CV with enhanced solubility and dissolution, but without crystalline changes. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/23328872/A_novel_surface_attached_carvedilol_solid_dispersion_with_enhanced_solubility_and_dissolution_ L2 - https://dx.doi.org/10.1007/s12272-013-0008-7 DB - PRIME DP - Unbound Medicine ER -