A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution

Lee, Sung Neung, Poudel, Bijay Kumar, Tran, Tuan Hiep, Marasini, Nirmal, Pradhan, Roshan, Lee, Young Im, Lee, Dong Won, Woo, Jong Soo, Choi, Han-Gon, Yong, Chul Soon and Kim, Jong Oh (2013) A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution. Archives of Pharmacal Research, 36 1: 79-85. doi:10.1007/s12272-013-0008-7


Author Lee, Sung Neung
Poudel, Bijay Kumar
Tran, Tuan Hiep
Marasini, Nirmal
Pradhan, Roshan
Lee, Young Im
Lee, Dong Won
Woo, Jong Soo
Choi, Han-Gon
Yong, Chul Soon
Kim, Jong Oh
Title A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution
Journal name Archives of Pharmacal Research   Check publisher's open access policy
ISSN 0253-6269
Publication date 2013
Sub-type Article (original research)
DOI 10.1007/s12272-013-0008-7
Open Access Status Not Open Access
Volume 36
Issue 1
Start page 79
End page 85
Total pages 7
Place of publication Seoul, Republic of Korea
Publisher Pharmaceutical Society of Korea
Language eng
Subject 3002 Drug Discovery
1313 Molecular Medicine
1605 Policy and Administration
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.
Keyword Solid dispersion
Carvedilol
Carrier
Solubility
Bioavailability
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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Created: Sat, 04 Jun 2016, 12:17:31 EST by Nirmal Marasini on behalf of School of Chemistry & Molecular Biosciences