title: A novel surface-attached carvedilol solid dispersion with enhanced solubility and dissolution.
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: College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
authors: Sung Neung
authors: SN
authors: Lee
authors: Bijay Kumar
authors: BK
authors: Poudel
authors: Tuan Hiep
authors: TH
authors: Tran
authors: Nirmal
authors: N
authors: Marasini
authors: Roshan
authors: R
authors: Pradhan
authors: Young Im
authors: YI
authors: Lee
authors: Dong Won
authors: DW
authors: Lee
authors: Jong Soo
authors: JS
authors: Woo
authors: Han-Gon
authors: HG
authors: Choi
authors: Chul Soon
authors: CS
authors: Yong
authors: Jong Oh
authors: JO
authors: Kim
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000737:chemistry* / Q000494:pharmacology; D002152:Calorimetry, Differential Scanning; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology; D000077261:Carvedilol; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003460:Crystallization; D057927:Hydrophobic and Hydrophilic Interactions; D008855:Microscopy, Electron, Scanning; D011205:Povidone / Q000737:chemistry; D011412:Propanolamines / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013499:Surface Properties; D014961:X-Ray Diffraction
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D002227:Carbazoles; D011412:Propanolamines; D012997:Solvents; D000077261:Carvedilol; D011205:Povidone