title: Physicochemical characterization of tacrolimus-loaded solid dispersion with sodium carboxylmethyl cellulose and sodium lauryl sulfate.
abstract: To develop a novel tacrolimus-loaded solid dispersion with improved solubility, various solid dispersions were prepared with various ratios of water, sodium lauryl sulfate, citric acid and carboxylmethylcellulose-Na using spray drying technique. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy, differential scanning calorimetery and powder X-ray diffraction. Furthermore, their solubility and dissolution were evaluated compared to drug powder. The solid dispersion at the tacrolimus/CMC-Na/sodium lauryl sulfate/citric acid ratio of 3/24/3/0.2 significantly improved the drug solubility and dissolution compared to powder. The scanning electron microscopy result suggested that carriers might be attached to the surface of drug in this solid dispersion. Unlike traditional solid dispersion systems, the crystal form of drug in this solid dispersion could not be converted to amorphous form, which was confirmed by the analysis of DSC and powder X-ray diffraction. Thus, the solid dispersion system with water, sodium lauryl sulfate, citric acid and CMC-Na should be a potential candidate for delivering a poorly water-soluble tacrolimus with enhanced solubility and no convertible crystalline.
authors: Research Center, Samil Pharmaceutical Co. Ltd., Ansan 712-749, Korea.
authors: Young-Joon
authors: YJ
authors: Park
authors: Dong-Sung
authors: DS
authors: Ryu
authors: Dong Xun
authors: DX
authors: Li
authors: Qi Zhe
authors: QZ
authors: Quan
authors: Dong Hoon
authors: DH
authors: Oh
authors: Jong Oh
authors: JO
authors: Kim
authors: Youn Gee
authors: YG
authors: Seo
authors: Young-Im
authors: YI
authors: Lee
authors: Chul Soon
authors: CS
authors: Yong
authors: Jong Soo
authors: JS
authors: Woo
authors: Han-Gon
authors: HG
authors: Choi
mesh_terms: D002266:Carboxymethylcellulose Sodium; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate; D012995:Solubility; D016559:Tacrolimus / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D012967:Sodium Dodecyl Sulfate; D002266:Carboxymethylcellulose Sodium; D016559:Tacrolimus