In vivo absorption comparison of nanotechnology-based silybin tablets with its water-soluble derivative. (April 2015)

• Record Type: Journal Article
• Authors: Xu, Di; Ni, Rui; Sun, Wei; Li, Luk Chiu; Mao, Shirui
• Is Part Of: Drug development and industrial pharmacy. Volume 41:Number 4(2015:Apr.)
• Page Start: 552
• Page End: 559
• Publication Date: 2015-04
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.3109/03639045.2014.884123
• Languages: English
• ISSNs: 0363-9045

Abstract

<abstract> <title>Abstract</title> <p>In this study, the <italic>in vivo</italic> oral absorption of a nanocrystal tablet formulation of a BCS II poorly water-soluble drug was compared with that of its water-soluble salt form. Silybin is used as the model drug, and its nanosuspension was prepared by high-pressure homogenization. Effect of process and formulation parameters on properties of the nansuspensions was investigated. Dried powder of the nanosuspension was prepared by spray drying and used for preparing tablets. A pharmacokinetic study was performed in Beagle dogs to compare the absorption for tablets of silybin nanocrystals and silybin meglumine. <italic>In vivo</italic> absorption of nanocrystal silybin tablet in Beagle dogs was determined. X-ray powder diffraction results indicated that silybin existed in a crystalline state after homogenization. <italic>In vivo</italic> absorption study in rats showed that the peroral absorption of silybin was enhanced remarkably by decreasing particle size. <italic>In vivo</italic> absorption of nanocrystal silybin tablet in Beagle dogs was comparable with that of the commercially available tablet of the water-soluble salt form of silybin. In conclusion, it is possible to increase the bioavailability of poorly soluble drugs by preparing its water-soluble derivative.</p> </abstract>