Browse > Article
http://dx.doi.org/10.4333/KPS.2003.33.1.061

Improved Dissolution Characteristics of Silymarin and Their Bioavailability in Rats  

Kim, Jeong-Hoon (Research Laboratories, Dong-A Pharmaceutical Co., Ltd.)
Jang, Sun-Woo (Research Laboratories, Dong-A Pharmaceutical Co., Ltd.)
Kweon, Jong-Weon (Research Laboratories, Dong-A Pharmaceutical Co., Ltd.)
Kim, Won-Bae (Research Laboratories, Dong-A Pharmaceutical Co., Ltd.)
Choi, Yong-Wook (College of Pharmacy, Chung-Ang University)
Publication Information
Journal of Pharmaceutical Investigation / v.33, no.1, 2003 , pp. 61-65 More about this Journal
Abstract
Silybin is the main component of Cardus marianus extracts originated from Silybum marianum and has a hepato-protective effect. It is a water-insoluble compound and poorly absorbed from the gastrointestinal tract, resulting in very low oral bioavailability(BA). Polymeric mixed-micelle precursor formulation was made to enhance the dissolution rate of silybin, showing the results of pH-independent release profile with increased dissolution. Oral BA of different preparations in rats was evaluated, revealing that the new formulation showed increased BA more than 2-fold and 4-fold compared to the marketed product and Cardus marianus extracts itself, respectively.
Keywords
Silymarin; Silybin; Micelle; Dissolution rate; Bioavailability;
Citations & Related Records
연도 인용수 순위
  • Reference
1 K. Parfitt, Martindale, The complete drug reference, 32nd Ed., Pharmaceutical Press, London, PP. 993-994 (1999)
2 G. Gatti and E. Pemcca, Plasma concentrations of free and conjugated silybin after oral intake of a Silybin phosphatidy-lcholine complex (silipide) in healthy volunteers, Int. J. Ctin.Pharmacol. Ther., 32, 614-617 (1994)
3 E. M. Martinelli, P. Morazzoni, S. Liviio and E. Uberti, Liquid chromatographic assay of silybin in human plasm aand urine, J. Liq. Chromatogr., 14, 1285-1296 (1991)   DOI   ScienceOn
4 R. Weyhennmeyer, H. Mascher and J. Birkmayer, Study on dose linearity of the pharmacokinetics of silibinin diastereomers using a new stereospecific assay, Int. J. Clin.Pharmaco., Ther. Tox., 30, 134-138 (1992)
5 B. Rickling, B. Hans, R. Kramarczyk, G. Krumbiegel and R. Weyhenmeyer, Two high performance liquid chromato-graphic assays for the determination of free and total silibinin diasteromers in plasma using column switching with electrochemical detection and reversed phase chromato-graphy with ultraviolet detection, J. Chromatogr. B, 670,267-277 (1995)   DOI   ScienceOn
6 H. Salmi, and S. Sama, Effect of silymarin on chemical, functional and morphological altemtions of the liver. A double-blind controlled study, Scand. J. Gastroenterol., 17, 517-521 (1982)   DOI   ScienceOn
7 P. Ferenci, B. Dragosics, H. Dittrich, H. Frank, L. Benda, H.Lochs, S. Meryn, W. Base and B. Schneider, Randomized controlled trial of silymarin treatment in patients with cirrhosis of the liver, J. Hepatol, 9, 105-113 (1989)   DOI   ScienceOn
8 K. Hruby, G. Csornos, M. Fuhrmann and H. Thaler, Chemotheraphy of amantia phalloid poisoning with intravenous silibinin, Human Toxicol, 2, 183-195 (1983)   DOI
9 P. Morazzoni, M. J. Magistretti, C. Giachetti, and G. Zanolo, Comparative bioavailability of silipide, a new flavanolignan complex in rats, Eur. J. Drug Metab. Pharmacokinet., 17,39-44 (1992)   DOI
10 D. Lorenz, P. W. Lucker, W. H. Mennicke and N. Wetzelsberger, Pharmacokinetic studies with silymarin in human serum and bile, Meth. and Find. Exptl. Clin. Pharmacol., 6, 655-661 (1984)
11 P. Morazzoni, A. Montalbett, S. Malandrino and G. Piffer, Comparative pharmacokinetics of silipide and silymarin in rat, Eur. J Drug Metab. Ph., 18, 289-97 (1993)   DOI   ScienceOn
12 D. Savio, P. Harrasser and G. Basso, Softgel capsule technology as an enhancer device for the absorption of natural principles in humans. A bioavailability cross-over randomized study on silybin, Arzneimiuel-Forsch., 48, 1104-1106 (1998)