Document Detail


Solid state mechanochemical simultaneous activation of the constituents of the Silybum marianum phytocomplex with crosslinked polymers.
MedLine Citation:
PMID:  18428992     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Simultaneous improvement of solubilization kinetics of main flavolignans of Silybum marianum extract was obtained cogrinding with two crosslinked polymers: micronized crospovidone, PVP-CL(R) and sodium carboxymethylcellulose, Ac-Di-Sol(R) in the 1:3 active-to-polymer weight ratio. By this process it was assessed that the main extract components lost its crystalline structure, and the powder surface area was increased by 2.1- and 1.7-fold in the coground products with Ac-Di-Sol(R) and PVP-CL(R), respectively. This activated status of the dry extract remained stable over a period of 2 years. Solubilization kinetics resulted ameliorated both in terms of entire dry extract and in terms of single components. When the 1/3 coground systems with PVP-CL(R) and Ac-Di-Sol(R) were dissolved in saturated conditions they gave a concentration improvement compared to the native product of 8 and 31 times of silybin A, 7 and 27 times of silybin B, whereas in the case of silychristin a double concentration was obtained only using Ac-Di-Sol(R). The in vivo studies on rats confirmed that this solubilization improvement corresponded to an effective oral bioavailability enhancement. The highest bioavailability improvement was obtained with Ac-Di-Sol(R), with a relative bioavailability of 88.6, 17.96, and 16.4 compared to the extract for silybin A, silybine B, and silychristine, respectively.
Authors:
D Voinovich; B Perissutti; L Magarotto; D Ceschia; P Guiotto; A R Bilia
Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  98     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2008-12-02     Completed Date:  2009-07-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  215-28     Citation Subset:  IM    
Copyright Information:
(c) 2008 Wiley-Liss, Inc. and the American Pharmacists Association
Affiliation:
Department of Pharmaceutical Sciences, University of Trieste, P. le Europa 1, I-34127 Trieste, Italy. vojnovic@units.it
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MeSH Terms
Descriptor/Qualifier:
Animals
Biomechanics / physiology
Cross-Linking Reagents / chemistry*,  pharmacokinetics*
Male
Milk Thistle / chemistry*
Plant Extracts / chemistry,  pharmacokinetics
Polymers / chemistry*,  pharmacokinetics*
Rats
Rats, Sprague-Dawley
Chemical
Reg. No./Substance:
0/Cross-Linking Reagents; 0/Plant Extracts; 0/Polymers

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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