Linked Life Data

16497407

Source:http://linkedlifedata.com/resource/pubmed/id/16497407

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2006-3-28
pubmed:abstractText
Deoxycholic acid (DOCA) is a bile acid that facilitates the gastrointestinal (GI) absorption of low molecular weight heparin (LMWH) by bonding chemically to it. The calculated coupling ratio and bioactivity of LMWH-DOCA was 3.6 and 126.8 IU/mg, respectively. This study examined the efficacy of orally administered LMWH-DOCA in rat, mouse and monkey models. When 100 mg/kg (12,680 IU/kg) of LMWH-DOCA was administered to rats or mice, its maximum anti-factor Xa activity was 0.76+/-0.15 and 0.15+/-0.03 IU/ml, respectively. On the other hand, when a single dose of 100 mg/kg LMWH-DOCA mixed with either a bile solution or 200 mg/kg free DOCA was administered to mice, the anti-factor Xa activity of LMWH-DOCA was 0.42-0.45 IU/ml. Fluorescence studies confirmed that the free bile acid induced the morphological change in LMWH-DOCA in the buffer solution. In the monkey experiments, the bioavailability of LMWH-DOCA after administering 200 mg/kg free DOCA orally was 6.8%, which was 8 times higher than that of LMWH (0.8%) and 4 times higher than that of LMWH-DOCA in the absence of free DOCA (1.7%). The absorption of orally administered LMWH-DOCA occurred in all parts of the small intestine, particularly in the ileum without causing any damage such as fusion of the microvilli and dissolution or disorientation of the cell layers. The optimum oral formulation for LMWH-DOCA delivery in each animal model was determined according to the different absorption behavior of LMWH-DOCA.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0168-3659
pubmed:author
pubmed:issnType
Print
pubmed:day
10
pubmed:volume
111
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
290-8
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Efficacy of orally active chemical conjugate of low molecular weight heparin and deoxycholic acid in rats, mice and monkeys.
pubmed:affiliation
Department of Chemical and Biological Engineering, Chungju National University, Chungbuk 380-702, Korea.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't