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The following message was posted to: PharmPK
Does anyone know the absorption and the absolute availabilty of
metformin in rats and mice?
Another question, after a mass balance, only the 85% of the iv injected
drug is recovered (no CO2 expected) Do I have to think that the drug is
not completely eliminated?
Thank in advance
Dr Roberto Conti
Sigma-Tau
Dep. of Endocrinology and Metabolism
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The following message was posted to: PharmPK
Dear Roberto,
several years ago we published a couple of papers on PK & PD of
metformin in rats (see below). The absolute oral bioavailability of
metformin in these studies was similar to that in humans (~40-50%).
Regarding the mass balance: I would advise to check the isotonicity
of the IV metformin solution, and ensure that the dose is infused
gradually (over at least 2-3 min). The unique chemical properties of
metformin together with high dose (we used 200 mg/kg) may potentially
lead to undesired effects at the site of IV administration and
interfere with drug distribution and elimination.
Best regards,
David.
David Stepensky
HHMI Postdoc Associate
Section of Immunobiology
Yale University School of Medicine
1. Stepensky et al., Pharmacokinetic-pharmacodynamic analysis of the
glucose-lowering effect of metformin in diabetic rats reveals first
pass pharmacodynamic effect. Drug Metab Dispos, 2002, 30(8) 861-8.
2. Stepensky et al., Preclinical evaluation of pharmacokinetic-
pharmacodynamic rationale for oral CR metformin formulation. J
Control Release. 2001, 71(1): 107-15.
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Please consider these links:
1. http://www.tidsskriftet.no/pls/lts/pa_lt.visSeksjon?
vp_SEKS_ID=1476235
2. http://db.doyma.es/cgi-bin/wdbcgi.exe/doyma/mrevista.pubmed_full?
rev=64&vol=30&num=8&pag=409
3. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?
db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=16265833&itool=iconab
str&query_hl=2&itool=pubmed_DocSum
4. http://care.diabetesjournals.org/cgi/content/full/28/10/2585
5. J Pharmacol Exp Ther. 1993 Sep;266(3):1454-62.
6. http://www.sciencedirect.com/science?
_ob=ArticleURL&_udi=B6WN4-4D6XMV6-3&_user=10&_coverDate=05%2F31%
2F1995&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_acct=C000050221&_versi
on=1&_urlVersion=0&_userid=10&md5=6420cad7ddcc0d323e1f886f8c0f6cf1
good luck
[Careful with the longer links - db]
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