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Hi All,
My group is working on a new broad spectrum antifungal compound which is
highly insoluble in water(below 100 ng/mL, the quantitation limit of our
present HPLC method), specially at physiological pH. How can we determine
the metabolic stability, plasma protein binding, and permeability across
CACO-2 cell line for its development? Any suggestion or reference will
help. Does any one knows a reference on such studies with insoluble oral
antifungals.
Thanks
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The following message was posted to: PharmPK
Have you tried any type of organic solvent (DMSO, EtOH)? As long as you are
below the 1% you should be safe (in most cases) while conducting the in
vitro experiments.
Sibel Ucpinar
In Vitro Drug Metabolism Division
CEDRA Corporation
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[Two replies - db]
From: Donna.S.Cox.at.dupontpharma.com
Date: Thu, 11 Oct 2001 08:59:57 -0400
MIME-Version: 1.0
Sibel-
During my graduate days we did many experiments utilizing in vitro models
(Caco-2 and BBMEC) to assess the permeability of a variety of compounds.
The "golden rule" that we followed was to stay around or below 2% DMSO (no
greater than 5% or it may begin to effect your monolayer integrity). Hope
this helps.
Donna
Donna S. Cox, Ph.D.
Research Scientist
Drug Metabolism & Pharmacokinetics Dept
Clinical Pharmacokinetics Group
Stine-Haskell Research Group
Bldg. S112/36
Phone: (302) 366-5055
Fax : (302) 451-0054
---
From: "Melethil, Srikumaran K."
Date: Thu, 11 Oct 2001 10:15:16 -0500
To: david.-at-.boomer.org
Subject: RE: PharmPK in vitro ADME of highly insoluble drugs
The following message was posted to: PharmPK
Can you tell me about the HPLC detection (eg. UV, fluorescence) you are
using?
Using a more sensitive detector is one way.
Srikumaran K. Melethil, Ph.D., JD (2001)
Professor, Pharmaceutics and Medicine
University of Missouri- Kansas City
203B Katz Hall (School of Pharmacy)
Kansas City, MO 64110
Phone: voice- 816-235-1794; fax - 816-235-5190
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