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The following message was posted to: PharmPK
Dear all,
I had a one compound; we have done the pharmacokinetic study in rats at oral & intravenous route of administration. An intravenous route, plasma concentrations was found more than 1000 ng/mL, whereas oral route, cmax in plasma was 15 ng/mL concentrations. What are the possible reasons to get such low concentrations in oral administration?
Thanking you and Regards
NageswaraRao Muddana
[Solubility, permeability? - db]
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There are many possible reasons, the most common ones are high metabolism due to first pass effect or low intestinal absorption. For the former the intrinsic clearance and the Met ID data could provide some answers. For the later reason, I'd check the Caco permeability for the other compounds with the same scaffold before you invest time and resources in another PK study.
I hope this helps,
MS
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The following message was posted to: PharmPK
Hi,
In addition to first pass metabolism and poor permeability, do you think shold we also consider the poor solubility and dissolution rate?
XD
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Dear Muddana,
That may be due to poor drug absorption or metabolism (first pass effect).
Dr Zafar.
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