Oral availability of drugs...

Dr. YL Du yd128 at albnyvms.bitnet
Tue Jan 10 12:21:39 EST 1995


In article <3eu38n$c3g at mserv1.dl.ac.uk>, mbasd at s-crim1.dl.ac.uk (A.
Sheppard) wrote:


> 1  Is it possible to predict whether a compound will be orally active?
You may look at the structure of the drug.  The drugs with lipophilic
structure will tend to be absorbed from  G.I.   Also you have to consider
the metabolism of the drugs.  Some drugs are metabolized quickly  in liver
and this makes the drug preactically inactive enev they are absorbed in
G.I.
> 2  On observing a compound has little or no oral activity, are there any
>    structural modifications which can be used to increase the oral activity
>    of the compound?
By  making it lipophilic.
> 3  Is it possible to use an adjuvant to increase the absorption of a
>    weakly orally active compound?
Probably not. 
> 4  Are there any in vitro test systems which will predict whether a
>    compound is orally active? If there are such test systems, are they
>    available commercially or have they been devloped in-house?
It should be done by testing the distribution ratio of the drug between
water and oil.
> I will summarise useful information to the net.
> 
> Andy Sheppard
> Ferring Research Institute
> mbasd at seqnet.dl.ac.uk
> 
> [crossposted to newsgroups bionet.general, bionet.molbio.methds-reagnts,
>  bionet.molec-model and the Computational Chemistry list]



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