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How to correlate experimental permeability to specific intestinal permeability properly and where to find transporter data in rats? #447
Thanks for your help, it's really helpful. I think the parameters "Effective surface area enhancement factor" is what I mentioned as "absorption surface area ratio". However, I am still not very sure if the calculation method I posted is right in terms of correlating our modified permeation to experimental effective permeability since no calculation method is introduced in the paper you cited.
And I also very want to know if there is a database giving the transporters expression of rats because we have added some P-gp inhibitor to our new formulation so that permeation would change. Is there any data source suggested? And how to calculate the kinetics for transporters to make the effective permeability consistent with literature?
Thanks for your help .
Dear Wang Wei,
I am not sure if the calculation method you posted can be applied. In PK-sim the specific intestinal permeability (P_int_Invitro) i.e. the surface area-normalized transcellular permeability of the innermost layer of the intestinal wall, is calculated from the drugs´ lipophilicity and effective molecular weight. In the Simulation the Intestinal permeability (transcellular) is used. The transformation is done via this formula:
Regarding the rat database: sorry there is no for PK-sim. You might use the human one and adjust expression levels, if you have literature for this or fit it to your data.
Hope this might help you.