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I need to solubilise a water-insoluble compound to have an IV
formulation to be used in animal studies, mainly rats and dogs.
We obtained good solubility results with a mixture of DMA and PEG 200
I know that this vehicle, when tested in anesthetized dogs, did not
produce any adverse effects on CV parameters like MAP, HR, PR...
Could anyone tell me similar data on other animal species?
Principal scientist DMPK department
NicOx Research Institute
Via L. Ariosto, 21
20091 Bresso, Milan, Italy
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The following message was posted to: PharmPK
once again I am concerned about the use of such "exotic" formulations
for PK studies. Do you really think you can ensure the relevance of
your data when dosing such vehicles ?
"Exotic" formulations should be only used for "proof of concept" in
animal models. But in PK studies where you calcultate parameters such
as Cl, Vd, Tmax, Cmax, half-life, ... from your data you should use
more relevant formulations as your data you will thereafter be used
extrapolation to humans for instance (by allometric scaling?). My
recommendation is that as you should try and find a nice formulation
(the one that you would not be afraid to dose to humans). If you
cannot set up one you have to
carefully analyse the future of your drug and to evaluate the risk of
failure due to solubility issues causing non-reproducibility of PK
Do you only dose IV or do you use IV as a reference to an oral route
As a consultant I can offer my expertise in developing a preclinical
formulation strategy based on the different types of studies (PK,
pharmacology, toxicology, preclinical proof of concept).
hope this helps,
PharmD, MS in formulation and biopharmaceutics
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