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Hi there,
Recently in an efficacy study we needed to dose several compounds to mice via IV injection. The compounds precipitated instantly from the solution upon the injection of original clear stock solution in pure DMSO. Is anybody can give some quick suggestion to that?
Thanks,
Patrick Yu
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Dear YU,
Have you tried to inject these solutions slowly after suitable dilution in sterile water?
Best regards
ALHANOUT Kamel
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The following message was posted to: PharmPK
It is a problem of formulation... you may need to add some surfactants
to your formulation to avoid precipitation upon injection
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The following message was posted to: PharmPK
You ought to look at Walt's programs or ACD to predict solubility
causing the least insult. I can only imagine you must have raised
blood pressure a bit and probably insulted a few organs as well. Try
in vitro to make sure you do not start dissolving Red cell in the
process.
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Dear Patrick,
The phenomenon means that your compounds have low solubility in the aqueous injection solutions.
You need to consider about the factors (such as pH values, et al) affecting the solubility of your compounds.
Add some solubilizers (such as PEG400) or adjust the pH values of the solutions to make your compounds solubilized, and take care of the osmotic pressure of the solution. When it comes to the in vivo study, a parallel group of the solution without drug is needed as a control group.
We used PEG400 as the solubilizer in an oral aqueous solution for rats before. It showed that PEG400 was inert. And the solubilization is satisfactory.
Best regards.
Xipei Wang, Ph.D student
Department of Pharmaceutics, School of Pharmacy
Peking University, Beijing
China
E-mail:wangxipei.at.gmail.com
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