I am planning to do injections in mice with Metripranolol. Found that the drug is practically insoluble in water/saline. What do people using this drug use as a solvent when they do injections? Thanks in advance for your answers.
What concentration are you planing to use it at? Its soluble in water at 589mg/L and one articles I found states in their abstract that they used saline as a vehicle control. Are you planning to use super high doses? In vivo studies in rabbits used only 0.03, 0.15 and 0.3 mg/kg. At this published dose level, water/saline should be good enough since max solubility would be 0.589mg/ml and most mice only weigh ~20-25g at 7 weeks old and likely won't go much past 30g when mature.
sources:
http://www.drugbank.ca/drugs/DB01214
http://www.ncbi.nlm.nih.gov/pubmed/2576986
Also if you look up the composition of ophthalmic solutions like OptiPranolol they list purified water as one of the ingredients, with the remaining chemicals serving as pH buffers and preservatives.
Good Luck.
I need to inject 40 mg/kg body weight. I need to inject young mice approx. 8 g. Therefore about .32 mg per mouse. Thanks for your answer.
In addition it will be a subcutaneous injection therefore the high conc.
I think you can use the opthalmic solution. It is supplied @ 300micrograms per 100 microliters.
Solubility of the metipranolol can be enhanced by addition of surfactants (SLS) in little amount. Another approach is using Hydro-alcoholic solution. In latter, we have to see the final volume. Dose is also important parameter for the same.
Usually, we add surfactants/cyclodextrin for solubility enahancement in animal studies (PK/PD).
Dear Dr. Kanan:
During my tests on rats using poorly water soluble drugs, I found very useful to dissolved compounds in DMSO 8%, but also using physical combinations methods such as ultrasonic disruption. To use DMSO will avoid possible side reactions to certain solvents in the animal tests. Best regards.