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Dear friends,
My work currently involved animal studies.
I am suppose to deliver a very lipophilic diterpenoids into 8 weeks mice. The compound does not dissolve well in 10%DMSO/90%Saline.
Just wondering if there is any recommended vehicle to be used? I prefer to deliver via intra peritoneal route.
Thank you very much for you time !
Regards,
Jonathan
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Title: Vehicle Selection
Good day to you
I am facing some problem in selecting the right vehicle for a lipophilic diterpenoids into 8 week mice.
I have tried dissolving the above compound in 10%DMSO90%Saline which ultimately formed sediments.
At the moment I have two vehicles in my mind, PEG400 and Cremophor EL. I have yet to try both of them as I need to carefully select the right one due to time and money constraint.
Hence, I hope I can seek some advices from you on the better vehicle selection and the right doses.
I prefer to formulate for intraperitoneal injection.
Thank you for your precious time
Jonathan
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The following message was posted to: PharmPK
Hi Jonathan,
You can try following vehicles:
1. 40 %w/v hydroxyl beta cyclodextrin (H\0x03B2CD) in water
2. 8% N-methyl Pyrrolidone (NMP), 45% PEG-400 in water
3. 10% w/v N-methyl pyrrolidone (NMP), 40% v/v Propylene glycol in water
You can also try
4. 10% w/v Solutol HS-15, 10% v/v Ethanol and 10 mM Na2CO3 in water
I hope, if you can try the above combinations (may be required some changes in ration) you will definitely succeed.
Thanks,
Sudipta Basu
Senior Research Scientist-DMPK
Sai Advantium Pharma Ltd, Pune, India
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Hi,
The solution prepared for parental administration should be always be clear,
You may have to select a perfect cocktail mixture.
The mixture may contain organic solvents, solubilizers , co-solvents with normal saline.
The mixture of 2 to 10 % methanol + 0.5 to 2 % of NN Dimethyl acetamide or Dimethyl formamide + 30 to 40 % PEG 200 with remaining concentration made up to with Normal saline.
May be this cocktail will serve your purpose
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HI Jonathan,
try to dissolve your compound in a 1:1 mix of NMP (N-Methyl-2-Pyrrolidone) and Solutol HS 15. Sonicate if needed and then dilute 5X with Saline. Solutol is very similar to Cremaphor in its properties but is a lot less toxic.
Let me know if this works for you.
regards
Neal
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