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I am working to prepare two lipophilic compounds for oral gavage in
mice. The compounds are water insoluble, so I would like to generate
an emulsion with TPGS. Can anyone provide a useful protocol for
preparing an emulsion of TPGS with lipophilic drugs? I am curious
when adding the compounds to melted TPGS if the temperature must be
above the melting point for the drug or if it is sufficient to stay
above the melting point for TPGS?
Thanks in advance for any information.
Steve
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Dear Steve,
Take TPGS in a solvent like PEG 400 or Ethanol (1:1) and melt.
Maintain the temperature of the whole system at 37-40oC and dissolve
your drug in it. Then add water maintained at 37-40oc and stirr
continously to obtain solution.
Hope this will help you.
Manthena Varma
Dr. Manthena VS Varma
NDDS-Pharmaceutical R&D,
Nicholas Piramal Research Center,
1, Nirlon Complex, Off Western Express Highway,
Near NSE Complex, Goregaon (E),
Mumbai-400 063, INDIA.
email: varma_mvs.at.yahoo.com or vmanthena.-at-.nicholaspiramal.co.in
Phone: +91 22 3081 8914; +91 932 426 9193
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The following message was posted to: PharmPK
Dear Stephen,
regarding the use of TGPS with a lipophilic drug in an emulsion you
should consider the following :
- 1st way of formulating : you blend the active drug and TGPS heating
up to the higher melting temperature (probably the drug's one). This
method can be used if the drug's melting point is not too high (TGPS
is degraded over 190*C).
-2nd way : you solubilize the drug and TGPS in a relevant organic
solvent and you evaporate the solvent to get your drug "entrapped" in
TGPS. This method can be used if you find a suitable organic solvent.
Hope this helps,
Frederic
Frederic Doc
ACRITER - Drug discovery consulting
www.acriter-consulting.com
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