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Greetings
We have an oily substance, very poorly water-soluble (about 0.1 mg
per mL), which we need to give iv in order to assess its oral
bioavailability. We want to give a dose in the range 20-50 mg to an
animal.
Does anyone have experience of dispersing lipophilics in Intralipid?
(Intralipid is a commercial product, comprising a sterile fat
emulsion of soybean oil, egg phospholipids and glycerol in water. It
comes in two strengths, 10% and 20%.)
Naturally, other suggestions would be welcome.
With thanks,
Stuart McLean
School of Pharmacy
University of Tasmania
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I have no experience with that product but I have used cyclodextrins with
some success
Dave
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Dear friend
We have an interesting method to increase the solubility for IV
studies. Take blood from the same animal you are going to use for i.v
kinetics and isolate plasma from that. Use the plasma to solubilise
the drug with constant shaking in a closed tube. Inject this back to
the same animal after passing it through online 0.22=B5 filter. Plasma
protein binding sites probably increases the solubility of the water
insoluble drug. By this way we have solubilized a water insoluble
compound for its i.v. kinetics in rats (J Chromatography B 738
(2000) 431-436) . This method can also be successfully employed in
higher animals too. I hope it works in your case also.
We don't have any specific experience with the Intralipid. From the
composition of Intralipid, it is somewhat like liposomes. Liposomes
could be an another suitable approach to solubilise, however it can
change the disposition of the drug. High concentration reaches in
liver and circulating macrophages.
Velpandian.T
Sr.Demonstrator
Pharmacokinetic laboratory
Department of Pharmcology
All India Institute of Medical Sciences
New Delhi, India
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Dear Stuart,
I used ethanol:propylene glycol:water (10:70:20
v/v/v)for a compound with water solubility 45 mg/l.
Your compound has more than double the solubility of
the compound I tested so it may be possible to reduce
the percentage of propylene glycol and increase water
content.
Sunil Bajad
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Hello,
JB Musser et al. Anesth Analg 1999;88:671-5 used intralipid to dissolve
halothane for IV injection and proved that anesthesia via the IV route is
similar to inhalation. No serious side effects were reported.
However, they did not measure halothane in intralipid.
We use a similar approach with some success using intralipid 20% and
halothane 10 vol%.
Sincerely,
Martin Anetseder
Dept of Anesthesiology
Univ Wuerzburg
Germany
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