Hi,Back to the Top
I have a question concerning the formulation for oral gavage of a
poorly water soluble compound. I am able to get the compound into
solution for IV using 40:50:10 Propylene glycol:water:ethanol at pH 3,
but this is at 5 mM concentration. With the more concentrated oral
formulation (50mM), I have tried various solvents ie. 50%glyerin,
1%gamma-cyclodextrin, 10-15% hydroxypropyl-beta-cyclodextrin and 0.5%
CMC for a suspension. Even at the low pH, this compound will not
dissolve in these various solvents and 0.5% CMC did not give a good
suspension, very chunky solid. I have some things that I can still try
ie. PVP, sodium lauryl sulfate, but I am quickly running out of ideas.
This is for early animal studies meant to be a screening tool, so I was
hoping to keep it relatively simple, but at this point I am willingly
to try anything. Hope you guys can help me.
200-20353 64th Ave.
Hello Kerri-Ann,Back to the Top
what is the purpose of your study ? Do you have to make the proof of
concept that your drug is efficient in animals or do you want to have
preliminary PK data ?
The objective has to be well understood if you want to set up a
For the proof of concept the aim of your formulation is to allow the
max amount of drug being absorbed. You can then use what I call "exotic
vehicles" such as PVP, HPbCD and so on.
If you want to early screen for PK properties you have to choose a
"cleaner" formulation. In this way I would recommend the use of a
suspension in some metylcellulose or CMC up to 1% in water. I would
recommend to stir and even to perform some sonication to homogenize the
Hope this helps,
Pfizer Global R&D
Hello Dang,Back to the Top
Did you tried wetting your drug before attempting to prepare
may like to try this.Wet the weighed powdered drug in a mortar with few
of Tween-80, triturate this till you obtain a uniform paste, then
geometrically dilute this paste with 0.5 % w/v sodium CMS in water, with
constant trituration to make up the volume. Though simple it works most
times to obtain a uniform suspension for preclinical studies.
Vijay V Upreti
Graduate Student, Dept. of Pharmaceutical Sciences
University of Maryland
HSF-II, 20 Penn Street
I have read about a formulation of emulphor/ethanol/saline (1:1:18).Back to the Top
work with very insoluble compounds and to deliver them IP, they are
10% DMSO/20% Tween-80/70% saline.
-Jodi Wood, Ph.D.
School of Pharmacy
University of Connecticut
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