Sublingual midazolam using oral tablets?

[blase deviant]

Sublingual is supposed to be far more bioavailable, but I'm concerned that with the high ratio of fillers/binders to drug, a regular oral tab isn't the same as far as sublingual is concerned.

I was reading pubmed, where all the reports said sublingual was far more effective, and none of them but one mentioned a specially formulated tablet with a regulated pH (and I assume other measures to make it suitable for sublingual), but I was wondering if the other reports used either a pure midazolam solution (intended for IV/whatever), or a tablet specially formulated for it...

 

[BilZ0r]

It's likely they used pure power formulated in some way. In one paper I found, where they gave the drugs to children:

Injectable midazolam was mixed with a thick grape syrup and placed under the tongue

.

I would have thought extractict midazolam from pills would have been pretty easy. Just crush and extract into a non-polar solvent.

 

[blase deviant]

So you're saying that instead of dissolving in water, running through a filter, and evaporating the water; I should use a non-polar solvent, run it through a coffee filter, and anything that gets left in the filter after it dries is midazolam?

(Yeah, from this post you can obviously tell I got locked out of my damn chem course)

 

[BilZ0r]

Actually, midazolam maleate is water soluble... I just found this one:

J Pharm Biomed Anal. 1991;9(6):451-5. Related Articles, Links

Solubility and acid-base behaviour of midazolam in media of different pH, studied by ultraviolet spectrophotometry with multicomponent software.

Andersin R.

Department of Pharmacy, University of Helsinki, Finland.

The solubility of midazolam is less than 0.1 mg ml-1 at neutral pH and it increases considerably in acidic media. A pKa value of 6.04 at 24 +/- 1 degree C was calculated from the solubility data. In acidic media midazolam is reversibly converted to the corresponding benzophenone (open-ring form). The extent of this reaction was investigated by assaying the two compounds simultaneously by UV spectrophotometry with multicomponent software. The structure of the benzophenone derivative was verified by IR, MS and 1H and 13C NMR spectrometry.

You should do a test, most binders and fillers are water soluble, but in these pills they might not be... you're midazolam will disolve in acidic water, or non-polar solvents.... use whatever the rest of the pill doesn't disolve in.