Extraction of loperamide from immodium ad

[fluxist]

Can anyone offer a suitable extraction method for obtaining (water insoluble) loperamide hcl from Immodium ad? Bulk loperamide is terribly expensive.

The inactive incredients are the following: Dibasic Calcium Phosphate, Magnesium Stearate, Microcrystalline Cellulose, Colloidal Silicon Dioxide, FD&C Blue #1, D&C Yellow #10.

Alternately, if someone could explain that these chemicals would not be harmful if (hypothetically) actively transported across the blood-brain barrier, this would also suffice.

[Rhodium]

None of the other chemicals would be healthy to have transported across the BBB, but fortunately that won't happen.

[taig]

If you're not able to extract the loperamide - which due to the small amounts per pill will have a rather low yield if not working very carefully - you could try to find a way to help the loperamide through the BBB.

There were several studies trying to archieve that. One is to combine the lope with quinidine as the latter will inhibit the PGP which is resposible for pumping the lope directly out of the brain. There were noticeable results, but no euphoria just a slight respiratory depression (plus major constipation I guess). This won't cause any binders to cross the BBB.

Another attempt is to dealing with nanoparticles as they somehow help the lope cross the BBB - but nanoparticles of any kind are very expensive and using them in the right way would require a real lab.



For the extraction I would try extracting the lope as the base with chloroform, or extract the salt using an alcohol - the shorter the chain the better the solubility.

[fluxist]

On the contrary, creating a drug-loaded nanoparticle matrix is quite trivial. All neccessary chemicals are available easily and cheaply as reagents (save loperamide).

The clandestine techniques are in the process of being refined, but may i suggest:

Kreuter, J. Pharm Acta Helv. 58:196-209 (1983)

Additional info available upon request.

[taig]

That's some interesting news to me. When I was looking into that loperamide matter about 1-2 years ago I only found ultra-expensive nanoparticles for sale and the procedures I read looked rather difficult.

But now it seems like there is much to get from loperamide, if one can really relatively easiely make the loperamide cross the BBB that would be quite a breakthrough. Kind of like an OTC fentanyl...