Denaturants for sympathomimetic amine salts

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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514305, A61K 4718

Patent

active

061368644

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

It is believed that the legal and widely available acid salts of sympathomimetic amines, such as the decongestants pseudoephedrine hydrochloride, pseudoephedrine sulfate, ephedrine hydrochloride and phenylpropanolamine hydrochloride, are being used in the chemical synthesis of illegal drugs such as methamphetamine, amphetamine, methcathinone, and cathinone. This invention, by the incorporation of one or more denaturant compounds, renders commercially available, "over the counter" ("OTC") medications containing sympathomimetic amine salts much less suitable as starting materials in the production of illegal drugs. The denaturant(s) exhibit chemical or physical properties which make the isolation of the pure sympathomimetic amine salt difficult or essentially infeasible from a product containing a combination of the denaturant(s) and the sympathomimetic amine salt. Because the isolation of pure sympathomimetic amine salt is rendered impractical, attempts to use compositions proposed in this invention as a source of starting material for the synthesis of illegal drugs will result in compromised yields of adulterated product.
In one preferred embodiment, the term "denaturant" refers to a compound whose separation from sympathornimetic amine salts is difficult or essentially infeasible, so that the synthesis of illegal drugs from the compositions of the invention is rendered impracticable and/or produces illegal drugs in an adulterated form. In another preferred embodiment, the term "denaturant" refers to materials that physically interfere with the extraction of the sympathomimetic amine salts from the pharmaceutical products (i.e. , emulsifies and/or alters viscosity of the pharmaceutical products in solution), so that the purification of the sympathomimetic amine salts from the pharmaceutical products is rendered impractical. The denaturant is understandably pharmacologically and biologically acceptable to mammals due to its presence in OTC medications.


BACKGROUND OF THE INVENTION



2.1 Sympathomimetic Pharmaceuticals

Sympathomimetic compounds, as the name implies, exert biological effects similar to those produced by activation of the sympathetic nervous system. For example, the pharmaceutical compound pseudoephedrine acts as an indirect sympathomimetic agent by causing adrenergic nerve endings to release norepinephrine, thereby stimulating .alpha. and .beta. norepinephrine receptors, particularly in blood vessels of the upper respiratory tract. This, in turn, results in vasoconstriction and shrinkage of swollen tissues in the sinuses and nasal passages.


2.2. The Problem of Illegal Conversion

Methamphetamine is a powerful and destructive drug sold illegally on the street as "crack, "meth" and "speed". Illegal use of methamphetamine is becoming increasingly common. In California alone, hospitals have seen more than a 300 percent increase in emergency room admissions from methamphetamine abuse in the last ten years.
One of the most efficient starting materials in the synthesis of methamphetamine is ephedrine, which is heavily regulated and therefore difficult to obtain. Increasingly, pseudoephedrine, an enantiomer of ephedrine, is being used in the production of methamphetamines. Pseudoephedrine can be obtained from a pseudoephedrine salt, such as pseudoephedrine hydrochloride, which is a common ingredient in over-the-counter ("OTC") medications.
Pseudoephedrine hydrochloride may be isolated from OTC medications by suspending/dissolving the commercial products in water. The resulting slurry/solution is filtered and then treated with base to neutralize the amine salt, pseudoephedrine hydrochloride, thereby producing pseudoephedrine free base. The free base, which has limited water solubility, is then extracted into a water immiscible solvent such as ether. This extraction serves as a purification step. Acidification to regenerate the amine hydrochloride followed by extraction into water is normally adequate to produce suitably pure pseudoephedrine hydrochloride.
It can be underst

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Uncle Fester; Secrets of Methamphetamine Manufacture Fourth Edition; 1996; pp. 154-159.
Table of Cough Cold Products Sold in the United States.

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