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Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance

a technology of physiologically active and psychoactive alkaloids and amines, which is applied in the direction of animal repellents, drug compositions, peptide/protein ingredients, etc., can solve the problems of not getting the desired effect, increase the technical difficulty of isolating, inhibit and/or prevent the de-formulation of a drug product, and reduce the economic viability

Inactive Publication Date: 2008-11-27
PISGAH LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a method for supplying a pharmaceutical formulation that is bio-available through an oral administration route but is not bio-available through illicit or abuse-intended routes of administration. The invention also provides a pharmaceutical composition that exhibits anti-abuse characteristics, preventing de-formation or extraction of the active pharmaceutical ingredient. The invention further provides a drug substance and drug product that can be used to treat a therapeutic ailment or have prophylactic properties. The invention also provides a process for preparing organic acid addition salts of amine-containing pharmaceutically active compounds."

Problems solved by technology

The patient receives the intended dosage when used properly, but the desired effect is not obtained if not used properly.

Method used

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  • Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
  • Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
  • Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance

Examples

Experimental program
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Effect test

example 1

Preparation of Phentermine Pamoate

[0181]Phentermine HCl (37.3 g) was suspended in USP H2O (700.0 g) and stirred to achieve a solution (0.05 g / g) and a pH 5.3. The solution was transferred to a metered addition funnel. A solution of disodium pamoate (45.0 g) was prepared by dissolving in USP water (902.0 g) to give a clear solution at a pH 10.4. The solution was adjusted to about pH 9.4 with 0.2N HCl and clarified by solution filtration. At 20° C., the Phentermine HCl solution was added to the stirred disodium pamoate solution at a controlled rate over about 2.5 hours and the addition funnel rinsed with USP H2O (20.0 g) into the reaction mixture. The mixture was stirred for 1 h then warmed to 70° C. where more precipitation was observed. The mixture was heated from about 70° C. to 95° C. over about 1 h then cooled. Solids were collected by filtration and washed with USP H2O (3×200 g) and dried on a vacuum Buchner for about 3 h. The solids collected (83.5 g) were transferred to a dryi...

example 2

Preparation of Ephedrine Pamoate

[0182]Ephedrine Hydrochloride (6.1 g) was stirred in USP water (45.0 g) to yield a solution pH of about 4.9. In a separate flask a disodium pamoate (6.5 g) solution was prepared using USP water (54.0 g) to yield a solution pH of about 9.5. The ephedrine HCl solution was transferred to a metered addition funnel and added to the disodium pamoate solution over approximately 1 h. When about one-half of the addition was completed, the solution became opaque. USP water (2.6 g) was used to rinse in the residue from the addition funnel. The opaque mixture was heated from about 26° C. to near 80° C. The reaction was stirred at about 80° C. for approximately 4.5 h. A thick residue settled in the reaction vessel as the solution cooled. The solution was decanted and the residue transferred to drying dishes. The residue was dried at about 100° C. under vacuum (nitrogen sweep) for about 5.5 h. Drying was continued for about 66 h, the solid ground with a mortar and ...

example 3

Alternate Preparation of Ephedrine Pamoate

[0183]Ephedrine Hydrochloride (7.1 g) was stirred in methanol (62.6 g). Disodium pamoate (8.0 g) was stirred in USP water (71.0 g) and adjusted to about pH 9.5. The methanolic ephedrine hydrochloride solution was added to the disodium pamoate solution over a period of about 1.75 h. The reaction solution was heated to about 60° C. for around 4.5 h then cooled. The reactor was equipped with a distillation head and aqueous methanol was removed by heating. The opaque mixture was cooled and a residue settled to the bottom of the reaction vessel. The solution was carefully decanted and the residue was transferred to a drying dish. The material was placed in a vacuum drying oven (103° C.) for 24 h with a nitrogen sweep. Ephedrine Pamoate was obtained as a solid, 8.4 g (66.6%) 2:1 ephedrine pamoate (by HPLC assay) and characterized by DSC (FIG. 2), FTIR (FIG. 5) and PXRD (FIG. 8).

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Abstract

Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Description

CROSS-REFERENCE TO COPENDING APPLICATIONS[0001]The present application is related to co-pending U.S. patent application Ser. No. 11 / 595,379 filed Nov. 10, 2006.BACKGROUND OF THE INVENTION[0002]The present application is related to pharmaceutically acceptable salts of alkaloids or amine containing compounds, particularly those exhibiting physiological and / or psychological activity in humans and simultaneously designed for targeted release in a controlled pH range so as to eliminate or reduce the compound's physiological or psychological response when used in, or for, medically non-sanctioned, and / or illegitimate purposes. The invention embodies a platform technology for incorporating a targeted release mechanism within an organic-acid addition salt of amine-containing pharmaceutically active compounds. More specifically, many final dose drug products are formulated with active pharmaceutical ingredients (drug substances) that provide pain relief, mood alteration or modification, sens...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/55A61K31/192A61K31/195A61P25/30C07C65/00C07D223/14C07C69/76C07C229/02A61K31/205A61K31/235
CPCA61K31/192A61K31/195A61K31/205A61K31/235A61K31/55A61P25/30
Inventor BRISTOL, DAVID WILLIAMKING, CLIFFORD RILEYMITCHENER, JR., JOSEPH PIKEAUDIA, VICKI HAYNES
Owner PISGAH LAB
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