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US 8,575,151 B1Granted
Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance
AssigneePisgah National Laboratories, Inc.
InventorsDavid William Bristol, Clifford Riley King, Joseph Pike Mitchener, Jr., Vicki Haynes Audia
Life of this patent
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Abstract
Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.
Claims24
A process for preparing organic acid addition salts of amine containing pharmaceutically active compounds comprising the steps of:
- a) dissolving of an amine containing pharmaceutically active compound selected from the group consisting of phentermine, ephedrine, pseudoephedrine and benzphetamine in a suitable solvent;
- b) preparing a solution comprising pamoate;
- b) combining the solution of amine containing pharmaceutically active compound, and the solution of pamoic acid to form the reaction mixture;
- c) warming said reaction mixture;
- e) allowing said reaction mixture to react;
- f) isolating said organic acid addition salt of amine containing pharmaceutically active compound by filtration, centrifugation or concentration, and
- g) drying the isolated or purified material to remove reaction solvent wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- a) selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- b) combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- c) mixing the combined ingredients to provide blend uniformity;
- d) sieving, screening or milling the mixture to obtain a uniform consistency;
- e) adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C. and further comprising executing a wet or dry granulation procedure.
2 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- converting the mix into a beaded material and filling capsules so as to provide a timed or controlled release pharmacokinetic profile.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- converting the mix by pressing into tablets.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- coating the tablet with an enteric coating.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- used in a therapeutic dosage formulation for at least one ailment selected from of pain, cough, cold, allergy, sinus condition, obesity, attention deficit disorder, psychological or mental debilitation and nausea.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- wherein said pharmaceutically active compound comprises a mixture of physical forms.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- administered for at least one purpose selected from anti-convulsant, anti-depressant, analgesic, anesthetic, anxiolytic, psychotropic, hallucinogenic, hypnotic, anorexic, and treatment of cough, cold and/or sinus condition.
4 more elements
A process for preparing a pharmaceutically acceptable drug product exhibiting drug abuse prevention properties comprising the steps of:
- selecting an organic acid addition salt of an amine containing active pharmaceutical ingredient selected from the group consisting of phentermine pamoate, ephedrine pamoate, pseudoephedrine pamoate, benzphetamine pamoate, imipramine zinafoate and imipramine salicylate;
- combining the organic acid addition salt with excipients and processing aids to yield a mixture;
- mixing the combined ingredients to provide blend uniformity;
- sieving, screening or milling the mixture to obtain a uniform consistency;
- adding ingredients to the mixture for desired proportions of each ingredient to yield a final formulated mix wherein said pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound has a phase transition temperature of at least 100° C.;
- and
- administered by one method delivery presentation selected from solid oral delivery, oral suspension delivery, parenteral delivery, transdermal delivery and inhalation delivery.
4 more elements
A process for preparing organic acid addition salts of amine containing pharmaceutically active compounds comprising the steps of:
- a) dissolving imipramine in a suitable solvent to form an imipramine solution;
- b) preparing an organic acid solution comprising one of BON acid or salicylic acid;
- c) combining the imipramine solution with said acid solution to form a reaction mixture;
- d) warming said reaction mixture;
- e) allowing said reaction mixture to react to form a drug substance selected from the group consisting of imipramine xinafoate or imipramine salicylate;
- f) isolating said drug substance by filtration, centrifugation or concentration,
- g) drying the isolated or purified drug substance to remove reaction solvent.
4 more elements
Dependencies are inferred from the claim text.