Phenidate drug formulations having diminished abuse potential

• US 20020035126A1
• Filed: 09/18/2001
• Published: 03/21/2002
• Est. Priority Date: 12/04/1995
• Status: Active Grant

• Current Assignee: Celgene Corporation (Bristol-Myers Squibb Company)
• Original Assignee: Celgene Corporation (Bristol-Myers Squibb Company)
• Inventors: Zeitlin, Andrew L., Dariani, Maghsoud M.
• Granted Patent: US 6,528,530 B2
• Time in Patent Office: Days
• US Class Current: 514/317
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/4458 only substituted in position 2, e.g. methylphenidate
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: C07D 211/34 with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• CPC Class Codes: C12P 17/12 containing a six-membered hetero ring
• CPC Class Codes: C12P 41/006 by reactions involving C-N bonds, e.g. nitriles, amides, hydantoins, carbamates, lactames, transamination reactions, or keto group formation from racemic mixtures

Abstract

Phenidate drug formulations are provided having reduced potential for drug abuse. Dosage forms for treating Attention Deficit Disorder, Attention Deficit Hyperactivity Disorder, AIDS Dementia Complex and cognitive decline in HIV-AIDS are provided which minimize drug hypersensitivity, toxicity, side effects, euphoric effect, and drug abuse potential. Such dosage forms comprise D-threo stereoisomer of a phenidate in the substantial absence of all other stereoisomers.

Claims

1. A pharmaceutical unit dosage comprising a pharmaceutically effective amount of a compound having the formula

2. The unit dosage of claim 1 wherein said compound is D-threo-methylphenidate.

3. The unit dosage of claim 2 comprising from about 1 to about 50 milligrams of D-threo-methylphenidate.

4. The unit dosage of claim 2 comprising from about 2 to about 20 milligrams of D-threo-methylphenidate.

5. The unit dosage of claim 2 comprising from about 2½

to about 12 milligrams of D-threo-methylphenidate.

6. The unit dosage of claim 3 in a form suitable for oral administration.

7. The unit dosage of claim 5 in a form suitable for injection or infusion.

8. A pharmaceutical unit dosage of D-threo-methylphenidate substantially free of other stereoisomers of methylphenidate.