Phenidate drug formulations having diminished abuse potential

• US 6,528,530 B2
• Filed: 09/18/2001
• Issued: 03/04/2003
• Est. Priority Date: 12/04/1995
• Status: Expired due to Term

• Current Assignee: Celgene Corporation (Bristol-Myers Squibb Company)
• Original Assignee: Celgene Corporation (Bristol-Myers Squibb Company)
• Inventors: Zeitlin, Andrew L., Dariani, Maghsoud M.
• Primary Examiner(s): HENLEY III, RAYMOND J
• Application Number:
  US09/955,556
• Publication Number:
  US 20020035126A1
• Time in Patent Office: 532 Days
• Field of Search: 514/317
• 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 from about 1 to about 50 milligrams of compound having the formula:

or a pharmaceutically acceptable salt thereof, wherein R₁ is C₁-C₄ alkyl, and R₂ is hydrogen or C₁-C₄ alkyl, in a pharmaceutically acceptable carrier or diluent, said dosage form having less than 10% by weight of other stereoisomers of the compound or salt.

2. The unit dosage of claim 1 comprising from about 2 to about 20 milligrams of said compound.

3. The unit dosage of claim 1 comprising from about 2½

to about 12 milligrams of said compound.

4. The unit dosage of claim 1 in a form suitable for oral administration.