Immediate release composition resistant to abuse by intake of alcohol

• US 9,005,660 B2
• Filed: 02/05/2010
• Issued: 04/14/2015
• Est. Priority Date: 02/06/2009
• Status: Expired due to Fees

• Current Assignee: Egalet, Ltd. (Assertio Holdings, Inc.)
• Original Assignee: Egalet, Ltd. (Assertio Holdings, Inc.)
• Inventors: Tygesen, Peter Holm, Oevergaard, Jan Martin, Oestman, Joakim
• Primary Examiner(s): Gembeh, Shirley V
• Application Number:
  US12/701,248
• Publication Number:
  US 20100204259A1
• Time in Patent Office: 1,894 Days
• Field of Search: 424/466, 424/495, 514/282, 514/629
• US Class Current: 424/466
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2893 Tablet coating processes mechanical aspects A61J3/06
• CPC Class Codes: A61P 25/32 Alcohol-abuse

Abstract

The present invention relates to immediate release pharmaceutical compositions for oral administration that are resistant to abuse by intake of alcohol. In particular, this disclosure provides immediate release pharmaceutical compositions comprising a polyglycol having a molecular weight of from about 900 to about 17,000 daltons, a drug substance, one or more effervescent agents, and, optionally, one or more disintegrants, such that the composition is formulated to be resistant to abuse by intake of alcohol.

Claims

1. An immediate release pharmaceutical composition, wherein the composition is resistant to alcohol-induced dose dumping, the composition comprising:

a. one or more drug substances; and

b. a polymer matrix resistant to alcohol-induced dose dumping,

wherein the drug substance is dispersed within the polymer matrix, and wherein the polymer matrix consists essentially of

(i) a polyglycol having a molecular weight of from 900 to about 17,000 Daltons;

(ii) one or more effervescent agents; and

(iii) one or more disintegrants.

2. The immediate release pharmaceutical composition according to claim 1, wherein the composition is resistant to abuse by intake of alcohol when the alcohol is ingested either:

a. together with the composition, or

b. within a period of up to 60 minutes before and up to 60 minutes after the intake of the composition.

3. The immediate release pharmaceutical composition of claim 1, wherein the composition is suitable for administration to a patient that ingests three or more alcoholic beverages daily.

4. The immediate release pharmaceutical composition of claim 3, wherein the composition is resistant to alcohol-induced dose dumping when a patient to whom the composition is administered ingests an alcoholic beverage either:

a. together with the composition, or

b. within a period of up to 60 minutes before and up to 60 minutes after ingesting the composition.

5. The immediate release pharmaceutical composition according to claim 1, wherein the one or more effervescent agents comprise a water soluble organic acid and a water soluble bicarbonate.

6. The immediate release pharmaceutical composition according to claim 1, wherein the polyglycol has a molecular weight selected from 1000, 1100, 1900, 2000, 2800, 2900, 3350, 4400, 5800, 6000, 8000, 8400, 10,000, 12,000, 14,600, and 17,000 Daltons.

7. The immediate release pharmaceutical composition according to claim 1, wherein the one or more drug substances is selected from the group consisting of anaesthetics, analgesics, opioids, antipyretics, antimigraine agents, antiepileptics, anti-parkinson agents, dopaminergic agents, antipsychotics, anxiolytics, sedatives, antidepressants, psychostimulating agents used for ADHD and nootropics, and agents used in addictive disorders.

8. The immediate release pharmaceutical composition according to claim 7, wherein the one or more effervescent agents comprise a water soluble organic acid and a water soluble bicarbonate.

9. The immediate release pharmaceutical composition according to claim 7, wherein the polyglycol has a molecular weight selected from 1000, 1100, 1900, 2000, 2800, 2900, 3350, 4400, 5800, 6000, 8000, 8400, 10,000, 12,000, 14,600, or 17,000 Daltons.

10. The immediate release pharmaceutical composition according to claim 7, wherein the composition is resistant to alcohol-induced dose dumping when the alcohol is ingested either:

a. together with the composition, or

b. within a period of up to 60 minutes before and up to 60 minutes after ingesting the composition.

11. The immediate release pharmaceutical composition according to claim 7, wherein the one or more drug substances is released from the composition in the stomach with a release profile that is dependent on the concentration of ethanol, such that an increased ethanol concentration results in a decreased rate of drug release.

12. The immediate release pharmaceutical composition according to claim 1, wherein the one or more disintegrants is selected from the group consisting of sodium starch glycolate, povidone, sodium alginate, alginic acid, calcium alginate, carboxymethylcellulose calcium, carboxymethylcellulose sodium, powdered cellulose, chitosan, croscarmellose sodium, crospovidone, cross-linked polyvinylpyrrolidone, hydroxypropyl starch, hydroxypropyl cellulose low-substituted, magnesium aluminium silicate, methylcellulose, microcrystalline cellulose, pregelatinized starch, docusae sodium, guar gum, and polacrilin potassium.

13. The immediate release pharmaceutical composition according to claim 1, wherein the concentration of the one or more disintegrants in the composition is in an amount selected from about 1% to about 60% by weight and about 5% to about 50% by weight.