Preventing or reducing drug abuse and overdose events

• US 9,211,292 B2
• Filed: 02/14/2012
• Issued: 12/15/2015
• Est. Priority Date: 04/21/2010
• Status: Active Grant

• Current Assignee: Alitair Pharmaceuticals Inc.
• Original Assignee: Alitair Pharmaceuticals Inc.
• Inventors: Howard, William Wayne, Kavesh, Sheldon, Somma, Russell Francis
• Primary Examiner(s): Parad, Dennis J
• Application Number:
  US13/385,322
• Publication Number:
  US 20130034503A1
• Time in Patent Office: 1,400 Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/37 Coumarins, e.g. psoralen
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61P 25/30 for treating abuse or dependence

Abstract

A method and compositions for treating a patient that prevent or reduce drug abuse and overdose events.

Claims

1. A method of treating a patient that prevents or reduces drug abuse and overdose events with drugs, said method comprising:

oral administration of a first amount of a pharmaceutical composition comprising at least one drug bound to at least one ion exchange resin as a resinate, said ion exchange resins being selected from the group consisting of a cationic ion exchange resin and a anionic ion exchange resin, each said ion exchange resin being bound to at least one drug, wherein each bound drug, measured as the unbound state, is less than about 75 percent of its saturation concentration in its resinate leaving unused binding capacity in its ion exchange resin, said saturation concentration being defined as the larger of;

(a) the weight of drug per weight of washed and dried resinate after at least three hours of stirred aqueous resination reaction in a slurry of the drug in de-ionized water at a temperature in the range of 59 to 61°

C. with the initial weight of drug being at least fourfold that of the weight of ion exchange resin present; and

(b) the weight of drug per weight of washed and dried resinate after at least three hours of stirred aqueous resination reaction in a slurry of the drug at a temperature in the range of 59 to 61°

C. with the initial weight of drug being at least fourfold that of the weight of ion exchange resin present, and at a pH having a value within about ±

1 unit of the pK_a of the drug;

said unused ion exchange binding capacity acting as an ion sink limiting the cumulative release of each bound drug to less than about twice the cumulative release from said first amount if immediately after the administration of said first amount of said pharmaceutical composition, a second equal amount of said pharmaceutical composition is ingested by said patient.

2. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 50 percent of its saturation concentration in its resinate.

3. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 40 percent of its saturation concentration in its resinate.

4. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 30 percent of its saturation concentration in its resinate.

5. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 20 percent of its saturation concentration in its resinate.

6. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 10 percent of its saturation concentration in its resinate.

7. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 5 percent of its saturation concentration in its resinate.

8. The method of treating a patient as described in claim 1, wherein each said bound drug, measured as the unbound state, is less than about 1 percent of its saturation concentration in its resinate.

9. The method of claim 1, wherein said pharmaceutical composition additionally comprises at least one unbound drug, said unbound drug having a complementary therapeutic effect to any said bound drug.

10. The method of claim 9, wherein each said unbound drug has an LD₅₀ at least twice as high as any drug bound in a resinate.

11. The method of claim 9, wherein each said unbound drug has an LD₅₀ at least three times as high as any drug bound in a resinate.

12. The method of claim 9, wherein each said unbound drug has an LD₅₀ at least four times as high as any drug bound in a resinate.

13. The method of claim 9, wherein each said unbound drugs has an LD₅₀ at least six times as high as any drug bound in a resinate.

14. The method of claim 9, wherein each said unbound drug has an LD₅₀ at least eight times as high as any drug bound in a resinate.

15. The method of claim 9, wherein each said unbound drug has an LD₅₀ at least ten times as high as any drug bound in a resinate.

16. The method of claim 1 wherein said pharmaceutical composition comprises warfarin bound to a strong base ion exchange resin as a resinate.

17. The method of claim 1, wherein if immediately after said administration of said first amount of said pharmaceutical composition, a second equal amount is ingested by said patient, said unused ion exchange binding capacity acts as an ion sink to limit the cumulative release of each bound drug to less than about 1.35 times the cumulative release from said first amount.

18. The method of claim 1, wherein if immediately after said administration of said first amount of said pharmaceutical composition, a second amount is ingested by said patient, such that the total amount of said pharmaceutical composition ingested is four times said first amount, said unused ion exchange binding capacity acts as an ion sink to limit the increase in cumulative release of each bound drug to less than about twice the cumulative release from said first amount.

19. The method of claim 1, wherein if immediately after said administration of said first amount of said pharmaceutical composition, a second amount is ingested by said patient such that the total amount of said pharmaceutical composition ingested is eight times said first amount, said unused ion exchange binding capacity acts as an ion sink to limit the increase in cumulative release of each bound drug to less than about six times the cumulative release from said first amount.

20. The method of claim 1, wherein if immediately after said administration of said first amount of said pharmaceutical composition, a second amount is ingested by said patient such that the total amount of said pharmaceutical composition ingested is eight times said first amount, said unused ion exchange binding capacity acts as an ion sink to limit the increase in cumulative release of each bound drug to less than about 2.5 times the cumulative release from said first amount.