CA2477004A1 - Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances - Google Patents

Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances Download PDF

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Publication number
CA2477004A1
CA2477004A1 CA002477004A CA2477004A CA2477004A1 CA 2477004 A1 CA2477004 A1 CA 2477004A1 CA 002477004 A CA002477004 A CA 002477004A CA 2477004 A CA2477004 A CA 2477004A CA 2477004 A1 CA2477004 A1 CA 2477004A1
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Canada
Prior art keywords
composition
controlled substance
active form
chemical moiety
controlled
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Granted
Application number
CA002477004A
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French (fr)
Other versions
CA2477004C (en
Inventor
Thomas Piccariello
Randal J. Kirk
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Shire LLC
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Individual
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Priority to CA2740256A priority Critical patent/CA2740256A1/en
Publication of CA2477004A1 publication Critical patent/CA2477004A1/en
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Publication of CA2477004C publication Critical patent/CA2477004C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral delivery. When delivered by the oral route the controlled substance is released in a time-dependent manner (sustained release) by acid hydrolysis and/or enzymatic cleavage. When administered by injection the controlled substance is released in a time-dependent manner (sustained release) by way of serum enzymes.

Claims (31)

1. A pharmaceutical composition comprising:
a controlled substance; and an amino acid or polypeptide covalently bound to said controlled substance in a manner that renders said controlled substance pharmacologically inactive.
2. The composition of claim 1, wherein said controlled substance is released in active form in the presence of acid present in the stomach or in the presence of enzymes present in the intestinal tract or blood serum.
3. The composition of claim 2, adapted for oral administration, wherein said controlled substance is released in active form in the presence of acid present in the stomach or in the presence of enzymes present in the intestinal tract.
4. The composition of claim 1, wherein said polypeptide comprises less than 70 amino acids.
5. The composition of claim 1, wherein said polypeptide comprises less than 50 amino acids.
6. The composition of claim 1, wherein said polypeptide comprises less than amino acids.
7. The composition of claim 1 wherein said chemical moiety is polyserine.
8. The composition of claim 1 wherein said chemical moiety is bound to said controlled substance by an ester or carbonate bond.
9. The composition of claim 1 wherein said controlled substance is codeine.
10. The composition of claim 1 wherein said controlled substance is fentanyl.
11. The composition of claim 1 wherein said controlled substance is hydrocodone.
12. The composition of claim 1 wherein said controlled substance is hydromorphone.
13. The composition of claim 1 wherein said controlled substance is levorphanol.
14. The composition of claim 1 wherein said controlled substance is methadone.
15. The composition of claim 1 wherein said controlled substance is morphine
16. The composition of claim 1 wherein said controlled substance is oxycodone.
17. The composition of claim 1 wherein said controlled substance is propoxyphene.
18. The composition of claim 1 wherein said controlled substance is sufentanyl.
19. The composition of claim 1 wherein said controlled substance is amphetamine.
20. The composition of claim 1 wherein said controlled substance is methylphenidate.
21. The composition of claim 1 wherein said chemical moiety is a polypeptide.
22. The composition of claim 1 wherein said chemical moiety is an amino acid.
23. The composition of claim 1 wherein said chemical moiety is a protein.
24. The composition of claim 3 that releases said controlled substance in a pharmacologically active form when administered to a human patient by the oral route.
25. The composition of claim 3 that is resistant to release of said controlled substance in a pharmacologically active form when administered by the intranasal route thus diminishing or preventing a euphoric effect.
26. The composition of claim 3 that is resistant to release of said controlled substance in a pharmacologically active form when administered by inhalation thus diminishing or preventing a euphoric effect.
27. A composition of claim 3 that is resistant to release of said controlled substance in a pharmacologically active form when administered by parenteral injection thus diminishing or preventing a euphoric effect.
28. A method for delivering a controlled substance to a patient so as to obtain a therapeutic, but not a substantial euphoric effect, comprising orally administering the composition of claim 1 to said patient.
29. A method for delivering a controlled substance to a patient so as to obtain a therapeutic, but not a substantial euphoric effect, comprising parenterally administering the composition of claim 1 to said patient.
30. A composition of claim 1 wherein the said chemical moiety is an oligopeptide.
31. A composition of claim 30 wherein the said oligopeptide is specifically designed to be cleaved by intestinal enzymes.
CA2477004A 2002-02-22 2003-02-24 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances Expired - Fee Related CA2477004C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2740256A CA2740256A1 (en) 2002-02-22 2003-02-24 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US35836802P 2002-02-22 2002-02-22
US60/358,368 2002-02-22
US36208202P 2002-03-07 2002-03-07
US60/362,082 2002-03-07
PCT/US2003/005525 WO2003072046A2 (en) 2002-02-22 2003-02-24 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2740256A Division CA2740256A1 (en) 2002-02-22 2003-02-24 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances

Publications (2)

Publication Number Publication Date
CA2477004A1 true CA2477004A1 (en) 2003-09-04
CA2477004C CA2477004C (en) 2011-05-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA2477004A Expired - Fee Related CA2477004C (en) 2002-02-22 2003-02-24 Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances

Country Status (9)

Country Link
US (1) US7622441B2 (en)
EP (2) EP2319540A1 (en)
JP (1) JP4878732B2 (en)
KR (1) KR100822498B1 (en)
AU (2) AU2003219863C1 (en)
CA (1) CA2477004C (en)
ES (1) ES2500117T3 (en)
IL (2) IL163667A0 (en)
WO (1) WO2003072046A2 (en)

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