Dosage forms for the delivery of drugs of abuse and related methods
First Claim
Patent Images
1. An abuse-deterrent drug formulation comprising a melt-processed mixture ofa) at least one abuse-relevant drug,b) at least one cellulose ether or cellulose ester, andc) at least one alkyl alkacrylate polymer, alkacrylate polymer, or a combination thereof,wherein the amount of the drug that is extracted in vitro from the formulation by 40% aqueous ethanol within one hour at 37°
- C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
C.; and
wherein the drug formulation is adapted so as to be useful for oral administration to a human 3, 2, or 1 times daily.
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Accused Products
Abstract
A dosage form and method for the delivery of drugs, particularly drugs of abuse, characterized by resistance to solvent extraction, tampering, crushing, or grinding, and providing an initial burst of release of drug followed by a prolonged period of controllable drug release.
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Citations
104 Claims
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1. An abuse-deterrent drug formulation comprising a melt-processed mixture of
a) at least one abuse-relevant drug, b) at least one cellulose ether or cellulose ester, and c) at least one alkyl alkacrylate polymer, alkacrylate polymer, or a combination thereof, wherein the amount of the drug that is extracted in vitro from the formulation by 40% aqueous ethanol within one hour at 37° - C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
C.; andwherein the drug formulation is adapted so as to be useful for oral administration to a human 3, 2, or 1 times daily. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 104)
- C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
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17. A monolithic, sustained release oral dosage formulation comprising a melt-processed mixture of:
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a) an analgesically effective amount of at least one an abuse-relevant drug, b) at least one cellulose ether or cellulose ester, and c) at least one alkyl alkacrylate polymer, alkacrylate polymer, or a combination thereof, wherein the amount of the drug that is extracted in vitro from the formulation by 40% aqueous ethanol within one hour at 37°
C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
C.; andwherein the drug formulation is adapted for sustained release so as to be useful for oral administration to a human 3, 2, or 1 times daily. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)
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29. An oral sustained release dosage formulation of a drug characterized by at least two of the following features:
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a) the drug that is extracted from the formulation by 40% aqueous ethanol within one hour at 37°
C. in vitro is less than or equal twice the amount of the drug that is extracted by 0.01 N hydrochloric acid in vitro within one hour at 37°
C.,b) the formulation does not break under a force of 150 newtons, preferably 300 newtons, more preferably 450 newtons, yet more preferably 500 newtons as measured by “
Pharma Test PTB 501”
hardness tester, andc) the formulation releases at least 15% of the one drug and not more than 45% of the one drug during the first hour in vitro dissolution testing and preferably also in vivo. - View Dependent Claims (30, 31, 32, 33, 34, 35, 36, 37, 38, 39)
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- 40. A non-milled, melt-extruded drug formulation comprising a drug with abuse potential.
- 46. A monolithic, non-milled, non-multiparticulated, melt-extruded drug formulation comprising a drug with abuse potential having a diameter from about at least 5.1 mm to about 10 mm and a length from about 5.1 mm to about 30 mm.
- 52. An abuse-deterrent drug formulation formed by a process comprising melt extruding the formulation having at least one therapeutic drug and directly shaping the extrudate into a dosage form without (an intermediate) milling step or multiparticulating step.
- 54. A process for the manufacture of an abuse-resistant drug dosage formulation comprising melt extruding a formulation comprising at least one therapeutic drug further comprising directly shaping the extrudate into a dosage form without (an intermediate) milling step or multiparticulating step.
- 56. A monolithic, non-milled, melt-extruded drug formulation comprising a drug with abuse potential wherein the monolithic formulation has a substantially similar drug release profile to a crushed form of the monolithic formulation wherein the monolithic formulation is crushed at about 20,000 rpm to about 50,000 rpm in a coffee grinding machine for about 60 seconds.
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61. An abuse-deterrent drug formulation comprising a melt-processed mixture of
at least one abuse-relevant drug, and at least one rate altering pharmaceutically acceptable polymer, copolymer, or a combination thereof, wherein the amount of the drug that is extracted from the formulation by 40% aqueous ethanol within one hour at 37° - C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
C.; andwherein the drug formulation is adapted so as to be useful for oral administration to a human 3, 2, or 1 times daily. - View Dependent Claims (62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75)
- C. is less than or equal to twice the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
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76. An abuse-deterrent drug formulation comprising a melt-processed mixture of
a) at least one abuse-relevant drug, wherein said drug is hydrocodone, b) at least one cellulose ether or cellulose ester, and c) at least one acrylic polymer, methacrylic polymer, or a combination thereof, wherein the drug formulation is adapted so as to be useful for oral administration to a human 3, 2, or 1 times daily; - and
wherein about 90% of the hydrocodone is released in vitro at about 4-6 hours when adapted to be administered 3 times a day, at about 6-10 hours when adapted to be administered 2 times a day and about 16-22 hours when adapted to be administered 1 time a day. - View Dependent Claims (77, 78)
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79. An abuse-deterrent drug formulation comprising a melt-processed mixture of
at least one opioid; -
at least one rate altering pharmaceutically acceptable polymer, copolymer, or a combination thereof; wherein the amount of the drug that is extracted from the formulation by 40% aqueous ethanol within one hour at 37°
C. is about 70% to about 110% of the amount of the drug that is extracted by 0.01 N hydrochloric acid within one hour at 37°
C.; andwherein the drug formulation is adapted so as to be useful for oral administration to a human 3, 2, or 1 times daily. - View Dependent Claims (80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103)
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Specification