Abuse Resistant and Extended Release Formulations and Method of Use Thereof
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Accused Products
Abstract
The present invention is in the field of oral, abuse resistant pharmaceutical compositions of opioids, extended release pharmaceutical compositions of opioids and extended release abuse resistant pharmaceutical compositions of opioids and the use thereof for the treatment of pain. The present invention is also directed to extended release pharmaceutical compositions and the use thereof for preventing or minimizing the risk of opioid abuse and/or opioid toxicity from either intentional or unintentional tampering. The present invention is further directed at a method of preventing or minimizing the risk of opioid abuse and/or opioid toxicity from either intentional or unintentional tampering.
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Citations
180 Claims
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1-160. -160. (canceled)
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161. An abuse deterrent monolithic solidified oral dosage form prepared by a thermal process comprising the following material:
- (a) a therapeutically effective amount of opioid agonist or a pharmaceutically acceptable salt thereof or a mixture thereof;
(b) one or more compounds selected from the group consisting of;
(i) hydrogenated Type I or Type II vegetable oils;
(ii) polyoxyethylene stearates and distearates;
(iii) glycerol monostearate;
(iv) poorly water soluble, high melting point (mp=45 to 100°
C.) waxes; and
(c) one or more additional pharmaceutically acceptable excipients, wherein the material are substantially uniformly dispersed, wherein abuse-deterrent and extended-release properties are simultaneously provided, wherein, upon physical tampering of the dosage form, the in-vitro release rate by weight of the opioid agonist from the dosage form over the first hour when measured by the USP paddle method at 100 rpm in 900 mL aqueous buffer at a pH of between 1.6 and 7.2 at 37°
C. is less than for an immediate release form of the opioid agonist, and wherein, upon physical tampering of the dosage form, the in-vivo dose-normalized Cmax upon first administration of the opioid agonist from the dosage form is less than for an immediate release form of the opioid agonist. - View Dependent Claims (167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180)
- (a) a therapeutically effective amount of opioid agonist or a pharmaceutically acceptable salt thereof or a mixture thereof;
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162. An abuse deterrent monolithic solidified oral dosage form prepared by a thermal process comprising the following material:
- (a) a therapeutically effective amount of opioid agonist or a pharmaceutically acceptable salt thereof or a mixture thereof;
(b) one or more compounds selected from the group consisting of;
(i) hydrogenated Type I or Type II vegetable oils;
(ii) polyoxyethylene stearates and distearates;
(iii) glycerol monostearate;
(iv) poorly water soluble, high melting point (mp=45 to 100°
C.) waxes; and
(c) at least one pharmaceutically acceptable excipient selected from the group comprising a thixotrope and a release rate modifier, wherein the thixotrope and release rate modifier provide further abuse deterrence, wherein the material are substantially uniformly dispersed, wherein abuse-deterrent and extended-release properties are simultaneously provided, wherein, upon physical tampering of the dosage form, the in-vitro release rate by weight of the opioid agonist from the dosage form over the first hour when measured by the USP paddle method at 100 rpm in 900 mL aqueous buffer at a pH of between 1.6 and 7.2 at 37°
C. is less than for an immediate release form of the opioid agonist, and wherein, upon physical tampering of the dosage form, the in-vivo dose-normalized Cmax upon first administration of the opioid agonist from the dosage form is less than for an immediate release form of the opioid agonist. - View Dependent Claims (163, 164, 165, 166)
- (a) a therapeutically effective amount of opioid agonist or a pharmaceutically acceptable salt thereof or a mixture thereof;
Specification