Sustained release opioid formulations and method of use
First Claim
1. A sustained-release oral dosage form comprising a subunit, wherein the subunit comprises an opioid analgesic and a sustained-release material, wherein the dissolution rate in-vitro of the subunit, when measured by standard USP Drug Release test of U.S. Pharmacopeia (2003) <
- 724>
, is;
a. less than about 10% within about 6 hours and at least about 60% within about 24 hours;
b. less than about 10% within about 8 hours and at least about 60% within about 24 hours;
C. less than about 10% within about 10 hours and at least about 60% within about 24 hours;
or d. less than about 10% within about 12 hours and at least about 60% within about 24 hours;
the dosage form providing a duration of therapeutic effect of about 24 hours.
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Abstract
The invention combines two different subunits with different release profiles in novel sustained-release oral dosage forms. In particular, the oral dosage forms include a subunit that comprises an opioid analgesic and a sustained-release material, wherein the dissolution rate in-vitro of the subunit, when measured by the standard USP Drug Release test of U.S. Pharmacopeia XXVI (2003) <724>, is less than about 10% within about 6 hours and at least about 60% within about 24 hours; less than about 10% within about 8 hours and at least about 60% within about 24 hours; less than about 10% within about 10 hours and at least about 60% within about 24 hours; or less than about 10% within about 12 hours and at least about 60% within about 24 hours; the dosage form providing a duration of therapeutic effect of about 24 hours.
343 Citations
44 Claims
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1. A sustained-release oral dosage form comprising a subunit, wherein the subunit comprises an opioid analgesic and a sustained-release material, wherein the dissolution rate in-vitro of the subunit, when measured by standard USP Drug Release test of U.S. Pharmacopeia (2003) <
- 724>
, is;
a. less than about 10% within about 6 hours and at least about 60% within about 24 hours;
b. less than about 10% within about 8 hours and at least about 60% within about 24 hours;
C. less than about 10% within about 10 hours and at least about 60% within about 24 hours;
ord. less than about 10% within about 12 hours and at least about 60% within about 24 hours;
the dosage form providing a duration of therapeutic effect of about 24 hours. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 37, 38, 39, 44)
- 724>
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25. A sustained-release oral dosage form comprising a first subunit and a second subunit, wherein the first subunit comprises a first opioid analgesic and the second subunit comprises a second opioid analgesic, wherein the first and second opioid analgesics can be the same or different, wherein the first subunit releases substantially all of the first opioid analgesic within about 12 hours and the second subunit releases less than about 10% of the second opioid analgesic within about 6 hours and at least about 60% of the second opioid analgesic within about 24 hours, wherein the dissolution rate in-vitro is measured by standard USP Drug Release test of U.S. Pharmacopeia XXVI (2003) <
- 724>
, such that;
a. the oral dosage form releases from about 35% to about 65% of the first and second opioid analgesic after about 10 hours;
b. the oral dosage form releases not more than about 10% of the first and second opioid analgesic after about 1 hour;
orc. the oral dosage form releases not less than about 70% of the first and second opioid analgesic after about 20 hours, the dosage form providing a duration of therapeutic effect of about 24 hours. - View Dependent Claims (26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 43)
- 724>
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40. An oral dosage form comprising an opioid analgesic in sustained-release form, which, at steady-state, provides:
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a. a maximum opioid plasma concentration (Cmax) and an opioid plasma concentration at about 24 hours after administration (C24), wherein the ratio of Cmax to C24 is less than about 2;
1;
b. a maximum opioid plasma concentration (Cmax), and an opioid plasma concentration at about 12 hours after administration (C12), and an opioid plasma concentration at about 24 hours after administration (C24), wherein the average opioid plasma concentration between Cmax and C12 is substantially equal to the average opioid plasma concentration between C12 and C24;
c. a first maximum opioid plasma concentration (Cmax1) between about 0 hours and about 12 hours after administration, and a second maximum opioid plasma concentration (Cmax2) between about 12 hours and about 24 hours after administration;
d. a first maximum opioid plasma concentration (Cmax1) between about 0 hours and about 12 hours after administration, a second maximum opioid plasma concentration (Cmax2) between about 12 hours and about 24 hours after administration, and an opioid plasma concentration at about 24 hours after administration (C24), wherein the average plasma opioid concentration between about Cmax1 and about Cmax2 is substantially equal to the average opioid plasma concentration between about Cmax2 and about C24;
e. a first opioid maximum plasma concentration (Cmax1) and a first minimum opioid plasma concentration (Cmin1) between about 0 hours and about 12 hours after administration, a second maximum opioid plasma concentration (Cmax2), and an opioid plasma concentration at about 24 hours after administration (C24), wherein the ratio of Cmax1 to Cmin1 is less than about 2;
1 or the ratio of Cmax2 to C24 is less than about 2;
1;
orf. a first maximum opioid plasma concentration (Cmax1) and a first minimum opioid plasma concentration (Cmin1) between about 0 hours and about 12 hours after administration, a second opioid maximum plasma concentration (Cmax2), and an opioid plasma concentration at about 24 hours after administration (C24), wherein the difference between the ratio of Cmax1 to Cmin1 and the ratio of Cmax2 to C24 is less than about 30%.
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41. A sustained-release oral dosage form comprising a first subunit and a second subunit, wherein:
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a. the first subunit and the second subunit comprise an opioid analgesic, wherein the dosage form, at steady-state, provides a maximum opioid plasma concentration (Cmax) and an opioid plasma concentration at about 24 hours after administration (C24), wherein the ratio of Cmax to C24 is less than about 2;
1;
orb. the first subunit and the second subunit comprise an opioid analgesic, the first subunit comprises a first release-retarding material and the second subunit comprises a second release-retarding material, wherein the first and second release-retarding material can be the same or different, and wherein the dosage form, at steady-state, provides a maximum opioid plasma concentration (Cmax) and an opioid plasma concentration at about 24 hours after administration (C24), wherein the ratio of Cmax to C24 is less than about 2;
1.
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42. An oral dosage form comprising an opioid analgesic in sustained-release form, which at steady-state, provides a first Area Under the Curve (AUC1) between 0 and about 12 hours and a second Area Under the Curve (AUC2) between 12 hours and about 24 hours, wherein the difference between AUC2 and AUC1 is less than about 50%.
Specification