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US 2016/0243041 A1Published application
Gastric retentive extended release pharmaceutical compositions
AssigneeMallinckrodt Inc.
InventorsKRISHNA R. DEVARAKONDA, MICHAEL J. GIULIANI, VISHAL K. GUPTA, RALPH A. HEASLEY, SUSAN SHELBY
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Abstract
The present disclosure provides extended release pharmaceutical compositions comprising an opioid and an additional active pharmaceutical ingredient, wherein the composition exhibits gastric retentive properties which are achieved by a combination of a physical property of the composition and release of the opioid, wherein upon administration to a subject, the composition has at least one pharmacokinetic parameter that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.
Claims20
A method of treating acute pain in a human subject comprising:
- administering to the subject in need thereof a solid oral dosage form comprising:
- (a) at least one immediate release portion comprising acetaminophen in an amount selected from the group consisting of about 125 mg to about 325 mg, and hydrocodone or a pharmaceutically acceptable salt thereof in an amount selected from the group consisting of about 1.5 mg to about 4.0 mg;
- and
- (b) at least one extended release portion comprising acetaminophen in an amount selected from the group consisting of about 125 mg to about 325 mg, and hydrocodone or a pharmaceutically acceptable salt thereof in an amount selected from the group consisting of about 4.5 mg to about 6.5 mg wherein the total amount of acetaminophen in the solid oral dosage form is 325 mg and the total amount of hydrocodone or a pharmaceutically acceptable salt in the solid oral dosage form is about 7.5 mg;
- and
- wherein upon administration of two solid oral dosage forms the subject attains therapeutic blood levels of both the hydrocodone and the acetaminophen within about one hour after administration of the solid oral dosage forms and maintains analgesia for about 12 hours after administration of the solid oral dosage forms.
3 more elements
A method of treating acute pain in a human subject over a 12-hour dosing cycle comprising:
- administering to the subject in need thereof a solid oral dosage form comprising:
- (a) at least one immediate release portion comprising about 125 mg to about 325 mg of acetaminophen and about 1.5 mg to about 4.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof;
- and
- (b) at least one extended release portion comprising about 125 mg to about 325 mg of acetaminophen and about 4.5 mg to about 6.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof;
- wherein the total amount of acetaminophen in the solid oral dosage form is 325 mg and the total amount of hydrocodone or a pharmaceutically acceptable salt in the solid oral dosage form is about 7.5 mg;
- wherein upon placement of the solid oral dosage form in an in vitro dissolution test comprising USP Paddle Method at a paddle speed of about 100 rpm in 900 ml of 0.1 N HCl using a USP type II apparatus at a constant temperature of 37° C., the drug release profile substantially corresponds to the following:
- after 15 minutes, about 20% to about 40%, by weight, of the total amount of hydrocodone or salt thereof in the solid oral dosage form is released and about 50% to about 55%, by weight, of the total amount of acetaminophen in the solid oral dosage form is released;
- after 1 hour, about 40% to about 50%, by weight, of the total amount of hydrocodone or salt thereof in the solid oral dosage form is released and about 50% to about 70%, by weight, of the total amount of acetaminophen in the solid oral dosage form is released;
- and after 12 hours, from about 95% to about 100%, by weight, of the total amount of the hydrocodone or salt is released and from about 90% to about 100%, by weight, of the total amount of the acetaminophen is released.
6 more elements
A method of treating acute pain in a human subject over a 12-hour dosing cycle comprising:
- administering to the subject in need thereof a solid oral dosage form comprising:
- (a) at least one immediate release portion comprising about 125 mg to about 325 mg of acetaminophen, and about 1.5 mg to about 4.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof;
- and
- (b) at least one extended release portion comprising about 125 mg to about 325 mg of acetaminophen, and about 4.5 mg to about 6.5 mg of hydrocodone or a pharmaceutically acceptable salt thereof;
- wherein the total amount of acetaminophen in the solid oral dosage form is 325 mg and the total amount of hydrocodone or a pharmaceutically acceptable salt in the solid oral dosage form is about 7.5 mg;
- and
- wherein upon administration of the solid oral dosage form the subject, the solid oral dosage form produces a mean AUC for hydrocodone from about 12.0 ng·hr/mL/mg to about 19.0 ng·hr/mL/mg and a mean AUC for acetaminophen from about 35.0 ng·hr/mL/mg to about 80.0 ng·hr/mL/mg.
4 more elements
Dependencies are inferred from the claim text.