Formulation of metaxalone
AssigneeiCeutica, Inc.
InventorH. William Bosch
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Abstract
Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms.
Claims48
A unit dosage form of metaxalone containing between 100 and 600 mg of metaxalone, wherein the dissolution rate of the metaxalone, when tested in a Sotax Dissolution Apparatus using 1000 ml of 0.01 N HCl (pH=2) at 37° C. and Type 2 Apparatus (paddle) set to a rotational speed of 100 rpm, is such that at least 80% dissolves in 60 min.
The unit dosage form of any of the forgoing claims wherein the mean AUC∞ per mg of metaxalone in the fasted state is 80% to 125% of 18.7 ng·h/mL.
The unit dosage form of any of the forgoing claims wherein the mean AUC∞ in the fasted stated is 80%-125% of 7479 ng·h/mL when a total dose selected from 200, 225, 250, 275, 300, 325, 350, 375, 400, 425, 450, 475, 500, 525, 550, 575, 600 or 625 mg is administered.
The unit dosage form of any of the forgoing claims wherein the mean AUC∞ in the fasted stated is 80%-125% of 15044 ng·h/mL when a total dose selected from 200, 225, 250, 275, 300, 325, 350, 375, 400, 425, 450, 475, 500, 525, 550, 575, 600 or 625 mg is administered.
The unit dosage form of any of the forging claims wherein the mean Cmax in the fasted state is greater (e.g., at least 10%, 20%, 30%, 40%, 50%, 60%, 70% or 80% greater) than 983 ng/mL at a total dose that provides a mean AUC∞ in the fasted stated is 80%-125% of 7479 ng·h/mL.
The unit dosage form of any of the forging claims wherein the mean Cmax in the fasted state is greater than 1816 ng/mL at a total dose that provides a mean AUC∞ in the fasted stated is 80%-125% of 15044 ng·h/mL.
The unit dosage form of any of the forgoing claims wherein the Tmax in the fasted state is less than 2.7 hrs, 2.5 hrs, 2.3 hrs, 2.1 hrs, 1.9 hrs or 1.7 hrs.
The unit dosage form of any of the forgoing claims wherein the Tmax in the fed state is less than 2.7 hrs, 2.5 hrs, 2.3 hrs, 2.1 hrs, 1.9 hrs or 1.7 hrs.
Dependencies are inferred from the claim text.