US2021169845A1PendingUtilityA1

Novel dosage forms of rofecoxib and related methods

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Assignee: TREMEAU PHARMACEUTICALS INCPriority: Nov 13, 2019Filed: Feb 23, 2021Published: Jun 10, 2021
Est. expiryNov 13, 2039(~13.3 yrs left)· nominal 20-yr term from priority
Inventors:Bradford C. SippyRaymond D. SkwierczynskiTravis E. Helm
A61K 31/341A61K 9/2054A61K 9/20A61P 29/00A61P 19/02A61K 31/365A61K 9/16
68
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Claims

Abstract

The subject matter disclosed herein relates to novel doses and dosage forms of rofecoxib having a therapeutic benefit.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A formulation comprising 17.5 mg of rofecoxib, or a pharmaceutically acceptable salt thereof, wherein the formulation achieves a mean C max  plasma concentration of more than 180 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         2 . The formulation of  claim 1 , wherein the formulation achieves a mean C max  plasma concentration of more than 190 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         3 . The formulation of  claim 2 , wherein the formulation achieves a mean C max  plasma concentration of more than 200 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         4 . The formulation of  claim 3 , wherein the formulation achieves a mean C max  plasma concentration of about 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         5 . The formulation of  claim 1 , wherein the formulation achieves a mean C max  plasma concentration within 80-125% of 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         6 . The formulation of  claim 1 , wherein the formulation achieves a mean plasma AUC 0-∞  of more than 3000 h*ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         7 . The formulation of  claim 1 , wherein the formulation achieves a higher mean plasma C max  and a higher mean plasma AUC 0-∞  in a population of healthy female adults less than 65 years of age compared to a population of healthy male adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         8 . The formulation of  claim 1 , wherein the formulation achieves a higher mean plasma AUC 0-∞  in Caucasian adults less than 65 years of age compared to healthy African American adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         9 . The formulation of  claim 1 , wherein the formulation achieves an arithmetic mean plasma concentration of at least 2.0 ng/ml at 15 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         10 . The formulation of  claim 1 , wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         11 . The formulation of  claim 1 , wherein the formulation is a liquid dosage form. 
     
     
         12 . The formulation of  claim 11 , wherein the liquid dosage form is a solution. 
     
     
         13 . The formulation of  claim 11 , wherein the liquid dosage form is a suspension. 
     
     
         14 . The formulation of  claim 11 , wherein the liquid dosage form is a syrup. 
     
     
         15 . The formulation of  claim 1 , wherein the formulation is a tablet formulation. 
     
     
         16 . The formulation of  claim 15 , wherein the formulation further comprises a disintegrant. 
     
     
         17 . The formulation of  claim 15 , wherein the rofecoxib has a d90 particle size in the range of about 10 μm to about 12 μm, a d50 particle size in the range of about 3 μm to about 4 μm, and a d10 particle size in the range of about 0.5 μm to about 1.0 μm. 
     
     
         18 . A formulation comprising 17.5 mg of rofecoxib, or a pharmaceutically acceptable salt thereof, wherein the formulation achieves a mean plasma AUC 0-∞  of more than 3000 h*ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         19 . The formulation of  claim 18 , wherein the formulation achieves a mean C max  plasma concentration of more than 167 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         20 . The formulation of  claim 19 , wherein the formulation achieves a mean C max  plasma concentration of more than 180 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         21 . The formulation of  claim 20 , wherein the formulation achieves a mean C max  plasma concentration of more than 190 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         22 . The formulation of  claim 21 , wherein the formulation achieves a mean C max  plasma concentration of more than 200 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         23 . The formulation of  claim 22 , wherein the formulation achieves a mean C max  plasma concentration of about 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         24 . The formulation of  claim 18 , wherein the formulation achieves a mean C max  plasma concentration within 80-125% of 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         25 . The formulation of  claim 18 , wherein the formulation achieves a higher mean plasma C max  and a higher mean plasma AUC 0-∞  in a population of healthy female adults less than 65 years of age compared to a population of healthy male adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         26 . The formulation of  claim 18 , wherein the formulation achieves a higher mean plasma AUC 0-∞  in Caucasian adults less than 65 years of age compared to healthy African American adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         27 . The formulation of  claim 18 , wherein the formulation achieves an arithmetic mean plasma concentration of at least 2.0 ng/ml at 15 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         28 . The formulation of  claim 18 , wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         29 . The formulation of  claim 18 , wherein the formulation is a liquid dosage form. 
     
     
         30 . The formulation of  claim 29 , wherein the liquid dosage form is a solution. 
     
     
         31 . The formulation of  claim 29 , wherein the liquid dosage form is a suspension. 
     
     
         32 . The formulation of  claim 29 , wherein the liquid dosage form is a syrup. 
     
     
         33 . The formulation of  claim 18 , wherein the formulation is a tablet formulation. 
     
     
         34 . The formulation of  claim 33 , wherein the formulation further comprises a disintegrant. 
     
     
         35 . The formulation of  claim 33 , wherein the rofecoxib has a d90 particle size in the range of about 10 μm to about 12 μm, a d50 particle size in the range of about 3 μm to about 4 μm, and a d10 particle size in the range of about 0.5 μm to about 1.0 μm. 
     
     
         36 . A formulation comprising 17.5 mg of rofecoxib, or a pharmaceutically acceptable salt thereof, wherein the formulation achieves an arithmetic mean plasma concentration of at least 2.0 ng/ml at 15 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         37 . The formulation of  claim 36 , wherein the formulation achieves an arithmetic mean plasma concentration of at least 79 ng/ml at 45 minutes following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         38 . The formulation of  claim 36 , wherein the formulation achieves a mean C max  plasma concentration of more than 167 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         39 . The formulation of  claim 38 , wherein the formulation achieves a mean C max  plasma concentration of more than 180 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         40 . The formulation of  claim 39 , wherein the formulation achieves a mean C max  plasma concentration of more than 190 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         41 . The formulation of  claim 40 , wherein the formulation achieves a mean C max  plasma concentration of more than 200 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         42 . The formulation of  claim 41 , wherein the formulation achieves a mean C max  plasma concentration of about 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         43 . The formulation of  claim 36 , wherein the formulation achieves a mean C max  plasma concentration within 80-125% of 224 ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         44 . The formulation of  claim 36 , wherein the formulation achieves a mean plasma AUC 0-∞  of more than 3000 h*ng/ml following oral administration of a single dose of the formulation to a population of healthy adults less than 65 years of age. 
     
     
         45 . The formulation of  claim 36 , wherein the formulation achieves a higher mean plasma C max  and a higher mean plasma AUC 0-∞  in a population of healthy female adults less than 65 years of age compared to a population of healthy male adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         46 . The formulation of  claim 36 , wherein the formulation achieves a higher mean plasma AUC 0-∞  in Caucasian adults less than 65 years of age compared to healthy African American adults less than 65 years of age following oral administration of a single dose of the formulation. 
     
     
         47 . The formulation of  claim 36 , wherein the formulation is a liquid dosage form. 
     
     
         48 . The formulation of  claim 47 , wherein the liquid dosage form is a solution. 
     
     
         49 . The formulation of  claim 47 , wherein the liquid dosage form is a suspension. 
     
     
         50 . The formulation of  claim 47 , wherein the liquid dosage form is a syrup. 
     
     
         51 . The formulation of  claim 36 , wherein the formulation is a tablet formulation. 
     
     
         52 . The formulation of  claim 51 , wherein the formulation further comprises a disintegrant. 
     
     
         53 . The formulation of  claim 51 , wherein the rofecoxib has a d90 particle size in the range of about 10 μm to about 12 μm, a d50 particle size in the range of about 3 μm to about 4 μm, and a d10 particle size in the range of about 0.5 μm to about 1.0 μm.

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