US2021137878A1PendingUtilityA1

Novel dosage forms of rofecoxib and related methods

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Assignee: TREMEAU PHARMACEUTICALS INCPriority: Nov 13, 2019Filed: Dec 18, 2020Published: May 13, 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 9/16A61K 31/365
67
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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
1 - 30 . (canceled) 
     
     
         31 . A solid dosage 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. 
     
     
         32 . The solid dosage formulation of  claim 31 , 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. 
     
     
         33 . The solid dosage formulation of  claim 32 , 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. 
     
     
         34 . The solid dosage formulation of  claim 33 , 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. 
     
     
         35 . The solid dosage formulation of  claim 31 , 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. 
     
     
         36 . The solid dosage formulation of  claim 31 , 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. 
     
     
         37 . The solid dosage formulation of  claim 31 , 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. 
     
     
         38 . The solid dosage formulation of  claim 31 , 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. 
     
     
         39 . The solid dosage formulation of  claim 31 , 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. 
     
     
         40 . The solid dosage formulation of  claim 31 , 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. 
     
     
         41 . The solid dosage formulation of  claim 31 , wherein the solid dosage formulation further comprises a disintegrant. 
     
     
         42 . The solid dosage formulation of  claim 31 , 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. 
     
     
         43 . A solid dosage 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. 
     
     
         44 . The solid dosage formulation of  claim 43 , 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. 
     
     
         45 . The solid dosage formulation of  claim 44 , 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. 
     
     
         46 . The solid dosage formulation of  claim 43 , 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. 
     
     
         47 . The solid dosage formulation of  claim 43 , 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. 
     
     
         48 . The solid dosage formulation of  claim 43 , 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. 
     
     
         49 . The solid dosage formulation of  claim 43 , 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. 
     
     
         50 . The solid dosage formulation of  claim 43 , 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. 
     
     
         51 . The solid dosage formulation of  claim 43 , wherein the solid dosage formulation further comprises a disintegrant. 
     
     
         52 . The solid dosage formulation of  claim 43 , 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. 
     
     
         53 . A solid dosage 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. 
     
     
         54 . The solid dosage formulation of  claim 53 , 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. 
     
     
         55 . The solid dosage formulation of  claim 53 , 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. 
     
     
         56 . The solid dosage formulation of  claim 53 , 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. 
     
     
         57 . The solid dosage formulation of  claim 53 , 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. 
     
     
         58 . The solid dosage formulation of  claim 53 , 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. 
     
     
         59 . The solid dosage formulation of  claim 53 , wherein the solid dosage formulation further comprises a disintegrant. 
     
     
         60 . The solid dosage formulation of  claim 53 , 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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