Patent EA-003639-B1 (EA)
Title: Valdecoxib compositions
Inventor: NADKARNI SREEKANT
IPC: A61K31/42
Filed: 2000-12-06
Abstract: 1. A pharmaceutical composition comprising particulate valdecoxib in an amount of about 1 mg to about 100 mg per dose and one or more pharmaceutically acceptable excipients, wherein a single dose, upon oral administration to a fasting subject, provides a time course of blood serum concentration of valdecoxib having at least one of (a) a time to reach a threshold concentration for therapeutic effect not greater than about 0.5 h after administration; (b) a time to reach maximum concentration (Tmax) not greater than about 3 h after administration; and (c) a maximum concentration (Cmax) not less than about 100 ng/ml. 2. The composition of Claim 1 wherein the threshold concentration for therapeutic effect is about 20 ng/ml. 3. The composition of Claim 2 wherein a single dose, upon oral administration to a fasting subject, provides a time course of blood serum concentration of valdecoxib having each of (a) a time to reach a concentration of 20 ng/ml not greater than about 0.5 h after administration; (b) a time to reach maximum concentration (Tmax) not greater than about 3 h after administration; and (c) a maximum concentration (Cmax) not less than about 100 ng/ml. 4. The composition of Claim 1 wherein the valdecoxib is in an amount of about 5 mg to about 40 mg per dose. 5. The composition of any of Claims 1 to 4 that is a tablet wherein the excipients comprise one or more diluents in an amount of about 5% to about 99%, one or more disintegrants in an amount of about 0.2% to about 30%, one or more binding agents in an amount of about 0.5% to about 25%, and one or more lubricants in an amount of about 0.1 % to about 10%, by weight of the composition. 6. The composition of Claim 5 wherein the binding agent is pregelatinized starch. 7. The composition of any of Claims 1 to 4 that is a tablet wherein the excipients comprise lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, pregelatinized starch and magnesium stearate. 8. The composition of Claim 1 further comprising one or more opioid or analgesic drugs. 9. The composition of any of Claims 1 to 8 wherein Dgo of the valdecoxib particles is less than about 75 mum. 10. The composition of any of Claims 1 to 8 wherein the valdecoxib particles have a weight average particle size of about 1 mum to about 10 mum. 11. The composition of any of Claims 1 to 8 wherein the valdecoxib particles have a weight average particle size of about 10 mum to about 1000 mum. 12. A method of preparing a composition of any of Claims 5 to 7 comprising a step of wet granulating valdecoxib together with one or more diluents and a binding agent, drying the resulting granules and compressing the resulting dry granulate to form a tablet. 13. A method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising orally administering to the subject a composition of any of Claims 1 to 12 once or twice a day. 14. A method of use of a composition of any of Claims 1 to 12 in manufacturing a medicament for treatment or prophylaxis of a cyclooxygenase-2 mediated disorder in a subject in need thereof.