Controlled release formulation for treating COPD

A method for preventive treatment of a mammal at risk of developing a disease wherein the prevention can be effected by administering a PDE4 inhibitor wherein the effective amount of said PDE4 inhibitor causes adverse events at a particular useful concentration when administered as an immediate-release oral preparation, the method comprising administering said inhibitor as a pharmaceutically acceptable, controlled release formulation which contains an amount of said inhibitor equal to or greater than that of said concentration of the inhibitor which causes said adverse events when administered as an immediate-release oral preparation, and which contains an amount which has a prophylactic effect for up to 24 hours post administration.

A method of administering a PDE4 inhibitor in a therapeutically effective, non-adverse event causing amount, wherein said inhibitor when administered in that amount would cause adverse events if administered as an immediate-release oral preparation, which method comprises confecting said inhibitor with at least one pharmaceutically acceptable excipient capable of forming a controlled release formulation and said inhibitor in said amount and administering the formulation to a mammal in need thereof.

An improved method for preventing the onset of or treating a mammal suffering from a diseases which can be treated by inhibiting the PDE 4 enzyme wherein the improvement comprises administering to said mammal a controlled release formulation comprising a PDE4 inhibitor mixed with at least one pharmaceutically acceptable excipient capable of forming a controlled release formulation wherein said formulation has a release profile that provides a therapeutically effective, non-adverse-causing concentration of said inhibitor which is effective for up to about 24 hours.

A stable controlled release pharmaceutical composition comprising a controlled release excipient, dibasic calcium phosphate, a PDE4-specific inhibitor in an amount of 10 mg and 60 mg, optionally other excipients, and between about 0.5-2.0% weight/weight of water.

A process for preparing a pharmaceutically formulation for effectively treating inflammation in a mammal with a PDE4 inhibitor while avoiding adverse events, the process comprising mixing a pharmaceutically acceptable excipient capable of forming a controlled-release formulation with a therapeutically effective amount of a PDE4 inhibitor, which amount if administered as an immediate release preparation would clause adverse events.