Doxycycline Formulations, and Methods of Treating Rosacea

A method for treating papules and pustules of rosacea in a human in need thereof, comprising orally administering a once a day dose of a pharmaceutical composition to the human, the pharmaceutical composition comprising:

• a capsule, wherein the capsule is coated with a delayed release layer;
• wherein the delayed release layer comprises about 4 to 6 mg of doxycycline, or a pharmaceutically acceptable salt thereof, and a binding agent, and wherein the delayed release layer is coated with an enteric coating;
• wherein the enteric coating dissolves at pH of about 5 to 6, and wherein the enteric coating is coated with an immediate release layer;
• wherein the immediate release layer comprises about 32 mg of doxycycline, or a pharmaceutically acceptable salt thereof, and a binding agent,
• wherein the relative mean Cmax of the pharmaceutical composition is within 80.00% to 125.00% of a Cmax value of 510±220.7 ng/mL, after administration of a single dose of the pharmaceutical composition to humans in a fasting state;
• and
• wherein the relative mean AUC(0-∞) of the pharmaceutical composition is within 80.00% to 125.00% of a AUC(0-∞) value of 9227±3212.8 ng·hr/mL, after administration of a single dose of the pharmaceutical composition to humans in a fasting state.

A pharmaceutical composition in unit dose form for orally delivering doxycycline to a human, the pharmaceutical composition comprising:

• a capsule, wherein the capsule is coated with a delayed release layer;
• wherein the delayed release layer comprises about 4 to 6 mg of doxycycline, or a pharmaceutically acceptable salt thereof, and a binding agent, and wherein the delayed release layer is coated with an enteric coating;
• wherein the enteric coating dissolves at pH of about 5 to 6, and wherein the enteric coating is coated with an immediate release layer;
• wherein the immediate release layer comprises about 32 mg of doxycycline, or a pharmaceutically acceptable salt thereof;
• and wherein after administration of a single dose to humans in a fasting state, the Cmax has a range of about 230 ng/mL to about 1120 ng/mL, and the AUC(0-∞) has a range of about 4800 ng·hr/mL to about 15,600 ng·hr/mL.