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Claims for Patent: 8,394,405

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Claims for Patent: 8,394,405

Title:Once daily formulations of tetracyclines
Abstract: Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.
Inventor(s): Chang; Rong-Kun (Rockville, MD), Raoufinia; Arash (Springfield, VA), Shah; Niraj (Owings Mills, MD)
Assignee: Supernus Pharmaceuticals, Inc. (Rockville, MD)
Application Number:12/926,932
Patent Claims: 1. An oral pharmaceutical composition comprising about 40 mg of total doxycycline, which at a once-daily dosage will give steady state blood levels of doxycycline of a minimum of 0.1 .mu.g/ml and a maximum of 1.0 .mu.g/ml, wherein the composition consists of 70 to 80 percent of the doxycycline formulated as an immediate release (IR) formulation and 20 to 30 percent of the doxycycline formulated as a delayed release (DR) formulation.

2. The composition of claim 1, which at a once-daily dosage will give steady state blood levels of the doxycycline of between 0.3 .mu.g/ml to 0.8 .mu.g/ml.

3. The composition of claim 1, wherein the ratio of IR to DR is 75:25.

4. The composition of claim 1, which is in the form of a granule, tablet, pellet, powder, sachet, capsule, gel, dispersion or suspension.

5. The composition of claim 1, which is in a dosage form of a combination of pellets.

6. The composition according to claim 1, wherein the DR formulation comprises at least one enteric polymer.

7. The composition of claim 6, wherein the enteric polymer is cellulose acetate phthalate; hydroxypropyl methylcellulose phthalate; polyvinyl acetate phthalate; hydroxypropyl methylcellulose acetate succinate; cellulose acetate trimellitate; hydroxypropyl methylcellulose succinate; cellulose acetate succinate; cellulose acetate hexahydrophthalate; cellulose propionate phthalate; a copolymer of methylmethacrylic acid and methyl methacrylate; a copolymer of methyl acrylate, methylmethacrylate and methacrylic acid; a copolymer of methylvinyl ether and maleic anhydride; ethyl methyacrylate-methylmethacrylate-chlorotrimethylammonium ethyl acrylate copolymer; zein; shellac; poly(methacylic acid-co-ethyl acrylate) 1:1, or combinations thereof.

8. The composition according to claim 1, wherein the DR formulation is in the form of granules, pellets, or tablet.

9. The composition according to claim 1, wherein one or more pharmaceutically acceptable excipients is incorporated in the IR formulation, the DR formulation, or both.

10. The composition of claim 9, wherein the one or more pharmaceutically acceptable excipients is a binder, a disintegration agent, a filling agent, a surfactant, a solubilizer, a stabilizer, and combinations thereof.

11. The composition of claim 10, wherein the binder is selected from the group consisting of methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, and polyvinylpyrrolidone/vinyl acetate copolymer.

12. The composition of claim 10, wherein the disintegration agent is selected from the group consisting of cornstarch, pregelatinized starch, cross-linked carboxymethylcellulose, sodium starch glycolate, and cross-linked polyvinylpyrrolidone.

13. The composition of claim 10, wherein the filling agents are selected from the group consisting of lactose, calcium carbonate, calcium phosphate, calcium sulfate, microcrystalline cellulose, dextran, starches, sucrose, xylitol, lactitol, mannitol, sorbitol, sodium chloride, and polyethylene glycol.

14. The composition of claim 10, wherein the surfactants are selected from the group consisting of sodium lauryl sulfate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, bile salts, and glyceryl monostearate.

15. The composition of claim 10, wherein the solubilizers are selected from the group consisting of citric acid, succinic acid, fumaric acid, malic acid, tartaric acid, maleic acid, glutaric acid, sodium bicarbonate, and sodium carbonate.

16. The composition of claim 10, wherein the stabilizers are selected from the group consisting of antioxidation agents, buffers, and acids.

17. A method for treating rosacea in a mammal in need thereof, comprising administering an oral pharmaceutical composition comprising about 40 mg of total doxycycline, which at a once-daily dosage will give steady state blood levels of doxycycline of a minimum of 0.1 .mu.g/ml and a maximum of 1.0 .mu.g/ml, wherein the composition consists of 70 to 80 percent of the doxycycline formulated as an immediate release (IR) formulation and 20 to 30 percent of the doxycycline formulated as a delayed release (DR) formulation.

18. The method of claim 17, wherein the mammal is a human.

19. The method of claim 17, which at a once-daily dosage, administration of the composition will give steady state blood levels of the doxycycline of between 0.3 .mu.g/ml to 0.8 .mu.g/ml.

20. A process for preparing a once-daily oral pharmaceutical composition according to claim 1, the process comprising combining (i) an immediate release (IR) formulation comprising 70 to 80 percent of the total doxycycline with (ii) a delayed release (DR) formulation comprising 20 to 30 percent of the total doxycycline.
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