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Claims for Patent: 7,749,532

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Claims for Patent: 7,749,532

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:10/819,620
Patent Claims: 1. An oral pharmaceutical composition of 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, the composition consisting of (i) an immediate release (IR) portion comprising a drug, wherein the drug consists of about 30 mg doxycycline; (ii) a delayed release (DR) portion comprising a drug, wherein the drug consists of about 10 mg doxycycline, in which the DR portion is in the form of pellets coated with at least one enteric polymer; and (iii) one or more pharmaceutically acceptable excipients.

2. The composition of claim 1 in which the IR portion is in the form of pellets.

3. The composition of claim 2 in which the pellets are contained in a capsule.

4. 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.

5. The composition of claim 1 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.

6. The composition of claim 5 wherein the binder is selected from the group consisting of methylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, and polyvinylpyrrolidone/vinyl acetate copolymer.

7. The composition of claim 5 wherein the disintegration agent is selected from the group consisting of cornstarch, pregelatinized starch, cross-linked carboxymethylcellulose, sodium starch glycolate, and cross-linked polyvinylpyrrolidone.

8. The composition of claim 5 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.

9. The composition of claim 5 wherein the surfactants are selected from the group consisting of sodium lauryl sulfate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, bile salts, and glyceryl monostearate.

10. The composition of claim 5 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.

11. The composition of claim 5 wherein the stabilizers are selected from the group consisting of antioxidation agents, buffers, and acids.

12. The composition of claim 1 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; therefor combinations thereof.

13. The oral pharmaceutical composition of claim 2, wherein the pellets of the IR portion constitute about 80 percent to about 70 percent of the total pellets in the composition.

14. The oral pharmaceutical composition of claim 13, wherein the pellets of the IR portion constitute about 75 percent of the total pellets in the composition.

15. A method for treating rosacea in a mammal in need thereof, comprising administering to the mammal a daily dose of an oral pharmaceutical composition of 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, the composition consisting of (i) an immediate release (IR) portion comprising a drug, wherein the drug consists of about 30 mg doxycycline; (ii) a delayed release (DR) portion comprising a drug, wherein the drug consists of about 10 mg doxycycline, in which the DR portion is in the form of pellets coated with at least one enteric polymer; and (iii) one or more pharmaceutically acceptable excipients.

16. The method of claim 15, wherein the mammal is a human.

17. The method of claim 15, wherein the pellets of the composition are contained in a capsule.

18. The method of claim 15, 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.

19. The method of claim 15, wherein the one or more pharmaceutically acceptable excipients of the composition is a binder, a disintegration agent, a filling agent, a surfactant, a solubilizer, a stabilizer, and combinations thereof.

20. A process for preparing an oral pharmaceutical composition, 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, consisting of combining (i) an immediate release (IR) portion comprising a drug, wherein the drug consists of about 30 mg doxycycline; (ii) a delayed release (DR) portion comprising a drug, wherein the drug consists of about 10 mg doxycycline, in which the DR portion is in the form of pellets coated with at least one enteric polymer; and (iii) one or more pharmaceutically acceptable excipients.

21. The process of claim 20 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.
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