US2016113880A1PendingUtilityA1

Once Daily Formulations of Tetracyclines

Assignee: TCD ROYALTY SUB LLCPriority: Apr 7, 2003Filed: Jun 2, 2015Published: Apr 28, 2016

Est. expiryApr 7, 2023(expired)· nominal 20-yr term from priority

Inventors:Rong-Kun Chang Arash Raoufinia Niraj Shah

A61P 3/10A61P 5/18A61P 43/00A61P 27/04A61P 29/00A61P 27/02A61P 31/04A61P 19/00A61P 17/02A61P 17/10A61P 17/08A61P 17/00A61P 19/02A61P 1/02A61K 9/5078A61K 9/2027A61K 9/2054A61K 9/5084A61K 9/167A61K 31/65A61K 9/4808A61K 9/209

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References

Claims

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.

Claims

exact text as granted — not AI-modified

What is claimed is: 
     
         1 . An oral pharmaceutical composition containing a tetracycline, which at a once-daily dosage will give steady state blood levels of the tetracycline of a minimum of about 0.1 μg/ml and a maximum of about 1.0 μg/ml. 
     
     
         2 . The composition of  claim 1 , which at a once-daily dosage will give steady state blood levels of the tetracycline of between about 0.3 μg/ml to about 0.8 μg/ml. 
     
     
         3 . The composition of  claim 1 , wherein the tetracycline is doxycycline. 
     
     
         4 . The composition of  claim 3 , wherein between 50 mg. and 25 mg. doxycycline is present. 
     
     
         5 . The composition of  claim 3 , wherein about 40 mg. doxycycline is present. 
     
     
         6 . The composition of  claim 4 , which is an immediate release formulation. 
     
     
         7 . The composition of  claim 5 , which is an immediate release formulation. 
     
     
         8 . The composition of  claim 1 , which is a combination of a component containing a tetracycline in an immediate release (IR) formulation and a second component containing a tetracycline in a delayed release (DR) formulation, wherein the ratio of IR to DR is from about 99:1 to about 70:30. 
     
     
         9 . The composition of  claim 8 , wherein the tetracycline is doxycycline. 
     
     
         10 . The composition of  claim 9 , wherein the ratio of immediate release component to delayed release component is from about 80:20 to about 70:30. 
     
     
         11 . The composition of  claim 9 , wherein the ratio of immediate release component to delayed release component is 75:25. 
     
     
         12 . The composition of  claim 1 , which is in the form of a granule, tablet, pellet, powder, sachet, capsule, gel, dispersion or suspension. 
     
     
         13 . The composition of  claim 12 , which is in a dosage form of a combination of pellets, wherein a portion of the pellets are of an immediate release formulation and the remaining pellets are of a delayed release formulation. 
     
     
         14 . The composition of  claim 13 , wherein the pellets are contained in a capsule. 
     
     
         15 . The composition of  claim 9 , wherein the IR and DR components are compressed into a tablet. 
     
     
         16 . The composition of  claim 15 , which is a layered tablet, wherein one layer contains the DR component and another layer contains the IR component. 
     
     
         17 . The composition of  claim 12 , which is a layered pellet, wherein the DR portion comprises the core of the pellet, and the IR portion surrounds the core. 
     
     
         18 . An oral pharmaceutical dosage form containing between 25 and 50 mg. of a tetracycline. 
     
     
         19 . The dosage form of  claim 18 , wherein the tetracycline is doxycycline. 
     
     
         20 . The dosage form of  claim 19 , which contains about 40 mg. of doxycycline. 
     
     
         21 . The dosage form of  claim 18 , which is in an immediate release formulation. 
     
     
         22 . The dosage form of  claim 18 , which is a granule, tablet, pellet, powder, sachet, capsule, gel, dispersion or suspension. 
     
     
         23 . The dosage form of  claim 19 , which is a tablet containing the doxycycline with pharmaceutically acceptable excipient(s). 
     
     
         24 . The dosage form of  claim 19 , which is a capsule containing pellets of doxycycline with pharmaceutically acceptable excipient(s). 
     
     
         25 . The dosage form of  claim 19 , wherein a portion thereof is of a delayed release formulation, and another portion is of an immediate release formulation. 
     
     
         26 . A method for treating a collagenase dependent disease or condition, and/or acute or chronic inflammatory condition in a mammal, comprising administering a daily dose of a tetracycline composition according to  claim 1  to the mammal, for at least a time sufficient to ameliorate the disease or condition. 
     
     
         27 . The method of  claim 26 , wherein the mammal is a human. 
     
     
         28 . The method of  claim 26 , wherein the disease or condition is selected from periodontal disease, rosacea, acne, dry eye, rheumatoid arthritis, hyperparathyroidism, and diabetes. 
     
     
         29 . The method of  claim 28 , wherein the disease is periodontal disease. 
     
     
         30 . The method of  claim 29 , wherein the tetracycline is doxycycline. 
     
     
         31 . The method of  claim 28 , wherein the condition is rosacea. 
     
     
         32 . The method of  claim 31 , wherein the tetracycline is doxycycline. 
     
     
         33 . The method of  claim 28 , wherein the condition is dry eye. 
     
     
         34 . The method of  claim 33 , wherein the tetracycline is doxycycline. 
     
     
         35 . The method of  claim 30 , wherein between 50 mg. and 25 mg. doxycycline is present in the composition. 
     
     
         36 . The method of  claim 35 , wherein about 40 mg. doxycycline is present in the composition. 
     
     
         37 . The method of  claim 30 , which is an immediate release composition. 
     
     
         38 . The method of  claim 30 , wherein the composition is in the form of a dosage unit that contains an immediate release portion and a delayed release portion. 
     
     
         39 . The method of  claim 32 , wherein between 50 mg. and 25 mg. doxycycline is present in the composition. 
     
     
         40 . The method of  claim 39 , wherein about 40 mg. doxycycline is present in the composition. 
     
     
         41 . The method of  claim 32 , which is an immediate release composition. 
     
     
         42 . The method of  claim 32 , wherein the composition is in the form of a dosage unit that contains an immediate release portion and a delayed release portion. 
     
     
         43 . The method of  claim 34 , wherein between 50 mg. and 25 mg. doxycycline is present in the composition. 
     
     
         44 . The method of  claim 43 , wherein about 40 mg. doxycycline is present in the composition. 
     
     
         45 . The method of  claim 34 , which is an immediate release composition. 
     
     
         46 . The method of  claim 34 , wherein the composition is in the form of a dosage unit that contains an immediate release portion and a delayed release portion. 
     
     
         47 . A process for preparing a once-daily oral pharmaceutical composition containing a tetracycline, which will give steady state blood levels of the tetracycline of a minimum of about 0.1 μg/ml and a maximum of about 1.0 μg/ml, comprising combining between 50 mg. and 25 mg. doxycycline with orally pharmaceutically acceptable excipients. 
     
     
         48 . The process of  claim 41 , wherein the tetracycline is doxycycline.

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