US2007141162A1PendingUtilityA1

Injectable compositions for the controlled delivery of pharmacologically active compound

59
Individually held — no corporate assignee on recordPriority: Oct 19, 2001Filed: Jan 31, 2007Published: Jun 21, 2007
Est. expiryOct 19, 2021(expired)· nominal 20-yr term from priority
Inventors:Yerramilli V. S. N. MurthyRobert Suva
A61P 9/10A61P 9/00A61P 9/12A61P 9/06A61P 25/00A61P 25/22A61P 31/04A61P 31/10A61P 31/00A61P 23/02A61K 9/0019A61K 47/12A61K 31/496A61K 31/65A61K 47/10A61K 47/14A61K 47/26A61K 47/20A61K 31/7034A61K 31/24A61K 31/7048A61K 9/0024A61K 47/22A61K 31/00
59
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Claims

Abstract

The present invention provides compositions and methods for extending the release times and lowering the toxicity of pharmacologically active compounds. The compounds comprise a salt of the pharmacologically active compound with a lipophilic counterion and a pharmaceutically acceptable water soluble solvent combined together to form an injectable composition. The lipophilic counterion may be a saturated or unsaturated C 8 -C 22 fatty acid, and preferably may be a saturated or unsaturated C 10 -C 18 fatty acid. When injected into a mammal, at least a portion of the composition precipitates and releases the active compound over time. Thus, the composition forms a slowly releasing drug depot of the active compound in the mammal. Therefore, the present invention enables one to provide a controlled dose administration of the active compound for a periods of up to 15 days or even longer. Many compounds can be administered according to the present invention including, but not limited to, tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and turbinafine.

Claims

exact text as granted — not AI-modified
1 - 64 . (canceled)  
   
   
       65 . A pharmaceutical composition comprising 
 (i) a salt comprising roxithromycin and a lipophilic counterion and    (ii) a pharmaceutically acceptable solvent,    wherein the salt and the solvent form a solution and wherein at least a portion of the salt precipitates when the composition is injected into water.    
   
   
       66 . The composition of  claim 65 , wherein the composition releases the roxithromycin over time when injected into a mammal.  
   
   
       67 . The composition of  claim 65 , wherein the composition is injectable.  
   
   
       68 . The composition of  claim 65 , wherein the lipophilic counterion is a fatty acid.  
   
   
       69 . The composition of  claim 68 , wherein the fatty acid is a saturated or unsaturated C8-C 22  fatty acid.  
   
   
       70 . The composition of  claim 69 , wherein the fatty acid is a saturated or unsaturated C10-C 18  fatty acid.  
   
   
       71 . The composition of  claim 70 , wherein the fatty acid is selected from the group consisting of lauric acid, linoleic acid, decanoic acid, and myristic acid.  
   
   
       72 . The composition of  claim 65 , wherein the lipophilic counterion is a dicarboxylic acid or polycarboxylic acid.  
   
   
       73 . The composition of  claim 72 , wherein the dicarboxylic acid or polycarboxylic acid is selected from the group consisting of polyaspartic acid, polyacrylic acid, sebacic acid, polysebacic acid, and polybenzoic acid.  
   
   
       74 . The composition of  claim 71 , wherein the fatty acid is lauric acid.  
   
   
       75 . The composition of  claim 74 , wherein the pharmaceutically acceptable solvent comprises about 90% glycerol formal and about 10% propylene glycol.  
   
   
       76 . The composition of  claim 65 , wherein the pharmaceutically acceptable solvent is selected from the group consisting of pyrrolidone, N-methyl pyrrolidone, polyethylene glycol, propylene glycol, glycerol formal, isosorbid dimethyl ether, ethanol, dimethyl sulfoxide, tetrahydrofufuryl alcohol, triacetin, and combinations thereof.  
   
   
       77 . The composition of  claim 76 , wherein the pharmaceutically acceptable solvent comprises about 90% glycerol formal and about 10% propylene glycol.  
   
   
       78 . The composition of  claim 76 , wherein the pharmaceutically acceptable solvent comprises N-methyl pyrrolidone.  
   
   
       79 . The composition of  claim 65 , wherein the roxithromycin is present in an amount of about 10 to 60 percent (w/v) of the composition.  
   
   
       80 . The composition of  claim 65 , wherein the roxithromycin is present in an amount of at least about 1 percent (w/v) of the composition.  
   
   
       81 . The composition of  claim 65 , wherein the roxithromycin is present in an amount of at least about 5 percent (w/v) of the composition.  
   
   
       82 . A method of providing a pharmacologically acceptable level of roxithromycin in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 65 .  
   
   
       83 . The method of  claim 82 , wherein injecting the composition provides a drug depot in the mammal.  
   
   
       84 . The method of  claim 83 , wherein the drug depot provides sustained release of the roxithromycin.  
   
   
       85 . The method of  claim 84 , wherein the drug depot provides extended release of the roxithromycin to provide a pharmacologically acceptable level of roxithromycin for between 1 and 15 days.  
   
   
       86 . The method of  claim 82 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       87 . The method of  claim 86 , wherein the mammal is a cat.  
   
   
       88 . A method of providing a pharmacologically acceptable level of roxithromycin in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 68 .  
   
   
       89 . The method of  claim 88 , wherein injecting the composition provides a drug depot in the mammal.  
   
   
       90 . The method of  claim 89 , wherein the drug depot provides sustained release of the roxithromycin.  
   
   
       91 . The method of  claim 90 , wherein the drug depot provides extended release of the roxithromyein to provide a pharmacologically acceptable level of roxithromycin for between 1 and 15 days.  
   
   
       92 . The method of  claim 88 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       93 . The method of  claim 92 , wherein the mammal is a cat.  
   
   
       94 . A method of providing a pharmacologically acceptable level of roxithromycin in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 74 .  
   
   
       95 . The method of  claim 94 , wherein injecting the composition provides a drug depot in the mammal.  
   
   
       96 . The method of  claim 95 , wherein the drug depot provides sustained release of the roxithromycin.  
   
   
       97 . The method of  claim 96 , wherein the drug depot provides extended release of the roxithromycin to provide a pharmacologically acceptable level of roxithromycin for between 1 and 15 days.  
   
   
       98 . The method of  claim 94 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       99 . The method of  claim 98 , wherein the mammal is a cat.  
   
   
       100 . A method of providing a pharmacologically acceptable level of roxithromycin in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 75 .  
   
   
       101 . The method of  claim 100 , wherein injecting the composition provides a drug depot in the mammal.  
   
   
       102 . The method of  claim 101 , wherein the drug depot provides sustained release of the roxithromycin.  
   
   
       103 . The method of  claim 102 , wherein the drug depot provides extended release of the roxithromycin to provide a pharmacologically acceptable level of roxithromycin for between 1 and 15 days.  
   
   
       104 . The method of  claim 100 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       105 . The method of  claim 104 , wherein the mammal is a cat.  
   
   
       106 . A method of treating a bacterial infection in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 65 .  
   
   
       107 . The method of  claim 106 , wherein the bacterial infection is a respiratory infection.  
   
   
       108 . The method of  claim 106 , wherein a single administration of the composition is administered to treat the bacterial infection.  
   
   
       109 . The method of  claim 106 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       110 . The method of  claim 109 , wherein the mammal is a cat.  
   
   
       111 . A method of treating a bacterial infection in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 68 .  
   
   
       112 . The method of  claim 111 , wherein the bacterial infection is a respiratory infection.  
   
   
       113 . The method of  claim 111 , wherein a single administration of the composition is administered to treat the bacterial infection.  
   
   
       114 . The method of  claim 111 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       115 . The method of  claim 114 , wherein the mammal is a cat.  
   
   
       116 . A method of treating a bacterial infection in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 74 .  
   
   
       117 . The method of  claim 116 , wherein the bacterial infection is a respiratory infection.  
   
   
       118 . The method of  claim 116 , wherein a single administration of the composition is administered to treat the bacterial infection.  
   
   
       119 . The method of  claim 116 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       120 . The method of  claim 119 , wherein the mammal is a cat.  
   
   
       121 . A method of treating a bacterial infection in a mammal comprising injecting the mammal with the pharmaceutical composition of  claim 75 .  
   
   
       122 . The method of  claim 121 , wherein the bacterial infection is a respiratory infection.  
   
   
       123 . The method of  claim 121 , wherein a single administration of the composition is administered to treat the bacterial infection.  
   
   
       124 . The method of  claim 121 , wherein the mammal is a dog, cat, horse, or pig.  
   
   
       125 . The method of  claim 124 , wherein the mammal is a cat.

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