US2004208934A1PendingUtilityA1

Inorganic-polymer complexes for the controlled release of compounds including medicinals

65
Assignee: ROYER BIOMEDICAL INCPriority: Sep 22, 1997Filed: May 5, 2004Published: Oct 21, 2004
Est. expirySep 22, 2017(expired)· nominal 20-yr term from priority
A61K 47/56A61K 9/0019A61K 9/0014A61K 9/1652A61K 47/36A61K 47/58A61K 47/02
65
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Claims

Abstract

The production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals are disclosed. Advantageously, the inorganic used is calcium sulfate.

Claims

exact text as granted — not AI-modified
1 - 67 . (Canceled)  
     
     
         68 . A solid composition for the controlled release of an active agent comprising an active agent and a matrix polymer dispersed throughout a solid calcium phosphate matrix, wherein said composition is the hydration reaction product of a mixture comprised of: 
 a) the active agent,    b) calcium phosphate, and    c) a matrix polymer and/or complexing agent which slows the release of said active agent from said solid matrix.    
     
     
         69 . A solid composition as in  claim 68  wherein said composition is in the form of a bead, wafer, tablet, sphere, granule or cylinder.  
     
     
         70 . A solid composition as in  claim 68  wherein the matrix polymer is selected from the group consisting of hyaluronic acid, dextran, and protein.  
     
     
         71 . A solid composition as in  claim 68  wherein the matrix polymer is selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, polyvinylalcohol, starch, zanthan, cellulose and cellulose derivatives.  
     
     
         72 . A solid composition as in  claim 68  wherein the complexing agent is selected from the group consisting of dextran sulfate, chondroitin sulfate, polyglutamic acid, polyaspartic acid, polynucleotides, a cationic polypeptide,cyclodextrin, pentosan polysulfate, cyclodextrins, polyoxyethylene alcohol, ester or ether, and defatted albumin.  
     
     
         73 . A solid composition for the controlled release of an active agent comprising: 
 (a) an active agent;    (b) calcium sulfate or phosphate; and    (c) a matrix polymer which slows the release of said active agent, wherein said composition is a solid matrix due to hydration of calcium sulfate or phosphate in an aqueous mixture of said active agent, said matrix polymer and said calcium sulfate or phosphate, and wherein    said composition is in the form of a bead, wafer, tablet, sphere granule or cylinder.    
     
     
         74 . A solid composition for the controlled release of an active agent consisting of: 
 (a) an active agent;    (b) calcium sulfate or phosphate; and    (c) a matrix polymer which slows the release of said active agent, wherein    said composition is a solid matrix due to hydration of calcium sulfate or phosphate in an aqueous mixture of said active agent, said matrix polymer and said calcium sulfate or phosphate.    
     
     
         75 . A solid composition for the controlled release of an active agent comprising: 
 (a) an active agent;    (b) calcium sulfate or phosphate; and    (c) polyethylene glycol, wherein    said composition is a solid matrix due to hydration of calcium sulfate or phosphate in an aqueous mixture of said active agent, said polyethylene glycol and said calcium sulfate or phosphate.    
     
     
         76 . A solid composition for the controlled release of an active agent comprising: 
 (a) an active agent;    (b) calcium sulfate or phosphate; and    (c) dextran sulfate, wherein    said composition is a solid matrix due to hydration of calcium sulfate or phosphate in an aqueous mixture of said active agent, said dextran sulfate and said calcium sulfate or phosphate.    
     
     
         77 . A solid composition for the controlled release of an active agent comprising an active agent which is dispersed throughout a solid matrix reaction product of an aqueous mixture comprised of: 
 (a) an active agent,    (b) calcium sulfate or phosphate,    (c) a matrix polymer in an amount sufficient to slow the release of said active agent, and    (d) water in an amount sufficient to form a solid matrix due to the hydration of said calcium sulfate or phosphate, wherein    said composition is in the form of a bead, wafer, tablet, sphere, granule or cylinder.    
     
     
         78 . A solid composition for the controlled release of an active agent comprising: 
 (a) an active agent;    (b) calcium sulfate or phosphate;    (c) a matrix polymer which slows the release of said active agent, and    (d) a salt of a fatty acid; wherein    said composition is a solid matrix due to hydration of calcium sulfate or phosphate in an aqueous mixture of said active agent, said matrix polymer and said calcium sulfate or phosphate.    
     
     
         79 . A solid composition for the controlled release of an active agent comprising an active agent which is dispersed throughout a solid matrix reaction product of an aqueous mixture comprised of: 
 (a) an active agent,    (b) calcium sulfate or phosphate,    (c) a matrix polymer in an amount sufficient to slow the release of said active agent,    (d) water in an amount sufficient to form a solid matrix due to the hydration of said calcium sulfate or phosphate, and    (e) a salt of a fatty acid.    
     
     
         80 . The solid composition of any one of claims  78 - 79 , wherein said salt of a fatty acid comprises calcium stearate.  
     
     
         81 . A method of producing sustained release of an active agent in a mammal comprising administering to said mammal a solid composition comprising an active agent which is dispersed throughout a solid matrix reaction product of an aqueous mixture comprised of a) active agent, b) calcium phosphate, c) a matrix polymer, and/or a complexing agent.  
     
     
         82 . A method as in  claim 81  wherein said active agent is an antiinfective.  
     
     
         83 . A method as in  claim 82 , further comprising a chondroprotective agent.  
     
     
         84 . A method as in  claim 81  wherein said active agent is an antineoplastic agent.  
     
     
         85 . A method as in  claim 81 , wherein said active agent is an antiinflammatory agent.  
     
     
         86 . A method of scaffolding bone or filling a defect in bone comprising administering to said bone a composition comprising: calcium phosphate; and a matrix polymer and/or complexing agent which slows the release of said active agent, wherein said composition becomes a solid matrix due to hydration of calcium phosphate in an aqueous mixture of said active agent, said matrix polymer and/or complexing agent and said calcium phosphate.  
     
     
         87 . A method as in any one of claims  81 - 86 , wherein the solid matrix further comprises a salt of a fatty acid.  
     
     
         88 . A method as in  claim 87 , wherein the salt of a fatty acid comprises calcium stearate.

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