Compositions having enhanced pharmacokinetic characteristics

Abstract

Compositions comprising a therapeutic component and an efficacy enhancing component that enhances the pharmacokinetic disposition of the therapeutic component is disclosed. In one embodiment, the therapeutic component includes an alpha-2-adrenergic agonist. In another embodiment, the efficacy enhancing components include fatty acids. In a preferred embodiment, the therapeutic component and the efficacy enhancing component forms a complex.

What is claimed is:  
     
         1 . A composition comprising: 
 a therapeutic component in a therapeutically effective amount, and    an efficacy enhancing component in an effective amount to enhance the pharmacokinetic disposition of the therapeutic component; the efficacy enhancing component being selected from the group consisting of anionic polymers, fatty acids, derivatives thereof; the efficacy enhancing component forms a complex with the therapeutic component and mixtures thereof, the complex remaining substantially intact in an aqueous environment.    
     
     
         2 . A composition of  claim 1  wherein the efficacy enhancing component is present in an amount effective to enhance the permeability of the therapeutic component relative to the permeability of the therapeutic component without the efficacy enhancing component.  
     
     
         3 . A composition of  claim 1  wherein the therapeutic component comprises an alpha-2-adrenergic agonist.  
     
     
         4 . A composition of  claim 3  wherein the alpha-2-adrenergic component comprises a quinoxaline component.  
     
     
         5 . A composition of  claim 4  wherein the quinoxaline component is selected from the group consisting of quinoxaline, (2-imidozolin-2-ylamino) quinoxaline, 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, and derivatives thereof and mixtures thereof.  
     
     
         6 . A composition of  claim 1  wherein the therapeutic component is selected from the group consisting of NMDA antagonists, antibacterials, antihistamines, decongestants, antiinflammatories, antiparasitics, miotics, anticholinergics, adrenergics, antivirals, local anesthetics, antifungals, amoebicidals, trichomonocidals, analgesics, mydriatics, antiglaucoma drugs, carbonic anhydrase inhibitors, ophthalmic diagnostic agents, ophthalmic agents used as adjuvants in surgery, chelating agents, antineoplastics, antihypertensives, muscle relaxants, diagnostics, derivatives thereof and mixtures thereof.  
     
     
         7 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of fatty acids, derivatives thereof and mixtures thereof.  
     
     
         8 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of saturated fatty acids and unsaturated fatty acids, derivatives thereof and mixtures thereof.  
     
     
         9 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of a fatty acid with more than 12 carbon atoms per molecule, derivatives thereof and mixtures thereof.  
     
     
         10 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of a docosahexanoic acids, derivatives thereof and mixtures thereof.  
     
     
         11 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of a linolenic acid, derivatives thereof and mixtures thereof.  
     
     
         12 . A composition of  claim 1  wherein the efficacy enhancing component has a therapeutic effect.  
     
     
         13 . A composition of  claim 1  wherein the efficacy enhancing component has a therapeutic effect while being in a complex with the therapeutic component.  
     
     
         14 . A composition of  claim 1  wherein the efficacy enhancing component has a therapeutic effect while not being in a complex with the therapeutic component.  
     
     
         15 . A composition of  claim 1  wherein the efficacy enhancing component is effective to reduce intraocular pressure when the composition is administered to the eye.  
     
     
         16 . A composition of  claim 1  wherein the efficacy enhancing component is selected from the group consisting of prostanoids, derivatives thereof and mixtures thereof.  
     
     
         17 . A composition of  claim 1  wherein the efficacy enhancing component is present in an amount effective to enhance the movement of the therapeutic component across a lipid membrane.  
     
     
         18 . A composition of  claim 1  wherein the efficacy-enhancing component is present in an amount effective to enhance the movement of the therapeutic component across a biological membrane under physiological conditions.  
     
     
         19 . A composition of  claim 1  wherein the therapeutic component comprises a 5-bromo-6-(2-imidozolin-2-ylamino)quinoxaline, 
 the efficacy enhancing component is selected from the group consisting of docosahexanoic acids, derivatives thereof, linolenic acids, derivative thereof, prostanoids, derivatives thereof and mixtures thereof; and  
 the efficacy enhancing component enhances the movement of the therapeutic component across a biological membrane under physiological conditions.  
 
     
     
         20 . A composition of  claim 1  wherein the complex is present in a form other than a solution.  
     
     
         21 . A composition of  claim 1  wherein the complex is dissociable in a biological environment to provide a therapeutic effect.  
     
     
         22 . A composition of  claim 1  which includes at least one additional therapeutic component and the efficacy enhancing component is complexed with both the therapeutic component and the additional therapeutic component.  
     
     
         23 . A composition of  claim 1  wherein a single therapeutic component forms a complex with more than one efficacy enhancing component.  
     
     
         24 . A composition of  claim 1  which is ophthalmically acceptable.  
     
     
         25 . A composition of  claim 1  which further comprises a carrier.  
     
     
         26 . A composition comprising: 
 an adrenergic agonist;    a fatty acid selected from the group consisting of docosahexanoic acids, derivatives thereof, linolenic acids, derivatives thereof and mixtures thereof,    wherein the adrenergic agonist forms a complex with the fatty acid, the complex substantially remains intact in an aqueous environment.    
     
     
         27 . A composition comprising a complex and a carrier component, the complex comprising: 
 a therapeutic component, and    an efficacy enhancing component, wherein the efficacy enhancing component comprises anionic polymers, derivatives thereof, fatty acids, derivatives thereof and mixtures thereof.    
     
     
         28 . A composition of  claim 27  wherein the therapeutic component comprises an alpha-2-adrenergic agonist.  
     
     
         29 . A composition of  claim 28  wherein the alpha-2-adrenergic agonist includes a quinoxaline component.  
     
     
         30 . A composition of  claim 29  wherein the quinoxaline component is selected from the group consisting of quinoxaline, (2-imidozolin-2-ylamino) quinoxaline, 5-bromo-6- (2-imidozolin-2-ylamino) quinoxaline.  
     
     
         31 . The composition of  claim 27  wherein the therapeutic component is selected from the group consisting of NMDA antagonists, antibacterials, antihistamines, decongestants, antiinflammatories, antiparasitics, miotics, anticholinergics, adrenergics, antivirals, local anesthetics, antifungals, amoebicidals, trichomonocidals, analgesics, mydriatics, antiglaucoma drugs, carbonic anhydrase inhibitors, ophthalmic diagnostic agents, ophthalmic agents used as adjuvants in surgery, chelating agents, antineoplastics, antihypertensives, muscle relaxants, diagnostics, derivatives thereof and mixtures thereof.  
     
     
         32 . A composition of  claim 27  which has a pH of about 7 or greater.  
     
     
         33 . A composition of  claim 27  which has a pH in a range of about 7 to about 9.  
     
     
         34 . A composition of  claim 27  wherein the carrier component is a saline solution.  
     
     
         35 . A composition of  claim 27  which is ophthalmically acceptable.