US2013164341A1PendingUtilityA1

Preparation of formulations of angiotensin ii at1 receptors antagonists for the treatment of arterial hypertension, other cardiovascular illnesses and its complications

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Assignee: UNIV MINAS GERAISPriority: Apr 10, 2001Filed: Oct 22, 2012Published: Jun 27, 2013
Est. expiryApr 10, 2021(expired)· nominal 20-yr term from priority
Inventors:Rubén Dario Sinisterra MillánRobson Algusto Souza Dos SantosFrederic Jean Georges FrezardWashington Xavier De Paula
A61K 9/5036A61P 9/00A61K 9/19A61K 38/085A61K 9/0002A61K 31/41A61P 9/10A61P 9/12A61K 31/4184A61K 31/4155A61K 31/4178A61K 9/1652
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Claims

Abstract

Inclusion compounds consisting of certain Angiotensin II AT1 receptor antagonists and cyclodextrins are described. These inclusion compounds are useful in the treatment of hypertension.

Claims

exact text as granted — not AI-modified
1 - 13 . (canceled) 
     
     
         14 . A composition comprising an inclusion compound consisting essentially of a water-soluble active ingredient selected from the group consisting of Angiotensin II AT1 receptor antagonist or salt thereof and a hydrophilic cyclodextrin. 
     
     
         15 . The composition according to  claim 14 , wherein the water-soluble active ingredient is monopotassium salt. 
     
     
         16 . The composition according to  claim 14 , wherein the cyclodextrin is β-cyclodextrin. 
     
     
         17 . The composition according to  claim 14 , wherein the cyclodextrin is hydroxypropyl-8-cyclodextrin. 
     
     
         18 . The composition according to  claim 14 , wherein the composition is a controlled-release system. 
     
     
         19 . The composition according to  claim 14 , wherein the composition shows an approximately 6-fold increase in the duration of the effect of the water-soluble active ingredient in comparison to the water-soluble active ingredient alone. 
     
     
         20 . The composition according to  claim 14 , wherein the half-life of the water-soluble active ingredient is increased. 
     
     
         21 . The composition of  claim 14 , wherein the active ingredient is eprosartan. 
     
     
         22 . A composition comprising an inclusion compound consisting essentially of a water-soluble active ingredient selected from the group consisting of Angiotensin II AT1 receptor antagonist or salt thereof and a hydrophilic cyclodextrin, wherein the composition further comprises a biodegradable or biocompatible polymer that encapsulates the inclusion compound. 
     
     
         23 . The composition according to  claim 22  wherein the polymer has a degradable surface. 
     
     
         24 . The composition according to  claim 22 , wherein the polymer is chosen from (2-hydroxyethyl methacrylate) polyacrylamide, poly(lactic acid) (PLA), poly(glycolic acid) (PGA), poly(lactic-glycolic acid) (PLGA), and poly(anhydrides). 
     
     
         25 . The composition according to  claim 22 , wherein the composition is a controlled-release system. 
     
     
         26 . The composition according to  claim 22  wherein the half-life of the water-soluble active ingredient is increased. 
     
     
         27 . A process for the preparation of a composition according to  claim 22  comprising an inclusion compound consisting essentially of a water-soluble active ingredient selected from the group consisting of Angiotensin II AT 1 receptor antagonist or salt thereof and a hydrophilic cyclodextrin. 
     
     
         28 . The process of  claim 27 , wherein the active ingredient is eprosartan. 
     
     
         29 . A process for the preparation of a composition according to  claim 22  comprising an inclusion compound consisting essentially of a water-soluble active ingredient selected from the group consisting of Angiotensin II AT 1 receptor antagonist or salt thereof and a hydrophilic cyclodextrin. 
     
     
         30 . The process of  claim 29 , wherein the polymer has a degradable surface. 
     
     
         31 . A pharmaceutical composition comprising the composition as claimed in  claim 14  and a pharmaceuticaly acceptable diluent or excipient. 
     
     
         32 . The pharmaceutical composition according to  claim 31 , wherein the composition is for oral, intramuscular, intravenous, subcutaneous or inhalation administration. 
     
     
         33 . The pharmaceutical composition according to  claim 31 , wherein the composition is solid or liquid. 
     
     
         34 . The pharmaceutical composition according to  claim 31 , wherein the composition has an improved bioavailability in comparison with the pharmaceutical composition without a hydrophilic cyclodextrin chosen from β-cyclodextrin or hydroxypropyl-β-cyclodextrin. 
     
     
         35 . A method of treating arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 31 . 
     
     
         36 . The method of  claim 35 , wherein the active ingredient is eprosartan. 
     
     
         37 . A method of treating arteriosclerosis associated with arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 31 . 
     
     
         38 . A pharmaceutical composition comprising the composition as claimed in  claim 25  and a pharmaceutical acceptable diluent or excipient. 
     
     
         39 . The pharmaceutical composition according to  claim 38 , wherein the composition is for oral, intramuscular, intravenous, subcutaneous or inhalation administration. 
     
     
         40 . The pharmaceutical composition according to  claim 38 , wherein the composition is solid or liquid. 
     
     
         41 . The pharmaceutical composition according to  claim 38 , wherein the composition has an improved bioavailability in comparison with the pharmaceutical composition without a hydrophilic cyclodextrin chosen from β-cyclodextrin or hydroxypropyl-β-cyclodextrin. 
     
     
         42 . A method of treating arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 38 . 
     
     
         43 . A method of treating arteriosclerosis associated with arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 38 . 
     
     
         44 . A method of treating stroke associated with arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 31 . 
     
     
         45 . A method of treating stroke associated with arterial hypertension comprising administering to a patient in need thereof a therapeutically effective amount of at least one pharmaceutical composition of  claim 38 .

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