Complex of garcinol, cyclodextrin and method thereof

Abstract

The present disclosure discloses a pharmaceutical molecule of Garcinol chemically complexed with cyclodextrins and the use of the complexed molecule in prevention and management of cardiac dysfunction induced by chemotherapy, drugs and/or other insults to the heart caused by lifestyle and disease conditions. The disclosure also relates to a method of extraction and purification of high yield of 95-99% pure Garcinol from Garcinia species and a method of chemically complexing Garcinol with cyclodextrins to improve its stability and bioavailability.

1 . A complex of Garcinol and Cyclodextrin. 
     
     
         2 . The complex as claimed in  claim 1 , wherein mole ratio of the Garcinol to the Cyclodextrin ranges from about 1:1 to about 1:4.5. 
     
     
         3 . The complex as claimed in  claim 1 , wherein the complex is a chemical complex. 
     
     
         4 . The complex as claimed in  claim 1 , wherein the Garcinol is of purity ranging from about 95% to about 99%. 
     
     
         5 . The complex as claimed in  claim 1 , wherein the Cyclodextrin is selected from a group comprising α-cyclodextrin, β-cyclodextrin, 2-Hydroxy-propyl-β-cyclodextrin and derivatives thereof. 
     
     
         6 . The complex as claimed in  claim 1 , wherein the Cyclodextrin is β-cyclodextrin. 
     
     
         7 . The complex as claimed in  claim 1 , wherein the Cyclodextrin is suitable derivative of β-Cyclodextrin. 
     
     
         8 . A method for preparation of a complex of Garcinol and Cyclodextrin, said method comprising acts of,
 a) dissolving the Garcinol in a solvent with the Cyclodextrin to obtain a mixture;   b) refluxing the mixture to form a clear solution;   c) cooling the clear solution to obtain crystals of the complex of the Garcinol and the Cyclodextrin; and   d) filtering and drying the crystals to obtain the complex of Garcinol and Cyclodextrin.   
     
     
         9 . The method as claimed in  claim 8 , wherein the solvent is selected from a group comprising water, aliphatic alcohols with carbon atoms ranging from 1 to 4 and any combination thereof. 
     
     
         10 . The method as claimed in  claim 8 , wherein the Cyclodextrin is selected from a group comprising α-cyclodextrin, β-cyclodextrin, 2-Hydroxy-propyl-β-cyclodextrin and derivatives thereof. 
     
     
         11 . The method as claimed in  claim 8 , wherein the cooling of the clear solution is to a temperature ranging from about 0° C. to about 25° C. 
     
     
         12 . The method as claimed in  claim 8 , wherein the drying is carried out under vacuum. 
     
     
         13 . The method as claimed in  claim 8 , wherein the drying is carried out at a temperature ranging from about 75° C. to about 80° C. 
     
     
         14 . The method as claimed in  claim 8 , wherein mole ratio of the Garcinol to the Cyclodextrin ranges from about 1:1 to about 1:4.5. 
     
     
         15 . Garcinol of purity ranging from about 95% to about 99%. 
     
     
         16 . A method for extracting Garcinol, said method comprising acts of,
 a) shredding dried rind of  Garcinia Indica  or  Garcinia Cambogia  or combination thereof;   b) extracting the shredded rind using suitable solvent;   c) filtering to remove the cellulosic material and obtain clear solution;   d) passing the clear solution through absorbent column to segregate into different fractions and obtain yellow coloured fraction;   e) concentrating the yellow coloured fraction to obtain a waxy material;   f) treating the waxy material with a suitable solvent; and   g) filtering and drying the treated waxy material to obtain the Garcinol.   
     
     
         17 . The method as claimed in  claim 16 , wherein the solvent in steps (b) and (f) is independently selected from a group comprising toluene, benzene, carbon tetrachloride, trichloromethane, trichloromethane, Petroleum ether, ether solvents and any combination thereof. 
     
     
         18 . The method as claimed in  claim 16 , wherein the absorbent column is neutral alumina. 
     
     
         19 . A composition comprising complex of Garcinol and Cyclodextrin along with pharmaceutically acceptable excipients. 
     
     
         20 . The composition as claimed in  claim 19 , wherein the pharmaceutically acceptable excipients are selected from a group comprising binders, disintegrants, diluents, lubricants, plasticizers, permeation enhancers, solubilizers and any combination thereof. 
     
     
         21 . The composition as claimed in  claim 19 , wherein the composition is in a form selected from a group comprising tablet, capsule, powder, syrup, solution, aerosol and suspension. 
     
     
         22 . A composition comprising pharmaceutically acceptable amount of complex as claimed in  claim 1  or a composition as claimed in  claim 18  and any other compound which can improve condition of cardiac dysfunction or any composition comprising thereof. 
     
     
         23 . A method of managing and treating conditions of cardiac dysfunction said method comprising act of administering pharmaceutically effective amount of complex as claimed in  claim 1  or a composition as claimed in  claim 18  or  claim 22  to a subject in need thereof. 
     
     
         24 . The method as claimed in  claim 23 , wherein the pharmaceutically effective amount ranges from about 1 mg/kg to about 100 mg/kg of body weight per day. 
     
     
         25 . The method as claimed in  claim 23 , wherein the cardiac dysfunction is induced by chemotherapy drugs selected from a group comprising Doxorubicin, anthracycline derivatives and protease inhibitors. 
     
     
         26 . The method as claimed in  claim 23 , wherein the cardiac dysfunction is induced by inotropic agents selected from a group comprising Isoproterenol and Digitalis. 
     
     
         27 . The method as claimed in  claim 23 , wherein the cardiac dysfunction is induced by conditions of increased peripheral resistance and pressure selected from a group comprising stenosis, hypertension, myocardial infarction, ischemic heart disease and cardiomyopathy. 
     
     
         28 . The method as claimed in  claim 23 , wherein the method prevents heart failure induced by cardiac dysfunction. 
     
     
         29 . The method as claimed in  claim 23 , wherein the subject is an animal, including human being.