Standardized plant extract, process for obtaining the same and uses thereof

Abstract

The present invention refers to a process for obtaining a standardized extract having antinociceptive, anti-inflammatory and antipyretic properties, from at least one part of a plant of genus Aleurites . Furthermore, the present invention provides a pharmaceutical composition comprising an active ingredient of a pharmaceutically efficient quantity of standardized extract from at least one part of the plant of genus Aleurites . Finally, the present invention describes a method of treatment and use of the said extract, isolated or in a pharmaceutical composition, for the prevention, control or treatment of painful, inflammatory or febrile affections.

1 - 41 . (canceled) 
     
     
         42 . A standardized extract of at least one part of a plant of the genus  Aleurites , wherein said extract is distinguished by at least one of the aspects selected from the group consisting of: (i) chromatograms by high performance liquid chromatography (HPLC) specific to the soft extract and dry extract of the said plant of genus  Aleurites , (ii) NMR 0 13  spectrums of the 2″-O-rhamnosylswertisin marker measured at 300 MHz in deuterated methanol, (iii) NMR H 1  spectrums of the 2″-O-rhamnosylswertisin marker measured at 300 MHz in deuterated methanol, (iv) chromatograms by high efficiency liquid chromatography of the 2″-O-rhamnosylswertisin standardized purified by preparative thin-layer chromatography and (v) infra-red spectrum of the 2″-O-rhamnosylswertisin marker. 
     
     
         43 . The extract according to  claim 42 , wherein said HPLC chromatograms specific for soft extract and dry extract are represented in, but not limited to,  FIG. 2 . 
     
     
         44 . The extract according to  claim 42 , wherein said NMR C 13  spectrums are represented in, but not limited to,  FIG. 3 . 
     
     
         45 . The extract according to  claim 42 , wherein said NMR H 1  spectrums are represented in, but not limited to,  FIG. 4 . 
     
     
         46 . The extract according to  claim 42 , wherein said HPLC chromatograms of the 2″-O-rhamnosylswertisin standard are represented in, but not limited to,  FIG. 5 . 
     
     
         47 . The extract according to  claim 42 , wherein said infra-red spectrum of the 2″-O-rhamnosylswertisin marker are represented in, but not limited to,  FIG. 6 . 
     
     
         48 . The extract according to  claim 42 , comprising at least one active ingredient selected from the group consisting of alpha-amyrin, beta-amyrin, alpha-amirinone, beta-amirinone, swertisin, with the said extract being standardized in relation to its marker 2″-O-rhamnosylswertisin. 
     
     
         49 . The extract according to  claim 42 , wherein said standardized extract of  Aleurites moluccana  contains a ratio of 2″-O-rhamnosylswertisin in the range of 0.05 to 15%. 
     
     
         50 . The extract according to  claim 42 , comprising analgesic, anti-inflammatory and antipyretic properties, in mammals. 
     
     
         51 . A pharmaceutical composition comprising: (i) a pharmaceutically effective quantity of the standardized extract in accordance with  claim 42  and (ii) at least one pharmaceutically acceptable carrier. 
     
     
         52 . The pharmaceutical composition according to  claim 51 , wherein said standardized extract is present in a quantity that represents between 5 and 90% of the composition's total weight. 
     
     
         53 . The pharmaceutical composition according to  claim 52 , wherein said standardized extract is present in a quantity that represents between 20 and 80% of the composition's total weight. 
     
     
         54 . The pharmaceutical composition according to  claim 51 , comprising, additionally, at least one pharmaceutically active substance selected from the group consisting of synthetic and semi-synthetic substances, biological molecules, vitamins and other derivative substances of plant origin. 
     
     
         55 . The pharmaceutical composition according to  claim 51 , comprising pharmaceutically appropriate forms for oral, topical, intravenous, subcutaneous, intramuscular, intravaginal and/or rectal administration. 
     
     
         56 . The pharmaceutical composition according to  claim 55 , wherein said pharmaceutical composition is selected from among tablets, capsules (either soft or hard), pills, powders, granules, simple pills, coated pills, chewable tablets, effervescent tablets, sublingual pills, controlled release pills, dragees, globules, elixirs, suspensions, syrups and emulsions, each of which may contain immediate, controlled, prolonged or retarded release formulations, ointments, unguents, creams, emulsions, gels, solutions, pastes, aerosols, transdermic, bolus or infusion, subcutaneous or intramuscular systems, suppositories, ovules, ointments, creams and the similar. 
     
     
         57 . A process for preparing the standardized extract according to  claim 42 , comprising the use of at least one part of a plant of the genus  Aleurites , and comprising the stages of:
 (i) collecting, drying and subdividing the plant material;   (ii) pre-extracting;   (iii) extracting with extractor solvent;   (iv) filtrating the extract;   (v) concentrating the extract;   (vi) pasteurising;   (vii) drying; and   (viii) proceeding qualitative and quantitative analysis (standardisation) of the extract, with said standardized extract being distinguished by the 2″-O-rhamnosylswertisin marker.   
     
     
         58 . The process according to  claim 57 , wherein said plant is selected from the group consisting of  A. trisperma, A. cordata, A. montana, A. fordii, A. montance, A. rockinghamensis  and  A. moluccana.    
     
     
         59 . The process according to  claim 57 , wherein said plant of the genus  Aleurites  is  Aleurites moluccana  L. Wild. 
     
     
         60 . The process according to  claim 59 , wherein said plant material comprises at least the leaves of  Aleurites moluccana  L. Wild. 
     
     
         61 . The process according to  claim 57 , wherein the collecting stage of the plant material occurs in dry weather. 
     
     
         62 . The process according to  claim 57 , wherein the pre-extraction stage is performed by agitation in an alcoholic medium at room temperature. 
     
     
         63 . The process according to  claim 57 , wherein the extractor solvent used for the extraction stage is selected from a group consisting of, but not limited to, water, methanol, ethanol, propanol, isopropanol, propyleneglycol, acid solution, ethyl acetate, dichloromethane, chloroform, hexane, glycerine, acetone, petroleum ether, supercritical fluid, and similar or a combination thereof. 
     
     
         64 . The process according to  claim 63 , wherein said extractor solvent is a hydro-alcoholic solution of water:ethanol in which the ratio of water does not exceed the ratio of alcohol. 
     
     
         65 . The process according to  claim 63 , wherein said extractor solvent is a hydro-alcoholic solution of water:ethanol at a ratio selected between 2:8, 3:7, 4:6 and 1:1. 
     
     
         66 . The process according to  claim 63 , wherein said extractor solvent is a hydro-alcoholic solution of water:ethanol at a ratio of 3:7. 
     
     
         67 . The process according to  claim 57 , wherein the ratio of extractor solvent:plant material used in the extraction stage varies between approximately 1:1 and 20:1. 
     
     
         68 . The process according to  claim 57 , wherein said ratio of extractor solvent:plant material is of 10:1. 
     
     
         69 . The process according to  claim 57 , wherein the pasteurisation stage is performed at a temperature of approximately 95° C., for approximately 3 minutes. 
     
     
         70 . The process according to  claim 57 , wherein the stage for concentrating the extract provides a concentration of approximately 20% to 50% of solids in the extract and is capable of completely eliminating the alcohol. 
     
     
         71 . The process according to  claim 57 , wherein the drying stage is performed in conditions appropriate to maintain the quantitative and qualitative characteristics of the extract. 
     
     
         72 . The process according to  claim 71 , wherein the drying stage is performed by the spray-drying technique, in the presence of a drying adjuvant. 
     
     
         73 . The process according to  claim 72 , wherein the drying adjuvant is selected from a group consisting colloidal silicon dioxide, modified cassaya starch, tricalcium phosphate, maltodextrin, cyclodextrins, microcrystalline cellulose, lactose or a combination thereof, added in a proportion of approximately 10 to 40% in relation to the ratio of total solids in the extract. 
     
     
         74 . The process according to  claim 57 , optionally comprising a depigmentation stage of the extract, using a procedure selected from the group consisting of active charcoal treatment, adsorption resin treatment or membrane ultrafiltration. 
     
     
         75 . The process according to  claim 57 , optionally comprising a stabilisation stage of the extract, in the presence of a stabilising agent, with the said stabilising agent being selected from the group consisting of derivates of thyol, ascorbic acid and its derivatives, cysteine, glutathione, or a combination of the above and the similar. 
     
     
         76 . A method of treating pain, inflammation and/or fever in a mammal comprising administering to the mammal an effective quantity of the standardized extract according to  claim 42 . 
     
     
         77 . A method of treating pain, inflammation and/or fever in a mammal comprising administering to the mammal at least one effective quantity of the pharmaceutical composition according to  claim 51 . 
     
     
         78 . The method according to  claim 74 , wherein the dose to be administered provides 0.1 to 50 mg of the standardized extract per kilogram of the patient's body weight. 
     
     
         79 . A method of treating pain, inflammation and/or fever in a mammal comprising administering to the mammal an effective quantity of 2″-O-rhamnosylswertisin, isolated and purified, from the extract according to  claim 42 .