Pharmaceutical Composition on the Basis of Stachytarpheta SP., a Process for obtaining the same and its use for Treating Vitiligo

Abstract

This invention generally refers to the process to obtain a compound and a standard pharmaceutical product from one or more parts of plant of the Stachytarpheta (Verbenaceae family) species, as well as roots, stems, barks, and leaves of plants in the form of extracts or enriched fractions, or pure isolated compounds or compounds obtained from synthesis, used alone or mixed with other natural or synthetic products, in different ratios, in order to integrate pharmaceutical compositions to be used by appropriate routes (topic or oral), particularly in the form of tablets, capsules, dyes, emulsions, W/O and O/W (creams and gels), liposomes, microcapsules, nanoparticles, aerosols, ointments, and the like, as well as formulations for slow-release implants, used to treat vitiligo.

1 . PHARMACEUTICAL COMPOSITION characterized in that it has one or more compounds, in its free form or in pharmaceutically acceptable salts, selected from the group of iridoids, flavonoids and ethyl phenyl propane glycosilate derivatives, obtained by synthesis, semi-synthesis or isolates from alcoholic, hydroalcoholic, aqueous, or organics extracts of one or more parts of the  Stachytarpheta  species. 
     
     
         2 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the compound has both chemical structures I and II of the iridoids group: 
       
         
           
           
               
               
           
         
       
       wherein R is identical or different and each one is independently selected among H, CH 3 , COCH 3 , alkali metals, halogens, monosaccharides, disaccharides or polysaccharides, CO(CH 2 ) n CH 3 , (CH 2 ) n CH 3 , where n ranges from 2 to 16. 
     
     
         3 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the compound has the chemical structure III of the flavonoids group: 
       
         
           
           
               
               
           
         
       
       wherein R is identical or different and each one is independently selected among H, CH 3 , CH 2 CH 3 , CH 2 OH, COCH 3 , alkali metals, halogens, monosaccharides, disaccharides or polysaccharides, CO(CH 2 ) n CH 3 , (CH 2 ) n CH 3 , where n ranges from 2 to 16. 
     
     
         4 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the compound has the chemical structures IV, V, VI, and VII of the ethyl phenyl propane glycosilate derivatives group: 
       
         
           
           
               
               
           
         
       
       wherein R is identical or different and each one is independently selected among H, CH 3 , CH 3 CH 3 , CH 2 OH, COCH 3 , alkali metals, halogens, monosaccharides, disaccharides or polysaccharides, CO(CH) n CH 3 , (CH 2 )CH 3 , where n ranges from 2 to 16. 
     
     
         5 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the extracts are obtained from  Stachytarpheta cayensensis, Stachytarpheta jamaicensis  and  Stachytarpheta eliotis  species, alone or in mixtures. 
     
     
         6 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that parts of plants of the  Stachytarpheta  genus are stems, roots, barks and leaves. 
     
     
         7 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that it has 0.001 to 90% of one or more compounds with chemical structure (I), (II), (III), (IV), (V), (VI), and (VII) in their free form or in pharmaceutically acceptable salts. 
     
     
         8 . PHARMACEUTICAL COMPOSITION according to  claims 1  and  7 , characterized in that the compounds are in the form of pharmaceutically acceptable salts, such as chlorate, sulfate or borate. 
     
     
         9 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized by the fact of containing 0.001 to 99% of the extract in weight out of the total weight of ingredients. 
     
     
         10 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the dosing range from 0.001 to approximately 5000 mg/kg/day, split into one or more times a day. 
     
     
         11 . PHARMACEUTICAL COMPOSITION according to  claim 10 , characterized in that the dosing contents range preferably from approximately 200 to approximately 400 mg/kg/day, split into one or more times a day. 
     
     
         12 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that contains approximately 0.001 mg to 5000 mg of the extract containing one or more compounds. 
     
     
         13 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that the compounds are used alone or mixed with each other or associated to extracts, fixed oils, essential oils, fragrances, powders or excipients from other natural or synthetic origins, or used as associated to the drug(s), vitamin(s), salt(s), monosaccharides, disaccharides or polysaccharides, or other pharmaceutically acceptable excipients, appropriate to oral, topical, injectable or inhalable application. 
     
     
         14 . PHARMACEUTICAL COMPOSITION according to  claim 13 , characterized in that it contains 0.001% to 991 of one or more compounds. 
     
     
         15 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that it is encapsulated into a hard gelatinous capsule or a soft gelatinous capsule. 
     
     
         16 . PHARMACEUTICAL COMPOSITION according to  claim 1 , characterized in that it is presented in the form of pure or combined extract as tablets, capsules, dyes, syrups and similar others or in the form of w/o and o/w emulsions (creams and gels), liposomes, microcapsules, nanoparticles, aerosols, sprays, ointments, and the like, injectable liquids, powders, lyophilized, patches, as well as formulations for slow-release implants or similar others used as adjuvant and other synthetic or natural pharmaceutically acceptable vehicles. 
     
     
         17 . PHARMACEUTICAL PRODUCT containing a pharmaceutical composition according to  claim 1 , characterized in that it is a phytodrug, a phytotherapic medication or a synthetic drug. 
     
     
         18 . PROCESS to obtain the phytotherapeutic pharmaceutical compounds characterized in that it comprises the following stages:
 (a) Pulverize, or grind, or chop, or crumb one or more parts of the plants of the  Stachytharpheta  genus, as well as its roots, stems, barks and leaves, whether green or dried, or their mixtures;   (b) Extraction by percolation, or maceration, or soxlhet, or using gases in supercritical state, or extraction using a base or acid medium or an organic solvent or extraction by steam distillation;   (c) Drying of the organic solution by means of a system under reduced pressure, or spray-dryer, or under room temperature;   (d) Separation and purification.   
     
     
         19 . PROCESS to obtain the pharmaceutical compound according to the claim  18 , characterized in that the inlet and outlet temperatures of the spray-dryer concentration process, whose stage (c) ranges between 150-190° C. and 80-90′C, respectively. 
     
     
         20 . PROCESS to obtain the pharmaceutical compound according to the  claim 18 , characterized in that the temperature under reduced pressure system, on stage (c), ranges between 25-100′C. 
     
     
         21 . PROCESS to obtain the pharmaceutical compound according to the  claim 18 , characterized in that the extraction of item (b), is carried out in aqueous media, or acidified or basified, or using organic solvents, or its mixtures. 
     
     
         22 . PROCESS to obtain the pharmaceutical compound according to the  claim 21 , characterized in that the extraction of acid/base may be performed with strong or weak acids, whether diluted or concentrated, alone or mixed, such as acetic acid, hydrochloric acid, formic acid; and the base used in the extraction process is formed by concentrate or diluted bases, whether alone or in mixtures such as, for example, ammonium hydroxide (NH 4 OH) and sodium carbonate (Na 2 CO 3 ). 
     
     
         23 . PROCESS to obtain the pharmaceutical compound according to the  claim 21 , characterized in that the organic solution used on stage (b), comprised of halogenate compounds, alcohols, ethers, esters, aldehydes, ketones, alkanes, cycloalkanes, phenolic compounds, benzenes and derivatives, whether alone or their mixtures. 
     
     
         24 . PROCESS to obtain the pharmaceutical compound according to the  claim 18 , characterized in that separation and purification of compounds, on item (d), is carried out using chromatographic arts with or without pressure, such as chromatography at atmospheric pressure, chromatography at low, medium or high pressure, using the normal stationary phase as silica gel or inverse phase as C-8 or C-18, or liquid/liquid partition as chromatography against current, or centrifugal partition, or using ion exchange resins or filtration membranes. 
     
     
         25 . PROCESS to obtain the pharmaceutical compound according to the claim  24 , characterized in that resulting in at least one of the compounds or their mixtures in free form or in salt form, of chemical structure (I), (II), (III), (IV), (V), (VI) and (VII), wherein R is identical or different and each one is independently selected among H, CH 3 , CH 2 CH 3 , CH 2 OH, COCH 3 , alkali metals, halogens, monosaccharides, disaccharides or polysaccharides, CO(CH 2 ) n CH 3 , (CH 2 ) n CH 3  (where n ranges from 2 to 16). 
     
     
         26 . PHARMACEUTICAL COMPOSITION characterized in that being used for treatment or prophylaxis of vitiligo, comprising of one or more compounds obtained by the process of  claim 18 , in its free form or in pharmaceutically acceptable salts. 
     
     
         27 . USE of pharmaceutical compounds characterized in that they are used alone or mixed in different ratios with each other, to be used in pharmaceutical compositions of medications used via oral, topical, injectable or inhalable routes, in the form of tablets, capsules, dyes, syrups and similar or in the form of emulsions W/O and O/W (creams and gels), liposomes, microcapsules, nanoparticles, aerosols, ointments, and the like, as well as formulations for slow-release implants, used for treatment and therapeutic prophylaxis of vitiligo.