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Pharmaceutical composition on the basis of stachytarpheta sp., a process for obtaining the same and its use for treating vitiligo

a technology of stachytarpheta and composition, which is applied in the preparation of sugar derivatives, plant ingredients, sugar derivatives, etc., can solve the problems of vitiligo manifestations that are not satisfactory to existing treatments, diprosalic solution, and accumulation of toxic free radicals that may damage the melanocytes, etc., to achieve the effect of increasing the feasibility of industrial production, easy to find in nature, and increasing the siz

Inactive Publication Date: 2010-02-04
ACHE LAB FARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0005]Recent researches have demonstrated the existence of specific biochemical failures on the catalase activity and an accumulation of hydrogenated peroxide in the skin of vitiligo patients. The catalase suggests that keratinocytes in vitiligo are capable of recycling the 5,6,7,8-tetrahydrobiopterin (6-BH4), an adjuvant factor for the hydroxylation of L-phenylalanine into L-tyrosine. This may break the supply of L-thyroxine for the melanin production, increasing the catecholamine by the keratinocytes, resulting in the accumulation of toxic free radicals that may damage the melanocytes.
[0009]Use of melagenine: it helps decreasing the patches in 75% of the patients.
[0019]The species used in this invention are more easily found in nature than Stachytarpheta polyura, mentioned on the prior art, in larger quantities, as well as larger sizes, increasing the feasibility of the production in industrial scale. Such species, popularly known as gervão, gerbão, overjão, chá-do-Brasil (“verbena / vervain”), among other popular names, are used in the traditional medicine as cicatrizant, treatment for stomach problems and antifebrile.

Problems solved by technology

This may break the supply of L-thyroxine for the melanin production, increasing the catecholamine by the keratinocytes, resulting in the accumulation of toxic free radicals that may damage the melanocytes.
Use of Diprosalic: Diprosalic solution, less efficient than melagenine, is topically used on the patches.
In light of the foregoing, it was demonstrated that the existing treatments are not satisfactory to fight vitiligo manifestations.
This species, Stachytarpheta polyura, is rarely found in nature, and its diminutive size makes the production of the extract in industrial scale unfeasible, costly and unprofitable.

Method used

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  • Pharmaceutical composition on the basis of stachytarpheta sp., a process for obtaining the same and its use for treating vitiligo
  • Pharmaceutical composition on the basis of stachytarpheta sp., a process for obtaining the same and its use for treating vitiligo

Examples

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example 1

Methodology Used to Obtain Alcoholic Extract

[0064]In a bowl of an extractor equipped with mechanical agitation, add 100 Kg of leaves or aerial parts of the plant (of one of the three mentioned species), dried in ovens with controlled temperature of 60° C. and grounded in electrical mill. Then, add 280 liters of ethanol at 96° GL, with frequent stirring, during 72 to 144 hours (2 to 4 days). After that process, filter the extract in vacuum through 100-μm filters. Using this methodology, a yield of approximately 240 liters of extract solution is obtained. After evaporation of the solvent in rotary evaporator with reduced pressure, a concentrated alcoholic extract is achieved, with the following results per plant, on average: 18% of Stachytarpheta cayensensis; 16.5% of Stachytarpheta jamaicensis and 19.7% of Stachytarpheta eliotis.

example 2

Methodology Used to Obtain Hydroalcoholic Extract

[0065]To a stainless steel percolator, add 50 Kg of leaves or aerial parts of the plant (of one of the three mentioned species), dehydrated under shadow over stainless steel nets, during 24 hours. Then, add 80 liters of a hydroalcoholic solution (ethanol:water 1:1) and allow it to percolate for 8 days, with daily and occasional stirring. By the end of the period, filtrate the extract in 100-μm filters and concentrate it in rotary evaporator under reduced pressure. This methodology results in a yield of concentrated hydroalcoholic extract per plant in the following order: 15 to 21% of Stachytarpheta cayensensis; 17 to 20% of Stachytarpheta jamaicensis and 15 to 22% of Stachytarpheta eliotis.

example 3

Methodology Used to Obtain Aqueous Extract

[0066]To obtain the aqueous extract of one of the three Stachytarpheta species, add to a percolation bowl with controlled temperature 50 Kg of the leaves of previously selected aerial parts, dried under 65° C. in an oven with forced aeration and, then, ground it in an electric mill. Then, add 100 liters of distilled water to the bowl and heat it to 90° C. for 4 hours in a row. During that period, stir it occasionally. Then, filtrate it using 100-μm filters and, lastly, concentrate the extract (filtrate) in a rotary evaporator under reduced pressure. This extraction process results in the following yields: 7.4 to 11.2% of Stachytarpheta cayensensis; 6.5 to 8.9% of Stachytarpheta jamaicensis and 7.2 to 11.5% of Stachytarpheta eliotis in relation to the weight of the vegetable material used in the extraction process.

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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 (Verhenaceae 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.

Description

[0001]This invention generally refers to the obtention of a compound and a standard pharmaceutical product from roots, stems, barks, and leaves of plants of the Stachytarpheta (Verbenaceae family) genus, in the form of extracts or enriched fractions, or pure isolated compounds or compounds obtained from synthesis or semi-synthesis, used alone (pure extract) 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 and manifestations thereof—loss of skin pigment.BASIS OF THE INVENTION[0002]The name vitiligo was used for the first time by the Roman physician Celsus (50 a.C.). It originates from the Latin word vitilus, which means wh...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/352A61K31/70A61K31/715A61P17/00A61K9/48A61K9/127A61K9/14C07D311/02C07H1/08
CPCA61K36/85A61K31/352A61P17/00A61P37/00
Inventor QUEIROZ FERREIRA, EMERSON
Owner ACHE LAB FARM
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