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 plants 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.

Description

CROSS REFERENCE TO RELATED APPLICATIONS

[0001] The present application is the U.S. National Phase of International Patent Application Serial No. PCT / BR2007 / 000316, filed on Nov. 14, 2007, which claims priority to Brazilian Patent Application Serial No. PI07007671, filed on Feb. 15, 2007, both of which are hereby incorporated by reference in their entireties.

[0002] 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, m...

Examples

example 1

Methodology Used to Obtain Alcoholic Extract

[0069]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 cayensens; 16.5% of Stachytarpheta jamaicensis and 19.7% of Stachytarpheta eliotis.

example 2

Methodology Used to Obtain Hydroalcoholic Extract

[0070]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

[0071]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.

CROSS REFERENCE TO RELATED APPLICATIONS

[0001] The present application is the U.S. National Phase of International Patent Application Serial No. PCT / BR2007 / 000316, filed on Nov. 14, 2007, which claims priority to Brazilian Patent Application Serial No. PI07007671, filed on Feb. 15, 2007, both of which are hereby incorporated by reference in their entireties.

[0002] 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, m...

Examples

example 1

Methodology Used to Obtain Alcoholic Extract

[0069]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 cayensens; 16.5% of Stachytarpheta jamaicensis and 19.7% of Stachytarpheta eliotis.

example 2

Methodology Used to Obtain Hydroalcoholic Extract

[0070]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

[0071]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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