BR102018077328B1 - LIGHTENING PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DISORDERS THAT CAUSE INCREASED MELANIN DEPOSIT AND HYPERPIGMENTATION OF THE SKIN, AND ITS USE FOR THE MANUFACTURE OF A SEMISOLID PRODUCT - Google Patents
LIGHTENING PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DISORDERS THAT CAUSE INCREASED MELANIN DEPOSIT AND HYPERPIGMENTATION OF THE SKIN, AND ITS USE FOR THE MANUFACTURE OF A SEMISOLID PRODUCT Download PDFInfo
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- XUMBMVFBXHLACL-UHFFFAOYSA-N Melanin Chemical compound O=C1C(=O)C(C2=CNC3=C(C(C(=O)C4=C32)=O)C)=C2C4=CNC2=C1C XUMBMVFBXHLACL-UHFFFAOYSA-N 0.000 title claims abstract description 20
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 16
- 238000004519 manufacturing process Methods 0.000 title claims description 7
- 208000031066 hyperpigmentation of the skin Diseases 0.000 title description 4
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 claims abstract description 20
- BDJRBEYXGGNYIS-UHFFFAOYSA-N nonanedioic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 claims abstract description 20
- 208000035475 disorder Diseases 0.000 claims abstract description 14
- BJRNKVDFDLYUGJ-RMPHRYRLSA-N hydroquinone O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-RMPHRYRLSA-N 0.000 claims abstract description 14
- BJRNKVDFDLYUGJ-ZIQFBCGOSA-N alpha-Arbutin Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-ZIQFBCGOSA-N 0.000 claims abstract description 13
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 13
- 229940116918 octadecenedioic acid Drugs 0.000 claims abstract description 11
- SBLKVIQSIHEQOF-UPHRSURJSA-N Octadec-9-ene-1,18-dioic-acid Chemical compound OC(=O)CCCCCCC\C=C/CCCCCCCC(O)=O SBLKVIQSIHEQOF-UPHRSURJSA-N 0.000 claims abstract description 10
- IMQLKJBTEOYOSI-UHFFFAOYSA-N Phytic acid Natural products OP(O)(=O)OC1C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C(OP(O)(O)=O)C1OP(O)(O)=O IMQLKJBTEOYOSI-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000002738 chelating agent Substances 0.000 claims abstract description 9
- 239000007854 depigmenting agent Substances 0.000 claims abstract description 9
- 239000000467 phytic acid Substances 0.000 claims abstract description 9
- 229940068041 phytic acid Drugs 0.000 claims abstract description 9
- 235000002949 phytic acid Nutrition 0.000 claims abstract description 9
- 239000011782 vitamin Substances 0.000 claims abstract description 9
- 229940088594 vitamin Drugs 0.000 claims abstract description 9
- 229930003231 vitamin Natural products 0.000 claims abstract description 9
- 235000013343 vitamin Nutrition 0.000 claims abstract description 9
- IMQLKJBTEOYOSI-GPIVLXJGSA-N Inositol-hexakisphosphate Chemical compound OP(O)(=O)O[C@H]1[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@H](OP(O)(O)=O)[C@@H]1OP(O)(O)=O IMQLKJBTEOYOSI-GPIVLXJGSA-N 0.000 claims abstract description 8
- 229960004705 kojic acid Drugs 0.000 claims abstract description 8
- 239000003755 preservative agent Substances 0.000 claims abstract description 8
- 206010040865 Skin hyperpigmentation Diseases 0.000 claims abstract description 7
- 125000000129 anionic group Chemical group 0.000 claims abstract description 7
- 229960000271 arbutin Drugs 0.000 claims abstract description 7
- 239000002585 base Substances 0.000 claims abstract description 7
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- 239000003974 emollient agent Substances 0.000 claims abstract description 7
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 7
- BEJNERDRQOWKJM-UHFFFAOYSA-N kojic acid Chemical compound OCC1=CC(=O)C(O)=CO1 BEJNERDRQOWKJM-UHFFFAOYSA-N 0.000 claims abstract description 7
- WZNJWVWKTVETCG-UHFFFAOYSA-N kojic acid Natural products OC(=O)C(N)CN1C=CC(=O)C(O)=C1 WZNJWVWKTVETCG-UHFFFAOYSA-N 0.000 claims abstract description 7
- BJRNKVDFDLYUGJ-UHFFFAOYSA-N p-hydroxyphenyl beta-D-alloside Natural products OC1C(O)C(O)C(CO)OC1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000003223 protective agent Substances 0.000 claims abstract description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000006071 cream Substances 0.000 claims description 10
- 239000006210 lotion Substances 0.000 claims description 9
- 229960004311 betamethasone valerate Drugs 0.000 claims description 6
- 206010008570 Chloasma Diseases 0.000 claims description 5
- SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 claims description 5
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims description 4
- 208000003351 Melanosis Diseases 0.000 claims description 4
- VYGQUTWHTHXGQB-FFHKNEKCSA-N Retinol Palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C VYGQUTWHTHXGQB-FFHKNEKCSA-N 0.000 claims description 4
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims description 4
- 229940033280 alpha-arbutin Drugs 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
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- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 2
- VYGQUTWHTHXGQB-UHFFFAOYSA-N Retinol hexadecanoate Natural products CCCCCCCCCCCCCCCC(=O)OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C VYGQUTWHTHXGQB-UHFFFAOYSA-N 0.000 claims description 2
- 206010040844 Skin exfoliation Diseases 0.000 claims description 2
- XVAMCHGMPYWHNL-UHFFFAOYSA-N bemotrizinol Chemical compound OC1=CC(OCC(CC)CCCC)=CC=C1C1=NC(C=2C=CC(OC)=CC=2)=NC(C=2C(=CC(OCC(CC)CCCC)=CC=2)O)=N1 XVAMCHGMPYWHNL-UHFFFAOYSA-N 0.000 claims description 2
- 229960004101 bemotrizinol Drugs 0.000 claims description 2
- 239000003086 colorant Substances 0.000 claims description 2
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 claims description 2
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical compound CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 claims description 2
- 229940108325 retinyl palmitate Drugs 0.000 claims description 2
- 235000019172 retinyl palmitate Nutrition 0.000 claims description 2
- 239000011769 retinyl palmitate Substances 0.000 claims description 2
- 239000004408 titanium dioxide Substances 0.000 claims description 2
- -1 vitamin acetate Chemical class 0.000 claims description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- WBZKQQHYRPRKNJ-UHFFFAOYSA-L disulfite Chemical compound [O-]S(=O)S([O-])(=O)=O WBZKQQHYRPRKNJ-UHFFFAOYSA-L 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 230000002087 whitening effect Effects 0.000 abstract description 14
- 239000013543 active substance Substances 0.000 abstract description 6
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 abstract 1
- 229950006825 dexamethasone valerate Drugs 0.000 abstract 1
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- 239000000203 mixture Substances 0.000 description 8
- 230000009471 action Effects 0.000 description 7
- 239000004480 active ingredient Substances 0.000 description 5
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 210000001519 tissue Anatomy 0.000 description 4
- 230000003110 anti-inflammatory effect Effects 0.000 description 3
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- 210000002615 epidermis Anatomy 0.000 description 3
- 210000003630 histaminocyte Anatomy 0.000 description 3
- 230000003054 hormonal effect Effects 0.000 description 3
- 208000000069 hyperpigmentation Diseases 0.000 description 3
- 230000003810 hyperpigmentation Effects 0.000 description 3
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- 229960004441 tyrosine Drugs 0.000 description 3
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 2
- 210000001789 adipocyte Anatomy 0.000 description 2
- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 description 2
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- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 1
- XUIIKFGFIJCVMT-LBPRGKRZSA-N L-thyroxine Chemical compound IC1=CC(C[C@H]([NH3+])C([O-])=O)=CC(I)=C1OC1=CC(I)=C(O)C(I)=C1 XUIIKFGFIJCVMT-LBPRGKRZSA-N 0.000 description 1
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- MHUWZNTUIIFHAS-CLFAGFIQSA-N dioleoyl phosphatidic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(COP(O)(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC MHUWZNTUIIFHAS-CLFAGFIQSA-N 0.000 description 1
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- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/35—Ketones, e.g. benzophenone
- A61K8/355—Quinones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
- A61K8/361—Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
- A61K8/492—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
Abstract
A invenção refere-se à uma composição farmacêutica clareadora para o tratamento de distúrbios que provocam o aumento de depósito de melanina e a hiperpigmentação da pele, compreendendo um complexo clareador composto pelos agentes farmaceuticamente ativos em uma concentração centesimal(p/p)de 5,00% a 15,00% para a hidroquinona; 8,00% a 10,00% para o ácido fítico 35%; 3% a 7% o para 4-hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin); 2,00% a 5,00% para o ácido azeláico; 0,50% a 2,00% para o ácido octadecenodióico; 7,00 a 8,00% de gluconoloctona; 3,00% a 5,00% de Nano Kojico, 4,00% a 6,00% para o ácido kójico e 0,05% a 1,00% para o valerato de dexametasona; e os gentes farmaceuticamente inertes sendo os conservates, os emulsificantes, os agentes protetores anti UVA e UVB, os emolientes, os agentes despigmentantes, os quelantes, as bases aniônicas, as vitaminas e a água.The invention relates to a whitening pharmaceutical composition for the treatment of disorders that cause increased melanin deposition and skin hyperpigmentation, comprising a whitening complex composed of pharmaceutically active agents in a centesimal concentration (w/w) of 5. 00% to 15.00% for hydroquinone; 8.00% to 10.00% for phytic acid 35%; 3% to 7% o for 4-hydroxyphenyl-alpha-D-glucopyranoside (Alfa Arbutin); 2.00% to 5.00% for azelaic acid; 0.50% to 2.00% for octadecenedioic acid; 7.00 to 8.00% gluconoloctone; 3.00% to 5.00% Nano Kojico, 4.00% to 6.00% for kojic acid and 0.05% to 1.00% for dexamethasone valerate; and pharmaceutically inert agents, including preservatives, emulsifiers, anti-UVA and UVB protective agents, emollients, depigmenting agents, chelators, anionic bases, vitamins and water.
Description
[01] A presente invenção é destinada ao setor da saúde, cujo o principal objetivo é o tratamento de distúrbios associadas ao aumento da hiperpigmentação da pele que pode acometer homens e mulheres.[01] The present invention is intended for the health sector, whose main objective is the treatment of disorders associated with increased skin hyperpigmentation that can affect men and women.
[02] A presente invenção consiste de uma composição farmacêutica clareadora para o tratamento de distúrbios que provocam o aumento de depósito de melanina e a hiperpigmentação da pele compreendendo um complexo clareador composto pela hidroquinona, o ácido fítico 35%, o hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin), o ácido azeláico, o ácido octadecenodióico, o Nano Kojico, (VII) a valerato de betametasona. E outros agentes, sendo os agentes farmaceuticamente inertes, como os conservantes, os emulsificantes, os agentes protetores anti UVA e UVB, os emolientes, os agentes despigmentantes, os quelantes, as bases aniônicas, as vitaminas e a água.[02] The present invention consists of a whitening pharmaceutical composition for the treatment of disorders that cause increased melanin deposition and skin hyperpigmentation comprising a whitening complex composed of hydroquinone, phytic acid 35%, hydroxyphenyl-alpha-D -glucopyranoside (Alpha Arbutin), azelaic acid, octadecenedioic acid, Nano Kojico, (VII) betamethasone valerate. And other agents, being pharmaceutically inert agents, such as preservatives, emulsifiers, anti-UVA and UVB protective agents, emollients, depigmenting agents, chelators, anionic bases, vitamins and water.
[03] O tecido cutâneo é considerado o maior órgão do corpo humano. Estruturalmente, este tecido se divide em três camadas: a epiderme, a derme e a hipoderme. A epiderme é a camada mais superficial, composta de células epiteliais estratificadas e de forma pavimentosa, intimamente unidas e avascular e sendo até 90% de queratinócitos.[03] Skin tissue is considered the largest organ in the human body. Structurally, this tissue is divided into three layers: the epidermis, the dermis and the hypodermis. The epidermis is the most superficial layer, composed of stratified epithelial cells with a squamous shape, closely united and avascular, with up to 90% keratinocytes.
[04] A derme é composta por um tecido conjuntivo denso, irregular e elástico de grande resistência, formando um suporte entre a epiderme e o tecido subcutâneo subjacente. Apresentando grande quantidade de fibroblastos, colágenos, células do sistema imune como macrófagos e mastócitos.[04] The dermis is composed of dense, irregular and elastic connective tissue of great resistance, forming a support between the epidermis and the underlying subcutaneous tissue. Presenting a large amount of fibroblasts, collagens, immune system cells such as macrophages and mast cells.
[05] A camada mais interna do tecido é a hipoderme ou tecido subcutâneo, composto por uma rede de células adiposas e vasos sanguíneos. A hipoderme atua como um reservatório de energia devido ao seu grande número de células adiposas, assim, efetua um papel de destaque como um isolante de calor e na absorção de impactos, protegendo os órgãos mais internos.[05] The innermost layer of tissue is the hypodermis or subcutaneous tissue, composed of a network of fat cells and blood vessels. The hypodermis acts as an energy reservoir due to its large number of fat cells, thus playing a prominent role as a heat insulator and shock absorber, protecting the most internal organs.
[06] Pelo fato deste tecido sofrer ação constante de agentes nocivos externos de natureza química, biológica e de radiações ionizantes; bem como dos agentes endógenos devido as alterações hormonais ou a formação de espécies reativas de oxigênio e metabólitos, ele apresenta um forte processo de renovação e proteção celular.[06] Due to the fact that this tissue suffers constant action from external harmful agents of a chemical, biological nature and ionizing radiation; as well as endogenous agents due to hormonal changes or the formation of reactive oxygen species and metabolites, it presents a strong process of cellular renewal and protection.
[07] Este mecanismo de renovação e proteção é constante e acelerado, sendo altamente efetivo. Entretanto, quando esse mecanismo falha, podem aparecer distúrbios ou doenças de natureza inflamatória, resultando no aparecimento de manchas provocadas pela hiperpigmentação.[07] This renewal and protection mechanism is constant and accelerated, being highly effective. However, when this mechanism fails, disorders or diseases of an inflammatory nature may appear, resulting in the appearance of spots caused by hyperpigmentation.
[08] O melasma é um grande exemplo de distúrbios ocasionados pela ação dos agentes nocivos. É uma condição que se caracteriza pelo surgimento de manchas escuras na pele, mais comumente na face, mas também pode ser de ocorrência extra facial (Sociedade Brasileira de Dermatologia).[08] Melasma is a great example of disorders caused by the action of harmful agents. It is a condition characterized by the appearance of dark spots on the skin, most commonly on the face, but can also occur extrafacially (Brazilian Society of Dermatology).
[09] Afeta frequentemente as mulheres, mas podem ser observados em homens. Sua principal causa está relacionada ao fator hormonal, devido ao uso de anticoncepcionais por um longo tempo ou durante o período gestacional (cloasma gravídico) quando 50% das mulheres podem desenvolvê-lo em consequência das alterações hormonais durante o período gravídico (British Association of Dermatology).[09] It often affects women, but can be seen in men. Its main cause is related to the hormonal factor, due to the use of contraceptives for a long time or during the gestational period (chloasma gravidarum) when 50% of women can develop it as a result of hormonal changes during the pregnancy period (British Association of Dermatology ).
[10] Um outro distúrbio envolvendo o processo de hiperpigmentação é a ancatosis nigricans, a qual afeta majoritariamente a região das pregas cutâneas (pescoço, virilhas, axilas e regiões em torno dos mamilos), se apresentando por vezes uma área acastanhada. Podem ser ocasionadas em pacientes com quadro de obesidade ou diabetes, e também por longos períodos de uso de corticoides e contraceptivos (Rosário; F. Caldeira; J. Medicina Interna. Vol.8, N.4, 2001).[10] Another disorder involving the hyperpigmentation process is ancatosis nigricans, which mainly affects the skin folds region (neck, groin, armpits and regions around the nipples), sometimes presenting a brownish area. They can be caused in patients with obesity or diabetes, and also due to long periods of use of corticosteroids and contraceptives (Rosário; F. Caldeira; J. Medicina Interna. Vol.8, N.4, 2001).
[11] Os distúrbios de hiperpigmentação não causam dores ou queimações ou qualquer outro tipo de sintoma. Seu efeito é agravado por afetar o bem-estar do paciente, principalmente as mulheres que podem ser vítimas de constrangimento ou estresse psicológico.[11] Hyperpigmentation disorders do not cause pain or burning or any other type of symptoms. Its effect is aggravated by affecting the patient's well-being, especially women who may be victims of embarrassment or psychological stress.
[12] Dentro do estado da técnica são apresentadas diversas formas ou produtos para o tratamento de distúrbios relacionados com a hiperpigmentação. Os documentos de patentes PI 04155157, US 2013171079 e BR 1120130057033 ensinam produtos para o clareamento da pele contendo, em parte, os ativos presente na referida composição. Entretanto, o diferencial da presente invenção é a combinação de agentes ativos e não ativos em uma concentração centesimal (p/p) que representa alta eficiência e segurança no clareamento da pele. Um segundo diferencial apresentado por esta invenção no clareamento da pele é o uso combinado de um creme e uma loção amplificadora durante o tratamento de clareamento da pele.[12] Within the state of the art, various forms or products are presented for the treatment of disorders related to hyperpigmentation. Patent documents PI 04155157, US 2013171079 and BR 1120130057033 teach products for skin whitening containing, in part, the active ingredients present in said composition. However, the difference of the present invention is the combination of active and non-active agents in a proximate concentration (w/w) that represents high efficiency and safety in skin whitening. A second difference presented by this invention in skin whitening is the combined use of a cream and an amplifying lotion during the skin whitening treatment.
[13] O principal objeto desta invenção é uma composição farmacêutica clareadora para o tratamento de distúrbios que provocam o aumento de depósito de melanina e a hiperpigmentação da pele, compreendendo um complexo clareador composto pelos agentes farmaceuticamente ativos em uma concentração centesimal(p/p)de 5,00% a 15,00% para a hidroquinona; 8,00% a 10,00% para o ácido fítico 35%; 3% a 7% o para 4-hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin); 2,00% a 5,00% para o ácido azeláico; 0,50% a 2,00% para o ácido octadecenodióico; 7,00 a 8,00% de gluconoloctona; 3,00% a 5,00% de Nano Kojico, 4,00% a 6,00% para o ácido kójico e 0,05% a 1,00% para o valerato de betametasona; e os agentes farmaceuticamente inertes sendo os conservantes, os emulsificantes, os agentes protetores anti UVA e UVB, os emolientes, os agentes despigmentantes, os quelantes, as bases aniônicas, as vitaminas e a água.[13] The main object of this invention is a whitening pharmaceutical composition for the treatment of disorders that cause increased melanin deposition and hyperpigmentation of the skin, comprising a whitening complex composed of pharmaceutically active agents in a centesimal concentration (w/w) from 5.00% to 15.00% for hydroquinone; 8.00% to 10.00% for phytic acid 35%; 3% to 7% o for 4-hydroxyphenyl-alpha-D-glucopyranoside (Alfa Arbutin); 2.00% to 5.00% for azelaic acid; 0.50% to 2.00% for octadecenedioic acid; 7.00 to 8.00% gluconoloctone; 3.00% to 5.00% Nano Kojico, 4.00% to 6.00% for kojic acid and 0.05% to 1.00% for betamethasone valerate; and pharmaceutically inert agents being preservatives, emulsifiers, anti-UVA and UVB protective agents, emollients, depigmenting agents, chelators, anionic bases, vitamins and water.
[14] Um outro objeto da invenção é o uso da referida composição para a fabricação de um produto cosmético apresentado na forma farmacêutica semi-sólida.[14] Another object of the invention is the use of said composition for the manufacture of a cosmetic product presented in semi-solid pharmaceutical form.
[15] O último objeto da presente invenção é o uso do produto cosmético semi-sólido, fabricado a partir da composição ensinada nesta invenção, ser aplicado para o tratamento de distúrbios que provocam o aumento de depósito de melanina e hiperpigmentação da pele, como exemplo o melasma, a psoríase, a acne, a acantose nigricans.[15] The last object of the present invention is the use of the semi-solid cosmetic product, manufactured from the composition taught in this invention, to be applied to the treatment of disorders that cause increased melanin deposits and hyperpigmentation of the skin, as an example melasma, psoriasis, acne, acanthosis nigricans.
[16] Para o melhor entendimento da invenção, foi denominado de agente farmaceuticamente ativo aquela matéria prima contida na composição que apresentam uma ação farmacológica, tendo como o resultado a redução do depósito de melanina ou uma ação anti-inflamatória. O agente farmaceuticamente inativo é a matéria prima sem efeito farmacológico, mas que fornece características organolépticas, estabilidade e conservam a composição.[16] For a better understanding of the invention, a pharmaceutically active agent was called that raw material contained in the composition that presents a pharmacological action, resulting in the reduction of melanin deposition or an anti-inflammatory action. The pharmaceutically inactive agent is the raw material without pharmacological effect, but which provides organoleptic characteristics, stability and preserves the composition.
[17] A presente invenção ensina uma composição farmacêutica clareadora para o tratamento de distúrbios que provocam o aumento da hiperpigmentação da pele, compreendendo um complexo clareador composto pelos agentes farmaceuticamente ativos como a hidroquinona, o ácido fítico 35%, 4- hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin), ácido azeláico, o ácido octadecenodióico, de gluconoloctona, de Nano Kojico, o ácido kójico e o valerato de betametasona; e os agentes farmaceuticamente inertes sendo os conservates, os emulsificantes, os agentes protetores anti UVA e UVB, os emolientes, os agentes despigmentantes, os quelantes, as bases aniônicas, as vitaminas e a água.[17] The present invention teaches a whitening pharmaceutical composition for the treatment of disorders that cause increased skin hyperpigmentation, comprising a whitening complex composed of pharmaceutically active agents such as hydroquinone, phytic acid 35%, 4-hydroxyphenyl-alpha- D-Glucopyranoside (Alpha Arbutin), Azelaic Acid, Octadecenedioic Acid, Gluconoloctone, Nano Kojico, Kojic Acid and Betamethasone Valerate; and pharmaceutically inert agents being preservatives, emulsifiers, anti-UVA and UVB protective agents, emollients, depigmenting agents, chelators, anionic bases, vitamins and water.
[18] Em uma concentração farmaceuticamente aceitável, os agentes ativos que compreende o complexo clareador da presente invenção, apresentam uma concentração centesimal (p/p) que varia entre 5,00% a 15,00% para a hidroquinona; 8,00% a 10,00% para o ácido fítico 35%; 3% a 7% para o 4- hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin); 2,00% a 5,00% para o ácido azeláico; 0,50% a 2,00% para o ácido octadecenodióico; 7,00 a 8,00% de gluconoloctona; 3,00% a 5,00% de Nano Kojico, 4,00% a 6,00% para o ácido kójico e 0,05% a 1,00% para o valerato de betametasona.[18] At a pharmaceutically acceptable concentration, the active agents comprising the whitening complex of the present invention have a proximate concentration (w/w) that varies between 5.00% and 15.00% for hydroquinone; 8.00% to 10.00% for phytic acid 35%; 3% to 7% for 4-hydroxyphenyl-alpha-D-glucopyranoside (Alfa Arbutin); 2.00% to 5.00% for azelaic acid; 0.50% to 2.00% for octadecenedioic acid; 7.00 to 8.00% gluconoloctone; 3.00% to 5.00% Nano Kojico, 4.00% to 6.00% for kojic acid and 0.05% to 1.00% for betamethasone valerate.
[19] A eficácia da composição farmacêutica para o clareamento da pele é devido a associação dos diferentes ativos dentro de uma concentração segura para o paciente. Os ativos possuem mecanismos de ação diferentes, que em conjunto desempenham efeitos sinérgicos aumentando a eficiência do tratamento.[19] The effectiveness of the pharmaceutical composition for skin whitening is due to the association of different active ingredients within a safe concentration for the patient. The active ingredients have different mechanisms of action, which together have synergistic effects, increasing the efficiency of the treatment.
[20] A seguir, são apresentados a indicação e o mecanismo de ação dos ativos empregados na composição:[20] The indication and mechanism of action of the assets used in the composition are presented below:
[21] -Hidroquinona - Despigmentante. Atua provocando mudanças estruturais nas membranas das organelas dos melanócitos, acelerando a degradação dos melanossomas.[21] -Hydroquinone - Depigmenting agent. It works by causing structural changes in the membranes of melanocyte organelles, accelerating the degradation of melanosomes.
[22] -Ácido Fítico - é um agente despigmentante, mas também apresenta bons efeitos como agente quelante e conservante.[22] - Phytic Acid - is a depigmenting agent, but also has good effects as a chelating and preservative agent.
[23] - Hidroxifenil-alfa-D-glucopiranósido (Alfa arbutin)- despigmentante. Atua bloqueando a biossíntese epidermal da melanina, através da inibição da oxidação enzimática da tirosina, a DOPA.[23] - Hydroxyphenyl-alpha-D-glucopyranoside (Alpha arbutin) - depigmenting agent. It works by blocking the epidermal biosynthesis of melanin, through the inhibition of the enzymatic oxidation of tyrosine, DOPA.
[24] -Ácido Azeláico - ácido dicarboxílico e atua como antiacnéico. Controla o ciclo de renovação celular dentro do folículo piloso, evitando seu bloqueio por material queratinoso e devido a isso, possui ação anticomedogênica. Além de ter uma ação anti-inflamatória.[24] -Azelaic Acid - dicarboxylic acid and acts as an anti-acne agent. It controls the cell renewal cycle within the hair follicle, preventing it from being blocked by keratinous material and due to this, it has an anti-comedogenic action. In addition to having an anti-inflammatory action.
[25] -Ácido octadecenodióico (Oda White) - Despigmentante. Atua inibindo os fatores de PPAR (Peroxisome Proliferator- Activated Recepto) que regulam a expressão dos genes para a produção da melanina.[25] -Octadecenedioic acid (Oda White) - Depigmenting agent. It works by inhibiting PPAR (Peroxisome Proliferator- Activated Recepto) factors that regulate the expression of genes for melanin production.
[26] -Gluconoloctona - Polihidroxiácido esfoleante, que descama suavemente a pele sem provocar seu ressecamento, devido à sua ação hidratante;[26] -Gluconoloctone - Exfoliating polyhydroxy acid, which gently peels the skin without causing it to dry out, due to its moisturizing action;
[27] -Nano Kójico - Despigmentante. Inibe a tirosina.[27] -Nano Kojic - Depigmenting. Inhibits tyrosine.
[28] -Ácido Kójico - Despigmentante. Inibe a oxidação a L- tiroxina por ser um agente quelante do cobre. Íon fundamental para a conversão do L-tirosina em L-dihidroxifenilalanina (L-DOPA).[28] -Kojic Acid - Depigmenting. Inhibits oxidation to L-thyroxine as it is a copper chelating agent. Fundamental ion for the conversion of L-tyrosine into L-dihydroxyphenylalanine (L-DOPA).
[29] -Valerato de Betametasona - Corticoide com forte ação anti-inflamatória, principalmente no combate a reações alérgicas em fase aguda. Seu mecanismo de ação atua diminuindo a densidade de mastócitos, diminuição da quimiotaxia e ativação dos eosinófilos, diminuição da produção de citocinas por linfócitos, monócitos, mastócitos e eosinófilos, e inibindo o metabolismo do ácido araquidônico.[29] -Betamethasone Valerate - Corticosteroid with strong anti-inflammatory action, mainly to combat allergic reactions in the acute phase. Its mechanism of action acts by decreasing the density of mast cells, decreasing chemotaxis and activation of eosinophils, decreasing the production of cytokines by lymphocytes, monocytes, mast cells and eosinophils, and inhibiting the metabolism of arachidonic acid.
[30] São empregados mais de um agente inerte na referida composição para que seja alcançada a melhor estabilidade e eficiência, podem ser qualquer um conhecido do estado da técnica, contanto que esteja em uma concentração centesimal (p/p) farmaceuticamente aceitável, sendo preferencialmente o 8% de Ascorsilane C®, e/ou 0,5% de Unicid®, e/ou 0,3% de metabissulfito de sódio, e/ou 0,08% de butil hidroxitolueno (BTH) e/ou 0,50% de Optiphen® e/ou 4,00% propanediol como agentes conservantes; 5,00% de Tinosorb S® como agente protetor anti UVA/UVB; 2,00% de Emulium 22®, e/ou 2,50% de Aristoflex AVL® e/ou 1,00% de Amphsol K® como agentes emulsificantes; 2,00% de Dermol® e/ou 2,00% Net® FS como agentes emolientes; 0,30% de dissodio EDTA como um agente quelante; 0,24% de CI 77491, e/ou 0,22% de CI 77492 e/ou 0,16% CI 77499 e/ou 5,00% dióxido de titânio como corantes; 6,00% de Lanette N® e/ou Emulzome® como base aniônica; 5,00% de palmitato de vitamina A e/ou 0,50% de acetato de vitamina como agentes vitamínicos; 1,00% de álcool desodorizado e 22,85% de água.[30] More than one inert agent is used in said composition to achieve the best stability and efficiency, they can be any known in the art, as long as it is in a pharmaceutically acceptable proximate concentration (w/w), preferably being o 8% Ascorsilane C®, and/or 0.5% Unicid®, and/or 0.3% sodium metabisulfite, and/or 0.08% butyl hydroxytoluene (BTH) and/or 0.50 % Optiphen® and/or 4.00% propanediol as preservative agents; 5.00% Tinosorb S® as anti-UVA/UVB protective agent; 2.00% Emulium 22®, and/or 2.50% Aristoflex AVL® and/or 1.00% Amphsol K® as emulsifying agents; 2.00% Dermol® and/or 2.00% Net® FS as emollient agents; 0.30% disodium EDTA as a chelating agent; 0.24% CI 77491, and/or 0.22% CI 77492 and/or 0.16% CI 77499 and/or 5.00% titanium dioxide as colorants; 6.00% Lanette N® and/or Emulzome® as an anionic base; 5.00% vitamin A palmitate and/or 0.50% vitamin acetate as vitamin agents; 1.00% deodorized alcohol and 22.85% water.
[31] A referida composição compreendendo seus agentes farmaceuticamente ativos e inertes é usada para fabricação de um produto cosmético podendo ser apresentado nas seguintes formas farmacêuticas semi-sólidas: cremes, pomadas, géis, unguentos, loções e demais formas conhecidas dentro do estado da técnica. Preferencialmente, a composição farmacêutica é usada na fabricação de creme e loção que são aplicados no tratamento de distúrbios associados ao aumento de depósito de melanina e a hiperpigmentação da pele.[31] Said composition comprising its pharmaceutically active and inert agents is used to manufacture a cosmetic product and can be presented in the following semi-solid pharmaceutical forms: creams, ointments, gels, ointments, lotions and other forms known within the prior art . Preferably, the pharmaceutical composition is used in the manufacture of cream and lotion that are applied in the treatment of disorders associated with increased melanin deposition and skin hyperpigmentation.
[32] O tratamento consiste na aplicação do creme e da loção, que durante a terapia desempenham ações sinérgicas que levam à cura ou a redução dos efeitos dos distúrbios associadas ao aumento de depósito de melanina e a hiperpigmentação da pele.[32] The treatment consists of applying the cream and lotion, which during therapy perform synergistic actions that lead to the cure or reduction of the effects of disorders associated with increased melanin deposits and skin hyperpigmentation.
[33] Durante o tratamento, o creme desempenha um maior efeito para a despigmentação da pele. Por essa razão, a concentração dos ativos com ação despigmentante deve ser maior comparado com a loção. Em uma relação de concentração centesimal (p/p), que apresenta eficácia e segurança durante o tratamento, é preferencialmente 12,00% de hidroquinona; 10,00% de ácido fítico 35%; 8,00% de Ascorbosilane C®; 5,00% de 4-hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin); 3,00% nano kójico; 2,5% de ácido azelaico; 1,00% de ácido octadecenodióico.[33] During treatment, the cream has a greater effect on skin depigmentation. For this reason, the concentration of active ingredients with depigmenting action must be higher compared to the lotion. In a proximate concentration ratio (w/w), which presents efficacy and safety during treatment, it is preferably 12.00% hydroquinone; 10.00% phytic acid 35%; 8.00% Ascorbosilane C®; 5.00% 4-hydroxyphenyl-alpha-D-glucopyranoside (Alfa Arbutin); 3.00% nano kojic; 2.5% azelaic acid; 1.00% octadecenedioic acid.
[34] A loção tem a função de amplificar ou prolongar por algumas semanas o efeito despigmentante apresentado pelo creme durante o tratamento. Por essa razão, a concentração dos ativos com ação despigmentante deve ser menor do que comparado com a do creme, sendo uma concentração centesimal (p/p) aceitável preferencialmente 8,00% de gluconoloctona; 5,00% de ácido azelaico; 5,00% de hidroquinona; 5,00% de 4- hidroxifenil-alfa-D-glucopiranósido (Alfa Arbutin); 5,00% de ácido kójico e 1,00% de ácido octadecenodióico.[34] The lotion has the function of amplifying or prolonging for a few weeks the depigmenting effect presented by the cream during the treatment. For this reason, the concentration of active ingredients with depigmenting action must be lower than that of the cream, with an acceptable proximate concentration (w/w) preferably being 8.00% of gluconoloctone; 5.00% azelaic acid; 5.00% hydroquinone; 5.00% 4-hydroxyphenyl-alpha-D-glucopyranoside (Alfa Arbutin); 5.00% kojic acid and 1.00% octadecenedioic acid.
[35] Os distúrbios que promovem o aumento de depósito de melanina e a hiperpigmentação da pele, para os quais são indicados o creme e a loção amplificadora ensinadas nessa invenção, compreendem preferencialmente mas, não se limitando a estas, como o melasma, a psoríase, a acne, a acantose nigricans, sendo ainda capaz de promover o processo de esfoliação da pele.[35] Disorders that promote increased melanin deposition and hyperpigmentation of the skin, for which the cream and amplifying lotion taught in this invention are indicated, preferably include, but are not limited to, such as melasma, psoriasis , acne, acanthosis nigricans, and is also capable of promoting the skin exfoliation process.
Claims (13)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BR102018077328-3A BR102018077328B1 (en) | 2018-12-27 | LIGHTENING PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DISORDERS THAT CAUSE INCREASED MELANIN DEPOSIT AND HYPERPIGMENTATION OF THE SKIN, AND ITS USE FOR THE MANUFACTURE OF A SEMISOLID PRODUCT |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BR102018077328-3A BR102018077328B1 (en) | 2018-12-27 | LIGHTENING PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DISORDERS THAT CAUSE INCREASED MELANIN DEPOSIT AND HYPERPIGMENTATION OF THE SKIN, AND ITS USE FOR THE MANUFACTURE OF A SEMISOLID PRODUCT |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR102018077328A2 BR102018077328A2 (en) | 2020-07-07 |
| BR102018077328B1 true BR102018077328B1 (en) | 2024-06-18 |
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