BRPI1106368B1 - eye drops for treatment of intraocular inflammatory process - Google Patents

eye drops for treatment of intraocular inflammatory process Download PDF

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Publication number
BRPI1106368B1
BRPI1106368B1 BRPI1106368-8A BRPI1106368A BRPI1106368B1 BR PI1106368 B1 BRPI1106368 B1 BR PI1106368B1 BR PI1106368 A BRPI1106368 A BR PI1106368A BR PI1106368 B1 BRPI1106368 B1 BR PI1106368B1
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BR
Brazil
Prior art keywords
gold
inflammatory process
treatment
eye drops
inflammatory
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BRPI1106368-8A
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Portuguese (pt)
Inventor
Felipe Dal Pizzol
David Valter Pereira
Marcos Marques Da Silva Paula
Original Assignee
Fundação Educacional De Criciuma - Fucri
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Priority to BRPI1106368-8A priority Critical patent/BRPI1106368B1/en
Publication of BRPI1106368A2 publication Critical patent/BRPI1106368A2/en
Publication of BRPI1106368B1 publication Critical patent/BRPI1106368B1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/242—Gold; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

COLÍRIO PARA TRATAMENTO DE PROCESSO INFLAMATÓRIO INTRA-OCULAR constituído por água, citrato de sódio e ouro na forma nanoparticulada, ou seja, em partículas com uma escala de grandeza de nanômetros. Neste medicamento o ouro é o agente antiinflamatório, o citrato é o agente redutor e estabilizante e a água é o veículo.Eye drops for the treatment of an intra-ocular inflammatory process consisting of water, sodium citrate and gold in nanoparticulate form, that is, in particles with a nanometer scale. In this medicine, gold is the anti-inflammatory agent, citrate is the reducing and stabilizing agent and water is the vehicle.

Description

Setor tecnológico da invençãoTechnological sector of the invention

A presente invenção se refere, de modo geral, ao setor tecnológico de composições e medicamentos para o tratamento de processo inflamatório intra-ocular (uveíte).The present invention refers, in general, to the technological sector of compositions and drugs for the treatment of intraocular inflammatory process (uveitis).

Estado da técnica conhecidoKnown state of the art

Os corticosteróides são frequentemente utilizados na oftalmologia, principalmente nas doenças de caráter inflamatório e nas doenças imunológicas. A opção pela via de administração vai depender do tipo de doença e da intensidade da inflamação.Corticosteroids are often used in ophthalmology, mainly in inflammatory diseases and immunological diseases. The choice of route of administration will depend on the type of disease and the intensity of the inflammation.

Citam-se antiinflamatórios hormonais (glicocorticóides: prednisolona, dexametasona, betametasona, fluormetolona ) e não hormonais (diclofenaco sódico e flurbiprofeno ). Alguns antiinflamatórios não-esteróides (AINEs) de uso ocular. O diclofenaco sódico é um derivado do ácido fenilacético e o flurbiprofeno do ácido propiônico(2-4). As duas drogas inibem a produção de prostaglandinas e tromboxanos, através da inibição da ação da enzima ciclo-oxigenase sobre o ácido aracdônico por um mecanismo competitivo, tempo-dependente e irreversível. Além disso, o diclofenaco ainda reduz a produção de leucotrienos in vitrodesviando parcialmente o ácido aracdônico e os triglicerídeos(5-6).Hormonal anti-inflammatory drugs (glucocorticoids: prednisolone, dexamethasone, betamethasone, fluorometolone) and non-hormonal ones (sodium diclofenac and flurbiprofen) are mentioned. Some non-steroidal anti-inflammatory drugs (NSAIDs) for eye use. Diclofenac sodium is a derivative of phenylacetic acid and flurbiprofen of propionic acid (2-4). Both drugs inhibit the production of prostaglandins and thromboxanes, by inhibiting the action of the enzyme cyclooxygenase on arachidonic acid by a competitive, time-dependent and irreversible mechanism. In addition, diclofenac also reduces the production of leukotrienes in vitrodes partially bypassing arachidonic acid and triglycerides (5-6).

O efeito antiinflamatório e imunossupressor dos glicocorticóides ocorre devido às suas seguintes ações: 1. Promovem apoptose das células linfóides; 2. Interferem na circulação das células imunes, diminuem o número de linfócitos periféricos, principalmente linfócitos T e inibem o acúmulo de neutrófilos no local da inflamação; 3. Inibem a síntese de citoquinas; 4. Modulam direta e indiretamente a função das células B; 5. Inibem a resposta proliferativa dos monócitos ao fator de estimulação de colônias e sua diferenciação em macrófagos, também inibindo as suas funções fagocíticas e citotóxicas; 6. Inibem o movimento de células e fluídos a partir do compartimento intravascular; 7. Inibem a ação da histamina, a síntese das prostaglandinas e a ação dos ativadores do plasminogênio.The anti-inflammatory and immunosuppressive effect of glucocorticoids occurs due to its following actions: 1. They promote apoptosis of lymphoid cells; 2. They interfere with the circulation of immune cells, decrease the number of peripheral lymphocytes, mainly T lymphocytes and inhibit the accumulation of neutrophils at the inflammation site; 3. Inhibit cytokine synthesis; 4. Directly and indirectly modulate the function of B cells; 5. Inhibit the proliferative response of monocytes to the colony stimulating factor and its differentiation into macrophages, also inhibiting their phagocytic and cytotoxic functions; 6. Inhibit the movement of cells and fluids from the intravascular compartment; 7. Inhibit the action of histamine, the synthesis of prostaglandins and the action of plasminogen activators.

Novidade e objetivos da invençãoNovelty and objectives of the invention

A presente invenção objetiva o controle do processo inflamatório. Todas as drogas compreendidas pelo estado da técnica, acima listadas, são baseadas em compostos orgânicos. O princípio ativo da invenção é baseado em metal nanoparticulado, mais especificamente ouro, aplicado na forma de colírio, caracterizando um medicamento sobremaneira mais eficiente que os convencionais, sem qualquer efeito colateral (como catarata subcapsular posterior, glaucoma, infecções oculares oportunistas).The present invention aims to control the inflammatory process. All drugs comprised by the prior art, listed above, are based on organic compounds. The active principle of the invention is based on nanoparticulate metal, more specifically gold, applied in the form of eye drops, featuring a drug that is extremely more efficient than conventional ones, without any side effects (such as posterior subcapsular cataract, glaucoma, opportunistic eye infections).

A novidade e a inventividade residem na constatação de que ouro na forma nanoparticulada é antiinflamatório e seu uso como colírio para tratar processo inflamatório intra-ocular. Este resultado derivou de pesquisas do uso nanoparticulas em modelo animal de uveíte induzida por Ips, por medidas de parâmetros inflamatórios nos olhos dos animais e por comparação com o antiinflamatório padrão nestas condições. O dito colírio proposto é composto por água, que é o veículo, Citrato de Sódio, que atua como agente redutor e o ouro, que de forma surpreendente atua na forma nanoparticulada como agente antiinflamatório.The novelty and inventiveness lie in the finding that gold in the nanoparticulate form is anti-inflammatory and its use as eye drops to treat intraocular inflammatory process. This result derived from research on the use of nanoparticles in an animal model of uveitis induced by Ips, by measures of inflammatory parameters in the eyes of animals and by comparison with the standard anti-inflammatory in these conditions. The proposed eye drops are composed of water, which is the vehicle, Sodium Citrate, which acts as a reducing agent and gold, which surprisingly acts in the nanoparticulate form as an anti-inflammatory agent.

As diminutas dimensões das nanopartículas potencializam o efeito antiinflamatório em função da elevada área superficial, o que permite utilização de pequenas concentrações de ouro.The tiny dimensions of the nanoparticles enhance the anti-inflammatory effect due to the high surface area, which allows the use of small concentrations of gold.

Descrição detalhada da invençãoDetailed description of the invention

A presente invenção se refere a um colírio para tratamento de processo inflamatório intra-ocular constituído por água, citrato de sódio e ouro na forma nanoparticulada, ou seja, em partículas com uma escala de grandeza de nanômetros. Neste medicamento o ouro é o agente antiinflamatório, o citrato é o agente redutor e estabilizante e a água é o veículo.The present invention relates to eye drops for the treatment of an intraocular inflammatory process consisting of water, sodium citrate and gold in the nanoparticulate form, that is, in particles with a nanometer scale. In this medicine, gold is the anti-inflammatory agent, citrate is the reducing and stabilizing agent and water is the vehicle.

A produção de ouro em nano partículas pode ser realizada através de vários processos convencionais compreendidos pelo estado da técnica. O ouro metálico dividido em finas partículas exibe novas propriedades devido à extensa área superficial, tendo sido comprovado através de testes que o mesmo passa a ter efeito antiinflamatório.The production of gold in nanoparticles can be carried out through several conventional processes understood by the state of the art. Metallic gold divided into fine particles exhibits new properties due to the extensive surface area, having been proven through tests that it has an anti-inflammatory effect.

Na concretização preferencial da invenção, o ouro está presente na solução em 40ppm ( partes por milhão) ou 40 mg/L de ouro. A concentração preferencial de Citrato de Sódio é 1,14 x 10‘5 g / L. A reação que ocorre é Au3+ + NaBH4 —> Au°.In the preferred embodiment of the invention, gold is present in the solution in 40ppm (parts per million) or 40 mg / L of gold. The preferred concentration of Sodium Citrate is 1.14 x 10 '5 g / L. The reaction that occurs is Au3 + + NaBH4 -> Au °.

Tratou-se no presente relatório descritivo de uma invenção dotada de aplicação industrial, novidade e atividade inventiva, todos os requisitos determinados por lei para obter uma patente de invenção.This specification describes an invention endowed with industrial application, novelty and inventive step, all the requirements determined by law to obtain an invention patent.

Claims (3)

1. COLÍRIO PARA TRATAMENTO DE PROCESSO INFLAMATÓRIO INTRA-OCULAR caracterizado por ser constituído por água, citrato de sódio e ouro na forma nanoparticulada.1. EYE DROPS FOR TREATMENT OF INTRA-OCULAR INFLAMMATORY PROCESS characterized by being composed of water, sodium citrate and gold in the nanoparticulate form. 2. COLÍRIO PARA TRATAMENTO DE PROCESSOINFLAMATÓRIO INTRA-OCULAR como reivindicado em 1 e ainda caracterizado por o ouro estar presente em 40ppm ou 40 mg/L.2. EYE-DROPS FOR TREATING INTRA-OCULAR INFLAMMATORY PROCESS as claimed in 1 and further characterized by the fact that gold is present at 40ppm or 40 mg / L. 3. COLÍRIO PARA TRATAMENTO DE PROCESSO INFLAMATÓRIO INTRA-OCULAR como reivindicado em 1 e ainda io caracterizado por a concentração de Citrato de Sódio ser 1,14 x 10'5 g/L.3. EYE-DROPS FOR TREATING THE INTRA-OCULAR INFLAMMATORY PROCESS as claimed in 1 and furthermore characterized by the concentration of Sodium Citrate being 1.14 x 10'5 g / L.
BRPI1106368-8A 2011-10-28 2011-10-28 eye drops for treatment of intraocular inflammatory process BRPI1106368B1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
BRPI1106368-8A BRPI1106368B1 (en) 2011-10-28 2011-10-28 eye drops for treatment of intraocular inflammatory process

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Application Number Priority Date Filing Date Title
BRPI1106368-8A BRPI1106368B1 (en) 2011-10-28 2011-10-28 eye drops for treatment of intraocular inflammatory process

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BRPI1106368A2 BRPI1106368A2 (en) 2013-10-08
BRPI1106368B1 true BRPI1106368B1 (en) 2020-12-22

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Publication number Priority date Publication date Assignee Title
CN111588733B (en) * 2016-11-28 2022-08-12 深圳深见医药科技有限公司 Application of gold clusters or substances containing gold clusters in preparation of drugs for preventing and/or treating glaucoma

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Date Code Title Description
B03A Publication of an application: publication of a patent application or of a certificate of addition of invention
B07D Technical examination (opinion) related to article 229 of industrial property law
B06F Objections, documents and/or translations needed after an examination request according art. 34 industrial property law
B07E Notice of approval relating to section 229 industrial property law
B07A Technical examination (opinion): publication of technical examination (opinion)
B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: A61K 33/00 , A61K 31/28 , A61K 31/194 , A61K 9/51 , A61P 29/00 , A61P 27/02

Ipc: A61K 33/242 (2019.01), A61K 9/14 (2006.01), A61K 9

B09A Decision: intention to grant
B16A Patent or certificate of addition of invention granted

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 28/10/2011, OBSERVADAS AS CONDICOES LEGAIS.