ES2925732A1 - ophthalmic composition - Google Patents
ophthalmic composition Download PDFInfo
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- ES2925732A1 ES2925732A1 ES202100093A ES202100093A ES2925732A1 ES 2925732 A1 ES2925732 A1 ES 2925732A1 ES 202100093 A ES202100093 A ES 202100093A ES 202100093 A ES202100093 A ES 202100093A ES 2925732 A1 ES2925732 A1 ES 2925732A1
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- Prior art keywords
- ophthalmic composition
- pirenoxine
- bromfenac
- pilocarpine
- bss
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
DESCRIPCIÓNDESCRIPTION
Composición oftálmicaophthalmic composition
Objeto de la invenciónObject of the invention
La invención, tal como expresa el enunciado de la presente memoria descriptiva, se refiere a una composición oftálmica.The invention, as expressed in the title of this specification, refers to an ophthalmic composition.
Más en particular, el objeto de la invención se centra en una mejorada composición para el tratamiento farmacológico de la presbicia que, estando basada en un colirio ya conocido con una fórmula que comprende una concentración de pilocarpina al 1-1,5% y bromfenaco, 1.8 mgrs en solución salina balanceada estéril (BSS), se distingue por incluir además, en dicha fórmula, pirenoxina sódica en una proporción de 0,05mg/ml que, como agente anti-cataratas, supone una mejora de la fórmula citada haciendo que la eficacia del colirio sea mucho más prolongada en el tiempo, mejorando y alargando la independencia de las gafas de cerca en pacientes Présbitas a los que está destinado, mejorando notablemente la calidad de vida de los mismos.More particularly, the object of the invention focuses on an improved composition for the pharmacological treatment of presbyopia which, being based on an already known eye drop with a formula that comprises a concentration of pilocarpine at 1-1.5% and bromfenac, 1.8 mgrs in sterile balanced saline solution (BSS), is distinguished by also including, in said formula, sodium pirenoxine in a proportion of 0.05mg/ml which, as an anti-cataract agent, represents an improvement of the aforementioned formula, making the The effectiveness of the eye drops is much longer in time, improving and lengthening the independence of near glasses in Presbyopic patients for whom it is intended, notably improving their quality of life.
Campo de aplicación de la invenciónField of application of the invention
El campo de aplicación de la presente invención se enmarca dentro del sector de la industria farmacéutica, centrándose particularmente en el ámbito de los fármacos oftalmológicos.The field of application of the present invention falls within the pharmaceutical industry sector, focusing particularly on the field of ophthalmological drugs.
Antecedentes de la invenciónBackground of the invention
Como es sabido, la Presbicia, también denominada vista cansada, es un defecto ocular asociado a la edad que aparece generalmente entre los 40-45 años y ocasiona dificultad para ver de cerca. Se debe a la reducción del poder de acomodación del cristalino que provoca disminución de la capacidad para enfocar objetos cercanos.As is known, Presbyopia, also called tired eyesight, is an eye defect associated with age that generally appears between 40-45 years of age and causes difficulty seeing up close. It is due to the reduction of the accommodation power of the lens that causes a decrease in the ability to focus on close objects.
La acomodación es la capacidad que permite a las personas ver con nitidez objetos cercanos a expensas de la función del músculo ciliar que cambia la forma del cristalino y aumenta el poder óptico del ojo. La función del músculo ciliar depende del grado de estimulación parasimpática de los receptores muscarínicos, además a través de la modulación de la pupila, contrayendo la pupila para crear un "efecto de estenopeico” y aumentar la profundidad de campo, mejorando aún más, la visión de cerca. Disminuir el tamaño de la pupila: aumenta tanto la profundidad de campo como la profundidad de enfoque.Accommodation is the ability that allows people to see close objects clearly at the expense of ciliary muscle function that changes the shape of the lens and increases the optical power of the eye. Ciliary muscle function depends on the degree of parasympathetic stimulation of muscarinic receptors, furthermore through modulation of the pupil, contracting the pupil to create a "pinhole effect" and increasing depth of field, further improving vision. Decrease Pupil Size: Increases both depth of field and depth of focus.
Los síntomas aparecen entre los 40-45 años y progresan hasta los 60 aproximadamente. Consisten en una dificultad creciente para la visión nítida de objetos cercanos.Symptoms appear between 40-45 years of age and progress until approximately 60 years of age. They consist of an increasing difficulty in clearly seeing nearby objects.
"La necesidad de corrección de la Presbicia es un punto importante de insatisfacción visual para los pacientes Emétropes sanos mayores de 40 años” y tener opciones no quirúrgicas para eliminar la necesidad de gafas o lentes de contacto en Présbitas jóvenes, sería una estrategia bienvenida a nuestro armamentarium de corrección de la Presbicia.“The need for Presbyopia correction is a major point of visual dissatisfaction for healthy Emmetropic patients over 40 years of age” and having non-surgical options to eliminate the need for glasses or contact lenses in young Presbyopic women would be a welcome strategy in our Presbyopia correction armamentarium.
Actualmente no existe en el mercado farmacéutico, ningún tratamiento tópico, seguro, eficaz y bien tolerado que pueda ser utilizado, para compensar la Presbicia. La etiología de la Presbicia aún no está bien definida, pero los cambios que se producen en el Cristalino, en la Zónula y en el Músculo Ciliar, contribuyen probablemente a la pérdida progresiva de la capacidad de Acomodación.There is currently no safe, effective and well-tolerated topical treatment on the pharmaceutical market that can be used to compensate for Presbyopia. The etiology of Presbyopia is not yet well defined, but the changes that occur in the Lens, in the Zonula and in the ciliary muscle, probably contribute to the progressive loss of accommodation capacity.
Si existe, sin embargo, un tratamiento farmacológico, consiste en la estimulación de los receptores muscarínicos, mediante la instilación de un colirio, divulgado en el documento de patente n° ES253855B1, y cuyo titular es el propio solicitante de la presente invención, consistente en una composición para la activación de la función del músculo ciliar y del esfínter de la Pupila. La estimulación farmacológica de la función ciliar con dicho colirio logra mejorar la Acomodación, que unido a la mejoría en la profundidad de foco ocasionada por el efecto estenopeico provocado por la miosis obtenida, permite que los pacientes vuelvan a enfocar en todas las distancias, hasta que aparecen los primeros síntomas de “esclerosis del cristalino” y por supuesto de la pérdida de elasticidad del mismo.If there is, however, a pharmacological treatment, it consists of the stimulation of the muscarinic receptors, through the instillation of an eye drop, disclosed in patent document No. ES253855B1, and whose owner is the applicant of the present invention, consisting of a composition for the activation of the function of the ciliary muscle and the Pupil sphincter. The pharmacological stimulation of the ciliary function with said eye drops manages to improve Accommodation, which together with the improvement in the depth of focus caused by the pinhole effect caused by the miosis obtained, allows patients to focus again at all distances, until The first symptoms of "lens sclerosis" appear and of course the loss of elasticity of the lens.
Es por ello, que sería deseable poder alargar la efectividad de dicho fármaco.That is why it would be desirable to be able to extend the effectiveness of said drug.
Por otra parte, es también conocido que la Pirenoxina Sódica 0,05 mg/ml, es un estabilizador de membrana de células del Cristalino, normalizando su metabolismo e impidiendo la fijación de substancias opacificantes a las proteínas del mismo. La Pirenoxina es, pues, un agente anti cataratas.On the other hand, it is also known that Sodium Pirenoxine 0.05 mg/ml is a lens cell membrane stabilizer, normalizing its metabolism and preventing the fixation of opacifying substances to its proteins. Pirenoxine is thus an anti-cataract agent.
El objetivo de la presente invención, es pues, el desarrollo de un colirio para la corrección de la presbicia mejorado mediante la combinación del mismo con un agente anti-cataratas como la Pirenoxima Sódica para poder ampliar y alargar su efectividad.The objective of the present invention, therefore, is the development of an eye drop for the correction of presbyopia improved by combining it with an anti-cataract agent such as Pyrenoxime Sodium in order to amplify and lengthen its effectiveness.
Explicación de la invenciónExplanation of the invention
La composición oftálmica que la invención propone se configura, pues, como una solución óptima al objetivo anteriormente señalado, estando los elementos caracterizadores que la distinguen convenientemente recogidos en las reivindicaciones finales que acompañan a la presente descripción.The ophthalmic composition that the invention proposes is configured, therefore, as an optimal solution to the aforementioned objective, the characterizing elements that conveniently distinguish it being collected in the final claims that accompany this description.
Más concretamente, como se ha apuntado en apartados anteriores, la invención se refiere a una composición oftálmica para el tratamiento farmacológico de la presbicia mejorada, la cual, estando basada en un colirio ya conocido y divulgado en la patente n° ES253855B1 del proprio solicitante, con una fórmula que comprende una concentración de pilocarpina al 1-1,5% y bromfenaco, 1.8 mgrs en solución salina balanceada estéril (BSS), se distingue por el hecho de que además, en dicha fórmula, se incluye un agente anti-cataratas, concretamente pirenoxina sódica en una proporción de 0,05mg/ml, lo cual supone una mejora de la fórmula citada.More specifically, as has been pointed out in previous sections, the invention refers to an ophthalmic composition for the pharmacological treatment of improved presbyopia, which, being based on an eye drop already known and disclosed in patent number ES253855B1 of the applicant himself, with a formula that includes a concentration of pilocarpine at 1-1.5% and bromfenac, 1.8 mgrs in sterile balanced salt solution (BSS), is distinguished by the fact that an anti-cataract agent is also included in said formula , specifically sodium pirenoxine in a proportion of 0.05mg/ml, which represents an improvement of the cited formula.
Dicho fármaco puede desempeñar un papel importante en la prevención y retraso de la aparición de Cataratas. El efecto anti-cataratas de la Pirenoxina resulta de la inhibición de la combinación sulfhidrilo de sustancias quinoides con proteínas del Cristalino y la inhibición conduce al mantenimiento de la transparencia del Cristalino, así como a la conservación durante años de su elasticidad, todo ello hace que la eficacia del nuevo colirio sea mucho más prolongada en el tiempo, mejorando y alargando en el tiempo, la independencia de las gafas de cerca en pacientes Présbitas, mejorando notablemente la calidad de vida de nuestros pacientes.Said drug can play an important role in the prevention and delay of the appearance of Cataracts. The anti-cataract effect of Pirenoxine results from the inhibition of the sulfhydryl combination of quinoid substances with Lens proteins and the inhibition leads to the maintenance of the transparency of the Lens, as well as the preservation of its elasticity for years, all of which makes the effectiveness of the new eye drops is much longer in time, improving and lengthening in time, the independence of near glasses in Presbyopic patients, notably improving the quality of life of our patients.
Más específicamente, la composición oftálmica objeto de la invención consiste en un colirio de 8 o 9 ml, para conseguir una concentración de pilocarpina final entre 1-1,5%, bromfenaco 1.8 mgrs, y pirenoxina sódica 0.05mg/ml, todo ello en una solución salina balanceada (BSS). More specifically, the ophthalmic composition object of the invention consists of an 8 or 9 ml eye drop, to achieve a final concentration of pilocarpine between 1-1.5%, bromfenac 1.8 mgrs, and sodium pirenoxine 0.05mg/ml, all in a balanced salt solution (BSS).
Descrita suficientemente la naturaleza de la presente invención, así como la manera de ponerla en práctica, no se considera necesario hacer más extensa su explicación para que cualquier experto en la materia comprenda su alcance y las ventajas que de ella se derivan, haciéndose constar que podrá ser llevada a la práctica en otras formas de realización que difieran en detalle siempre que no se modifique lo fundamental. Having sufficiently described the nature of the present invention, as well as the way of putting it into practice, it is not considered necessary to make its explanation more extensive so that any person skilled in the art understands its scope and the advantages derived from it, stating that it may be implemented in other embodiments that differ in detail as long as the fundamentals are not changed.
Claims (2)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES202100093A ES2925732A1 (en) | 2021-04-06 | 2021-04-06 | ophthalmic composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES202100093A ES2925732A1 (en) | 2021-04-06 | 2021-04-06 | ophthalmic composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2925732A1 true ES2925732A1 (en) | 2022-10-19 |
Family
ID=83637912
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES202100093A Pending ES2925732A1 (en) | 2021-04-06 | 2021-04-06 | ophthalmic composition |
Country Status (1)
| Country | Link |
|---|---|
| ES (1) | ES2925732A1 (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0885612A1 (en) * | 1997-06-06 | 1998-12-23 | Pharmaconsult s.a.s. | Pirenoxine for the topical treatment of inflammatory conditions |
| ES2538551A2 (en) * | 2013-12-20 | 2015-06-22 | Eurocanarias Oftalmológica, Sl | Ophthalmic composition for the correction of presbyopia (Machine-translation by Google Translate, not legally binding) |
-
2021
- 2021-04-06 ES ES202100093A patent/ES2925732A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0885612A1 (en) * | 1997-06-06 | 1998-12-23 | Pharmaconsult s.a.s. | Pirenoxine for the topical treatment of inflammatory conditions |
| ES2538551A2 (en) * | 2013-12-20 | 2015-06-22 | Eurocanarias Oftalmológica, Sl | Ophthalmic composition for the correction of presbyopia (Machine-translation by Google Translate, not legally binding) |
Non-Patent Citations (1)
| Title |
|---|
| TSUNEYOSHI YUKARI ET AL. Author Correction: Suppression of presbyopia progression with pirenoxine eye drops: experiments on rats and non-blinded, randomized clinical trial of efficacy.. Scientific reports England 16 Apr 2020. , 16/04/2020, Vol. 10, Páginas 6757 ISSN 2045-2322 (Electronic), (DOI: doi:10.1038/s41598-020-62436-7 pubmed:32296100) * |
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| BA2A | Patent application published |
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