CN103565801B - For treating compositions and the said composition application in treatment ocular disease of eyeground macular edema - Google Patents
For treating compositions and the said composition application in treatment ocular disease of eyeground macular edema Download PDFInfo
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Abstract
For treating compositions and the said composition application in treatment ocular disease of eyeground macular edema.Belong to pharmaceutical technology field.This compositions being used for treating eyeground macular edema includes by weight percentage: (a) polyphenol compound of 0.4% ~ 71%, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 0.6% ~ 93%, (c) ubiquinone of 0% ~ 97% or pantothenylol, (d) docosahexenoic acid of 0% ~ 87% or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.Said composition can be used for improving patient's vision stability intraocular pressure and reducing all kinds of inflammation of eye, such as oculopathy such as eyeground macular edema.The present invention can prevent, stablize, control or treat eyeground macular edema for the compositions and Therapeutic Method treating eyeground macular edema, strengthens optical fundus healthy.Intraocular pressure can also be stablized simultaneously, keep or improve vision, alleviating various ocular disease or the macular edema caused because of operated eye and inflammation.Also treat diabetic complication, promote blood microcirculation, improve liver function.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of compositions for treating ocular disease and said composition
Application in treatment ocular disease.
Background technology
Blind and visual disorder principal disease is caused to have cataract in Chinese adult especially old people at present, old
Fundus flavimaculatus pathological changes, Myopia fundus flavimaculatus pathological changes, also glaucoma.The complication of diabetes patient is body in quite a few people
Eye, causes blurred vision now, the most blind.In European and American areas, blind principal disease is caused to have old fundus flavimaculatus sick
Become, glaucoma, cataract, and diabetic retinopathy.Arthritis, heart disease and visual deterioration be to over 70 people
In directly contribute three big diseases of daily life and moving obstacle.Root is it was predicted that to the year two thousand twenty, will have the American of nearly 6,000,000
Blind or amblyopia.
The deposit of liquid or protein is in the upper and lower accumulation of fundus flavimaculatus, and eyeground macular edema will occur, make optical fundus
Macula lutea is thickening and swelling is got up.It changes retinal cell function of eyes, inspires inflammation and causes visual loss.Eyeground macular edema can
Can occur in retina cell or extracellular.The accumulation of extracellular liquid more often occurs, and clinical discovery is more.It and blood
The change of pipe-retina shielding has direct relation.
One of reason of disease causing eyeground macular edema is retinal vein occlusion, including retina cardinal vein or point
Prop up vein occlusion.The feature of retinal vein occlusion is that retinal vein expands enlargement, the inter-retinal hemorrhage of secondary, Yi Jiyin
Blood vessel blockage, blood supply insufficiency and cause retinal ischemia.
There is several methods that for controlling the blocking of retina cardinal vein.The effect of the most grid-like Photocoagulation is poor.Vitreous body
Interior injection hormone may cause a series of serious adverse side effect such as cataract, Bulbi hypertonia.VEGF antibody
The current side effect of intravitreal injection more relatively small.Control to eyeground macular edema has certain prospect.Have big
The intravitreal injection of VEGF antibody is reacted and inconspicuous by the macular edema patient of 30 about percent.Separately
Outward, intravitreal injection belongs to " invasive " method, needs specialty ophthalmic surgeons operation, somewhat expensive.The more important thing is that it is main
Acting on is that symptom management but can not be cured, and patient needs the most repeatedly to accept intravitreal injection.The treatment of this regular injections is often
It is often to need to adhere to maintaining throughout one's life the state of an illness, brings a lot of inconvenience to patient.
The macular edema that diabetes cause makes the macula area in the middle part of retina thicken, and is to cause mistake in diabetics
Bright most common disease.Diabetic Macular portion edema patient account for about 1 14 in diabetics.Diabetes
The property generation of macular edema is closely connected with the degree weight of diabetic retinopathy and pathological changes duration length.
Diabetic retinopathy, because the shielding of interior blood vessel-retina is destroyed and causes, causes in blood plasma leaking material to view
Around film.Macular edema or blood capillary ischemia can directly endanger central vision.
Suffer from the type-II diabetes crowd of about 5 years, have 10 macular edema occurs.Suffer from two type glycosurias
Sick in vicennial patient, occur that the probability of macular edema can increase to more than 30 percent.Suffers from a type glycosuria
The crowd of sick about 5 years occurs that the probability of macular edema is relatively low, but is suffering from a patients with type Ⅰ DM up to vicennial
In patient, the probability of macular edema also can increase to more than 30 percent.With the appearance macula area water of insulin in patient
Swollen probability is higher.Photocoagulation is the standard treatments controlling the macular edema that diabetes cause.But photocoagulation pair
A lot of patient's curative effects are not good enough.Current Therapeutic Method also has intravitreal injection hormone.It is well known that such therapy meeting
Having side effect, it is one of them that intraocular pressure such as may be caused to increase.
The intravitreous endothelial cell growth factor (ECGF) content of the macular edema patient caused in diabetes is relatively high.Therefore use
Intravitreous endothelial cell growth factor (ECGF) antibody treats the method for the macular edema that the treatment diabetes becoming universal cause.But
The intravitreal injection of long term repeatability can increase infectious endophthalmitis occurrence probability, becomes a big fraud of intravitreal injection
Sick.
In industrialized country, cause central area vision blind or the main disease of low visual acuity is exactly that old optical fundus is yellow
Pinta becomes, and is also degeneration.In the U.S., nearly 10,000,000 populations suffer from old fundus flavimaculatus pathological changes, the nearlyest two million peoples
Suffer from fundus flavimaculatus pathological changes in old age in later stage, also referred to as wet age fundus flavimaculatus pathological changes.Another is that dry age optical fundus is yellow
Pinta becomes, and belongs to the maculopathy of commitment.Dry age fundus flavimaculatus pathological changes mainly becomes because of the old and feeble macular tissues of people
Thin and pigment spot is deposited on macula area the two factor and is caused.
In addition to above-described several diseases, other diseases such as glaucoma etc., some operated eye, medicine, it is possible to
Macular edema can be caused.For diabetes or hypertensive patient, the most feasible method is its diabetes of systemic treatment and height
Blood pressure, to reduce this disease further destruction for optical fundus.Such as oral drugs.But after systemic treatment, oral medication regards
The medicine of Omental lesion, it is relatively low that its active component can enter amphiblestroid bioavailability.Additionally active component needs at retina
Reaching a certain amount of competence exertion therapeutic effect, the dosage oral for this needs to increase, if to have side effect to work as consumption big for medicine
Time, it is possible to cause the harmful effect to whole body.
Summary of the invention
The present invention is in order to overcome defect present in background technology, and provides a kind of group for treating eyeground macular edema
Compound and said composition application in treatment ocular disease.The present invention develops a new direction, has battalion with to whole body
Composition that foster health-care effect is free from side effects again, with optimum proportioning, reach to treat eyeground macular edema purpose.
This compositions being used for treating eyeground macular edema includes by weight percentage: (a) Polyphenols of 0.4% ~ 71%
Compound, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 0.6% ~ 93%, (c) ubiquinone or general of 0% ~ 97%
Alcohol, (d) docosahexenoic acid of 0% ~ 87% or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.
The described compositions being used for treating eyeground macular edema includes by weight percentage: (a) polyphenol of 0.4% ~ 71%
Compounds, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 0.6% ~ 93%, (c) of 0.6% ~ 97% is general
Quinone or pantothenylol, (d) docosahexenoic acid of 0.15% ~ 87% or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.
The described compositions being used for treating eyeground macular edema includes: (a) polyphenol compound of 25 ~ 800 milligrams,
(b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 25 ~ 1800 milligrams, (c) ubiquinone of 0 ~ 1000 milligram or
Pantothenylol, d) docosahexenoic acid of 0 ~ 2000 milligram or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.
The described compositions being used for treating eyeground macular edema also includes the vitamin A of 0 ~ 1000 IU, 0 ~ 1000 milli
Gram vitamin B, the vitamin C of 0 ~ 2000 milligram, the vitamin D of 0 ~ 5000 IU and the vitamin E of 0 ~ 800 IU, 0 ~ 40
The zinc of milligram, the magnesium of 0 ~ 900 milligram, the carotenoid material of 0 ~ 500 milligram.
That states is each for improving patient's vision stability intraocular pressure and minimizing eye for treating the compositions of eyeground macular edema
Class inflammation.
Described for treating the compositions of eyeground macular edema for treating eyeground macular edema.
The described compositions being used for treating eyeground macular edema has due to diabetes, hypertension, blood for treating patient
Pipe disease includes arteriosclerosis, all kinds of ophthalmics, cancer, optical fundus blood vessel disease, some rare disease, and smoking or ocular surgical cause
Eyeground macular edema and other ocular disease, described optical fundus blood vessel disease includes central retinal vein occlusion, retina
Branch vein blocks, old fundus flavimaculatus degeneration, glaucoma or the combination of several disease.
The described compositions for treating eyeground macular edema takes in internal approach in oral, eye drip, vitreous body
Injection, intravenous drip, external preparation for skin, without intestinal, intraperitoneal, Sublingual or implant.
The described compositions internal daily dose of absorption being used for treating eyeground macular edema is: the former Hua Qing of 30 ~ 300mg
Element, 30 ~ 600mg thioctic acid, 50 ~ 300mg ubiquinone, 100 ~ 1500 milligrams of docosahexenoic acid or its ethyl ester, and/or 20 carbon
Five olefin(e) acids or its ethyl ester.
The described antiinflammatory adding medical treatment effective dose for treating the compositions of eyeground macular edema further to patient
Preparation, antibiotic medicine is oral formulations, eye drop, unguentum or transdermal patch, or adds by endothelial cell growth factor (ECGF) anti-to patient further
Body based composition, or farther include laser coagulation therapeutic scheme.
There is advantages that
The present invention can prevent for the compositions and Therapeutic Method treating eyeground macular edema, stablize, controls or treat eye
End macular edema, strengthens optical fundus healthy.Simultaneously can also stablize intraocular pressure, keep or improve vision, alleviate various ocular disease or because of
Macular edema that operated eye causes and inflammation.Also treat diabetic complication, promote blood microcirculation, improve liver function.
Accompanying drawing explanation
Fig. 1 is that left eye suffers from the eyeground macular edema patient optical fundus optical coherence when not taking the compositions of this invention
Tomoscan (OCT) photo.
Fig. 2 is optical fundus optical coherence tomography (OCT) photo after the compositions of the same clothes for patients present invention.
Detailed description of the invention
Present embodiments provide for a kind of compositions treating eyeground macular edema, wherein need containing (a) Polyphenols chemical combination
Thing, (b) thioctic acid, dihydrolipoic acid, or its salt or amide compound, (c) ubiquinone or pantothenylol, (d) two dodecahexaene
Acid or its esterified compound and/or eicosapentaenoic acid or its esterified compound.
Polyphenol substance is one or more procyanidin polymers.Combination mixture can include following vitamin simultaneously:
A kind of or the mixture of its several vitamin in A, B, C, D, E.This component can contain mineral, such as zinc further, magnesium
Oxide, or its esters, can be one of them, it is also possible to the two combines.In some cases, this component contains and pharmaceutically may be used
The carrier mass accepted.
In an object lesson, this invention component is 25-800 milligram anthocyanidin polymer, and 25-1800 milligram sulfur is pungent
Acid, 0-2000 milligram docosahexenoic acid or its esterified compound and/or eicosapentaenoic acid or its ethyl ester chemical combination
Thing, 0-1000 milligram ubiquinone;In another object lesson, 30-300 milligram former Hua Qingsu polymer, 30-600 milligram sulfur is pungent
Acid, 100-1500 milligram docosahexenoic acid or its esterified compound and/or eicosapentaenoic acid or its ethyl ester chemical combination
Thing, and 50-300 milligram ubiquinone.
This component can do piece agent, capsule or liquid oral.
Another examples of implementation of this invention, contain only following component (a) polyphenolic substance of effective dose, and (b) sulfur is pungent
Acid, or lipoate, or lipoic acid polyacrylamide, (c) ubiquinone or pantothenylol;(d) docosahexenoic acid or its ethyl lipid chemical combination
Thing and/or eicosapentaenoic acid or its ethyl ester compounds;This composition further can also be containing from following vitamin and ore deposit
Material selects one or more: vitamin A, B, C, D, E, the oxide of zinc or salt, and/or the oxide of magnesium or salt.This group
Become to contain carotenoid material further, such as terpenoid.
Present invention provides the method processing and controlling macular edema.Provide maintenance optical fundus in one embodiment
Macular edema prevents its method deteriorated.
In another case study on implementation, it is provided that the method that eyeground macular edema patient is effectively treated.Fundus flavimaculatus water
Swollen cause is numerous, including: diabetes, optical fundus blood vessel disease, some drugs, some non-common disease or indivedual eyes hands
Art causes.Wherein optical fundus blood vessel disease includes optical fundus central retinal vein occlusion, and Branch Retinal Vein blocks, old
Macular degeneration, glaucoma, or several sick syndrome combined.
This component introduces the method for human body and includes: oral, if necessary can also intravitreal injection, external preparation for skin, quiet
Arteries and veins is injected, parenteral absorption, and intraperitoneal introduces, and Sublingual or be orally introduced does not limits for administering mode.
One Therapeutic Method example, the dosage of every day: 30-300 milligram Hua Qingsu polymer, 30-600 milligram thioctic acid,
100-1500 milligram docosahexenoic acid or its esterified compound and/or eicosapentaenoic acid or its esterified compound,
With 50-300 milligram ubiquinone.
In some cases, the method processing, control or treating, also include allowing patient take the photograph in addition to taking this component simultaneously
Taking anti-inflammation drugs, this anti-inflammation drugs can be non-hormone antibiotic medicine.In the case of other, it is also possible to be the antibiotic medicine containing hormone
Thing.In some cases, precursor anti-inflammation drugs is used.Antibiotic medicine can be administered orally, and as collyrium external, can be paste, pass through
Transdermal patch, or through cornea, sclera/conjunctiva by way of.
In examples of implementation, Therapeutic Method can also include introducing vascular endothelial growth while taking this component
Factor antibody, or farther include to introduce carbonic anhydrase inhibitors or its early stage medicine.In examples of implementation, it is simultaneously introduced
Medicine can also include immunosuppressant, or its early stage medicine.In examples of implementation, Therapeutic Method also includes eye
Operation, such as laser light freezing method or photodynamic therapy.
The invention provides data to demonstrate stated component and can effectively treat eyeground macular edema and eliminate relevant
Symptom.
" effective dose " is that the quantity taken in or be administered can sufficiently achieve the benefited or preferable effect of patient.One has
Effect dosage can be that one or many is taken in, and takes or the dosage of application.Conduction in human body, or release depends on a lot
Parameter, the time interval used including each dosage unit, the bioavailability of therapeutic substance agent, introducing method.It is appreciated that
The effective dose level of the healing potion of the present invention depends on many factors, the activity of the component such as used, the biology of component
Availability, introducing method, patient age and body weight, health status, sex, the diet of patient, Time of Administration, drain degree, with
The medicine of Shi Bingyong, the medicine meanwhile taken because of other diseases, patient's coincident with severity degree of condition, treat and absorption mode.
Therapeutic dose can carry out the calculating of titration type by optimization safety and curative effect.Very common practice: try from test tubes and human body
Test and find out the relation of dosage and curative effect thus to the guidance that is provided with of the suitable dosage of patient.Animal test model typically may be used
With the effective dose for guiding treatment disease.These consider, and effective formula is the freshest with the process of absorption
Well known, and be described on the textbook of standard.Determining meaning with this consistent, treatment effective dose is a dosage here
Be enough to treat special disease, or in other words obtain response pharmacologically.
Here noun " is taken in " or the meaning of " administration " or " introducing " is including, but not limited to following manner: eye to
Medicine, oral, take in (intramuscular injection, peritoneum introduces, and sucks, and introduces, intravenous drip, ocular injection) through skin without intestinal
Nose spraying sucks, vagina, anus, Sublingual, urethra or external preparation for skin.External application can be jelly, ointment, cream, spraying, medicament for the eyes
Etc. form, various formula can be made, traditional harmless nontoxic medical science acceptable carrier or excipient may be contained, this
Depend on medicine incorporation way.This invention is not limited to above-mentioned absorption mode, formula or the time interval of administration.
Here " process " or " treatment " disease mean that 1) for had this disease tendency but the most do not produce
In the case of symptom, prophylactic generation;2) suppression disease limits disease development;3) disease or the contracting of its symptom are improved or make
Little;Process or treatment is to obtain the benefit of medicine or preferable effect, including clinical trial result.The purpose of the present invention,
Benefit or desired result can include, but are not limited to: alleviate, and relax or improve one or more symptom, reducing other medication
Dosage or growth are treated the interval time between treatment and are reached more preferable curative effect or maintain the state of an illness, reduce the serious journey of disease
Degree, stablizes current disease condition, slows down delay advancing of disease, and improvement alleviates the state of an illness and is partly or entirely eased no matter
It it is the alleviation that can detect or can't detect.For one side, the treatment of macular edema includes reducing or maintaining fundus flavimaculatus
Macula lutea layer thickness (can be measured by optical fundus optical coherence tomography (OCT)) after edema, is improved or maintains vision to make
No longer deteriorate.For Ling Yifangmian, the treatment of macular edema includes repairing eye ground blood vessel wall, improves ocular angiogenesis micro-
Circulation.The treatment of eyeground macular edema also includes slowing down fundus flavimaculatus degeneration.Additionally it is also possible to improve the eye of glaucoma
Pressure, alleviates the oxidation of optic cell and tissue.
Eyeground macular edema is owing to causing around hydrops in each layer of the retina of eye ground central fossa.Owing to changing
Become optical fundus functioning cell relatedness and encouraged inflammation reparation reaction, thus having reduced or DE.This is fundus flavimaculatus pair
In optical fundus environmental change have clinically relevant type reaction, in most of the cases, macular edema and blood vessel-retina screen
The change of barrier has relation.Eyeground macular edema continues half a year more than, it is believed that is chronic eyeground macular edema, needs to control
Treat.
The present invention includes four special combination being certified as safe component clinically: 1) polyphenolic substance, the most former
Hua Qingsu, 2) thioctic acid 3) ubiquinone, 4) Omega-3 fatty acid, including docosahexenoic acid or its esterified compound and/
Or eicosapentaenoic acid or its esterified compound.These materials can effectively treat fundus flavimaculatus with the combination of optimum proportioning
Edema.It is contemplated that each component has its advantage.When put together, they reduce the penetrance of blood vessel wall,
Protection retinal epithelium and endotheliocyte, increase microcirculation, reduces the side effect that VEGF is risen.Come further
Say that the formula of this invention oral may have certain help to the patient of diabetes and hypertension.
Thioctic acid, and its reduction-state, dihydrolipoic acid, it is possible to reduce the permeability that blood vessel is too high, reduce oxygen oneself
By being formed of base and being formed of cytochrome C.As potent antioxidant, it is possible to prevent epidermis and the endotheliocyte of blood vessel wall
Oxidation.Thioctic acid has water solublity and has again oil-soluble, and it can pass blood-retina shielding and enter optical fundus portion.By mouth
Taking mode, when taking a certain amount of, its bioavailability on optical fundus can reach the level for the treatment of.
Polyphenolic substance, such as catechol, epicatechin, multiclass Hua Qingsu can increase microcirculation, lowers microangiopathy
Become, the microangiopathies that particularly diabetes cause.
Europe rice Jia (Omega) fatty acid especially Europe rice Jia-3 fatty acid, from another point of view, has the property of anti-angiogenic regeneration
Matter thus protect optical fundus, it reduces the revascularization that produces because of vascular endothelial cell growth factor, keeps the sound of blood vessel.
Omega-3 fatty acid and the synergism being combined with the endothelial cell growth resisting factor of thioctic acid.
Ubiquinone generally exists on optical fundus, and its content increases with the age and reduces.It is known that road is when Omega-3 fat
Acid, and acetyl-L-carnitine and ubiquinone combine and can treat age phase in early days by improving mitochondria dysfunction
Closing fundus flavimaculatus degeneration, the present invention is then that ubiquinone, omega-3 fatty acid, thioctic acid and multiclass anthocyanidin are combined,
Need not L-acetylcarnitine and can play same purpose even preferably effect.
Therefore An embodiment provides a composition, containing following composition, each component reaches effective
Amount, (a) polyphenol compound, particularly extracts from plant.(b) thioctic acid, dihydrolipoic acid, and/or its salt or its acyl
Amine;(c) ubiquinone or pantothenylol;(d) docosahexenoic acid or its esterified compound and/or eicosapentaenoic acid or its ethyl
Ester compounds.
Polyphenolic substance, such as procyanidin are antioxidant.
" polyphenolic substance " refers at least two phenol structures, many phenolate on a construction unit in one embodiment
Compound is the most rarely known by the people.Can synthesize, or obtain by purifying from natural environment.Polyphenol in the present invention
Compound is from natural source.Polyphenolic substance includes but not limited to Hydrolysable Tannins acid, (glucose, or other are sugared or cyclic alcohol
Gallic acid ester) and phenolic group propionic ester, such as lignin, flavone compound, condensed tannin and phenolic acid.
Chromocor compound including, but not limited to flavonol, (or flavane-3 alcohol), flavone, anthocyanidin, isomery flavone, and
Neoflavone.In an object lesson, flavanol compound is procyanidin, or procyanidin apoplexy due to endogenous wind is a kind of.
The former Hua Qingsu of procyanidin class, also referred to as oligomer, or OPCs, refer to former Hua Qingsu, former Hua Qingsu analog,
Poly-lignins etc., especially such as flavane-3 alcohol (such as catechol, epicatechol and/or its polymer) and flavone (such as Pseudotsuga menziesii (Mirbel) Franco
Element), epicatechol structure is as follows:
Catechol structure is as follows:
Alpha-lipoic acid, sulfuration octanoic acid, or LIPOIC ACID, also it is called (R)-5-(1,2-disulphanes-3) valeric acid structure
As follows:.
Dihydrolipoic acid is 6, and 8-dimercapto octanoic acid structure is as follows:
The amide of thioctic acid can be, but not limited to, di alkylamino group ethylamino-lipoate.
Ubiquinone structure is as follows:
Pantothenylol is the reduction form of ubiquinone.
Docosahexenoic acid and eicosapentaenoic acid are all Europe rice Jia fatty acids, namely unsaturated fatty acid, double bond
Position is from the beginning of the 3rd of carbochain end the carbon atom..
The structure of docosahexenoic acid (DHA):
The structure of eicosapentaenoic acid (PHA) is as follows:
In one embodiment, this component contains vitamin further, can choose from following vitamin.Vitamin A,
B, C, D, E or a combination thereof.
In another embodiment, this component contains mineral, such as zinc, magnesium etc. further, can be oxide or salt
Form.
Another embodiment, on the one hand this invention component contains only basis and is: a) polyphenol compound, b) sulfur is pungent
Acid or dihydrolipoic acid, or its salt or amide, c) ubiquinone or pantothenylol, d) docosahexenoic acid or its ethyl ester and/or 20
Carbon 5 alkene acid or its ethyl ester.
On the other hand this component can also contain vitamin, mineral or its combination.
On the other hand this component can also contain carotenoid material, such as terpenoid, particularly can penetrate blood vessel-
The terpenoid of retina shielding.
The meaning of " composition substantially " or " containing only " is to get rid of those character changing this invention component in this patent
Composition.On the one hand, the fundamental property of this invention component includes biological effectiveness and avirulence.On the other hand, the base " contained only "
This character also includes that this component at least some of can pass through blood-retina barrier.This component does not contains more substantial amounts of plants
Extract, such as Pericarpium Citri tangerinae, Bulbus Allii, curcumin, Ye Xiang, black pepper, Cortex cocois radicis.On the one hand, this component does not contains considerable amount of following
The part of full fruit, such as Fructus Lycopersici esculenti, Brassica oleracea L. var. botrytis L., Chinese cabbage, Herba Spinaciae, and Radix Dauci Sativae.The component of this invention does not contains substantial amounts of Monas cuspurpureus Went
Rice, spermine acid, L-Tyrosine, biotin, choline, inositol, methyl yellow acyl methane, para-amino benzoic acid.Hyaluronic acid, iodine or
Its salt.The meaning less than a large amount of components referred to here is the 50% of component, 40%, 30%, 25%, 20%, 15%, 10%, 9%,
8%, 7%, 6%, 5%, 4%, 3%, 2%, 1%, 0.5%, 0.1% or 0.01% (weight by weight).
In one embodiment, this component contains pharmaceutically acceptable carrier further." pharmaceutically can connect
The carrier being subject to " cover any or all of solvent, disperse medium, coating, antibacterial and antifungal agents, isotonic agent, inhale
Receive the analog such as delayer.This kind of medium is used to be well-known for pharmaceutically active substance.Except with active component not
The reagent joined or avoid or medium, they uses in therapeutic component are ripe, and activity helper component can also add this
Component.
In a specific embodiments, this component contains about 20-800 milligram polyphenolic substance, such as procyanidin,
25-1800 milligram thioctic acid, dihydrolipoic acid or its salt or its amide,
20-1000 milligram ubiquinone or pantothenylol,
100-2000 milligram docosahexenoic acid or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.
The quantity of a kind of situation polyphenolic substance a) namely procyanidin is 25-200 milligram, 25-300 milligram, 25-
400 milligrams, 30-800 milligram, 30-600 milligram, 30-400 milligram, 40-300 milligram, 40-400 milligram, 40-800 milligram,
50-200 milligram, 50-300 milligram, 50-400 milligram, 50-800 milligram, 60-200 milligram, 60-300 milligram, 60-400 milligram,
60-800 milligram, 65-400 milligram, 65-800 milligram, 70-400 milligram, 70-600 milligram, 70-800 milligram, 80-500
Milligram, 80-800 milligram, 100-800 milligram, or 100-600 milligram.
A kind of situation, b) thioctic acid or dihydrolipoic acid or its salt, or the quantity of its amide is 25-1800 milligram, 25-
1500 milligrams, 25-1000 milligram, 25-800 milligram, 30-1800 milligram, 30-1600 milligram, 30-1200 milligram, 30-
1000 milligrams, 30-800 milligram, 50 800 milligrams, 50 1000 milligrams, 100 1000 milligrams, 100 1800 milligrams, 150 900
Milligram, 150 1500 milligrams, 150 1800 milligrams, 200 600 milligrams, 200 800 milligrams, 200 1000 milligrams, 200 1800
Milligram, 250 1800 milligrams, 250 900 milligrams, 250 1500 milligrams, 300 800 milligrams, 300 1800 milligrams, 300 1500
Milligram, 350 1000 milligrams, 400 1800 milligrams, 450 1800 milligrams, 500 1800 milligrams, 550 1800 milligrams or 600
1800 milligrams.
On the one hand, c) quantity of ubiquinone or pantothenylol is 0 1000 milligrams, 0 300 milligrams, 0 600 milligrams, 35 800 millis
Gram, 35 1000 milligrams, 40 600 milligrams, 40 1000 milligrams, 50 500 milligrams, 50 800 milligrams, 50 1000 milligrams, 60
1000 milligrams, 60 800 milligrams, 80 800 milligrams, 80 400 milligrams, 80 500 milligrams, 80 600 milligrams, 100 300 millis
Gram, 100 600 milligrams, 100 800 milligrams, 150-1000 milligram, 150 800 milligrams, 200 1000 milligrams, 220 800 millis
Gram, or 250 1000 milligrams.
D) docosahexenoic acid or its ethyl ester and/or eicosapentaenoic acid or its ethyl ester or merge together
Quantity be 0 2000 milligrams, 0 1000 milligrams, 100 600 milligrams, 100 1800 milligrams, 120 1000 milligrams, 120 2000
Milligram, 150 800 milligrams, 150 2000 milligrams, 200 2000 milligrams, 250 2000 milligrams, 400 2000 milligrams, 400
1500 milligrams, 500 1500 milligrams, 500 2000 milligrams, 600 1800 milligrams, 700 1800 milligrams, 800 1500 milligrams,
800 2000 milligrams or 1,000 2000 milligrams.
In another embodiment, this invention component contains: 30 300 milligrams of (a) polyphenolic substances, 30 600 milligrams (b)
Thioctic acid, or dihydrolipoic acid, its salt or its amide, 50 300 milligrams of (c) ubiquinone or pantothenylol, 100 1500 milligrams (d)
Docosahexenoic acid or its ethyl ester, and eicosapentaenoic acid or its ethyl ester.
In another embodiment, this invention component contains: 25 800 milligrams of former Hua Qingsu oligomer, 25 1800 milligrams
Thioctic acid, 100 2000 milligrams of docosahexenoic acid and eicosapentaenoic acid, 20 1000 milligrams of ubiquinone.
In any one embodiment above-described, component farther includes following at least one of which: the upper limit reaches
1000 IU vitamin A, the upper limit reaches 1000 milligrams of vitamin Bs, and the upper limit reaches 2000 milligrams of vitamin Cs, and the upper limit reaches 5000IU
Vitamin D, the upper limit reaches 800IU vitamin E, and the upper limit reaches 40 milligrams of equivalent being equivalent to zinc, and the upper limit reaches 900 milligrams quite
In the equivalent of magnesium, the upper limit reaches about 500 milligrams of terpenoids.
In one embodiment, this invention component contains: 0.4%-71% (weight by weight) former Hua Qingsu, 0.6%-93% (weight/
Weight) thioctic acid, 0.6%-97% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0.15%-87% (weight by weight) ubiquinone.
In one embodiment, this invention component contains: 2%-55% (weight by weight) former Hua Qingsu, and 2%-70% (weight by weight) sulfur is pungent
Acid, 10%-60% (weight by weight) docosahexenoic acid and merging eicosapentaenoic acid, 2%-45% (weight by weight) ubiquinone.
In one embodiment, this invention component contains: 2%-55% (weight by weight) former Hua Qingsu, and 2%-70% (weight by weight) sulfur is pungent
Acid, 15%-50% (weight by weight) docosahexenoic acid and merging eicosapentaenoic acid, 0.5%-40% (weight by weight) ubiquinone.
In one embodiment, this invention component contains 3%-60% (weight by weight) former Hua Qingsu, and 3%-70% (weight by weight) sulfur is pungent
Acid, 1%-50% (weight by weight) docosahexenoic acid and merging eicosapentaenoic acid, 0.2%-40%(weight by weight) ubiquinone.
In one embodiment, this invention component contains: 4%-60% (weight by weight) former Hua Qingsu, 4%-70% (weight by weight) sulfur
Octanoic acid, 1%-50% (weight by weight) docosahexenoic acid and merging eicosapentaenoic acid, 0.2%-30% (weight by weight) ubiquinone.
In one embodiment, this invention component contains: 5%-65% (weight by weight) former Hua Qingsu, 5%-70% (weight by weight) sulfur
Octanoic acid, 1%-50% (weight by weight) docosahexenoic acid and merging eicosapentaenoic acid, about 0.2%-25% (weight by weight) ubiquinone.
In one embodiment, this invention component contains: 10%-65% (weight by weight) former Hua Qingsu, 10%-70% (weight by weight) sulfur
Octanoic acid, 5%-45% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0.2%-25% (weight by weight) ubiquinone.
In another embodiment, this component contains: 15%-60% (weight by weight) former Hua Qingsu, and 15%-70% (weight by weight) sulfur is pungent
Acid, 5%-45% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0.2%-25% (weight by weight) ubiquinone.
In another embodiment, this component contains: 20%-65% (weight by weight) former Hua Qingsu, 10%-70% (weight by weight) sulfur
Octanoic acid, 0%-30% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0%-25% (weight by weight) ubiquinone.
In another embodiment, this component contains: 10%-60% (weight by weight) former Hua Qingsu, and 20%-60% (weight by weight) sulfur is pungent
Acid, 5%-30% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0.2%-20% (weight by weight) ubiquinone.
In another embodiment, this component contains: 25%-60% (weight by weight) former Hua Qingsu, and 10%-60% (weight by weight) sulfur is pungent
Acid, 10%-30% (weight by weight) docosahexenoic acid and eicosapentaenoic acid, 0.2%-20% (weight by weight) ubiquinone.
In certain embodiments, former Hua Qingsu, thioctic acid, docosahexenoic acid and eicosapentaenoic acid and ubiquinone combine
Account for together whole component quantity be at least 10%(weight by weight), or at least 15%, 20%, 25%, 30%, 35%, 40%, 45%,
50%, 60%, 70%, 80% or 90%(weight by weight).
Lower list 1 provides the dosage range of daily this component and illustrates:
Table 1 recipe ingredient scope citing daily
Composition | Enumerate compositing range: |
Omega-3 fatty acid | 0 1500 milligrams |
Thioctic acid | 30 600 milligrams |
Ubiquinone | 0 300 milligrams |
Former Hua Qingsu | 30 300 milligrams |
Vitamin D | 0 – 1500 IU |
Compound vitamin B | 0 800 milligrams |
Vitamin C | 0 500 milligrams |
Vitamin A | 0 – 1000 IU |
Vitamin E | 0 – 400 IU |
Zinc oxide | 0 35 milligrams |
Magnesium oxide | 0 450 milligrams |
Terpenoid | 0-500 milligram |
There is provided the using method of this invention different component collocation.These components can be prevented, stable and maintenance
And/or treatment eyeground macular edema, and can effectively improve vision, maintain intraocular pressure, draw by central retinal vein occlusion
Rise glaucoma have certain curative effect, slow down fundus flavimaculatus degeneration and/or reduce inflammation, moreover it is possible to treat or improve other one
A little diseases, orphan disease or operated eye and the macular edema that causes.
Therefore, in one embodiment, it is provided that to one Therapeutic Method of eyeground macular edema patient, it is simply that allow clothes for patients use
The effective dose of this invention said components of therapeutic effect can be reached.Provide the most in one embodiment by taking this group
Divide the effective dose with response to treatment, the method that eyeground macular edema patient's vision can be improved.
Thering is provided method in another embodiment is that to reduce fundus flavimaculatus sick by taking this invention component effective dose
The inflammation of people.
A kind of situation, fundus flavimaculatus patient may be due to but is not limited to diabetes or optical fundus blood vessel disease.Optical fundus blood
The initiation of pipe disease is probably due to the blocking of eye ground central vein, and eye ground branch vein blocks, it is also possible to due to
Old fundus flavimaculatus degeneration, glaucoma or several disease cause altogether.Be also likely to be operated eye or other not
Common disease and indirectly cause.
A kind of situation, total daily dose is as follows: 30 300 milligrams of former Hua Qingsu, 30 600 milligrams of thioctic acid, and 100 1500
Milligram docosahexenoic acid and eicosapentaenoic acid, 50 300 milligrams of ubiquinone.
In one embodiment, day takes in composition and intake is: 30 300 milligrams of former Hua Qingsu, 30 600 milligrams of sulfur
Octanoic acid, 100 1500 milligrams of docosahexenoic acid and eicosapentaenoic acid, 50 300 milligrams of ubiquinone, and at least following ingredients
One of: the upper limit is up to 1000IU vitamin A, and the upper limit is up to 800 milligrams of vitamin Bs, and the upper limit is up to 1000 milligrams of vitamin Cs, on
Limit for height reaches 2000IU vitamin D, and the upper limit is up to 400IU vitamin E, up to 35 milligrams amounts being equivalent to zinc of the upper limit, and the upper limit is up to
450 milligrams of amounts being equivalent to magnesium, the upper limit reaches 500 milligrams of terpenoids.
In some cases, patient can take in anti-inflammation formulation or its early stage medicine for the treatment of effective dose further, it
Can be eye drop, the unguentum of skin, can transdermal patch or grafting treatment.Patient can also take in anti-interior
The antibody of skin growth factor, can use non-bowel to take in way.In other cases, patient can accept ocular surgical,
The most radium-shine photic coacervation.
In above-mentioned all embodiments any one, the preparation of this invention component can be tablet, capsule, or is liquid, or
For eye drop, or it is emulsifiable paste, or is the patch that can penetrate skin, or implantation preparation.
Component administering mode or the absorption vivo approaches of the present invention can be oral, and eye vitreous is injected, external, tongue
Under, buccal, nasal cavity, feed without intestinal, intramuscular injection, peritoneum, vein or subcutaneous injection, mouthspray or nose spraying.Should
Component can by according to dosage according to take in internal in the way of do formula.
Can be with generally for the tablet of instant component (may contain adjuvant, or without adjuvant) or hard capsule or soft capsule
Known to method prepare, if requirement can also be covered by usual way peplos, internal component can be with sustained release.At this
This active component of the solid dosage forms of sample needs and at least one inert diluent mixes, such as but not limited to lactose, sucrose and shallow lake
Powder.Such dosage form is likely to containing the lubricant of other material, such as tablet in addition to inert diluent, tableting aids example
Such as magnesium stearate, rice flour and crystallite celluloid.Capsule, tablet or granular dosage form, it is also possible to containing buffer agent.Releasing of active component
Putting can also be only in certain section retards release of intestinal.Those components can be mixed in polymer or cured preparation.
Similar same dosage form solid constituent is used as lactose and high molecular polymerization ethylene glycol as soft, the filling of hard capsule
Agent.
Liquid component can also be with known method and the liquid pharmaceutically or accepted on health product and health medicine
Preparation is prepared.
If it is required, the component of the present invention can be incorporated to slow release or Targeting delivery system.Such as polymeric matrix,
Liposome, and microsphere particle.These can pass through bacteriological filtration filter sterilization, or with being dissolved in the disinfectant of sterilized water,
Or put into before use in the injectable media of sterilization.
This invention component can make granule, can add or be not added with adjuvant, and patient can directly take or component is added
In the liquid being suitable for, patient drinks the liquid containing component.This granule can contain effervescent tablet composition, and component so can be helped to have
It is dispersed in liquid medium to effect.
The mode of taking of this invention composition can be being used in combination with above-mentioned one or more preparations of preparation.
Without departing under the basic purpose of the present invention and obvious respects, embodiment and pharmaceutical formulation and instructions of taking are all
Can more known technical methods with on the basis of improve.
It is numerous that this component is released into internal mode, as oral, eye drop, system be released into (example is transdermal formula, nasal cavity,
Or suppository), parenteral (such as intramuscular, intravenous injection or subcutaneous).In some case, the method for being released into is oral, daily
Depending on number of times can be according to different factors such as state of an illness weights.Oral prescription can be tablet, granule, capsule, semi-solid, powder,
Slow release prescription, liquid, suspension, spraying or other suitable methods.Also has inhalation in addition.
Recipe and the selection of component, be released into internal mode, bioavailability, and treatment target the most relevant.Mouthful
Clothes are modal to take mode.The prescription that can be administered orally common are solid such as tablet, capsule, granule etc..But special
In the case of, oral soft capsule or liquid phase are to being more suitable for.
The component of the present invention can be containing the adjuvant of solid drugs, such as starch, celluloid, Pulvis Talci, glucose, sugarcane
Sugar, lactose, gelatin, Fructus Hordei Germinatus, rice flour, flour, whiting, silica gel, magnesium stearate, glycerol monostearate, sodium stearate, chlorine
Change sodium, drying defatted milk, and similar substance etc..Liquid or semi-solid adjuvant can from but be not limited only to following material select,
Glycerol, water, propylene glycol, ethanol, and all kinds of oil, including oil, animal oil, vegetable oil, or the oil of synthesis, Oleum Arachidis hypogaeae semen, Oleum Glycines, sesame
Oleum Sesami or mineral oil, emulsifying agent, concentrating agents, wax etc..Liquid-carrier, particularly prepares injecting fluid, including water, and saline,
G/W and glycerol etc..
The consumption of this component or effective dose can determine with prototype version, can be according to personal considerations, also can be according to its effect, toxicity
Learn data and this component is single use or is used in combination with other medicines or Therapeutic Method and changes.As for animal,
Its method can further determine the effect of this component.
Absorption method mediating recipe amount depends on therapeutic purposes, treated target cell and treated object.Can once or
Repeatedly take in.Concrete scheme needs to select as the case may be.
Said composition composition can be by oral, eye drop, non-bowel or anapnotherapy.Can be tablet, buccal tablet,
Grain, capsule, pill, ampoule, suppository and aerosol.Can also be aqueous or the suspension of nonaqueous dosage forms, solution, emulsion, sugar
Slurry, granule or powder face.Other medicine activity component, or various ingredients can also be contained.
More specifically, this patent component can be active component, can be conducted into internal with matched therapeutic modality, as
Oral, nasal-cavity administration, external application (includes transdermal patch, aerosol, oral cavity, Sublingual), parenteral conduction (include subcutaneous, intramuscular,
Intravenous, in skin etc.) and pulmonary administration.The absorption mode of this component and dosage can change according to age and the state of an illness.
This component needs this component is manufactured into the patch or sucker that can adhere for preparing medicament transdermal patch method,
Medicine slow release enters internal through skin absorption.For this angle, penetration enhancer can be used to increase medicine
Absorb.The manufacture of transdermal patch has a detailed description in following patent.U.S. Patent No. 5,407,713.; U.S.
Patent No. 5,352,456; U.S. Patent No. 5,332,213; U.S. Patent No. 5,336,168;
U.S. Patent No. 5,290,561; U.S. Patent No. 5,254,346; U.S. Patent No. 5,164,
189; U.S. Patent No. 5,163,899; U.S. Patent No. 5,088,977; U.S. Patent No. 5,
087,240; U.S. Patent No. 5,008,110; and U.S. Patent No. 4,921,475.
The component of the present invention may also be used for being for preparing treatments for the medicament of eyeground macular edema, prepares the side of the medicine of this component
Method and technology have been well known.
Above-mentioned component, including the case study on implementation that many is special, can use the medicine preparation production process of standard
Preparation, it is possible to treat disease as described herein with by the medication known to the world of medicine.
The examples below is used for illustrating this patent, but the invention is not limited in these examples.
One woman of 67 years old, due to left eye central retinal vein occlusion, began with eyeground macular edema in 2005,
Two had had been found that little glass-film wart at that time.Her blood item checks: low density cholesterol, blood glucose and blood triglyceride are higher than
Normal value,
Immediately at her left eye injection cortisone after optical fundus expert doctor inspection, eyeground macular edema disappears, but eye
Pressure is increased to 35-40mmHg, and doctor prescribed prescription collyrium controls intraocular pressure.Nearly her left eye of six months begins with cataract,
Quickly develop into the invisible thing of left eye, under doctor advised, do cataract operation.Post operation has found eyeground macular edema
Through developing into extremely serious degree.One optical fundus expert advice intravitreal injection Arastin (Avastin), this makes macula lutea water
Swell and disappeared in one month, but after 2-3 month, macular edema is returned to serious conditions, it is necessary to injection is (such as Fig. 1 institute again
Show), this photo is photographed in June, 2008, when being that eyeground macular edema recurs again after intravitreal injection Arastin 3 months
Shooting, macular edema is high-visible in this picture.Vision at that time is 20/40.Intraocular pressure is 35 mmHg.Immediately at glass
Glass internal injection Arastin, keeps normal, arrives 3 months within one month, edema recurs, and within the most every 3 months, edema is multiple
Send out, need again to repeat to accept intravitreal injection treatment.This patient accept intravitreal injection treatment before and after as long as five years.Show
Injection Arastin appearance again of eyeground macular edema after three months.The doctor told she, Arastin can maintain, but not
Can cure macular edema, this injection is by with her remaining years.Every three months needs injection, and such situation is at the beginning of 2005 the
Start after being once diagnosed as eyeground macular edema, continue for nearly five years.
In October, 2009, this latter two month of patient injection starts to take the component of the present invention, once a day, after four months
Time to this injection again goes to see the doctor.
Ophthalmologist finds that her vision is greatly improved.Current eyeground macular edema does not recur.Therefore this is that she is near
Through four months without again injecting after injecting Arastin for the first time over 5 years.In January, 2011, reexamine,
The most do not inject Arastin, do not find eyeground macular edema, vision 20/20, intraocular pressure 10mmHg.And when 2005
Vision is 20/40.So far triennium is not injected, and remains in that normal, (as in figure 2 it is shown, OCT photo was in 2011 one
Month), patient goes to see ophthalmologist routinely, arrives again the time of intravitreal injection, but is to take joining of the present invention specifically
Fang Hou.In terms of OCT photo, eyeground macular edema has disappeared, and therefore need not the injection of Arastin.Vision 20/20, eye
Press 9 mmHg.So far, the recipe ingredient of the daily present invention.Within 3 years, do not need to inject again, and macular edema occurs the most again.
89 years old patients women, she 70 years old time be diagnosed as type ii diabetes, she keeps on a diet under guidance and reduces sugar
Take the photograph, within 2009, her vision is decreased obviously, thus goes to see optical fundus expert doctor, finds that two eyes have diabetes to draw
The macular edema risen.She see all linear type article all in wavy, her blood pressure is normal, low density cholesterol and three acid glycerols
Fat is normal, and within 2010, she starts to take the component of the present invention, takes every day, adheres to 3 months, and she finds to see the ripple of thing
Wave curve phenomenon without.Her eyeground macular edema is obviously improved, and vision has been recovered.
One 78 years old male patient was once diagnosed as moist fundus flavimaculatus degeneration in 2005, the most also found
There is eyeground macular edema.This patient receives the treatment of pupil thermotherapy (TTT) and processes, and within 2010, starts to take this
The component of invention once a day, is adhered to four months, then is gone to see the doctor, and his eye eyesight improves, and eyeground macular edema substantially subtracts
Few.
One 79 years old women, left eye accepts cataract operation at the beginning of suffering from cataract 2011, postoperative discovery left eye has optical fundus yellow
Speckle edema, vision only have 20/60. she start to take the component of the present invention, once a day, check after three months, macular edema
Disappearing, vision is 20/20.
Claims (11)
1., for treating the compositions of eyeground macular edema, said composition is made up of following component by weight percentage: 0.4% ~
(a) polyphenol compound of 71%, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 0.6% ~ 93%,
(c) ubiquinone of 0.6% ~ 97% or pantothenylol, (d) docosahexenoic acid of 0.15% ~ 87% or its ethyl ester and/or eicosapentaenoic
Acid or its ethyl ester.
2. for treating the compositions of eyeground macular edema, it is characterised in that: said composition is made up of following component: 25 ~ 800 millis
Gram (a) polyphenol compound, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 25 ~ 1800 milligrams, 0
(c) ubiquinone of ~ 1000 milligrams or pantothenylol, d) docosahexenoic acid of 0 ~ 2000 milligram or its ethyl ester, and/or 20 carbon five
Olefin(e) acid or its ethyl ester.
3., for treating the compositions of eyeground macular edema, said composition is made up of following component: (a) polyphenol of 0.4% ~ 71%
Compounds, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 0.6% ~ 93%, (c) of 0.6% ~ 97% is general
Quinone or pantothenylol, (d) docosahexenoic acid of 0.15% ~ 87% or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester, 0 ~
The vitamin A of 1000 IU, the vitamin B of 0 ~ 1000 milligram, the vitamin C of 0 ~ 2000 milligram, the vitamin D of 0 ~ 5000 IU
And 0 ~ 800 vitamin E of IU, the zinc of 0 ~ 40 milligram, the magnesium of 0 ~ 900 milligram, the carotenoid material of 0 ~ 500 milligram.
4., for treating the compositions of eyeground macular edema, said composition is made up of following component: (a) of 25 ~ 800 milligrams is many
Phenolic compound, (b) thioctic acid, dihydrolipoic acid, lipoate or the lipoic acid polyacrylamide of 25 ~ 1800 milligrams, 0 ~ 1000 milligram
(c) ubiquinone or pantothenylol, the d) docosahexenoic acid of 0 ~ 2000 milligram or its ethyl ester, and/or eicosapentaenoic acid or its second
Ester, the vitamin A of 0 ~ 1000 IU, the vitamin B of 0 ~ 1000 milligram, the vitamin C of 0 ~ 2000 milligram, the dimension of 0 ~ 5000 IU
Raw element D and the vitamin E of 0 ~ 800 IU, the zinc of 0 ~ 40 milligram, the magnesium of 0 ~ 900 milligram, the carotenoid thing of 0 ~ 500 milligram
Matter.
5. the compositions for treating eyeground macular edema as claimed in claim 1, it is characterised in that: described (a) polyphenol
Compounds is the procyanidin of oligomerization.
6. the compositions for treating eyeground macular edema as claimed in claim 1 improves patient's vision stability eye for preparing
Pressure and the purposes of minimizing all kinds of anti-inflammatory drugs of eye.
7. the compositions for treating eyeground macular edema as claimed in claim 1 is for preparing treatment eyeground macular edema medicine
The purposes of thing.
8. the compositions for treating eyeground macular edema as claimed in claim 1 has due to glycosuria for preparing treatment patient
Eyeground macular edema that disease, hypertension, angiopathy, smoking or ocular surgical cause and the use of other ocular disease medicines
On the way, described angiopathy is selected from arteriosclerosis, optical fundus blood vessel disease;Described optical fundus blood vessel disease is selected from central retinal vein
Blocking, Branch Retinal Vein blocks, old fundus flavimaculatus degeneration, glaucoma or the combination of several disease.
9. the compositions for treating eyeground macular edema as claimed in claim 1, it is characterised in that: described compositions is taken the photograph
Enter internal approach for oral, eye drip, intravitreal injection, intravenous drip, external preparation for skin, intraperitoneal, Sublingual or to implant.
10. the compositions for treating eyeground macular edema as claimed in claim 1, it is characterised in that: described compositions
Taking in internal daily dose is: 30 ~ 300mg procyanidin, 30 ~ 600mg thioctic acid, 50 ~ 300mg ubiquinone, 100 ~ 1500 milligrams
Docosahexenoic acid or its ethyl ester, and/or eicosapentaenoic acid or its ethyl ester.
11. for treating the compositions of eyeground macular edema, and described compositions is made up of following component by weight percentage:
(a) polyphenol compound of 0.4% ~ 71%, (b) thioctic acid, dihydrolipoic acid, lipoate or the thioctic acid acyl of 0.6% ~ 93%
Amine, (c) ubiquinone of 0.6% ~ 97% or pantothenylol, (d) docosahexenoic acid of 0.15% ~ 87% or its ethyl ester and/or 20 carbon five
Olefin(e) acid or its ethyl ester;Having the anti-inflammation formulation of effective dose further, described anti-inflammation formulation is selected from oral formulations, eye drop, unguentum
Or transdermal patch;Or add by endothelial cell growth factor (ECGF) antibody class compositions to patient further;Or farther include laser coagulation
Therapeutic scheme.
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