CN109364019A - A kind of eye-drops preparations and preparation method thereof for preventing and treating cataract - Google Patents
A kind of eye-drops preparations and preparation method thereof for preventing and treating cataract Download PDFInfo
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- CN109364019A CN109364019A CN201811324473.1A CN201811324473A CN109364019A CN 109364019 A CN109364019 A CN 109364019A CN 201811324473 A CN201811324473 A CN 201811324473A CN 109364019 A CN109364019 A CN 109364019A
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- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
Abstract
The present invention relates to a kind of for preventing and treating the eye-drops preparations of cataract, and by weight percentage, the eye-drops preparations includes following component: lanolin alkane type tetracyclic triterpenoid 0.1% ~ 10%；Matrix 0.5% ~ 90%；Surfactant 0.05% ~ 25%；Isotonic regulator 0.5% ~ 15%；Preservative 0.001% ~ 0.5%；Antioxidant 0.001% ~ 0.5%；Water 3% ~ 98%.Eye-drops preparations quality of the invention is stablized, and preparation process is simple and convenient, and has carried out pharmacodynamic evaluation.
Description
The application be 2016/8/22 the applying date, application No. is 2016106969925, invention and created name is a kind of use
In the divisional application of the patent of invention of the eye-drops preparations for preventing and treating cataract and preparation method thereof.
Technical field
The present invention relates to a kind of eye-drops preparations and preparation method thereof for preventing and treating cataract.
Background technique
It can cause crystalline lens metabolic disorder, cause crystallins to be denaturalized and muddiness occurs, referred to as cataract.It is most white
Cataract or glaucoma is geriatric disease, but also has children innately to suffer from this disease, somebody injured, inflammation or it is sick after there is cataract.
According to World Health Organization's incomplete statistics, there are about 1600~21,000,000 people by whole world cataract blind person.Cataract one
As the course of disease it is slow, be that disease incidence is highest in ophthalmology disease, and most dangerous, in the feelings for being not treated in time or not paying attention to prevention
It is easy to cause eyes damage even to blind under condition.
The treatment of cataract includes two aspects, first is that drug therapy, second is that operative treatment.Early stage and mid-term cataract are suffered from
Person can often wait until the maturity period by drug therapy, but a possibility that there is no complete healing at present, crystalline by surgical removal muddiness
Body restores eyesight, but since the structure of postoperative crystalline lens itself is destroyed, and loses the regulating power of its own, and there is
A possibility that multiple complications occur, therefore seeking protective agents curative for effect is the most important thing.
(3 β) -8,24- lanostadiene -3- alcohol, is commonly called as lanosterol, is in lanolin alkane type tetracyclic triterpenoid
One kind, the entitled lanosterol of English, No. CAS is 79-63-0, chemistry entitled 3 β-Hydroxy-8,24-
Lanostadiene, it has recently been found that medicament for the eyes 6 weeks containing lanosterol are applied to the dog with cataract, the tight of cataract can be reduced
Weight degree, improves lenticular transparency, illustrates lanosterol or the compound with shares activity molecule, can be white to treat
Cataract or glaucoma provides another treatment means, but eye-drops preparations relevant to lanosterol has not been reported.
Summary of the invention
Technical problem to be solved by the invention is to provide a kind of eye-drops preparations for being effectively prevented and treated cataract and its
Preparation method.
In order to solve the above-mentioned technical problem, the present invention adopts the following technical scheme:
It is a kind of for preventing and treating the eye-drops preparations of cataract, by weight percentage, by 0.1%~10% sheep
Hair rouge alkane type tetracyclic triterpenoid and 90%~99.9% auxiliary material composition.
Preferably, the accounting of the lanolin alkane type tetracyclic triterpenoid is 0.1%~5%, is more selected as
0.1%~2%.
Preferably, the lanolin alkane type tetracyclic triterpenoid is lanosterol.
Preferably, the auxiliary material is selected from surfactant, isotonic regulator, preservative, antioxidant, matrix, pH
One of regulator, penetrating agent, excipient, stabilizer, organic solvent, water are a variety of.
Wherein, surfactant is also known as solubilizer.
It is further preferred that the surfactant is selected from pegoxol 7 stearate, diethylene glycol mono-ethyl
Ether, Labraso, polyoxyethylene stearate (40) ester, polyoxyethylene (35) castor oil, 40 hydrogen of polyethylene glycol
Change one in castor oil, lecithin, Tween-80, ethyl alcohol, polyethylene glycol, carbomer, poloxamer and hydroxypropyl-β-cyclodextrin
Kind or several combinations.
In the present invention, the additive amount of the surfactant account for the eye-drops preparations gross mass 0.05%~
25%, preferably 0.1%~10%, most preferably 0.1%~5%.
It is further preferred that the isotonic regulator is selected from sodium chloride, potassium chloride, glucose, mannitol, the third two
The combination of one or more of alcohol, glycerine, boric acid, borax.
In the present invention, the additive amount of the isotonic regulator account for the eye-drops preparations gross mass 0.05%~
25%, preferably 1%~15%, most preferably 5%~12%.
It is further preferred that the preservative is selected from triethanolamine, boric acid, borax, sodium citrate, Metagin
Ester, ethylparaben, propylben, ethyl hydroxy benzoate, phenylmercuric nitrate, benzalkonium chloride solution, ethyl hydroxy benzoate, benzene prick chlorine
The combination of one or more of ammonium, benzalkonium bromide, chlorhexidine acetate, polyquaternium, anesin, benzyl carbinol, thimerosal.
In the present invention, the additive amount of the preservative accounts for the 0.0001%~1% of the eye-drops preparations gross mass, excellent
It is selected as 0.0001%~0.1%, most preferably 0.0001%~0.02%.
It is further preferred that the antioxidant is selected from sodium thiosulfate, sodium pyrosulfite, sodium hydrogensulfite, Asia
Sodium sulphate, natrium adetate, Butylated Hydroxyanisole, Butylated Hydroxytoluene, alpha-tocopherol, four sodium acetate of cyclohexanediamine, N- hydroxy-ethylenediamine three
In acetic acid, six acetic acid of diethyl triamine, two mercapto ethyl glycines and ethylenediamine tetra-acetic acid, arabo-ascorbic acid and its sodium salt, thiocarbamide
One or more of combinations.
In the present invention, the additive amount of the antioxidant accounts for the 0.0001%~1% of the eye-drops preparations gross mass,
Preferably 0.001%~0.1%, most preferably 0.01%~0.02%.
It is further preferred that the matrix is selected from yellow petroleum jelly, albolene, lanolin, atoleine, hyalomitome
Sour sodium, polyvinyl alcohol, carbomer, xanthan gum, chitosan, xylan, polyacrylic acid, sodium alginate, methylcellulose, hydroxypropyl first
The combination of one or more of cellulose, povidone.
In the present invention, the additive amount of the matrix accounts for the 0.5%~90% of the eye-drops preparations gross mass, preferably
1%~85%.
It is further preferred that the pH adjusting agent is selected from sodium hydroxide, hydrochloric acid, sodium acetate, sodium carbonate, bicarbonate
The combination of one or more of sodium, disodium hydrogen phosphate, sodium dihydrogen phosphate, boric acid, citric acid, sodium citrate.
In the present invention, the additive amount of the pH adjusting agent accounts for the 0~15% of the eye-drops preparations gross mass.
It is further preferred that the penetrating agent is selected from lecithin, Sodium Hyaluronate, lauryl sodium sulfate, N- first
Base pyrrolidones, deoxysodium cholate, hydroxypropyl-cyclodextrin, Laurocapram, disodium ethylene diamine tetraacetate, Tween-80, the third two
The combination of one or more of alcohol.
In the present invention, the additive amount of the penetrating agent accounts for the 0%~20% of the eye-drops preparations gross mass, preferably
0.05%~20%, most preferably 0.1%~0.5%.
Preferably, the stabilizer is cholesterol, soybean lecithin, lecithin, glyceryl monooleate, tristearin, polyethylene
The combination of one or more of alcohol, polyethylene glycol, hydroxypropyl methylcellulose, polyvinylpyrrolidone, poloxamer.
In the present invention, the additive amount of the stabilizer accounts for the 0%~90% of the eye-drops preparations gross mass, preferably
0.05%~10%, most preferably 1%~5%.
Preferably, the excipient is mannitol, dextran, lactose, galactolipin, chitosan, arginine, Portugal's first
Amine, cyclodextrin, gelatin, glucose, inositol, sucrose, trehalose, sorbierite, xylitol, albumin, peptone, soluble shallow lake
The combination of one or more of powder, dextrin, Arabic gum, hydroxymethyl cellulose, syrup.
In the present invention, the additive amount of the excipient accounts for the 0%~95% of the eye-drops preparations gross mass, preferably
0.1%~20%, most preferably 1%~10%.
Preferably, the organic solvent is one of chloroform, ethyl alcohol, acetone, dimethyl sulfoxide, ethyl acrylate or several
The combination of kind.
Preferably, the water is water for injection.
Preferably, the eye-drops preparations is eye drops, eye ointment, gel for eye use, ophthalmically acceptable freeze-dried instant piece or ophthalmically acceptable nanometer
Liposome.
Preferably, by weight percentage, the eye-drops preparations includes following component:
It is further preferred that by weight percentage, the eye-drops preparations includes following component:
In the present invention, when the eye-drops preparations is eye drops, by weight percentage, the eye-drops preparations includes
Following component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
In the present invention, when the eye-drops preparations is eye ointment, by weight percentage, the eye-drops preparations includes such as
Lower component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
It is further preferred that by weight percentage, the eye-drops preparations includes following component:
In the present invention, when the eye-drops preparations is gel for eye use, by weight percentage, the eye-drops preparations packet
Include following component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
Further preferably, by weight percentage, the eye-drops preparations includes following component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
In the present invention, when the eye-drops preparations is ophthalmically acceptable freeze-dried instant piece, the eye-drops preparations includes lanolin
Alkane type tetracyclic triterpenoid and excipient, the lanolin alkane type tetracyclic triterpenoid and the excipient
Mass ratio is 1:9~30, preferably 1:9~20, most preferably 1:10~15.
By weight percentage, the eye-drops preparations includes following component:
In the present invention, when the eye-drops preparations is ophthalmically acceptable nano liposomes, by weight percentage, described is ophthalmically acceptable
Preparation includes following component:
Preferably, by weight percentage, the eye-drops preparations includes following component:
It is further preferred that by weight percentage, the eye-drops preparations includes following component:
It is a further object to provide the systems of the eye-drops preparations for preventing and treating cataract described in one kind
The lanolin alkane type tetracyclic triterpenoid and the auxiliary material are uniformly mixed and obtain the ophthalmically acceptable system by Preparation Method
Agent.
It, should be the preparation method comprises the following steps: by the lanolin alkane type four when the eye-drops preparations is eye drops in the present invention
Ring triterpene compound and the surfactant are mixed to form the first mixture, and the preservative and the water are mixed
It closes and forms the second mixture, after first mixture and the second mixture stirring and dissolving, by pressure sterilizing
Up to the eye drops.
Preferably, the temperature of the pressure sterilizing is 100~130 DEG C, and the time is 20~40min.
It, should be the preparation method comprises the following steps: by the lanolin alkane type Fourth Ring when the eye-drops preparations is eye ointment in the present invention
Triterpene compound, the matrix, the isotonic regulator, the heating fusing of antioxidant described in part form oily phase,
Water described in the surfactant, the remaining antioxidant, the preservative and part is dissolved by heating into shape
At mixed liquor, then the mixed liquor is added in the oily phase, adds the remaining water, be uniformly mixed to obtain the final product
The eye ointment.
Preferably, the temperature for heating fusing is 70~80 DEG C；The temperature of heating for dissolving is 70~80 DEG C.
It, should be the preparation method comprises the following steps: will be in the matrix described in addition when the eye-drops preparations is gel in the present invention
Water carry out wetting swelling, the preservative is then added, stirring and dissolving forms the first mixed liquor, by the lanolin alkane
Type tetracyclic triterpenoid and the surfactant are mixed to form the second mixed liquor, then by second mixed liquor
It is added in first mixed liquor, is uniformly mixed up to the gel.
It, should be the preparation method comprises the following steps: molten by the excipient when the eye-drops preparations is freeze-dried instant piece in the present invention
In water described in Xie Yu, the lanolin alkane type tetracyclic triterpenoid is then added, is freeze-dried i.e. after being uniformly dispersed
Obtain the freeze-dried instant piece.
It, should be the preparation method comprises the following steps: by the lanolin alkane when the eye-drops preparations is nano liposomes in the present invention
Type tetracyclic triterpenoid, the stabilizer, which are scattered in the organic solvent, forms the first mixed liquor, will be described
Matrix, the penetrating agent are scattered in water described in part, are formed the second mixed liquor, are dispersed first mixed liquor in
In second mixed liquor, third mixed liquor is formed, by the third mixed liquor vacuum rotary steam, obtains nanocrystal suspension
The antioxidant, the preservative, the remaining water, mixing is added to the nanocrystal suspension in liquid
Uniformly up to the nano liposomes.
Due to using the technology described above, the invention has the following advantages over the prior art:
Eye-drops preparations of the invention has good curative effect, and eye-drops preparations of the invention to the prevention and treatment of cataract
Quality is stablized, and prepares simple and convenient.
Figure of description
Fig. 1 is that phacoscotasmus degree is classified schematic diagram (Hiraoka T, 1995).
Specific embodiment
Technical scheme of the present invention will be further described combined with specific embodiments below, but the present invention should not necessarily be limited by this
A little embodiments.
Embodiment 1 to 5, comparative example 1: the composition of raw materials of lanosterol eye drops is referring to table 1, the preparation method comprises the following steps: weighing sheep
Hair sterol is added in surfactant, and stirring includes it sufficiently.Preservative is weighed to be dissolved in water for injection.By preservative
Aqueous solution is added in lanosterol mixture, stirring and dissolving.Pressure sterilizing, 115 DEG C, 30min.
Table 1
Embodiment 6 to 10, comparative example 2: the composition of raw materials of lanosterol eye ointment is referring to table 2, the preparation method comprises the following steps: weighing wool
Sterol, isotonic regulator, melts in Partial Antioxidation agent water-bath at matrix, is heated to 75 DEG C.Separately weigh surfactant, residue
Antioxidant, preservative are dissolved in partial syringe water, are heated to 75 DEG C.It is slowly added in oily phase, it is stirring while adding, add residue
Water for injection is uniformly mixed.
Table 2
Embodiment 11 to 15, comparative example 3: the composition of raw materials of lanosterol gel is referring to table 3, the preparation method comprises the following steps: by matrix
It is added in water for injection and soaks swelling, preservative, stirring and dissolving is added.It is molten by being stirred in lanosterol addition surfactant
Solution.Then lanosterol solution is slowly added in matrix solution, is uniformly mixed.
Table 3
Embodiment 16 to 20, comparative example 4: the composition of raw materials of the ophthalmically acceptable freeze-dried instant piece of lanosterol is referring to table 4, preparation method
Are as follows: stirring and dissolving in water for injection is added in excipient, lanosterol is added and is uniformly dispersed, it is filling in ready bubble-cap
In, it is freeze-dried and obtains.
Buffer is housed in another 5ml eye-drop liquid bottle.Eye-drop liquid bottle big bottle cap is unscrewed when use, is extruded tablet with thumb
It puts into bottle, screws bottle cap shaking.
Table 4
Embodiment 21 to 25, comparative example 5: the composition of raw materials of lanosterol nano liposomes referring to table 5, the preparation method comprises the following steps:
It by lanosterol, stabilizer, is scattered in organic solvent, obtains solution 1.Partial syringe is dispersed by matrix, penetrating agent swelling to use
In water, solution 2 is obtained.By 1 high speed shear of solution or ultrasonic disperse in solution 2, solution 3 is obtained.By 3 vacuum rotary steam of solution, must receive
Rice crystallization suspension, is solution 4.Antioxidant, preservative, remaining water for injection are added in solution 4, is uniformly mixed.
Table 5
Embodiment 1 to 25, comparative example 1 to 5 eye-drops preparations the therapeutic effect of cataract is studied
SD rat, in the sodium selenite solution of young rat the nape of the neck subcutaneous injection 2mmol/L concentration, injection dosage is 25 μ
mol/kg。
After modeling 4 days (D5), phacoscotasmus degree is checked under slit-lamp and is taken a picture, by Hiraoka T staging pair
Phacoscotasmus degree is classified, and is divided into 7 grades, see Table 6 for details.Slit lamp photography takes a full eye under normotopia diffused light of opening one's eyes to shine
It piece and one opens one's eyes (slit of illumination on the right side of 40 °, the wide 2mm of slit of illumination) photo under the slit of illumination of side position, is detailed in Fig. 1.
Table 6
Selected at random before animal modeling 8 it is without any processing as Normal group, D5 selects crystalline substance in modeling animal
The animal of 1~3 grade of shape body turbidity enters group, is grouped according to phacoscotasmus degree, guarantees that crystalline lens is mixed in grouping
Turbid degree is without significant difference.Respectively model control group, the experimental group of embodiment 1 to 25, the contrast groups of comparative example 1 to 5 and sun
Property control group, every group 8.
Model control group gives solvent.
Experimental group and contrast groups, eye drip gives embodiment 1 to 25, the eye drops in comparative example 1 to 5, dosage respectively
It is 0.015mg/.
Positive controls, eye drip give Phacolin 0.00225mg/.
Each administration group is administered daily 4 times, and successive administration 6 weeks (D5~D47).
Capacity: 15 μ l//time, eyes administration is administered.
Content (1) general clinical observation is investigated, it is primary to observe all animals during test daily, and observation is dead, falls ill, exhales
Suction, secretion, excrement and diet, drinking-water situation etc..Find that all animals are showed no exception by observation in 47 days.
(2) phacoscotasmus degree is classified respectively at D5, D7, D12, D19, D26, D33, D40, D47, and to crystalline substance
Shape body muddiness patch carries out diameter measurement, records every animal eyes phacoscotasmus patch diameter.In groups of animals is white
Hindering number of cases summary, see Table 7 for details, and see Table 8 for details for the summary of phacoscotasmus patch average diameter.
Table 7
Table 8
When evaluating drug to the generation change of cataract lenticular Physiology and biochemistry, selenite induced catatract model is most-often used
The characteristics of animal model, this model, has summary using and its with the relationship of mankind's cataract.Lanosterol eye-drops preparations pair
The progress of 1 grade and 2 grades SD rat selenite induced catatract has certain retarding action, and meaning can control the progress of cataract, to 3 grades
Cataract has certain rehabilitation and therapeutic effect.Lanosterol eye-drops preparations and commercially available Phacolin eye drops are subjected to pharmacodynamics
Comparison, test result is shown, in the therapeutic effect of early cataract, lanosterol eye drops is significantly better than Phacolin eye drip
Liquid.
Claims (10)
1. a kind of for preventing and treating the eye-drops preparations of cataract, it is characterised in that: by weight percentage, described is ophthalmically acceptable
Preparation includes following component:
Lanolin alkane type tetracyclic triterpenoid 0.1% ~ 10%；
Matrix 0.5% ~ 90%；
Surfactant 0.05% ~ 25%；
Isotonic regulator 0.5% ~ 15%；
Preservative 0.001% ~ 0.5%；
Antioxidant 0.001% ~ 0.5%；
Water 3% ~ 98%.
2. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: the wool
Rouge alkane type tetracyclic triterpenoid is lanosterol.
3. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: the matrix
For selected from yellow petroleum jelly, albolene, lanolin, atoleine, Sodium Hyaluronate, polyvinyl alcohol, carbomer, xanthan gum, shell
One or more of glycan, xylan, polyacrylic acid, sodium alginate, methylcellulose, hydroxypropyl methylcellulose, povidone
Combination.
4. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: the surface
Activating agent is selected from pegoxol 7 stearate, diethylene glycol monoethyl ether, Labraso, tristearin
Acid poly- hydrocarbon oxygen (40) ester, 40 rilanit special of polyethylene glycol, lecithin, Tween-80, ethyl alcohol, gathers polyoxyethylene (35) castor oil
The combination of one or more of ethylene glycol, carbomer, poloxamer and hydroxypropyl-β-cyclodextrin.
5. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: described is isotonic
Regulator is selected from one or more of sodium chloride, potassium chloride, glucose, mannitol, propylene glycol, glycerine, boric acid, borax
Combination.
6. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: the anti-corrosion
Agent is selected from triethanolamine, boric acid, borax, sodium citrate, methylparaben, ethylparaben, propylben, oxybenzene second
Ester, phenylmercuric nitrate, benzalkonium chloride solution, ethyl hydroxy benzoate, benzalkonium chloride, benzalkonium bromide, chlorhexidine acetate, polyquaternium,
The combination of one or more of anesin, benzyl carbinol, thimerosal.
7. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: the antioxygen
Agent is selected from sodium thiosulfate, sodium pyrosulfite, sodium hydrogensulfite, sodium sulfite, natrium adetate, Butylated Hydroxyanisole, fourth hydroxyl
Toluene, alpha-tocopherol, four sodium acetate of cyclohexanediamine, three acetic acid of N- hydroxy-ethylenediamine, six acetic acid of diethyl triamine, two mercapto ethyl glycinamides
The combination of one or more of propylhomoserin, ethylenediamine tetra-acetic acid, arabo-ascorbic acid and its sodium salt, thiocarbamide；The water is injection
Use water.
8. according to claim 1 for preventing and treating the eye-drops preparations of cataract, it is characterised in that: described is ophthalmically acceptable
Preparation is eye ointment.
9. a kind of such as described in any item of the claim 1 to 8 for preventing and treating the preparation side of the eye-drops preparations of cataract
Method, it is characterised in that: by the lanolin alkane type tetracyclic triterpenoid, the matrix, the isotonic regulator,
The heating fusing of antioxidant described in part forms oily phase, by the surfactant, the remaining antioxidant, institute
Water described in the preservative stated and part dissolves by heating to form mixed liquor, then the mixed liquor is added to the oily phase
In, the remaining water is added, is uniformly mixed up to the eye-drops preparations.
10. preparation method according to claim 9, it is characterised in that: the temperature of the heating fusing is 70 ~ 80 DEG C；
The temperature of the heating for dissolving is 70 ~ 80 DEG C.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2015105523626 | 2015-09-02 | ||
| CN201510552362 | 2015-09-02 | ||
| CN201610696992.5A CN106074568B (en) | 2015-09-02 | 2016-08-22 | Ophthalmic preparation for preventing and treating cataract and preparation method thereof |
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|---|---|---|---|
| CN201610696992.5A Division CN106074568B (en) | 2015-09-02 | 2016-08-22 | Ophthalmic preparation for preventing and treating cataract and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN109364019A true CN109364019A (en) | 2019-02-22 |
| CN109364019B CN109364019B (en) | 2021-12-28 |
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| CN201811324187.5A Active CN109481392B (en) | 2015-09-02 | 2016-08-22 | Ophthalmic preparation for preventing and treating cataract and preparation method thereof |
| CN201811324188.XA Active CN109481450B (en) | 2015-09-02 | 2016-08-22 | Ophthalmic preparation for preventing and treating cataract and preparation method thereof |
| CN201610696992.5A Active CN106074568B (en) | 2015-09-02 | 2016-08-22 | Ophthalmic preparation for preventing and treating cataract and preparation method thereof |
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| CN106344587A (en) * | 2016-08-24 | 2017-01-25 | 上海毕傲图生物科技有限公司 | Lanosterol compound preparation for eyes |
| DK3536698T3 (en) * | 2017-01-25 | 2021-09-27 | Guangzhou Ocusun Ophthalmic Biotechnology Co Ltd | LANOSTEROL PRODUCT COMPOUND AND USE THEREOF |
| CN108524448B (en) * | 2017-03-02 | 2019-10-18 | 新疆维吾尔自治区药物研究所 | A kind of euphadienol anti-cataract eye-drops preparations and its preparation method and application |
| JP7056480B2 (en) * | 2017-09-08 | 2022-04-19 | ライオン株式会社 | Ophthalmic composition and tear oil layer stabilizer |
| CN109820825A (en) * | 2017-11-23 | 2019-05-31 | 河北嘉硕生物科技有限公司 | It is a kind of for treating the pharmaceutical composition of eye disease |
| CN109985052A (en) * | 2017-12-29 | 2019-07-09 | 上海蓝木化工有限公司 | The new application of triterpene compound |
| WO2020129964A1 (en) * | 2018-12-18 | 2020-06-25 | 参天製薬株式会社 | Ursodeoxycholic acid-containing agent for treating or preventing presbyopia |
| WO2020177714A1 (en) * | 2019-03-04 | 2020-09-10 | 中山大学中山眼科中心 | Composition of lanosterol prodrug compound, preparation method therefor and use thereof |
| CN110404057A (en) * | 2019-07-09 | 2019-11-05 | 武汉华肽生物科技有限公司 | A kind of pharmaceutical composition and its application based on gene recombinant protein Tat-hMsrA |
| CN112336870B (en) * | 2020-12-03 | 2022-09-20 | 温州医科大学 | Sustained-release system with synergistic effect of various vitamins in eyes and preparation method thereof |
| CN113413415B (en) * | 2021-06-30 | 2022-09-27 | 东莞博盛生物科技有限公司 | Lanosterol eye drops and preparation method thereof |
| CN115737654A (en) * | 2021-09-03 | 2023-03-07 | 成都瑞沐生物医药科技有限公司 | Eye preparation for preventing and/or treating cataract by eye drop administration |
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| WO2016029199A1 (en) * | 2014-08-22 | 2016-02-25 | Kang Zhang | Compositions and methods to treat vision disorders |
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| CA837050A (en) * | 1970-03-17 | L. Bouthelier Jean | Method of and composition for the treatment of human carcinoma and hypercholestrolemia | |
| EP0785212A1 (en) * | 1996-01-22 | 1997-07-23 | Laboratoire Theramex | New 19-nor-pregnene derivatives |
| US7531520B2 (en) * | 2005-05-17 | 2009-05-12 | Morinaga Milk Industry Co., Ltd. | Drug and food or drink for improving pancreatic functions |
| JP5514098B2 (en) * | 2008-02-29 | 2014-06-04 | 公益財団法人名古屋産業科学研究所 | Lips for reaching the posterior segment and pharmaceutical compositions for posterior segment diseases |
| JP5579181B2 (en) * | 2008-08-05 | 2014-08-27 | アマゾニア・フイートメデイカメントス・リミタダ | Pharmaceutical use of Lanosta-8,24-dien-3-ol |
| GB201101669D0 (en) * | 2011-01-31 | 2011-03-16 | Ip Science Ltd | Carotenoid particles and uses thereof |
| WO2013063279A1 (en) * | 2011-10-25 | 2013-05-02 | The Trustees Of Princeton University | A high-loading nanoparticle-based formulation for water-insoluble steroids |
| CN104352361B (en) * | 2014-11-20 | 2017-05-24 | 广州神采化妆品有限公司 | Variable-colour transparent lipstick and preparation method thereof |
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| CN109364020A (en) | 2019-02-22 |
| CN106074568A (en) | 2016-11-09 |
| CN106074568B (en) | 2021-05-14 |
| CN109364020B (en) | 2021-12-28 |
| CN109364019B (en) | 2021-12-28 |
| CN109481450A (en) | 2019-03-19 |
| CN109481392B (en) | 2021-12-24 |
| CN109481450B (en) | 2021-07-23 |
| CN109481392A (en) | 2019-03-19 |
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