CN117547550A - Medicine for preventing and treating cataract and its prepn - Google Patents

Medicine for preventing and treating cataract and its prepn Download PDF

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Publication number
CN117547550A
CN117547550A CN202210924263.6A CN202210924263A CN117547550A CN 117547550 A CN117547550 A CN 117547550A CN 202210924263 A CN202210924263 A CN 202210924263A CN 117547550 A CN117547550 A CN 117547550A
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China
Prior art keywords
vitamin
weight
arginine
trimethylglycine
glycine
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CN202210924263.6A
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Chinese (zh)
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谢坤
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Individual
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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
    • A61K31/01—Hydrocarbons
    • A61K31/015—Hydrocarbons carbocyclic
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/30—Zinc; Compounds thereof
    • 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

Abstract

A medicine for preventing and treating cataract is prepared from carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride antibacterial agent, and humectant deionized water. The eye drops prepared by the method have no side effect, have the effects of anti-inflammatory, antioxidant and lens clarifying, and the practical application proves that the obtained eye drops have good effects in treating cataract, mosquito diseases, blurred vision, asthenopia and glaucoma.

Description

Medicine for preventing and treating cataract and its prepn
Technical Field
The invention relates to an eyedrop, in particular to a medicine for preventing and treating cataract and a preparation method thereof.
Background
Any of various causes such as aging, genetic, topical nutritional disorders, immune and metabolic abnormalities, trauma, poisoning, radiation, etc. can cause metabolic disorders in the lens, which can cause degeneration of the lens proteins and cause clouding, known as cataracts, when light is blocked by the clouded lens and cannot be projected on the retina, resulting in blurred vision. Frequently seen over 40 years of age, and the incidence increases with age. At present, the cataract investigation standard adopted in China is mainly referred to as follows: WHO proposed in 1982 that vision is less than 0.7, the lens was turbid, and no other eye disease causing vision deterioration was the diagnosis standard of cataract; simple grading criteria for WHO cataract in 2001. This is the main domestic standard of slit lamp inspection. Mydriasis-free digital fundus photography and reading diagnostic criteria are different. The diagnosis standard is as follows: the retinal small blood vessels cannot be seen clearly by the fundus image, and the cataract is confirmed by the blurred fundus image caused by the corneal disease except the anterior ocular segment photograph. The operation judgment standard is as follows: the fundus image cannot be seen clearly on the optic disc and retinal large blood vessels, and the fundus image is blurred due to the cornea disease except the anterior ocular segment photograph, so that the cataract is confirmed.
Numerous medical studies and clinical trials have demonstrated that human cell free radical damage is the source of all diseases. The radical is a substance lacking electrons (unsaturated electron substance). The free radical contends with the electrons of human cells everywhere in the human body, if the electrons of the cellular protein molecules are deprived, the protein is connected with branched chains to be alkylated, and abnormal molecules are formed, so that various diseases of the human body occur.
The existing common methods for treating eye diseases such as cataract and the like include modes of drug treatment, surgical treatment and the like, wherein the surgical treatment has damage or sequelae to human bodies and also has a certain risk; the traditional medicine treatment mostly adopts a mode of delaying cataract development, but has the disadvantages of unobvious effect, unstable manufacturing process and difficulty in eliminating a great amount of free radicals enriched by eyeballs, peripheral micro blood vessels, nerves and the like. In order to eliminate a large amount of free radicals generated by excessive eyes and environmental factors, according to relevant data, the blueberry, black matrimony vine, mulberry, vitamin E, vitamin C or selenium-containing high-efficiency substances and the like for resisting the free radicals are eaten, and the effects on myopia and cataract are not obvious. The prior method for treating cataract mainly adopts surgery or eye drops to delay the continuous development of cataract. Pharmaceutical treatments are also disclosed.
Thus, the present inventors believe that ocular overuse and environmental factors and functional aging meridian obstruction in modern people are fundamental causes of radical enrichment that cause significant enrichment of the ciliary muscle, lens, ocular and peripheral microvasculature and nerves. Furthermore, because of the enrichment of a large amount of free radicals, ciliary muscles of eyes cannot flexibly stretch, spasm of eyes and peripheral muscles, blood vessel blockage, and incapacitation of crystalline lenses, and generated metabolic wastes cannot be smoothly discharged, the excessive free radicals can cause the root causes of cataract, mosquito-flying symptoms, glaucoma and presbyopia. The therapeutic drugs are combined with each other in the middle and the west. The invention relates to a compound eye medicine composition, in particular to a compound eye medicine composition for treating cataract. The present invention has been made.
The invention aims to solve the defects of the prior eye drops and provide a medicine for preventing and treating cataract and a preparation method thereof. The carotenoid has carbonyl, hydroxyl, methoxy or epoxy groups, and the structure is that after the carotenoid reaches peroxide enrichment places such as cataract, the carbonyl, hydroxyl, methoxy and epoxy groups can combine with unstable oxygen of the peroxide to form one or more stable new compounds, and the new compounds can become easier to dissolve, so that vision recovery is achieved. Because of the different antioxidant pharmacological mechanisms of nine medicaments of carotenoid, vitamin E, vitamin C, arginine, inositol, glycine, arginine, trimethylglycine and zinc chloride, the composition of the pharmaceutical composition is a very ideal antioxidant mechanism for protecting the formulation of the optic nerve nutrition fundus macula.
Disclosure of Invention
The invention aims to provide a compound eye medicine composition composed of active ingredients such as carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride and the like; the invention also aims at providing a preparation method of the compound eye medicine composition.
The aim of the invention is realized by the following technical scheme.
The compound eye medicine composition is prepared from the following active ingredients in parts by weight:
0.1 to 10.0 parts by weight of carotenoid, 0.2 to 20.0 parts by weight of vitamin E, 0.2 to 20.0 parts by weight of vitamin C, 0.1 to 10.0 parts by weight of inositol, 0.3 to 10.0 parts by weight of glycine, 0.03 to 3.0 parts by weight of arginine, 0.3 to 30.0 parts by weight of trimethylglycine and 0.01 to 0.1 part by weight of zinc chloride;
the preferable proportion of the nine components is as follows: carotenoid 1:vitamin E2:vitamin C2:inositol 1:glycine 3:arginine 0.3:trimethylglycine 3:zinc chloride 0.01
The nine active ingredients are as follows: an isoform of carotenoids; an isoform of vitamin E, vitamin C; inositol, glycine, arginine, trimethylglycine, may be any salt thereof in a chemically acceptable form, such as: inositol phosphates, glycine hydrochloride, arginine hydrochloride, trimethylglycine hydrochloride, and the like.
The concentration of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride in the composition is 1-300% according to the weight ratio; the sum of the concentrations of the nine mixtures in the compound preparation is 12.31 percent by weight.
The optimal concentration of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride in the composition is 1%, 2%, 1%, 3%, 0.3%, 3% and 0.01% according to the weight ratio; the sum of the concentrations of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride in the compound preparation is 12.31 percent by weight.
The compound eye medicine composition of the invention can be mixed with pharmaceutically acceptable carriers to be prepared into various clinically acceptable dosage forms such as solution, suspension or emulsion, etc. The pH value of the compound preparation solution and the suspension ranges from pH5 to pH 8.
The pharmaceutically acceptable carrier in the preparation method can be an agent required by ophthalmic preparations, including antibacterial preservatives, common solvents, viscous agents and the like.
The antimicrobial preservative may be zinc chloride, benzalkonium chloride, cetrimex, chlorobutanol, methylparaben, propylparaben, phenethyl alcohol, disodium edetate, 2, 4-hexadienoic acid, M, or other known agents. The concentration range used is 0.001% to 1.0% by weight.
The co-solvents may be polyoxyethylene sorbitol fatty acid esters 20, 60 and 80, addition polymers of polypropylene glycol and ethylene oxide F-68, F-84 and P-103, cyclodextrins or other useful agents. The concentration used ranges from 0.01% to 2% by weight.
The viscosity agent may be polyvinyl alcohol, polyvinyl pyrrolidone, methyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose or other useful agents. The concentration used ranges from 0.01% to 2% by weight.
The composition and the compound preparation of the invention can enhance the drug effect through different pharmacologies, play a role in synergy, not only can inhibit the generation of aqueous solution in eyes so as to greatly resist free radicals in eyes to treat cataract, but also have a protective effect on lens optic nerves, and are used for local drug treatment of cataract.
The total dosage of the compound medicine is 0.001 mg to 10 mg of each eye. Through experimental study, all dosage proportions of the composition have the effects of treating cataract and protecting optic nerve of crystalline lens and nourishing fundus macula.
The following experimental examples and examples serve to further illustrate but not limit the invention.
Experimental example glutathione eye drops, pinok Xin Na eye drops are used singly and compared with compound new medicine (compound carotene eye drops) for clinical observation of cataract in one month
1. Patient data
30 patients (60 eyes total) were outpatients. 20 men and 10 women; average age 60 years (42-88 years), average course of disease 12 years (2-23 years).
2. Diagnostic criteria
1. The clinical basis is whether the capillary blood vessel is clear or not displayed by each eye slit lens, and the patient is selected as a standard.
2. Patients who had undergone crystal replacement surgery were excluded.
3. Therapeutic method
The glutathione eye drops are used by 10 patients (20 eyes) 2 times a day for 1 drop each time; 10 patients (20 eyes) were given 1 drop of pirenox Xin Na eye drops 2 times daily; 10 patients (20 eyes) are provided with compound new drugs (compound carotene eye drops); a total of 30 patients (60 eyes) were treated for 28 days as 1 course of treatment. The patient's vision, conjunctiva, cornea, iris, eyelash color, pupil, lens, fundus and applanation were recorded during one, two, three, four weeks of follow-up before and after the dose. The angle field of view was examined prior to administration.
4. Therapeutic results
(1) Drug effect:
average vision
Average improvement amplitude (%)
(2) Side effects:
after administration, only individual patients have foreign body sensation and eye irritation, and the continuous administration is not influenced. The eye examination, the eyesight, the anterior ocular segment, the fundus, the visual field are not obviously changed, and the iris color is not obviously abnormal. No obvious side effects are seen throughout the body. Three groups of patients (glutathione eye drops, pirenox Xin Na eye drops and compound carotene eye drops) have no obvious difference.
5. Conclusion(s)
The eye drops of glutathione and piranok Xin Na are used for a short period of time for cataract patients, and the eyesight is not obviously improved. The compound carotene eye drops can obviously improve the eyesight of patients, and are statistically obviously superior to glutathione eye drops or piranok Xin Na eye drops which are singly used.
The following examples all achieve the effects of the above experimental examples.
Example 1 (solution formulation)
A. Placing polyvinyl alcohol into 0.3 ml of purified water, stirring uniformly, sterilizing under high pressure, and cooling the sterilized solution to room temperature;
B. dissolving benzalkonium chloride, edetate disodium, sodium chloride, sodium sulfide, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride in 0.7 ml purified water at room temperature, filtering and sterilizing;
C. mixing the solutions prepared in the step A and the step B until the solutions are uniform into a phase, adding sulfuric acid or hydrochloric acid or sodium hydroxide to adjust the pH value to 6.8, and then filling the solution into an eyedrop bottle.
The eye is administered topically, twice daily, one to two drops each time.
In the preparation, 10.0mg of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride are mixed, and the medicine has the effect higher than that of glutathione eye drops.
Example 2 solution formulation
(carotenoid: vitamin E: vitamin C: inositol: glycine: arginine: trimethylglycine: zinc chloride),
A. placing polyvinyl alcohol into 1.5L purified water, stirring uniformly, sterilizing under high pressure, and cooling the sterilized solution to room temperature;
B. dissolving benzalkonium chloride, disodium edentate, sodium chloride, sodium sulfide, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride in 3.5L purified water at room temperature, filtering, and sterilizing;
C. mixing the solutions prepared in the step A and the step B until the solutions are uniform into a phase, adding sulfuric acid or hydrochloric acid or sodium hydroxide to adjust the pH value to 6.8, and then filling the solution into an eyedrop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 3 (suspension formulation)
(carotenoid: vitamin E: vitamin C: inositol: glycine: arginine: trimethylglycine: zinc chloride),
A. preparation of powder slurry
Adding it's rosoprop into 20 g of pure hot water with the temperature of 50-70 ℃ and stirring uniformly; adding 50-70 deg.c pure hot water to 30 g to obtain its solution and filtering; autoclaving in a rapid cooling cycle, and ball milling at 50 to 55RPM for 18 to 19 hours to obtain a slurry.
Preparation of 2% Carbom (Carbomer) pulp
Adding the cabo mould 974P into 400 g of pure hot water with the temperature of 50-70 ℃ and stirring uniformly; purified water is added to 500 g, and the mixture is stirred uniformly and filtered to obtain 100 g of Kabo mould 974P slurry.
C. Preparation of formulation concentrate
Adding mannitol, polyvinyl alcohol, sodium chloride, disodium edetate and benzalkonium chloride into 100 g of pure hot water with the temperature of 50-70 ℃ in sequence, and filtering; adding the Kabo mould 974P slurry (see step B); purified water was then added to give 275 grams of the formulation concentrate.
Micronizing (carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride) and dissolving in 100 g purified water to obtain solution.
D. Aseptic mixing
Sterile filtration of the micronized solution of carotenoids, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride (see step C), and addition of the concentrate (see step C); regulating the pH value to 6.8+/-0.2 by using sodium hydroxide or hydrochloric acid; adding the powder slurry (see step A), and transferring all the powder slurry as far as possible; adding purified water to 500 g, and stirring thoroughly to obtain suspension preparation.
The eye is administered topically, twice daily, one to two drops each time.
Example 4 (emulsion)
Carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride,
an aqueous emulsion was prepared according to the following method:
A. micronizing boric acid, sodium borate, edetate disodium, benzalkonium chloride, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride, and sodium chloride sequentially adding 400 g purified water, dissolving and stirring until clear; the solution was filtered and sterilized.
B. 1600 g of purified water is heated to 90 ℃, polyvinyl alcohol is added, and stirring is carried out until uniform; heating to 121 ℃ for sterilization for 30 to 45 minutes while stirring; cooling to 50-55 ℃, and adding the solution prepared in the step A; continuously stirring to room temperature to obtain aqueous emulsion; the aqueous emulsion is filled into an eye drop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 5 (suspension formulation)
Carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride,
A. preparation of powder slurry
200 g of 50-70 ℃ pure hot water is added with Luo Suopu and stirred uniformly; adding 50-70 deg.c pure hot water to 300 g to obtain its solution and filtering; autoclaving in a rapid cooling cycle, and ball milling at 50 to 55RPM for 18 to 19 hours to obtain a slurry.
Preparation of 2% Carbom (Carbomer) pulp
Adding the cabo mould 974P into 4000 g of pure hot water with the temperature of 50-70 ℃ and stirring uniformly; purified water is added to 5000 g, and the mixture is stirred uniformly and filtered to obtain 1250 g of Kabo mould 974P slurry.
C. Preparation of formulation concentrate
Adding mannitol, polyvinyl alcohol, sodium chloride, disodium edetate and benzalkonium chloride into 1000 g of pure hot water with the temperature of 50-70 ℃ in sequence, and filtering; adding the Kabo mould 974P slurry (see step B); purified water was then added until 1750 grams of the formulation concentrate was obtained.
Micronizing carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride, dissolving in 1000 g purified water, and making into solution.
D. Aseptic mixing
Sterile filtration of the micronized solution of carotenoids, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride (see step C), and addition of the concentrate (see step C); regulating the pH value to 6.8+/-0.2 by using sodium hydroxide or hydrochloric acid; adding the powder slurry (see step A), and transferring all the powder slurry as far as possible; adding purified water to 3000 g, and stirring thoroughly to obtain suspension preparation.
The eye is administered topically, twice daily, one to two drops each time.
Example 6 (solution formulation)
Carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride,
A. placing polyvinyl alcohol into 1.5L purified water, stirring uniformly, sterilizing under high pressure, and cooling the sterilized solution to room temperature;
B. micronizing benzalkonium chloride, edetate disodium, sodium chloride, sodium sulfide, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride, dissolving in 3.5L purified water at room temperature, and filtering for sterilization;
C. mixing the solutions prepared in the step A and the step B until the solutions are uniform into a phase, adding sulfuric acid or hydrochloric acid or sodium hydroxide to adjust the pH value to 6.8, and then filling the solution into an eyedrop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 7 (solution formulation)
Micro-composition comprising carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride
A. Placing polyvinyl alcohol into 0.6 liter of purified water, stirring uniformly, sterilizing under high pressure, and cooling the sterilized solution to room temperature;
B. micronizing benzalkonium chloride, edetate disodium, sodium chloride, sodium sulfide, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride, dissolving in 1.4L purified water at room temperature, and filtering for sterilization;
C. mixing the solutions prepared in the step A and the step B until the solutions are uniform into a phase, adding sulfuric acid or hydrochloric acid or sodium hydroxide to adjust the pH value to 6.8, and then filling the solution into an eyedrop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 8 (solution formulation)
Micro-composition comprising carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride
A. Placing polyvinyl alcohol into 0.75 liter of purified water, stirring uniformly, sterilizing under high pressure, and cooling the sterilized solution to room temperature;
B. micronizing benzalkonium chloride, edetate disodium, sodium chloride, sodium sulfide, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride, dissolving in 1.75L purified water at room temperature, and filtering for sterilization;
C. mixing the solutions prepared in the step A and the step B until the solutions are uniform into a phase, adding sulfuric acid or hydrochloric acid or sodium hydroxide to adjust the pH value to 6.8, and then filling the solution into an eyedrop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 9 (emulsion)
Micro-composition comprising carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, and zinc chloride
A. Micronizing boric acid, sodium borate, edetate disodium, benzalkonium chloride, carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine, zinc chloride, and sodium chloride sequentially adding into 40 g purified water, dissolving and stirring until clear; the solution was filtered and sterilized.
B. 160 g of purified water is heated to 90 ℃, polyvinyl alcohol is added, and stirring is carried out until uniform; heating to 121 ℃ for sterilization for 30 to 45 minutes while stirring; cooling to 50-55 ℃, and adding the solution prepared in the step A; continuously stirring to room temperature to obtain aqueous emulsion; the aqueous emulsion is filled into an eye drop bottle.
The eye is administered topically, twice daily, one to two drops each time.
Example 10 (solution formulation)
1000 g of micronized mixture of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride is added with reagents required by ophthalmic preparations according to a conventional preparation method of pharmacy to prepare a solution.
The eye is administered topically, twice daily, one to two drops each time.

Claims (6)

1. The compound eye medicine composition is characterized by being prepared from the following active ingredients in parts by weight:
0.1 to 10.0 parts by weight of carotenoid, 0.2 to 20.0 parts by weight of vitamin E, 0.2 to 20.0 parts by weight of vitamin C, 0.1 to 10.0 parts by weight of inositol, 0.3 to 10.0 parts by weight of glycine, 0.03 to 3.0 parts by weight of arginine, 0.3 to 30.0 parts by weight of trimethylglycine and 0.01 to 0.1 part by weight of zinc chloride;
the preferable proportion of the nine components is as follows: carotenoid 1, vitamin E2, vitamin C2, inositol 1, glycine 3, arginine 0.3, trimethylglycine 3, and zinc chloride 0.01.
The concentration of carotenoid, vitamin E, vitamin C, inositol, glycine, arginine, trimethylglycine and zinc chloride is 1-300% according to the weight ratio; the sum of the concentrations of the nine mixtures in the compound preparation is 12.31 percent by weight.
2. The compound ophthalmic composition of claim 1, characterized in that the nine active ingredients: carotenoids or isoforms of carotenoids; vitamin E, vitamin C or an isoform thereof; the inositol, glycine, arginine, trimethylglycine may be any salt thereof in a chemically acceptable form, such as: inositol phosphates, glycine hydrochloride, arginine hydrochloride, trimethylglycine hydrochloride, and the like.
3. The compound ophthalmic composition of claim 1 or 2, wherein the composition is formulated as a suspension, emulsion or solution formulation in combination with a pharmaceutically acceptable carrier.
4. A compound ophthalmic composition according to claim 3, wherein the pH of the solution or suspension formulation ranges from pH5 to pH 8.
5. The use of a compound ophthalmic composition according to claim 1, 2 or 4 for the preparation of a medicament for the treatment of cataracts.
6. Use of a compound ophthalmic composition according to claim 3 for the preparation of a medicament for the treatment of cataracts.
CN202210924263.6A 2022-08-03 2022-08-03 Medicine for preventing and treating cataract and its prepn Pending CN117547550A (en)

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Application Number Priority Date Filing Date Title
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Publications (1)

Publication Number Publication Date
CN117547550A true CN117547550A (en) 2024-02-13

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