Eye drop for preventing and treating cataract and preparation method thereof

文档序号:1880567 发布日期:2021-11-26 浏览:13次 中文

阅读说明:本技术 一种用于预防和治疗白内障的眼药水及其制备方法 (Eye drop for preventing and treating cataract and preparation method thereof ) 是由 陈帝江 于 2021-09-30 设计创作,主要内容包括:本发明提供一种用于预防和治疗白内障的眼药水及其制备方法,属于医药制剂领域,按质量分数计,所述眼药水包括0.1-2%的两亲性牡蛎短肽,所述两亲性牡蛎短肽以季戊四醇为交联骨架,以牡蛎短肽为亲水链端,以羊毛甾醇为疏水端改性制备得到,所述具有两亲性的牡蛎短肽可在极性的溶剂中发生自组装,形成具有类似脂质体膜结构的纳米胶束,使其易于被细胞吸收,进一步提高药物利用率;本发明同时结合中药提取物用于预防和治疗白内障,所述纳米胶束还可作为载药载体,表现出显著的改善效果,且副作用小,安全性高。(The invention provides an eye drop for preventing and treating cataract and a preparation method thereof, belonging to the field of medical preparations, wherein the eye drop comprises 0.1-2% of amphiphilic oyster short peptide by mass, the amphiphilic oyster short peptide takes pentaerythritol as a cross-linked skeleton, oyster short peptide as a hydrophilic chain end and lanosterol as a hydrophobic end, and the amphiphilic oyster short peptide can be prepared by modification, can be subjected to self-assembly in a polar solvent to form a nano micelle with a similar liposome membrane structure, is easy to be absorbed by cells and further improves the utilization rate of drugs; the nano micelle can be used for preventing and treating cataract by combining with a traditional Chinese medicine extract, can also be used as a medicine carrying carrier, shows a remarkable improvement effect, and has small side effect and high safety.)

1. An eye drop for preventing and treating cataract, which is characterized in that the eye drop comprises 0.1-2% of amphiphilic oyster short peptide by mass fraction, and the preparation method of the amphiphilic oyster short peptide comprises the following steps:

(1) weighing pentaerythritol monoacetal, dissolving the pentaerythritol monoacetal in dichloromethane, adding dimethylaminopyridine and triethylamine after the pentaerythritol monoacetal is fully dissolved, stirring, heating to 50-60 ℃, adding succinic anhydride, continuously keeping the temperature, stirring and reacting for 20-24 hours, washing a reaction system after the reaction is finished by using a hydrochloric acid solution and deionized water in sequence, taking an organic phase, drying, purifying by using a silica gel column, and removing a solvent to obtain a carboxylated product;

wherein the mass ratio of the pentaerythritol monoacetal to the p-dimethylaminopyridine to the triethylamine to the succinic anhydride is 1: (0.5-0.6): (4-5): (3-4);

(2) dissolving the carboxylated product in dimethylformamide, fully mixing, respectively adding p-dimethylaminopyridine and N, N' -dicyclohexylcarbodiimide, stirring, heating to 60-70 ℃, adding lanosterol, continuing to keep the temperature, stirring and reacting for 10-14 hours, and removing the solvent after the reaction is finished to obtain an esterified product;

wherein the mass ratio of the carboxylation product to the dimethylaminopyridine to the N, N' -dicyclohexylcarbodiimide to the lanosterol is 1: (1.7-2.2): (0.9-1): (4-5);

(3) dissolving the esterification product in a mixing volume ratio of 3: 1, stirring and heating to 50-70 ℃, adding palladium carbon with the content of 10% of active substances, stirring and reacting for 10-16h under the condition of introducing hydrogen, and filtering to obtain a reduction product;

wherein the mass ratio of the esterification product to the palladium-carbon catalyst is 1: (0.2-0.5);

(4) adding the dimethylaminopyridine and the oyster short peptide into the reduction product, stirring, heating to 50-60 ℃, keeping the temperature, stirring, reacting for 4-8 hours, purifying by a silica gel column after the reaction is finished, and removing the solvent to obtain the amphiphilic oyster short peptide.

2. The eye drop for preventing and treating cataract as claimed in claim 1, wherein the oyster short peptide is prepared by the method comprising:

(1) weighing the soft tissue of the oyster, adding redistilled water according to the material-liquid ratio of 3-5ml/g for homogenization treatment to obtain an oyster homogenate, gradually heating the oyster homogenate to 90-100 ℃, preserving heat for 10-20min, adjusting the pH of the oyster homogenate to 6.5-7.5 after cooling to 45-50 ℃, adding Protamex compound protease, preserving heat for enzymolysis for 4h, carrying out water bath enzyme deactivation after the enzymolysis is finished, adding chitosan for flocculation after cooling, centrifuging, and filtering and separating enzymolysis liquid through multiple layers of gauze to obtain a supernatant;

wherein the addition amount of the composite protease is 3000-4000U/g, and the addition amount of the chitosan is 1-3g/100 ml;

(2) desalting the supernatant through cation exchange resin and anion exchange resin in turn to obtain an exchange solution, and passing the exchange solution through a first-stage ultrafiltration membrane and a second-stage ultrafiltration membrane in turn at room temperature to obtain an oyster oligopeptide solution;

wherein the molecular weight cut-off of the first-stage ultrafiltration membrane is 5kDa, and the ultrafiltration pressure is 0.15-0.18 MPa; the molecular weight cut-off of the second-stage ultrafiltration membrane is 1kDa, and the ultrafiltration pressure is 0.18-0.21 MPa.

3. The eye drop for preventing and treating cataract as claimed in claim 1, wherein the eye drop comprises 50-90% of Chinese medicine extract by mass.

4. The eye drop for preventing and treating cataract as claimed in claim 3, wherein the traditional Chinese medicine extract comprises the following components by weight: 7-9 parts of glossy privet fruit, 9-10 parts of cassia seed, 5-7 parts of butterflybush flower, 5-7 parts of pipewort and 3-5 parts of chamomile, wherein the preparation method of the traditional Chinese medicine extract comprises the following steps:

weighing the glossy privet fruit, the cassia seed, the pale butterflybush flower, the pipewort and the chamomile according to the weight ratio, adding double distilled water according to the liquid-material ratio of 100 ml/g after rinsing, decocting for 4-6h with slow fire, separating filtrate after cooling, and diluting the filtrate with the double distilled water to 1/2 of the volume before decocting.

5. The eye drop for preventing and treating cataract as claimed in claim 4, wherein the traditional Chinese medicine extract comprises the following components by weight: 8 parts of glossy privet fruit, 10 parts of cassia seed, 6 parts of butterflybush flower, 7 parts of pipewort and 3 parts of chamomile.

6. The eye drop for preventing and treating cataract as claimed in claim 1, wherein the eye drop comprises 0.1-2% of composite polyacrylamide nano particles by mass fraction, and the preparation method of the composite polyacrylamide nano particles comprises the following steps:

dissolving N-isopropylacrylamide, N' -methylenebisacrylamide and acryloyl piperazine propanesulfonate in double distilled water, filtering the mixed solution by using filter paper with the maximum reserved particle size of 8 mu m after full dissolution, taking filtrate, adding an initiator after the filtrate is subjected to nitrogen purging, stirring and reacting for 2-3h under the nitrogen atmosphere to obtain a polymerization product, placing the polymerization product in the double distilled water for dialysis and purification, freeze-drying, crushing and pulverizing to obtain the polymer;

wherein the mass ratio of the N-isopropyl acrylamide, the N, N' -methylene bisacrylamide and the acryloyl piperazine propanesulfonate is 1: (0.2-0.4): (1.1-1.6); the preparation method of the acryloyl piperazine propanesulfonate comprises the following steps:

weighing 4- (2-hydroxyethyl) -1-piperazine propanesulfonic acid and acrylate with equal molar ratio, dissolving in 1mol/L sodium hydroxide solution, stirring and refluxing for 1-2h, cooling after the reaction is finished, adding a large amount of anhydrous ether, separating precipitate, washing the precipitate with anhydrous ethanol, and drying to obtain the product.

7. The ophthalmic solution for preventing and treating cataract as claimed in claim 1, wherein the ophthalmic solution further comprises one or more of pH adjusting buffer, osmotic pressure regulator and preservative, the pH adjusting buffer is boric acid-borax system or citric acid-sodium citrate system, the osmotic pressure regulator is sodium chloride or glucose, and the preservative is ethyl benzoate, ethyl p-hydroxybenzoate, dodecyl dimethyl benzyl ammonium chloride and/or dodecyl dimethyl benzyl ammonium bromide.

8. The eye drop for preventing and treating cataract as claimed in claim 1, wherein the eye drop further comprises one or more of taurine, leucine, borneol, mint, vitamin or artificial tear.

Technical Field

The invention relates to the field of medicinal preparations, in particular to an eye drop for preventing and treating cataract and a preparation method thereof.

Background

Cataract is lenticular opacity caused by systemic diseases or local eye diseases, abnormal nutrition metabolism, poisoning, degeneration, trauma and other reasons, and is divided into several types: (1) senile cataract, most common, is more than 40 years old, and increases with age, the etiology is related to degenerative change of senile metabolism slowly, and is also considered to be related to factors such as sunlight long-term irradiation, endocrine disturbance, metabolic disturbance and the like, the senile cataract can be divided into two categories of nuclear and cortical types according to the initial turbid position, the visual disturbance is related to the turbid position and density, the posterior cortical and nuclear turbidity affects the vision early, the treatment is mainly performed by operation, contact glasses can be worn after the operation, and the artificial lens implantation can also be performed simultaneously by the operation; (2) concurrent cataract (with other eye diseases); (3) traumatic cataract; (4) metabolic cataracts (due to endocrine insufficiency, such as diabetic cataracts); (5) radiation cataract (associated with X-rays, beta-rays, gamma-rays, etc.); (6) drugs and toxic cataracts; if not treated in time, the whitening in the lens becomes more and more severe, eventually becoming completely blurred and the lens nucleus disintegrates, resulting in complete loss of vision.

For the drug treatment of cataract, the research and study stage is at present at home and abroad: some early cataracts, after taking medicine, the disease condition may slow down and develop, and the vision is slightly improved; some patients with intermediate stage cataract had no improvement in vision and lens opacity after administration; the medicine treatment of the cataract close to the mature stage has no practical significance.

At present, cataracts in the middle or mature stage can only be treated by surgery generally, although the surgical treatment is quick in recovery, the risk is high, the risk of blindness exists, and the cataracts are easy to relapse after the surgery, so that the development of a therapeutic drug and a therapeutic method for early cataracts has important practical significance for preventing or slowing down the development of cataract conditions.

Disclosure of Invention

In view of the above problems, the present invention provides an eye drop for preventing and treating cataract and a method for preparing the same.

The purpose of the invention is realized by adopting the following technical scheme:

an eye drop for preventing and treating cataract, which comprises 0.1-2% of amphiphilic oyster short peptide by mass fraction, and the preparation method of the amphiphilic oyster short peptide comprises the following steps:

(1) weighing pentaerythritol monoacetal, dissolving the pentaerythritol monoacetal in dichloromethane, adding dimethylaminopyridine and triethylamine after the pentaerythritol monoacetal is fully dissolved, stirring, heating to 50-60 ℃, adding succinic anhydride, continuously keeping the temperature, stirring and reacting for 20-24 hours, washing a reaction system after the reaction is finished by using a hydrochloric acid solution and deionized water in sequence, taking an organic phase, drying, purifying by using a silica gel column, and removing a solvent to obtain a carboxylated product;

wherein the mass ratio of the pentaerythritol monoacetal to the p-dimethylaminopyridine to the triethylamine to the succinic anhydride is 1: (0.5-0.6): (4-5): (3-4);

(2) dissolving the carboxylated product in dimethylformamide, fully mixing, respectively adding p-dimethylaminopyridine and N, N' -dicyclohexylcarbodiimide, stirring, heating to 60-70 ℃, adding lanosterol, continuing to keep the temperature, stirring and reacting for 10-14 hours, and removing the solvent after the reaction is finished to obtain an esterified product;

wherein the mass ratio of the carboxylation product to the dimethylaminopyridine to the N, N' -dicyclohexylcarbodiimide to the lanosterol is 1: (1.7-2.2): (0.9-1): (4-5);

(3) dissolving the esterification product in a mixing volume ratio of 3: 1, stirring and heating to 50-70 ℃, adding palladium carbon with the content of 10% of active substances, stirring and reacting for 10-16h under the condition of introducing hydrogen, and filtering to obtain a reduction product;

wherein the mass ratio of the esterification product to the palladium-carbon catalyst is 1: (0.2-0.5);

(4) adding the dimethylaminopyridine and the oyster short peptide into the reduction product, stirring, heating to 50-60 ℃, keeping the temperature, stirring, reacting for 4-8 hours, purifying by a silica gel column after the reaction is finished, and removing the solvent to obtain the amphiphilic oyster short peptide.

Preferably, the preparation method of the oyster short peptide comprises the following steps:

(1) weighing the soft tissue of the oyster, adding redistilled water according to the material-liquid ratio of 3-5ml/g for homogenization treatment to obtain an oyster homogenate, gradually heating the oyster homogenate to 90-100 ℃, preserving heat for 10-20min, adjusting the pH of the oyster homogenate to 6.5-7.5 after cooling to 45-50 ℃, adding Protamex compound protease, preserving heat for enzymolysis for 4h, carrying out water bath enzyme deactivation after the enzymolysis is finished, adding chitosan for flocculation after cooling, centrifuging, and filtering and separating enzymolysis liquid through multiple layers of gauze to obtain a supernatant;

wherein the addition amount of the composite protease is 3000-4000U/g, and the addition amount of the chitosan is 1-3g/100 ml;

(2) desalting the supernatant through cation exchange resin and anion exchange resin in turn to obtain an exchange solution, and passing the exchange solution through a first-stage ultrafiltration membrane and a second-stage ultrafiltration membrane in turn at room temperature to obtain an oyster oligopeptide solution;

wherein the molecular weight cut-off of the first-stage ultrafiltration membrane is 5kDa, and the ultrafiltration pressure is 0.15-0.18 MPa; the molecular weight cut-off of the second-stage ultrafiltration membrane is 1kDa, and the ultrafiltration pressure is 0.18-0.21 MPa.

Preferably, the eye drop comprises 50-90% of traditional Chinese medicine extract by mass.

Preferably, the traditional Chinese medicine extract comprises the following components in parts by weight: 7-9 parts of glossy privet fruit, 9-10 parts of cassia seed, 5-7 parts of butterflybush flower, 5-7 parts of pipewort and 3-5 parts of chamomile, wherein the preparation method of the traditional Chinese medicine extract comprises the following steps:

weighing the glossy privet fruit, the cassia seed, the pale butterflybush flower, the pipewort and the chamomile according to the weight ratio, adding double distilled water according to the liquid-material ratio of 100 ml/g after rinsing, decocting for 4-6h with slow fire, separating filtrate after cooling, and diluting the filtrate with the double distilled water to 1/2 of the volume before decocting.

Preferably, the traditional Chinese medicine extract comprises the following components in parts by weight: 8 parts of glossy privet fruit, 10 parts of cassia seed, 6 parts of butterflybush flower, 7 parts of pipewort and 3 parts of chamomile.

Preferably, the eye drop comprises 0.1-2% of composite polyacrylamide nanoparticles by mass, and the preparation method of the composite polyacrylamide nanoparticles comprises the following steps:

dissolving N-isopropylacrylamide, N' -methylenebisacrylamide and acryloyl piperazine propanesulfonate in double distilled water, filtering the mixed solution by using filter paper with the maximum reserved particle size of 8 mu m after full dissolution, taking filtrate, adding an initiator after the filtrate is subjected to nitrogen purging, stirring and reacting for 2-3h under the nitrogen atmosphere to obtain a polymerization product, placing the polymerization product in the double distilled water for dialysis and purification, freeze-drying, crushing and pulverizing to obtain the polymer;

wherein the mass ratio of the N-isopropyl acrylamide, the N, N' -methylene bisacrylamide and the acryloyl piperazine propanesulfonate is 1: (0.2-0.4): (1.1-1.6); the preparation method of the acryloyl piperazine propanesulfonate comprises the following steps:

weighing 4- (2-hydroxyethyl) -1-piperazine propanesulfonic acid and acrylate with equal molar ratio, dissolving in 1mol/L sodium hydroxide solution, stirring and refluxing for 1-2h, cooling after the reaction is finished, adding a large amount of anhydrous ether, separating precipitate, washing the precipitate with anhydrous ethanol, and drying to obtain the product.

Preferably, the eye drops further comprise one or more of a pH adjusting buffer, an osmotic pressure regulator and a preservative, wherein the pH adjusting buffer is a boric acid-borax system or a citric acid-sodium citrate system, the osmotic pressure regulator is sodium chloride or glucose, and the preservative is ethyl benzoate, ethyl p-hydroxybenzoate, dodecyl dimethyl benzyl ammonium chloride and/or dodecyl dimethyl benzyl ammonium bromide.

Preferably, the eye drops further comprise one or more of taurine, leucine, borneol, mint, vitamins or artificial tears.

The vitamins include one or more of vitamin B1, vitamin B2, vitamin B3, vitamin B5, vitamin B6, vitamin B12, vitamin C, vitamin D3, or vitamin E.

The invention has the beneficial effects that:

(1) lanosterol in the steroid can reverse the initial symptoms of cataract, but the problem of difficult absorption and the like caused by poor solubility needs to be applied by adopting an intraocular injection mode, so that the treatment risk is improved; according to the invention, based on lanosterol, pentaerythritol is taken as a cross-linking framework, micromolecular oyster short peptide is taken as a hydrophilic end, lanosterol is taken as a hydrophobic end, and modification is carried out to obtain the oyster short peptide with amphipathy; the nano micelle can be used for preventing and treating cataract by combining with a traditional Chinese medicine extract, can also be used as a medicine carrying carrier, shows a remarkable improvement effect, and has small side effect and high safety.

(2) The invention relates to a preparation method of a polymer nanoparticle with isopropyl hydrophobic sites and sulfated piperazine, which is characterized in that N-isopropylacrylamide, N' -methylenebisacrylamide and propylene piperazine propanesulfonate are taken as monomers, and the polymer nanoparticle is absorbed by cells and can form strong affinity with crystalline lens water-soluble protein, inhibit the denaturation or aggregation of the crystalline lens water-soluble protein and reverse crystalline lens opacification based on the carrier effect of a drug-loaded nano-micelle and the protein affinity of the polymer nanoparticle.

(3) The eye drop also contains various eye nutritional ingredients, and can improve and enhance the metabolism of eye tissues, promote the regeneration of tissue cells and prevent the development of cataract.

Detailed Description

The invention is further described with reference to the following examples.

Example 1

An eye drop for preventing and treating cataract comprises the following components in parts by weight:

90 parts of traditional Chinese medicine extract and 1 part of amphiphilic oyster short peptide;

the traditional Chinese medicine extract comprises the following components: 8 parts of glossy privet fruit, 10 parts of cassia seed, 6 parts of butterflybush flower, 7 parts of pipewort and 3 parts of chamomile; the preparation method of the traditional Chinese medicine extract comprises the following steps:

weighing glossy privet fruit, cassia seed, pale butterflybush flower, pipewort and chamomile according to the weight ratio, adding double distilled water according to the liquid-material ratio of 100 ml/g after rinsing, decocting for 4-6h with slow fire, separating filtrate after cooling, and diluting the filtrate with double distilled water to 1/2 of the volume before decocting to obtain the product;

the traditional Chinese medicine extract comprises the following components:

glossy privet fruit: is mature dry seed of Ligustrum lucidum belonging to Oleaceae, has sweet and bitter taste and cool property, and can enter liver and kidney channels, improve eyesight and blacken hair, and can be used for treating giddiness, tinnitus, dim eyesight, and blurred vision, enhancing vitality, refreshing, and relieving eye fatigue;

cassia seed: is dry mature seed of Cassia Torae semen of Leguminosae, is sweet and bitter in taste, slightly cold in nature, enters liver and large intestine channels, clears liver and improves eyesight, and moistens intestine and relieves constipation, and is applied to conjunctival congestion, swelling and pain, photophobia and lacrimation, heat accumulation or intestinal dryness caused by dare and irritability or wind heat of liver channels;

flos Buddlejae, is dried flower or flower bud of flos Buddlejae of Lonicera Japonica of Loganiaceae, has sweet taste and slightly cold nature, enters liver channel, has effects of dispelling pathogenic wind, cooling blood, moistening liver, and improving eyesight, and can be used for treating conjunctival congestion, swelling and pain, lacrimation, photophobia, cataract, and exophthalmos;

eriocaulon buergerianum (L.) Gaertn is dry head-shaped inflorescence with flower stem of Eriocaulon buergerianum (L.) Gaertn of Eriocaulon plant of Eriocaulon family, has sweet and mild taste, enters liver and stomach channels, and has effects of dispelling pathogenic wind, clearing heat, improving eyesight and removing nebula. Treating nebula, night blindness, headache, toothache, pharyngitis and epistaxis;

flos Chrysanthemi, the whole herb of the feverfew of Compositae, the taste is sweet, slightly bitter, the nature is slightly cold, enter stomach, liver two channels, can remove the great heat, stop headache and dizzy, accept the membrane of the eye tear nebula, the eyesight is very tranquil, the dark palpus tempura is tested, disperse damp and remove fever, relieve restlessness and relieve dryness;

the preparation method of the amphiphilic oyster short peptide comprises the following steps:

(1) weighing 1 part of pentaerythritol monoacetal according to the mass part, dissolving the pentaerythritol monoacetal in dichloromethane with the concentration of 0.5g/ml, respectively adding 0.5 part of dimethylaminopyridine and 4 parts of triethylamine after dissolving, stirring and heating to 60 ℃, adding 3.5 parts of succinic anhydride, keeping the temperature at 60 ℃, stirring and reacting for 24 hours, washing the mixture by using a hydrochloric acid solution and deionized water in sequence after the reaction is finished, separating an organic phase, adding solid anhydrous magnesium sulfate for drying, purifying the mixture by silica gel column chromatography after drying, carrying out online monitoring by using a 294nm ultraviolet detector, using a petroleum ether-ethyl acetate-methanol mixed system (V/V/V is 10:1:0.5) as a mobile phase, combining effluent liquid with the same components, and removing a solvent to obtain a carboxylated product;

(2) weighing 1 part of the carboxylated product according to the weight parts, dissolving the carboxylated product in dimethylformamide at the concentration of 0.5g/ml, respectively adding 2 parts of dimethylaminopyridine and 1 part of N, N' -dicyclohexylcarbodiimide after dissolving, stirring, heating to 70 ℃, adding 4.5 parts of lanosterol, continuing to perform heat preservation and stirring reaction for 12 hours, and removing the solvent after the reaction is finished to obtain an esterified product;

(3) weighing 1 part of the esterification product according to the parts by weight, and dissolving the esterification product in a mixing volume ratio of 3: 1, stirring and heating to 60 ℃, adding 0.3 part of palladium-carbon with the effective substance content of 10%, stirring and reacting for 12 hours under the hydrogen partial pressure of 1MPa, and filtering to obtain a reduction product;

(4) weighing 1 part of the reduction product according to the parts by weight, adding 0.5 part of p-dimethylaminopyridine and 0.3 part of oyster short peptide, stirring, heating to 60 ℃, keeping the temperature, stirring, reacting for 5 hours, purifying by a silica gel column after the reaction is finished, and removing a solvent to obtain the amphiphilic oyster short peptide;

the preparation method of the oyster short peptide comprises the following steps:

s1, weighing the soft tissue of the oyster, adding redistilled water according to the material-liquid ratio of 3-5ml/g for homogenization treatment to obtain an oyster homogenate, gradually heating the oyster homogenate to 90-100 ℃, preserving heat for 10-20min, cooling to 45-50 ℃, adjusting the pH of the oyster homogenate to 6.5-7.5, adding Protamex compound protease, preserving heat for enzymolysis for 4h, performing water bath enzyme deactivation after the enzymolysis is finished, adding chitosan for flocculation after cooling, centrifuging, filtering and separating enzymolysis liquid through a plurality of layers of gauzes to obtain a supernatant;

wherein the addition amount of the composite protease is 3000-4000U/g, and the addition amount of the chitosan is 1-3g/100 ml;

s2, sequentially desalting the supernatant through cation exchange resin and anion exchange resin to obtain an exchange solution, sequentially passing the exchange solution through a first-stage ultrafiltration membrane and a second-stage ultrafiltration membrane at room temperature to obtain an oyster short peptide solution, and freeze-drying to obtain the oyster short peptide;

wherein the molecular weight cut-off of the first-stage ultrafiltration membrane is 5kDa, and the ultrafiltration pressure is 0.15-0.18 MPa; the molecular weight cut-off of the secondary ultrafiltration membrane is 1kDa, and the ultrafiltration pressure is 0.18-0.21 MPa;

the eye drop also comprises a pH adjusting buffer, an osmotic pressure regulator and a viscosity regulator, wherein the pH adjusting buffer is a boric acid-borax system, the pH is adjusted to 6.0-8.0 (preferably 7.0), the osmotic pressure regulator is sodium chloride or glucose, the osmotic pressure is adjusted to 280-380 (preferably 300) mOsm/L, the viscosity regulator is sodium hyaluronate, and the viscosity is adjusted to 6-10 (preferably 8) mps.

Example 2

The difference from example 1 is that: the eye drop comprises the following components in parts by weight:

90 parts of traditional Chinese medicine extract, 1 part of amphiphilic oyster short peptide and 1 part of composite polyacrylamide nano particles;

the preparation method of the composite polyacrylamide nano particle comprises the following steps:

s1, weighing 4- (2-hydroxyethyl) -1-piperazine propanesulfonic acid and acrylate with equal molar ratio, dissolving the 4- (2-hydroxyethyl) -1-piperazine propanesulfonic acid and the acrylate in 1mol/L sodium hydroxide solution, respectively, stirring and refluxing for 1-2h, cooling after the reaction is finished, adding a large amount of anhydrous ether, separating and precipitating, washing the precipitate with anhydrous ethanol, and drying to obtain acryloyl piperazine propanesulfonic acid salt;

s2, weighing 1 part of N-isopropyl acrylamide, 0.3 part of N, N '-methylene bisacrylamide and 1 part of propylene piperazine propanesulfonate according to parts by weight, dissolving the N-isopropyl acrylamide, the N, N' -methylene bisacrylamide and the propylene piperazine propanesulfonate in double distilled water, filtering the mixed solution by Whatman No. 2 filter paper after the monomers are fully dissolved, taking a filtrate, ultrasonically degassing the filtrate for 10min, then carrying out nitrogen deoxidization for 30min, adding 0.1g/ml ammonium persulfate solution as an initiator, stirring and reacting for 2-3h under the nitrogen protection atmosphere to obtain a polymerization product, placing the polymerization product in the double distilled water for dialysis and purification for 96h (changing water once every 12 h), freeze-drying after purification, crushing and pulverizing to obtain the polymer.

Comparative example 1

The difference from example 1 is that: does not contain amphiphilic oyster short peptide.

Comparative example 2

The difference from example 2 is that: does not contain amphiphilic oyster short peptide.

Comparative example 3

The commercially available leucoketchun eye drops.

Examples of the experiments

Establishing a cataract animal model:

taking SD rat (body weight 160g-180g), injecting 3.5% chloral hydrate 1.5mL (1mL/100g) into abdominal cavity, performing anesthesia treatment, selecting compound tolbicamide eye drops to perform conventional mydriasis on SD rat, exposing two eyeballs of SD rat, placing in 300-320 nm ultraviolet cross-linking instrument, fixing ultraviolet ray to the eyes of SD rat at a distance of 14cm, simultaneously fixing the distance between SD rats at 6cm, irradiating once a day for 15min each time, and accumulating illumination intensity of 9kJ/m2In 7 days, an animal model of cataract was established. During which time the rat ocular lens was observed dynamically for turbidity after uv irradiation.

The total number of SD rats is 70, and the SD rats are randomly and averagely divided into 7 groups, namely a blank group, a model group, an experimental group to an experimental five group.

Blank group: normal SD rats without uv irradiation;

model group: rats that received uv irradiation for 7 days only;

one set of experiments: after 7 days of ultraviolet irradiation, rats were administered the eye drops of example 1 of the present invention by dropping for 10 days, 3 times/day, 10. mu.L/time;

two groups of experiments were carried out: after 7 days of ultraviolet irradiation, rats were administered the eye drops of example 2 of the present invention by dropping for 10 days, 3 times/day, 10. mu.L/time;

three groups of experiments were performed: after 7 days of ultraviolet irradiation, rats were administered the eye drops of comparative example 1 of the present invention by dropping for 10 days, 3 times/day, 10. mu.L/time;

four groups were tested: after 7 days of ultraviolet irradiation, rats were administered the eye drops of comparative example 2 of the present invention by dropping for 10 days, 3 times/day, 10. mu.L/time;

five groups of experiments: after 7 days of ultraviolet irradiation, rats were administered the eye drops of comparative example 3 of the present invention by dropping for 10 days, 3 times/day, 10. mu.L/time;

lens turbidity detection: the turbidity of the cortical region of the crystalline lens is detected by a slit lamp after mydriasis of the 7 groups of rats, the frequency is detected for 2 d/time, and the turbidity is scored according to LOCS III standard.

The results of the average haze measurements are shown in the following table:

0d 2d 4d 6d 8d 10d
blank group 0.28 0.28 0.29 0.28 0.28 0.29
Model set 2.11 2.19 2.42 2.63 2.86 3.21
Experiment group 2.09 1.72 1.34 0.93 0.61 0.38
Two groups of experiments 2.10 1.66 1.27 0.87 0.59 0.35
Three groups of experiments 2.11 2.01 1.82 1.60 1.38 1.22
Experiment four groups 2.11 1.95 1.63 1.31 1.12 0.84
Five groups of experiments 2.09 1.77 1.35 1.00 0.75 0.43

Finally, it should be noted that the above embodiments are only used for illustrating the technical solutions of the present invention, and not for limiting the protection scope of the present invention, although the present invention is described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications or equivalent substitutions can be made on the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention.

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