CN114288318A - Eye lotion containing schizophyllan and preparation method thereof - Google Patents
Eye lotion containing schizophyllan and preparation method thereof Download PDFInfo
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Abstract
The invention provides an eye lotion containing schizophyllan and a preparation method thereof. The eye lotion containing schizophyllan comprises schizophyllan, ectoin, an ophthalmic gel matrix, an osmotic pressure regulator and water. The eye lotion containing the schizophyllan is used for cleaning eyes, comprises the periphery of eyes and the surface of eyeballs, and can remove foreign matters or secretions such as dust, particles, pollen and the like; the eye lotion has the capabilities of relieving eye fatigue, ache, resisting radiation, preserving moisture, relieving eye dryness, eliminating inflammation and inhibiting bacteria, and has excellent effects on eye visual fatigue, eye dryness and other symptoms caused by wearing contact lenses for a long time.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to eye lotion containing schizophyllan and a preparation method thereof.
Background
Eyes are exposed in the air for a long time and are fragile departments of human bodies, and various eye diseases are inevitably caused by the invasion of dust, haze and cosmetics for a long time. The cornea is positioned at the forefront end of the human eye, the cornea structure is divided into an epithelial layer, a front elastic layer, a matrix layer, a rear elastic layer and an endothelial layer, and a large number of sensory nerves are distributed on the cornea, so that the cornea is one of the positions with the sharpest pain sensation of the human body. The eye lotion can relieve discomfort, dryness and the like of eyes to a certain extent, and has the effects of refreshing, relieving itching, promoting nutrition of eyes, keeping eyes moist and sanitary, avoiding conjunctival congestion and the like.
However, it is understood that the major functional components of commercially available eye washes include: the ampheniramine maleate, the chondroitin sodium sulfate, the dipotassium glycyrrhizinate, the vitamin B6, the taurine, the vitamin B12 and the like seem to have various components and rich nutrition, but hide in crisis. For example: the side effect of the chondroitin sodium sulfate is occasionally slight irritation, and the side effect on the glasses is obvious after long-term or frequent use, so that the drug-induced keratitis and the like can be caused; frequent supplementation with vitamin b6 in large amounts is likely to result in severe peripheral neuritis.
In addition, the eye lotion can be added with preservative to prolong the shelf life, and the preservative can damage the ocular surface by the following ways: microvilli that disrupt the corneal epithelium; has detergent-like effect on lipid layer to accelerate tear evaporation; indirectly destroying the stability of the tear film; reducing the growth and viability of corneal cells; resulting in ocular surface inflammatory responses, subconjunctival fibrosis, and the like. In addition, even if a preservative is added, bacterial contamination of the eye wash cannot be completely avoided due to factors such as the type, concentration, compatibility, use, and the like of the preservative.
In addition, the eye lotion is also added with anti-allergic drugs, such as chlorpheniramine maleate (commonly called chlorpheniramine), and although the content of the anti-allergic drugs is not high, the frequent use of the eye lotion causes drug dependence. Improper use of eye washes, eye drops, etc. can easily damage the flora environment of the ocular surface itself, leading to dysbacteriosis, thereby increasing the risk of ocular surface diseases.
CN111991415A discloses an eye care composition comprising 0.05-2% by mass of chondroitin sulfate, 0.01-2.5% by mass of hyaluronic acid, and 0.5-5% by mass of ectoin or an ophthalmology acceptable ectoin derivative in the eye care composition. The disclosed eye care composition can accelerate the repair of corneal injury by combining hyaluronic acid, ectoin and chondroitin sulfate in a certain weight ratio, however, the side effect of chondroitin sulfate sodium is occasionally slight irritation, the side effect on glasses is obvious after long-term or frequent use, and the situation of keratitis is aggravated; and hyaluronic acid has good moisturizing performance, but has common antibacterial and anti-inflammatory effects, and inevitably needs to be added with other auxiliary agents: surfactant (such as benzalkonium chloride), and effective components (such as taurine and vitamins).
CN111991270A discloses fullerene c60 energized eye drops and a preparation method thereof. The eye lotion is prepared from the following raw materials in parts by weight: 65-85 parts of water, 0.01-0.05 part of EDTA (ethylene diamine tetraacetic acid), 0.1-1.0 part of sodium hyaluronate, 1-10 parts of taurine, 1-5 parts of trehalose, 0.1-2 parts of sodium chloride, a pH regulator for regulating the pH of the eye lotion to be neutral, 10-25 parts of a functional extract and fullerene, wherein the content of the fullerene in the eye lotion is 0.1-0.8 mg/L. The aims of improving eyesight and relieving asthenopia are achieved by functional components of fullerene, sodium hyaluronate, taurine and functional extracts (cucumber fruit extract, witch hazel extract and the like). However, fullerene can cause certain irritation to skin, eyes are fragile organs of human bodies, and particularly, tolerance experiments are carried out before the fullerene is used by people who are sensitive and fragile. Hyaluronic acid has good moisturizing performance, but has common antibacterial and anti-inflammatory effects, and inevitably needs to be added with other auxiliary agents: surfactant (such as benzalkonium chloride), and effective components (such as taurine and vitamins).
Therefore, how to provide an eye lotion which has no irritation, no side effects, better comfort and smoothness, and can relieve various symptoms such as dry eyes, hyperemia and the like is a research focus in the field.
Disclosure of Invention
Aiming at the defects of the prior art, the invention aims to provide an eye lotion containing schizophyllan and a preparation method thereof. The eye lotion containing the schizophyllan is used for cleaning eyes, comprises the periphery of eyes and the surface of eyeballs, and can remove foreign matters or secretions such as dust, particles, pollen and the like; the eye lotion has the capabilities of relieving eye fatigue, ache, resisting radiation, preserving moisture, relieving eye dryness, eliminating inflammation and inhibiting bacteria, and has excellent effects on eye visual fatigue, eye dryness and other symptoms caused by wearing contact lenses for a long time.
In order to achieve the purpose, the invention adopts the following technical scheme:
in a first aspect, the present invention provides a schizophyllan-containing eye lotion comprising schizophyllan, ectoin, an ophthalmic gel matrix, an osmotic pressure regulator, and water.
In the eye lotion, the schizophyllan and the ectoine are added, and are matched with each other, so that the eye lotion has a synergistic effect and can further improve the moisturizing, anti-inflammatory, antibacterial and repairing effects; the eye lotion containing the schizophyllan has excellent capabilities of relieving eye fatigue, dryness, ache, resisting radiation, preserving moisture, relieving eye dryness, eliminating inflammation and inhibiting bacteria, and preventing complications such as keratitis. And other functional components, antibiotics, preservatives and the like are not required to be added, so that the eye protection mask has the effects of effectively sterilizing, enhancing the eye resistance, relieving asthenopia, relieving eye discomfort and the like.
Wherein, Schizophyllan (SPG) is one of the main active components of Schizophyllum commune, SPG belongs to a nonionic water-soluble high-polymer glucose, the main chain is composed of 1, 3-beta-D-glucopyranose units, each 3 glucose molecules generate a beta-1, 6-combined D-glucopyranose branch, and the Schizophyllan has good functions of enhancing immunity, preserving moisture, resisting oxidation and the like and improving the cellular immune function. It can easily penetrate into cornea, so as to eliminate inflammation and inhibit bacteria, and prevent complications such as keratitis.
In the method, ECTOIN (ECTOIN) which is named as tetrahydro-methyl pyrimidine carboxylic acid is an amino acid derivative, can balance the osmotic pressure of cells, and has good protection effect on enzyme, DNA, protein, nucleic acid, cell membranes and whole cells under adverse conditions of high temperature, severe cold, drought, extreme pH value, high pressure, high salt, high radiation and the like. In addition, the ring structure of the ectoine molecule is easy to form hydrogen bonds with water molecules, the association capability of the water molecules is enhanced, the water molecules are directionally arranged around the ring structure, and the spatial arrangement of the water molecules is changed; can also protect cornea and conjunctival cells, enhance the defense function of the cells and avoid the damage to eyes caused by long-term use of the prior ophthalmic preparation.
Preferably, the eye lotion containing schizophyllan comprises the following components in percentage by mass:
the amount of the schizophyllan may be, for example, 0.1 to 10%, such as 0.1%, 0.2%, 0.5%, 0.8%, 1%, 1.5%, 2%, 2.5%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, or the like, based on 100% by mass of the total schizophyllan-containing eye lotion.
The ectoin content is 0.01 to 5%, for example, 0.01%, 0.02%, 0.04%, 0.06%, 0.08%, 0.1%, 0.2%, 0.5%, 0.8%, 1%, 1.2%, 1.5%, 2%, 2.5%, 3%, 3.5%, 4%, 4.5%, 5%, or the like, based on 100% by mass of the total eye wash containing schizophyllan.
The ophthalmic gel matrix content is 0.01-3%, for example, 0.01%, 0.02%, 0.05%, 0.08%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.8%, 1%, 1.2%, 1.5%, 2%, 2.5%, 3%, etc., based on 100% by mass of the total schizophyllan-containing eye lotion.
The content of the osmotic pressure regulator is 0.01 to 2%, for example, 0.01%, 0.05%, 0.1%, 0.2%, 0.5%, 0.8%, 1%, 1.2%, 1.5%, 1.8%, 2%, etc., based on 100% by mass of the total eye wash containing schizophyllan.
The water content is 80 to 99%, for example, 80%, 82%, 84%, 86%, 88%, 90%, 92%, 94%, 96%, 98%, 99% or the like, based on 100% by mass of the total eye wash containing the schizophyllan.
Preferably, the schizophyllan is a small molecule schizophyllan.
Preferably, the molecular weight of the small molecular schizophyllan is 10-100kD, such as 10kD, 20kD, 30kD, 40kD, 50kD, 60kD, 70kD, 80kD, 90kD, 100kD, etc., preferably 10-30 kD.
In the invention, the eye lotion is preferably added with small molecular schizophyllan with the molecular weight of 10-100kD, because the small molecular schizophyllan is easier to permeate into the cornea of the eye, thereby further improving the multiple effects of the eye lotion such as antifungal, anti-inflammatory and promoting the corneal epithelium repair; and because the molecular weight is smaller, the prepared eye drop has strong water solubility, no toxicity, no side effect and further improved anti-inflammatory effect.
Preferably, the mass ratio of the schizophyllan to ectoin is 10 (0.5-3), and may be, for example, 10:0.5, 10:1, 10:1.5, 10:2, 10:2.5, 10:3, etc.
In the invention, the mass ratio of the schizophyllan to the ectoin is 10 (0.5-3), and the moisture retention, antifungal, anti-inflammatory and corneal epithelium repair promotion capability are optimized in the ratio. If the schizophyllan is too much and the ectochile is too little, the eye lotion has reduced moisture retention and water supplement capacity, so that the eye lotion has general relieving capacity on symptoms such as dry eye and the like; if the schizophyllan is too little, but the ectoin is too much, or the eye lotion is caused to have antifungal, anti-inflammatory and corneal epithelial repair effects.
Preferably, the ophthalmic gel matrix comprises any one or a combination of at least two of polyvinyl alcohol, medium molecular weight schizophyllan, gellan gum, poloxamer, carbomer, hydroxypropyl methylcellulose, or xanthan gum, preferably any one or a combination of at least two of polyvinyl alcohol, medium molecular weight schizophyllan, or hydroxypropyl methylcellulose.
Preferably, the molecular weight of the polyvinyl alcohol is 50-150kD, such as 50kD, 60kD, 70kD, 80kD, 90kD, 100kD, 110kD, 120kD, 130kD, 140kD, 150kD, etc.
Preferably, the molecular weight of the medium molecular weight schizophyllan is 100-.
Preferably, the poloxamer includes any one or a combination of at least two of poloxamer 407, poloxamer 188 or carbomer 934P.
Preferably, the carbomer comprises carbomer 940 and/or carbomer 974P.
Preferably, the ophthalmic gel matrix is a group of polyvinyl alcohol, medium molecular weight schizophyllan and hydroxypropyl methylcellulose.
Preferably, the mass ratio of the polyvinyl alcohol to the medium molecular weight schizophyllan to the hydroxypropyl methyl cellulose is (3-10): 0.1-5): 0.1-2;
wherein "3 to 10" may be, for example, 3, 4, 5, 6, 7, 8, 9, 10, etc.;
wherein "0.1 to 5" may be, for example, 0.1, 1, 2, 3, 4, 5, etc.;
here, "0.1 to 2" may be, for example, 0.1, 0.5, 1, 1.5, 2 or the like.
In the invention, the polyvinyl alcohol, the middle molecular weight schizophyllan and the hydroxypropyl methyl cellulose with the mass ratio of (3-10): (0.1-5): (0.1-2) are selected as the ophthalmic gel matrix as the preferable technical proposal, which can further ensure the comfort for cleaning the eyes, namely when the foreign matters such as dust, particles, pollen and the like are removed around the eyes and on the surfaces of the eyeballs or the secretion of the eyes is washed out, the ophthalmic gel matrix further reduces the mechanical friction of the eyelids to the wound, relieves the pain and is beneficial to the wetting of the eyes.
Preferably, the osmotic pressure regulator comprises any one of sodium chloride, glucose, borax, boric acid, mannitol or glycerol or a combination of at least two of them.
Preferably, the eye wash containing schizophyllan further comprises a stabilizer.
Preferably, the stabilizer comprises any one of cysteine, cysteine salt, citric acid salt, tartaric acid or tartaric acid salt or a combination of at least two thereof.
Preferably, the stabilizer is 0.01 to 0.15% by mass of the total schizophyllan-containing eyewash, and may be, for example, 0.01%, 0.02%, 0.04%, 0.06%, 0.08%, 0.1%, 0.12%, 0.15%, etc.
Preferably, the pH of the eye wash containing schizophyllan is 5.5-8.0, for example, 5.5, 6.0, 6.2, 6.4, 6.6, 6.8, 7.0, 7.2, 7.4, 7.6, 7.8, 8.0, etc., preferably 6.0-7.0.
In a second aspect, the present invention provides a process for preparing an eyewash containing schizophyllan as described in the first aspect, said process comprising the steps of:
(1) mixing schizophyllan and water to obtain a schizophyllan solution;
(2) mixing the schizophyllan solution obtained in the step (1), ectoin, an ophthalmic gel matrix and an osmotic pressure regulator to obtain the eye lotion containing the schizophyllan.
Preferably, in step (1), the mixing temperature is 50-90 deg.C, such as 50 deg.C, 55 deg.C, 60 deg.C, 65 deg.C, 70 deg.C, 75 deg.C, 80 deg.C, 85 deg.C, 90 deg.C, etc., and the mixing time is 10-30min, such as 10min, 15min, 20min, 25min, 30min, etc.
Preferably, in step (1) and step (2), the mixing is performed under stirring, and the rotation speed of the stirring is 100-500rpm, such as 100rpm, 150rpm, 200rpm, 250rpm, 300rpm, 350rpm, 400rpm, 450rpm, 500rpm, and the like.
Preferably, in step (2), the mixing temperature is 50 ℃ or less, such as 50 ℃, 40 ℃, 30 ℃, 20 ℃, 10 ℃, 5 ℃ and the like, and the mixing time is 10-40min, such as 10min, 15min, 20min, 25min, 30min, 35min, 40min and the like.
Preferably, in the step (2), the mixing comprises the following specific steps: cooling the schizophyllan solution to 40-50 deg.C (e.g. 40 deg.C, 42 deg.C, 44 deg.C, 46 deg.C, 48 deg.C, 50 deg.C, etc.), adding ophthalmic gel matrix, stirring at 100-200rpm (e.g. 100rpm, 120rpm, 140rpm, 160rpm, 180rpm, 200rpm, etc.) for 5-10min (e.g. 5min, 6min, 7min, 8min, 9min, 10min, etc.), cooling to 20-40 deg.C (e.g. 20 deg.C, 25 deg.C, 30 deg.C, 40 deg.C, etc.), adding ectoin 100-500rpm (e.g. 100rpm, 200rpm, 300rpm, 400rpm, 500rpm, etc.) for 1-10min (e.g. 1min, 2min, 4min, 6min, 8min, 10min, etc.), and finally adding osmotic pressure regulator to 100-500rpm (e.g. 100rpm, 200rpm, 300rpm, 400rpm, etc.) 500rpm, etc.) for 1-10min (e.g., 1min, 2min, 4min, 6min, 8min, 10min, etc.) to obtain the eye lotion containing schizophyllan.
Compared with the prior art, the invention has the following beneficial effects:
(1) the eye lotion containing the schizophyllan is used for cleaning eyes, comprises the periphery of eyes and the surface of eyeballs, can remove foreign matters or secretions such as dust, particles and pollen, and the like, can relieve visual fatigue, has the effects of moistening, relieving fatigue, cleaning and the like on the eyeballs, and can enhance comfort and lubricating feeling;
(2) the eye lotion disclosed by the invention has the capabilities of relieving eye fatigue and ache, resisting radiation, preserving moisture, relieving eye dryness, eliminating inflammation and inhibiting bacteria, and has excellent effects on eye visual fatigue, eye dryness and other symptoms caused by wearing contact lenses for a long time.
Detailed Description
The technical solution of the present invention is further explained by the following embodiments. It should be understood by those skilled in the art that the examples are only for the understanding of the present invention and should not be construed as the specific limitations of the present invention.
The examples and comparative examples are carried out according to techniques or conditions described in the literature in the field or according to the product instructions, without specifying the particular technique or condition. The reagents or apparatus used are conventional products commercially available from a formal channel or may be prepared by the prior art, without reference to the manufacturer.
Example 1
The embodiment provides an eyewash containing schizophyllan, which comprises the following components in percentage by mass:
the preparation method of the eye lotion containing the schizophyllan comprises the following steps:
(1) mixing and stirring the schizophyllan and water at 80 ℃ and the rotating speed of 200rpm for 10min according to the proportion to completely dissolve the schizophyllan to obtain a uniform schizophyllan solution;
(2) cooling the obtained schizophyllan solution to 45 ℃, sequentially adding gellan gum, poloxamer 407 and hydroxypropyl methyl cellulose, stirring for 8min at 100rpm, cooling to 30 ℃, adding ectoin, stirring for 8min at 200rpm, adding an osmotic pressure regulator and a stabilizer, stirring for 3min at 200rpm, and obtaining the eye lotion containing the schizophyllan with the pH value of 6.5 and the osmotic pressure of 300 mOsm/L.
Example 2
The embodiment provides an eyewash containing schizophyllan, which comprises the following components in percentage by mass:
the preparation method of the eye lotion containing the schizophyllan comprises the following steps:
(1) mixing and stirring the schizophyllan and water at 75 ℃ and the rotating speed of 200rpm for 12min according to the proportion to completely dissolve the schizophyllan to obtain a uniform schizophyllan solution;
(2) firstly, cooling the obtained schizophyllan solution to 45 ℃, sequentially adding gellan gum, poloxamer 188 and hydroxypropyl methyl cellulose, stirring for 8min at 100rpm, then cooling to 30 ℃, adding ectoin, stirring for 8min at 200rpm, finally adding an osmotic pressure regulator and a stabilizer, stirring for 3min at 200rpm, and obtaining the eye lotion containing the schizophyllan with the pH of 6.6 and the osmotic pressure of 280 mOsm/L.
Example 3
The embodiment provides an eyewash containing schizophyllan, which comprises the following components in percentage by mass:
the preparation method of the eye lotion containing the schizophyllan comprises the following steps:
(1) mixing and stirring the schizophyllan and water at 70 ℃ and the rotating speed of 300rpm for 20min according to the proportion to completely dissolve the schizophyllan to obtain a uniform schizophyllan solution;
(2) cooling the obtained schizophyllan solution to 45 ℃, sequentially adding gellan gum, poloxamer 188 and hydroxypropyl methyl cellulose, stirring at 100rpm for 5min, cooling to 28 ℃, adding ectoin, stirring at 100rpm for 10min, adding an osmotic pressure regulator, and stirring at 100rpm for 10min to obtain an eye lotion containing schizophyllan with pH of 6.3 and osmotic pressure of 300 mOsm/L.
Example 4
This example provides an eye wash containing schizophyllan, differing from example 1 only in that the added schizophyllan has an average molecular weight of 100 kD; and step (1) needs to be mixed and stirred with water at 85 ℃ and the rotating speed of 500rpm for 30min to completely dissolve the schizophyllan, so as to obtain a uniform schizophyllan solution.
Example 5
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that the content of schizophyllan is 1.1%, the content of ectoin is 0.01%, and the contents of other components and the preparation method are the same as example 1.
Example 6
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that the content of schizophyllan is 0.5%, the content of ectoin is 0.6%, and the contents of other components and preparation method are the same as example 1.
Example 7
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that polyvinyl alcohol is not added to the ophthalmic gel base, the content of schizophyllan (average molecular weight 100kD) is increased to 0.8%, the content of hydroxypropyl methylcellulose is increased to 0.5%, and the contents of other components and the preparation method are the same as example 1.
Example 8
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that schizophyllan (average molecular weight 100kD) is not added to the ophthalmic gel base, the polyvinyl alcohol content is increased to 1.0%, the hydroxypropyl methylcellulose content is increased to 0.3%, and the contents of other components and the preparation method are the same as example 1.
Example 9
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that hydroxypropyl methylcellulose is not added to the ophthalmic gel base, the content of schizophyllan (average molecular weight 100kD) is increased to 0.5%, and the contents of other components and the preparation method are the same as example 1.
Example 10
This example provides an eye wash containing schizophyllan, which differs from example 1 only in that the ophthalmic gel matrix is completely replaced with a combination of 0.8% carbomer 974P and 0.5% hydroxypropyl methylcellulose, and the contents of other components and preparation method are the same as example 1.
Example 11
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that the ophthalmic gel matrix is completely replaced with 1.3% schizophyllan (average molecular weight 100kD), and the contents of other components and the preparation method are the same as example 1.
Example 12
This example provides an eye wash containing schizophyllan, which is different from example 1 only in that the ophthalmic gel matrix is completely replaced with 1.3% polyvinyl alcohol (average molecular weight 100kD), and the contents of other components and the preparation method are the same as example 1.
Comparative example 1
This comparative example provides an eye lotion which differs from example 1 only in that no schizophyllan was added, the ectoine content was increased to 1.2%, and the other component contents and preparation method were the same as example 1.
Comparative example 2
This comparative example provides an eye lotion which differs from example 1 only in that 1.0% of schizophyllan with an average molecular weight of 10kD is replaced by 1.0% of sodium hyaluronate with a molecular weight of 10kD, and the contents of other components and preparation method are the same as in example 1.
Comparative example 3
This comparative example provides an eye lotion which differs from example 1 only in that 1.0% of schizophyllan with an average molecular weight of 10kD is replaced by 1.0% of sodium acetylated hyaluronate with a molecular weight of 20kD, the contents of the other components and the preparation method are the same as in example 1.
Comparative example 4
This comparative example provides an eye lotion which differs from example 1 only in that 1.0% of schizophyllan with an average molecular weight of 10kD is replaced by 1.0% of sodium hyaluronate with a molecular weight of 100kD, and the contents of the other components and the preparation method are the same as in example 1. (ii) a And step (1) needs to be mixed and stirred with water at 70 ℃ and the rotating speed of 50rpm for 40min to completely dissolve the schizophyllan, so as to obtain a uniform schizophyllan solution.
Comparative example 5
This comparative example provides an eye lotion which differs from example 1 only in that the concentration of schizophyllan increased to 1.2% without addition of ectoin, and in that the concentrations of other components and the preparation method are the same as in example 1.
Test example 1
Irritation test
The test method comprises the following steps: 54 healthy New Zealand rabbits, which were not damaged by ocular examination, were selected and randomly divided into 18 groups, 3 rabbits/group, and physiological saline was given to the left and right eyes of group 1 as a control group, and physiological saline was also given to the left eyes of groups 2 to 18 as a self-control, and the eye wash containing schizophyllan provided in examples 1 to 12 and the eye wash provided in comparative examples 1 to 5 were given to the right eyes, respectively. Slowly dripping eye lotion into conjunctival sac of rabbit eyes, pressing nasolacrimal duct, passively closing eyes, washing eyes for 28d in 3 times respectively in the morning, at noon and at night, wherein the dosage of each eye lotion is 1mL, observing stimulation conditions of cornea, iris, conjunctiva, edema and secretion, and respectively scoring each group of rabbits according to the following table 1:
TABLE 1
The specific results are shown in table 2 below:
TABLE 2
As can be seen from the test data in Table 1, the eye lotion disclosed by the invention does not contain preservatives, is non-irritant, has no side effects, can be absorbed by eyes, avoids potential risks and toxic and side effects on the eyes caused by additives such as preservatives and the like, and has high stability.
Test example 2
Wetting test
Test samples: eye washes containing schizophyllan as provided in examples 1-12 and eye washes provided in comparative examples 1-5;
the test principle is as follows: atropine blocks M choline receptors, so that the sphincter pupillae and the ciliary muscles are relaxed, but excessive or long-term continuous application can cause lacrimal secretion obstacle ophthalmopathy which takes eye dryness as a main symptom, and common symptoms comprise eye dryness, easy tiredness, eye itch, foreign body sensation, burning sensation, thick secretion, intolerance of wind, photophobia and sensitivity to external stimulation; the amount of lacrimal secretion of the atropine group is obviously reduced, and whether the xerophthalmia caused by the atropine can be relieved or not is judged by applying the eye lotion, wherein the higher the amount of lacrimal secretion is, the better the relieving effect is;
the test method comprises the following steps:
(1) 54 healthy New Zealand rabbits with no damage to eye examination are taken at the age of 10 weeks, the rabbits are randomly divided into 18 groups and 3 groups, after adaptive feeding is carried out for 2 days, a Schirmer test is carried out, the tear secretion condition is determined, specifically, a tear detection filter paper strip is taken, one end of the tear detection filter paper strip is folded by 5mm, the tear detection filter paper strip is placed at 1/3 in the middle and outside of the lower eyelid of the rabbit eye, the tear detection filter paper strip is taken out after 5min, the wet length from the folded part is measured and recorded as the normal tear secretion condition, then 1 wt% atropine sulfate eye drops are applied, the continuous application is carried out for 2 weeks and 3 times per day, the phenomenon that the tear secretion (the wet length of lacrimal glands) is obviously reduced appears in each group of rabbit models, and the successful modeling of the rabbit models with atropine causing the xerosis angle/conjunctivitis is shown;
(2) after administration of the atropine sulfate eye drops 7d, normal saline was given to the left and right eyes of group 1 as a control group, and normal saline was also given to the left eyes of groups 2 to 18 as a self-control, and the right eyes corresponded to the eye lotion containing schizophyllan provided in examples 1 to 12 and the eye lotion provided in comparative examples 1 to 5, respectively; specifically, the eye washing liquid is slowly dripped into the conjunctival sac of the eye of the rabbit, the nasolacrimal duct is pressed, the eye is passively closed, the eye is continuously washed for 14d in each morning, noon and evening with the dosage of 1mL each time, the lacrimal secretion condition is recorded, and the lacrimal secretion growth rate is calculated; wherein the tear secretion increase rate (%) (length after administration-length before administration) is 100% per length before administration;
the specific results are shown in table 3 below:
TABLE 3
As can be seen from the test data in Table 2, the increased rate of lacrimal secretion of eye washing solution containing schizophyllan of the present invention was more than 80%, and the increased rate of lacrimal secretion of rabbit model as the most preferred examples 1-3 of the present invention was more than 97%. The eye lotion containing schizophyllan disclosed by the invention has a synergistic effect due to the mutual matching of the components, and can further improve the dry and astringent abilities, keep moisture and relieve eye dryness.
Test example 3
Anti-inflammatory assay
Test samples: eye washes containing schizophyllan as provided in examples 1-12 and eye washes provided in comparative examples 1-5;
the test principle is as follows:
(1) IL-6: adopting a double-antibody one-step sandwich method enzyme-linked immunosorbent assay (ELISA); and sequentially adding a specimen, a standard substance and an HRP-marked detection antibody into the coated micropores previously coated with the capture antibody of the rabbit interleukin 6(IL-6), incubating and thoroughly washing. The color is developed with the substrate TMB, which is converted to blue by the catalysis of peroxidase and to the final yellow color by the action of an acid. The shade of the color is positively correlated with the rabbit interleukin 6(IL-6) in the sample. Measuring absorbance (OD value) at the wavelength of 450nm by using an enzyme-labeling instrument, and calculating the concentration of the sample;
(2) TNF- α: adopting a double-antibody one-step sandwich method enzyme-linked immunosorbent assay (ELISA); and adding the specimen, the standard substance and the HRP-marked detection antibody into the coated micropores which are coated with the capture antibody of the rabbit tumor necrosis factor alpha (TNF-alpha) in advance in sequence, incubating and washing thoroughly. The color is developed with the substrate TMB, which is converted to blue by the catalysis of peroxidase and to the final yellow color by the action of an acid. The shade of the color was positively correlated with rabbit tumor necrosis factor alpha (TNF-alpha) in the sample. Measuring absorbance (OD value) at the wavelength of 450nm by using an enzyme-labeling instrument, and calculating the concentration of the sample;
the test method comprises the following steps: after the Schirmer test of test example 2 was completed, the right eye tissue to which the eye wash had been applied was sacrificed from each group, homogenized, and the protein was extracted to 4mg/L, and then rabbit interleukin 6(IL-6) kit (brand: Aegea Vittaria, Cat: TW10766), rabbit tumor necrosis factor alpha (TNF-alpha) kit (brand: Aegea Virginiana, Cat: TW11454) was used;
the specific results are shown in table 4 below:
TABLE 4
As can be seen from the test data in Table 4, after the eye lotion tears containing schizophyllan provided by the invention are applied, the inhibition rate of the tears containing schizophyllan on IL-6 can reach more than 60%, and the inhibition rate of the tears containing schizophyllan on TNF-alpha can reach more than 50% compared with the blank group; particularly, the most preferred examples 1 to 3 of the present invention have an inhibition rate of not less than 70% against IL-6, and an inhibition rate of not less than 60% against TNF-. alpha.as an inflammatory factor. The components of the eye lotion containing the schizophyllan are mutually matched, so that the eye lotion has a synergistic effect and can further improve the anti-inflammatory capability of the eye lotion.
Test example 4
Antibacterial test
Test samples: eye washes containing schizophyllan as provided in examples 1-12 and eye washes provided in comparative examples 1-5;
testing strains: staphylococcus aureus, candida albicans, pseudomonas aeruginosa, escherichia coli;
the test method comprises the following steps: the eye washes containing the schizophyllan provided in examples 1 to 12 and the eye washes provided in comparative examples 1 to 5 were serially diluted with the thawed agar medium to 2, 4, 8, 16, and 32 times, respectively, and poured into plate media containing drug concentrations at different dilution times of the eye washes. And (3) placing the plate inoculated with the test bacterium liquid into an incubator at 37 ℃ for culturing for 24h, and observing and recording the growth condition of each strain in culture media with different drug concentrations. The eye lotion of the invention adopts a multiple dilution method to determine the Minimum Inhibitory Concentration (MIC) of the eye drops, and the MIC represents the in vitro inhibitory strength;
the specific results are shown in table 5 below, "+" represents no bacterial growth and "-" represents bacterial growth:
TABLE 5
As shown in the test data in Table 5, the eye lotion of the present invention has excellent bacteriostatic ability without adding an antibacterial agent, thereby well avoiding the irritation of the bacteriostatic agent to the eyes, improving the medication comfort, having the advantages of convenient use, accurate dosage, uniform distribution on the surface of the cornea of the eye for a long time, no allergy, no irritation, no blurred vision, and effectively prolonging the action time of the drug and the cornea of the eye.
Test example 5
Clinical trial
Test samples: eye washes containing schizophyllan as provided in examples 1-12 and eye washes provided in comparative examples 1-5;
the testing personnel: volunteers 18-40 years old, and 85 people in total, and divided into 17 groups of 5 people;
the test method comprises the following steps: each group of volunteers wear the same contact lens (the specific degree is selected according to the ordinary use condition of the volunteers), and after wearing the contact lenses for 4 hours, the volunteers all have symptoms of visual fatigue, dry eyes, unsmooth eyes and the like with different degrees; after 4h, washing eyes of 5 persons in each group by using corresponding samples respectively, wherein the dosage is 1 mL;
the therapeutic effect criteria are shown in table 6 below:
TABLE 6
The specific test results are shown in table 7:
TABLE 7
The test results in Table 7 show that the eye lotion containing the schizophyllan provided by the invention can well moisten, relieve fatigue, clean and the like eye balls, is comfortable and smooth, and has excellent effects on eye visual fatigue, eye dryness and other symptoms caused by wearing contact lenses for a long time.
The applicant states that the present invention is illustrated by the above examples to the eye lotion containing schizophyllan and the preparation method thereof, but the present invention is not limited to the above examples, i.e. it does not mean that the present invention must be implemented by means of the above examples. It should be understood by those skilled in the art that any modification of the present invention, equivalent substitutions of the raw materials of the product of the present invention, addition of auxiliary components, selection of specific modes, etc., are within the scope and disclosure of the present invention.
Claims (10)
1. An eye wash containing schizophyllan, wherein the eye wash containing schizophyllan comprises schizophyllan, ectoin, an ophthalmic gel matrix, an osmotic pressure regulator and water.
2. The eyewash containing schizophyllan as claimed in claim 1, wherein the eyewash containing schizophyllan comprises by weight percent:
3. the eyewash containing schizophyllan as claimed in claim 1 or 2, characterized in that the schizophyllan is a small molecule schizophyllan;
preferably, the small molecule schizophyllan has a molecular weight of 10-100kD, preferably 10-30 kD.
4. The eyewash containing schizophyllan as claimed in any one of claims 1 to 3, wherein the mass ratio of schizophyllan to ectoin is 10 (0.5-3).
5. The eyewash containing schizophyllan according to any one of claims 1-4, characterized in that the ophthalmic gel base comprises any one or a combination of at least two of polyvinyl alcohol, medium molecular weight schizophyllan, gellan gum, poloxamer, carbomer, hydroxypropyl methylcellulose, or xanthan gum, preferably any one or a combination of at least two of polyvinyl alcohol, medium molecular weight schizophyllan, or hydroxypropyl methylcellulose;
preferably, the molecular weight of the polyvinyl alcohol is 50-150 kD;
preferably, the molecular weight of the medium molecular weight schizophyllan is 100-;
preferably, the poloxamer includes any one or a combination of at least two of poloxamer 407, poloxamer 188 or carbomer 934P;
preferably, the carbomer comprises carbomer 940 and/or carbomer 974P;
preferably, the ophthalmic gel matrix is a combination of polyvinyl alcohol, medium molecular weight schizophyllan, and hydroxypropyl methylcellulose;
preferably, the mass ratio of the polyvinyl alcohol to the medium molecular weight schizophyllan to the hydroxypropyl methyl cellulose is (3-10): (0.1-5): (0.1-2).
6. The eyewash containing schizophyllan as claimed in any one of claims 1 to 5, characterized in that the tonicity modifier comprises any one or a combination of at least two of sodium chloride, dextrose, borax, boric acid, mannitol or glycerol.
7. The eyewash containing schizophyllan as claimed in any one of claims 1 to 6, characterized in that the eyewash containing schizophyllan further comprises a stabilizer;
preferably, the stabilizer comprises any one of cysteine, cysteine salt, citric acid salt, tartaric acid or tartaric acid salt or a combination of at least two thereof;
preferably, the stabilizing agent accounts for 0.01-0.15% of the total mass of the eye lotion containing schizophyllan;
preferably, the pH of the eye wash containing schizophyllan is 5.5-8.0, preferably 6.0-7.0.
8. A process for preparing an eyewash containing schizophyllan as claimed in any one of claims 1 to 7, characterized in that the process comprises the steps of:
(1) mixing schizophyllan and water to obtain a schizophyllan solution;
(2) mixing the schizophyllan solution obtained in the step (1), ectoin, an ophthalmic gel matrix and an osmotic pressure regulator to obtain the eye lotion containing the schizophyllan.
9. The process for preparing an eyewash containing schizophyllan as claimed in claim 8, wherein in step (1), the temperature of mixing is 50-90 ℃ and the time of mixing is 10-30 min;
preferably, in the step (1) and the step (2), the mixing is performed under stirring, and the rotation speed of the stirring is 100-500 rpm.
10. The process for preparing an eyewash containing schizophyllan as claimed in claim 8 or 9, characterized in that in step (2), the temperature of the mixing is below 50 ℃ and the mixing time is 10-40 min;
preferably, in the step (2), the mixing comprises the following specific steps: firstly, cooling the schizophyllan solution to 40-50 ℃, adding the ophthalmic gel matrix, stirring at 200rpm of 100-.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN115068595A (en) * | 2022-06-24 | 2022-09-20 | 深圳中科欣扬生物科技有限公司 | Anti-radiation composition for eyes and preparation method and application thereof |
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| US20090156563A1 (en) * | 2005-11-30 | 2009-06-18 | Werner Baschong | Glucan Compositions |
| CN109381467A (en) * | 2018-10-24 | 2019-02-26 | 华南理工大学 | A kind of eyes flushing liquor and preparation method thereof for improving mobile phone visual fatigue and alleviating xerophthalmia |
| CN110974722A (en) * | 2019-12-24 | 2020-04-10 | 浙江立恩生物科技有限公司 | Application of biological polysaccharide in washing and protecting products |
| CN111991415A (en) * | 2020-09-11 | 2020-11-27 | 华熙生物科技股份有限公司 | Eye care composition and preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US20090156563A1 (en) * | 2005-11-30 | 2009-06-18 | Werner Baschong | Glucan Compositions |
| CN109381467A (en) * | 2018-10-24 | 2019-02-26 | 华南理工大学 | A kind of eyes flushing liquor and preparation method thereof for improving mobile phone visual fatigue and alleviating xerophthalmia |
| CN110974722A (en) * | 2019-12-24 | 2020-04-10 | 浙江立恩生物科技有限公司 | Application of biological polysaccharide in washing and protecting products |
| CN111991415A (en) * | 2020-09-11 | 2020-11-27 | 华熙生物科技股份有限公司 | Eye care composition and preparation method and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN115068595A (en) * | 2022-06-24 | 2022-09-20 | 深圳中科欣扬生物科技有限公司 | Anti-radiation composition for eyes and preparation method and application thereof |
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