阅读说明：本技术 一种角膜接触镜护理组合物及制备方法和应用 (Corneal contact lens nursing composition, preparation method and application ) 是由 陈炜 吴春生 杜立萍 陈雅婷 焦立学 于 2021-07-19 设计创作，主要内容包括：本发明公开了一种角膜接触镜护理组合物及制备方法和应用,所述角膜接触镜护理组合物包括杀菌护理溶液和还原中和剂,所述杀菌护理溶液的pH为3.0-7.0；所述杀菌护理溶液包括：以质量分数计,0.05wt％-0.8wt％碘络合物、0.1wt％-0.8wt.％碘化钾、0.001wt％-0.005wt％蛋白分解酶、0.01wt％-0.10wt.％非离子表面活性剂和0-0.80wt％渗透压调节剂,98.295wt％-99.839wt％H-(2)O；所述还原中和剂采用固体剂型或液体剂型。本发明的角膜接触镜护理组合物处理时间更短,安全性更好。(The invention discloses a corneal contact lens nursing composition, a preparation method and application thereof, wherein the corneal contact lens nursing composition comprises a sterilization nursing solution and a reduction neutralizer, and the pH value of the sterilization nursing solution is 3.0-7.0; the germicidal care solution comprises: 0.05 wt% -0.8 wt% of iodine complex, 0.1 wt% -0.8 wt% of potassium iodide, 0.001 wt% -0.005 wt% of proteolytic enzyme, 0.01 wt% -0.10 wt% of nonionic surfactant and 0-0.80 wt% of osmotic agent in percentage by massPressure regulator, 98.295 wt% -99.839 wt% H 2 O; the reduction neutralizer adopts a solid dosage form or a liquid dosage form. The corneal contact lens care composition has shorter treatment time and better safety.)

1. A corneal contact lens care composition comprising a germicidal care solution and a reducing neutralizing agent, wherein the germicidal care solution has a pH of 3.0 to 7.0;

the germicidal care solution comprises: calculated by mass fraction, 0.05 wt% -0.8 wt% of iodine complex, 0.1 wt% -0.8 wt% of potassium iodide, 0.001 wt% -0.005 wt% of proteolytic enzyme, 0.01 wt% -0.10 wt% of nonionic surfactant and 0-0.80 wt% of osmotic pressure regulator, 98.295 wt% -99.839 wt% of H₂O；

The reduction neutralizer is in a solid dosage form or a liquid dosage form;

when a solid dosage form is employed, the reducing neutralizer comprises: 0.50-16.00 wt.% iodine reducing depigmenting agent, 0.10-1.00 wt.% pH neutralizing agent and 83.00-99.40 wt.% excipient by mass fraction;

when a liquid dosage form is employed, the reducing neutralizer comprises: 0.50-16.00 wt.% iodine reducing depigmenting agent, 0.10-1.00 wt.% pH neutralizing agent and 83.00-99.40 wt.% water.

2. A corneal contact lens care composition according to claim 1, wherein the iodine complex is povidone-iodine and the effective iodine mass concentration in the iodine complex is 9% to 12%.

3. A corneal contact lens care composition according to claim 1, wherein said proteolytic enzyme is a complex protease.

4. A corneal contact lens care composition according to claim 1, wherein said nonionic surfactant is a polyoxyethylene/polyoxypropylene condensation polymer.

5. A corneal contact lens care composition according to claim 1, wherein said tonicity modifier is one of phosphate, borate, citrate, carbonate, tartrate, sodium chloride and inositol.

6. A corneal contact lens care composition according to claim 1, wherein said iodine reduction depigmenting agent is one of sodium thiosulfate, sodium sulfite, ascorbic acid, L-cysteine, calcium sulfite and glutathione.

7. A corneal contact lens care composition according to claim 1, wherein said pH neutralizing agent is one of sodium carbonate, sodium bicarbonate, calcium carbonate and calcium hydroxy phosphate.

8. A contact lens care composition according to claim 1, wherein the excipient is one or two of polyvinylpyrrolidone, soluble starch, acacia, polyvinyl alcohol, cyclodextrin, polyethylene glycol and modified cellulose.

9. A method of preparing a corneal contact lens care composition according to any one of claims 1 to 8, comprising the steps of preparing a germicidal care solution and reducing a neutralizing agent;

the preparation process of the sterilization care solution comprises the following steps:

step 1.1, adding water, an iodine complex and potassium iodide into an aseptic container, and stirring until the iodine complex and the potassium iodide are completely dissolved;

step 1.2, adding a proteolytic enzyme and an osmotic pressure regulator into the solution obtained in the step 1.1, and stirring until the proteolytic enzyme and the osmotic pressure regulator are completely dissolved;

step 1.3, adding a nonionic surfactant into the solution obtained in the step 1.2, stirring and dissolving, and standing until bubbles disappear to obtain a sterilization care solution;

when the reduction neutralizer adopts a solid dosage form, the preparation process is as follows:

mixing iodine reducing depigmenting agent, pH neutralizer and excipient, stirring, and pressing to obtain solid dosage form;

when the neutralizer is in a liquid dosage form, the preparation process is as follows:

mixing and stirring the iodine reducing depigmenting agent, the pH neutralizing agent and water to form the liquid preparation.

10. Use of a contact lens care composition according to any one of claims 1 to 8, characterized in that the contact lens is filled into a container with the contact lens and the contact lens is filled with a bactericidal care solution for 5 to 20 minutes, and then a reducing neutralizer is added; and adding 1mL of liquid dosage form reduction neutralizer or 1.0g of solid dosage form reduction neutralizer into every 10mL of sterilization care solution, and reacting until the liquid is faded and no bubbles are generated, thereby finishing the disinfection procedure.

Technical Field

The invention relates to the field of iodine care solution, and particularly relates to a corneal contact lens care composition, and a preparation method and application thereof.

Background

Myopia is one of the most common types of ametropic ophthalmic diseases. Contact lenses are more convenient, comfortable, beautiful and realistic compared to frame lenses. Therefore, its market share increases year by year. The corneal contact lenses include a corneal shaping lens, a rigid gas permeable corneal contact lens and a soft corneal contact lens. The corneal contact lens is directly attached to a lacrimal fluid layer of a cornea, a larger visual field is provided, the optical correction performance can be kept in all the watching directions, the prism effect of the glasses is eliminated, oblique astigmatism is eliminated, and the retinal aberration of the eyes is reduced. Because the lens is directly contacted with cornea, conjunctiva, tear film and the like, if the lens is not disinfected properly, acute and chronic conjunctivitis, corneal epithelium exfoliation, giant papillary conjunctivitis, corneal aseptic infiltration, scar, neovascularization and the like are easily caused, and the most serious is infectious keratitis.

Clinically, the corneal contact lens care solution is required to be efficient, safe and convenient. Can quickly kill bacterial microorganisms and remove protein, and has no irritation to eyes. The common corneal contact lens care solution mainly comprises chemical disinfection and H₂O₂Two broad categories of disinfection. In chemical disinfection, polyquaternary ammonium salts, polyhexamethylene biguanide, poly-aminopropyl biguanide, polyhexamethylene biguanide, myristoylpropyldimethylamine and the like are commonly used bactericides and have the advantages of simple and convenient application and good effect of killing bacteria. But it is less effective against fungi and acanthamoebae, and the residual chemicals may cause allergic reactions to some patients. H₂O₂Can generate active free oxygen to kill microbe effectively. But due to residual H₂O₂Is highly irritating to the eye and therefore needs to be neutralized before wearing. Although hydrogen peroxide has a good bactericidal effect, H remains₂O₂Opposite angleMembrane contact lenses have an age-damaging effect and are irritating to the eye. While neutralization was carried out using a platinum ring, H₂O₂The effective action time of the composition is short, and the sterilization effect of the composition is influenced. Therefore, the novel corneal contact lens care solution which has good sterilization effect, no residue and damage to the corneal contact lens is developed, and has important research and market values.

Disclosure of Invention

The invention aims to provide a corneal contact lens care composition, a preparation method and application thereof, aiming at overcoming the defects in the prior art.

In order to achieve the purpose, the invention adopts the following technical scheme:

a corneal contact lens care composition comprising a germicidal care solution and a reducing neutralizing agent, the germicidal care solution having a pH of from 3.0 to 7.0;

the germicidal care solution comprises: calculated by mass fraction, 0.05 wt% -0.8 wt% of iodine complex, 0.1 wt% -0.8 wt% of potassium iodide, 0.001 wt% -0.005 wt% of proteolytic enzyme, 0.01 wt% -0.10 wt% of nonionic surfactant and 0-0.80 wt% of osmotic pressure regulator, 98.295 wt% -99.839 wt% of H₂O；

The reduction neutralizer is in a solid dosage form or a liquid dosage form;

when a solid dosage form is employed, the reducing neutralizer comprises: 0.50-16.00 wt.% iodine reducing depigmenting agent, 0.10-1.00 wt.% pH neutralizing agent and 83.00-99.40 wt.% excipient by mass fraction;

when a liquid dosage form is employed, the reducing neutralizer comprises: 0.50-16.00 wt.% iodine reducing depigmenting agent, 0.10-1.00 wt.% pH neutralizing agent and 83.00-99.40 wt.% water.

Further, the iodine complex is povidone iodine, and the mass concentration of effective iodine in the iodine complex is 9% -12%.

Further, the proteolytic enzyme is a complex protease.

Further, the nonionic surfactant is a polyoxyethylene/polyoxypropylene polycondensate.

Further, the osmotic pressure regulator is one of phosphate, borate, citrate, carbonate, tartrate, sodium chloride and inositol.

Further, the iodine reduction fading reagent is one of sodium thiosulfate, sodium sulfite, ascorbic acid, L-cysteine, calcium sulfite and glutathione.

Further, the pH neutralizer is one of sodium carbonate, sodium bicarbonate, calcium carbonate and calcium hydroxy phosphate.

Further, the excipient is one or two of polyvinylpyrrolidone, soluble starch, gum arabic, polyvinyl alcohol, cyclodextrin, polyethylene glycol and modified cellulose.

A preparation method of a corneal contact lens care composition comprises the steps of preparing a sterilization care solution and reducing a neutralizer;

the preparation process of the sterilization care solution comprises the following steps:

step 1.1, adding water, an iodine complex and potassium iodide into an aseptic container, and stirring until the iodine complex and the potassium iodide are completely dissolved;

step 1.2, adding a proteolytic enzyme and an osmotic pressure regulator into the solution obtained in the step 1.1, and stirring until the proteolytic enzyme and the osmotic pressure regulator are completely dissolved;

step 1.3, adding a nonionic surfactant into the solution obtained in the step 1.2, stirring and dissolving, and standing until bubbles disappear to obtain a sterilization care solution;

when the reduction neutralizer adopts a solid dosage form, the preparation process is as follows:

mixing iodine reducing depigmenting agent, pH neutralizer and excipient, stirring, and pressing to obtain solid dosage form;

when the neutralizer is in a liquid dosage form, the preparation process is as follows:

mixing and stirring the iodine reducing depigmenting agent, the pH neutralizing agent and water to form the liquid preparation.

The application of a corneal contact lens nursing composition comprises pouring a sterilizing nursing solution into a container filled with a corneal contact lens for 5-20 minutes, and adding a reducing neutralizer; and adding 1mL of liquid dosage form reduction neutralizer or 1.0g of solid dosage form reduction neutralizer into every 10mL of sterilization care solution, and reacting until the liquid is faded and no bubbles are generated, thereby finishing the disinfection procedure.

Compared with the prior art, the invention has the following beneficial technical effects:

the iodine disinfection nursing composition has the advantages of shorter treatment time, lower cost and better safety. Compared with multifunctional nursing liquid, the iodine disinfection nursing combination has better microbicidal effect and no bactericide residue. Compared with hydrogen peroxide water-based care solution, the iodine disinfection care composition has the advantages of lower cost, no use of noble metal and no bactericide residue. Secondly, the product can judge the reaction end point by naked eyes (the bactericidal solution is yellowish brown, and the color gradually becomes lighter under the action of the reduction neutralizer until the bactericidal solution is colorless), so that the operation of a user is facilitated. Thirdly, potassium iodide and polymer iodine form dissociation equilibrium, maintain the iodine concentration in a certain range and enhance the sterilization effect. Fourthly, the surface acting force between the nonionic surfactant and the polymer iodine can enhance the dispersibility and stability of the povidone iodine.

Drawings

FIG. 1 is a graph showing the bactericidal effect of examples 1 to 7 on Candida albicans; wherein (a) is a bacterial agar plate culture map after the Candida albicans is treated by a comparative PBS, (b) is a bacterial agar plate culture map after the Candida albicans is treated in example 1, (c) is a bacterial agar plate culture map after the Candida albicans is treated in example 2, (d) is a bacterial agar plate culture map after the Candida albicans is treated in example 3, (e) is a bacterial agar plate culture map after the Candida albicans is treated in example 4, (f) is a bacterial agar plate culture map after the Candida albicans is treated in example 5, (g) is a bacterial agar plate culture map after the Candida albicans is treated in example 6, and (h) is a bacterial agar plate culture map after the Candida albicans is treated in example 7;

FIG. 2 shows the bactericidal effect of examples 1 to 7 on Escherichia coli; wherein (a) is a bacterial agar plate culture picture after the Escherichia coli is treated by a comparative PBS, (b) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 1, (c) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 2, (d) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 3, (e) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 4, (f) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 5, (g) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 6, and (h) is a bacterial agar plate culture picture after the Escherichia coli is treated in example 7;

FIG. 3 is a graph showing the bactericidal effect of examples 1 to 7 on Staphylococcus aureus; wherein (a) is a bacterial agar plate culture pattern after the treatment of Staphylococcus aureus with PBS as a control, (b) is a bacterial agar plate culture pattern after the treatment of Staphylococcus aureus in example 1, (c) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 2, (d) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 3, (e) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 4, (f) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 5, (g) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 6, and (h) is a bacterial agar plate culture pattern after the treatment of Escherichia coli in example 7;

FIG. 4 shows the disinfection effect of example 2 in the presence of organic substances; wherein (a) is a bacterial agar culture picture after the Escherichia coli is treated by the comparative PBS in the presence of organic substances, and (b) is a bacterial agar culture picture after the Escherichia coli is treated by the organic substances in the example 2;

FIG. 5 shows the simulated in-situ sterilization effect of example 2; wherein (a) is a bacterial agar plate culture picture after the low-water content non-ionic contact lens of the example 2 for treating the escherichia coli pollution, (b) is a bacterial agar plate culture picture after the high-water content non-ionic contact lens of the example 2 for treating the escherichia coli pollution, and (c) is a bacterial agar plate culture picture of the adopted escherichia coli.

Detailed Description

Embodiments of the invention are described in further detail below:

the invention relates to a corneal contact lens care composition based on iodine and an iodine complex, which comprises two parts, namely a sterilization care solution and a reduction neutralizer. When in use, the sterilization care solution components are added into a container with the corneal contact lens for acting for a period of time, and then the reduction neutralizer is added for neutralization and color fading treatment, and the sterilization care solution can be worn for use after a plurality of minutes.

The method specifically comprises the following steps:

(1) the effective sterilization component in the sterilization care solution is povidone iodine, and the addition amount of the povidone iodine is 0.05-0.80 wt%.

(2) Potassium iodide (KI) and an iodine complex are added into the sterilization care solution to form an iodine slow release system. The addition amount of KI is 0.10-0.80 wt%.

(3) The pH value of the sterilization care solution ranges from 3.0 to 7.0.

(4) The sterilization care solution is added with compound protease as corneal contact lens proteolytic enzyme, and the addition amount of the compound protease is 0.001 wt% -0.005 wt%.

(5) Nonionic surfactants, including but not limited to polyoxyethylene/polyoxypropylene condensation polymers, includingAndseries, specifically comprisingF127、L42、L43、L61、L81、31R2、17R1、17R4、304、701、901、904、908、1107、1304、1301、1307、90R4、150R1 in an amount of 0.01 wt.% to 0.10 wt.%.

(6) Phosphate, borate, citrate, carbonate, tartrate, inositol, sodium chloride, etc. are added into the sterilizing care solution as osmotic pressure regulator to regulate the final osmotic pressure of the product to be consistent with that of tears (260)-340mosm/kg·H₂O), and the addition amount of the additive is 0 to 0.80 weight percent.

(7) The reducing neutralizer is in solid dosage form or liquid dosage form, and the components of the solid dosage form comprise an iodine reducing depigmenting agent, a pH neutralizing agent and an excipient. Wherein the iodine reduction fading reagent is a substance which can perform oxidation reduction reaction with iodine to reduce the iodine into iodide ions, and oxidation products of the iodine reduction fading reagent are free from cell and human toxicity, and the substance comprises but is not limited to sodium thiosulfate, sodium sulfite, ascorbic acid, L-cysteine, calcium sulfite and glutathione, and the addition amount of the substance is 0.50-16.00 wt%; pH neutralizers refer to substances that raise the pH of the liquid component to near neutral, and are not cytotoxic per se as reaction products, including but not limited to sodium carbonate, sodium bicarbonate, calcium carbonate, calcium hydroxy phosphate, added in an amount of 0.10 wt.% to 1.00 wt.%; excipient (binder) refers to pharmaceutical and food additive excipient capable of binding the product into fixed shape in addition to the above substances, including but not limited to polyvinylpyrrolidone, starch, acacia, polyvinyl alcohol, cyclodextrin, polyethylene glycol, modified cellulose, and its addition amount is 83.00 wt% -99.40 wt%.

When a liquid formulation is adopted, the reducing neutralizer comprises the following components in percentage by mass: 0.50 wt.% to 16.00 wt.% iodine reducing depigmenting agent, 0.10 wt.% to 1.00 wt.% pH neutralizing agent, and 83.00 wt.% to 99.40 wt.% water.

(8) When in use, the sterilization care solution (10mL) is poured into a container filled with the corneal contact lens, after 5-10 minutes of action, the reduction neutralizer (1 mL of liquid component and 1g of solid component) is added for neutralization reaction. Reducing and neutralizing reaction for several minutes to discolor the liquid, and finishing the disinfection procedure.

In order to make the technical solutions of the present invention better understood and implemented by those skilled in the art, the present invention is further described below with reference to the following specific embodiments and the accompanying drawings, but the embodiments are not meant to limit the present invention.

Examples 1 to 7

The germicidal solutions of examples 1-7 are shown in the following table

The reducing neutralizer liquid dosage form components of examples 1-7 are shown in the table below

The components of the solid dosage forms of the reducing neutralizers of examples 1-7 are shown in the following table

Disinfecting effects of examples 1 to 7

The bacteria elimination rate test is carried out according to the disinfection effect experimental method in appendix A of national standard GB19192-2003 sanitation requirements for contact lens care solution. Candida albicans (ATCC 10231) (figure 1), Escherichia coli (ATCC 8739) (figure 2) and Staphylococcus aureus (ATCC 6538) (figure 3) were selected as representative strains, the neutralizer was a liquid dosage form of the selected reducing neutralizer, the procedure was performed according to appendix A, and the effect of the organic matter on the disinfection effect and the field test simulated (figure 4) were performed using example 2. As can be seen from the bacteria elimination rate (figure 1, figure 2 and figure 3), the no influence of organic matters on the sterilization effect (figure 4) and the simulation field test result (figure 5), the nursing liquid meets the national standard.