Liquid composition for improving contact lens wearing performance and use thereof

Abstract

This invention belongs to the field of contact lens care technology, and provides a liquid composition for improving the performance of contact lenses and its application. The liquid composition is a compound of perfluorocarbon and semi-fluorinated alkane, preferably perfluorobromooctane and perfluorohexyloctane mixed in a weight ratio of 5:1 to 1:5. This composition is a non-aqueous system, free of water, salt, and preservatives, and has extremely low surface tension. After being instilled into the eye, it can quickly spread and fill the gap between the cornea and the contact lens, forming a long-lasting lubricating film. Simultaneously, the perfluorocarbon component has excellent oxygen-carrying capacity, which can significantly improve the oxygen permeability of the contact lens. The composition of this invention can be applied before, during, and after contact lens wear, is suitable for all types of contact lenses, provides long-lasting lubrication, has minimal eye irritation, and poses no risk of bacterial contamination, effectively solving the technical problems of short lubrication time and significant ocular irritation associated with traditional water-based lubricants.

Description

Technical Field

[0001] This invention belongs to the field of pharmaceutical technology, specifically relating to a liquid composition for improving the wearing performance of contact lenses and its application. Background Technology

[0002] Contact lenses, also known as corneal contact lenses, are optical corrective devices that are directly attached to the cornea of ​​the eye. By directly contacting the cornea, they alter the refraction path of light, thereby correcting irregular corneal curvature and improving vision. They are primarily used to correct refractive errors such as myopia, hyperopia, and astigmatism. Some contact lenses are also used to treat eye diseases, such as keratitis or after intraocular surgery; these are also called bandage lenses, which can reduce the foreign body sensation in the eye and promote the healing of corneal diseases. Contact lenses are mainly divided into rigid gas permeable (RGP) lenses, soft contact lenses (SCL) lenses, and special types of contact lenses. Soft contact lenses are made of water-containing polymer compounds, are soft, comfortable to wear, and require less precise fitting techniques, resulting in the highest market share. However, they have relatively poor oxygen permeability, cannot be worn overnight, and are prone to protein deposits, requiring regular replacement. Rigid contact lenses are made of a hard, hydrophobic material, offering good oxygen permeability, resistance to protein deposits, and easy care. They also provide excellent optical image quality. However, fitting requires a higher level of skill and a certain adaptation period. Rigid lenses are effective in correcting corneal astigmatism, especially irregular astigmatism caused by keratoconus or corneal scarring.

[0003] The number of contact lens wearers worldwide continues to grow, with penetration rates in developed countries such as Europe, the United States, Japan, and South Korea reaching approximately 30%. Niche markets such as colored contact lenses and orthokeratology lenses are expanding rapidly. However, the incidence of adverse reactions related to contact lens use remains high; statistics show that about one-third of wearers experience contact lens-related complications to varying degrees.

[0004] To address the discomfort and dryness experienced during contact lens wear, current solutions primarily involve water-based contact lens lubricants. Typical formulations include moisturizing lubricants (such as sodium hyaluronate and hydroxypropyl methylcellulose), pH adjusters, osmotic pressure regulators, complexing agents, and preservatives, achieving temporary lubrication through water retention. However, water-based lubricants have inherent drawbacks: firstly, water evaporates quickly, resulting in short-lasting lubrication and low utilization efficiency; secondly, salts must be added to maintain physiological osmotic pressure, which can easily irritate damaged ocular surfaces; thirdly, the aqueous environment is prone to microbial growth, necessitating the addition of preservatives, which can exacerbate ocular surface damage with prolonged use; and fourthly, the shelf life after opening is short, posing a risk of bacterial contamination.

[0005] Patent document WO2018 / 206656 discloses a pharmaceutical composition containing a semi-fluorinated alkane for treating contact lens-related ocular dryness. This technology uses a single semi-fluorinated alkane, such as 1-perfluorohexyloctane (F6H8), as the active ingredient, but its application has significant limitations: for silicone hydrogel contact lenses, it can only be applied after lens removal and cannot be instilled into the eye during wear, thus failing to address lubrication and discomfort issues during wear; furthermore, the composition only addresses ocular dryness repair after lens removal and does not address lubrication improvement or oxygen permeability enhancement during contact lens wear.

[0006] Chinese patent CN111035615B discloses a gel-type rigid contact lens lubricant that adds carbomer and glycerol polyether to the traditional water-based formula, which prolongs the tear film breakup time to a certain extent. However, it is still essentially a water-based system and cannot fundamentally avoid problems such as bacterial growth, salt irritation, and short shelf life after opening.

[0007] In summary, existing technologies cannot simultaneously achieve: (1) lubrication that is usable throughout the wearing period of the contact lens; (2) a mild formula that is free of salt and preservatives; (3) the dual benefits of long-lasting lubrication and improved oxygen permeability; and (4) low risk of bacterial contamination and long shelf life after opening. Therefore, there is an urgent need to develop a new type of non-aqueous contact lens lubricant composition to solve the above-mentioned technical bottlenecks. Summary of the Invention

[0008] The purpose of this invention is to address the shortcomings of existing technologies and overcome the defects of existing contact lens lubricants. It solves problems such as short lubrication duration, low utilization efficiency, irritation and damage to the ocular surface from salt / preservatives, and shelf life after opening. At the same time, it further improves the oxygen permeability of contact lenses on the basis of lubrication, improves corneal oxygen supply, and enhances wearing comfort and safety. This invention provides a liquid composition for improving the wearing performance of contact lenses and its application.

[0009] The technical solution adopted in this invention is: a liquid composition for improving the wearing performance of contact lenses, the liquid composition comprising: Perfluorinated carbon as the first component; and semifluorinated alkane as the second component; The liquid composition is a non-aqueous system, containing no water, no salt, and no preservatives.

[0010] Preferably, the perfluorinated carbon is selected from one or more of perfluorotripropylamine, perfluorotributylamine, perfluorobromooctane, perfluoron-butyltetrahydrofuran, perfluorooctane, perfluoronaphthane, perfluoron-butylnaphthane, and perfluorophenanthrene.

[0011] Preferably, the semifluorinated alkane has the molecular formula C0. a H 2a+1 C b F2b+1 , where a is selected from any integer value from 3 to 10, and b is selected from any integer value from 3 to 10.

[0012] Preferably, the semifluorinated alkane is selected from C5H. 11 C4F9, C6H 13 C4F9, C6H 13 C6F 13 C8H 17 C6F 13 C8H 17 C8F 17 C9H 19 C6F 13 Or C 10 H 21 C6F 13 One or more of them.

[0013] Preferably, the perfluorinated carbon is perfluorobromooctane, and the semifluorinated alkane is perfluorobutylpentane or / and perfluorohexyloctane.

[0014] Preferably, the weight ratio of the first component to the second component in the liquid composition is 10:1 to 1:10.

[0015] Preferably, the weight ratio of the first component to the second component in the liquid composition is 5:1 to 1:5.

[0016] Preferably, the liquid composition contains dissolved oxygen, which is introduced into the liquid composition by means of bubbling or pressurizing.

[0017] Application of a liquid composition for improving the wearing performance of contact lenses, said liquid composition being used to prepare a substance that improves the lubrication and oxygen permeability of contact lenses.

[0018] Preferably, the liquid composition is a substance used to prepare artificial tears, eye drops, or non-aqueous contact lens lubricants.

[0019] The beneficial effects obtained by the present invention are as follows: When the liquid composition of the present invention is applied to the surface of a contact lens or the ocular surface, the liquid composition forms a lubricating layer between the contact lens and the cornea. The liquid composition spreads and fills the gap between the cornea and the contact lens quickly through low surface tension, while the oxygen-carrying capacity of perfluorocarbon improves the oxygen permeability of the contact lens.

[0020] 1. Significantly improved lubrication performance: The composition has extremely low surface tension and a spreading area more than 25 times that of commercially available water-based lubricants. It can quickly and completely cover the ocular surface and lens interface, resulting in more uniform and longer-lasting lubrication and significantly reduced foreign body sensation when wearing the lens.

[0021] 2. Synergistic improvement in oxygen permeability: The perfluorocarbon component has a high oxygen-carrying capacity, forming an oxygen-rich liquid layer between the contact lens and the cornea, improving corneal oxygen supply, relieving discomfort from hypoxia during prolonged wear, and reducing the risk of corneal complications.

[0022] 3. Extremely gentle formula: It is free of water, salt, and preservatives, avoiding the eye irritation problems of traditional water-based lubricants. It is suitable for long-term, high-frequency use and is gentle on people with sensitive eyes.

[0023] 4. Unrestricted application scenarios: It can be applied at any time before, during, or after wearing contact lenses, and is suitable for various types of contact lenses such as hydrogel, silicone hydrogel, and RGP lenses, breaking through the limitation of existing semi-fluorinated alkyl products that can only be used on silicone hydrogel lenses after removal.

[0024] 5. Excellent safety and stability: The non-aqueous system has no conditions for microbial growth, the risk of contamination is extremely low, and the shelf life after opening is much longer than that of water-based products; the composition is chemically inert, not easily degraded, and has good storage stability.

[0025] 6. Excellent user experience: The liquid has a suitable viscosity, and there is no greasy feeling or blurred vision after it is dropped in. It spreads quickly and the comfort is immediately apparent. Attached Figure Description

[0026] Figure 1 The bar chart shows the statistical results of the spreading area measured in the spreading performance comparison test of Examples 1-4 and Comparative Examples 1-3. Figure 2 Line graphs showing the comfort scores of Example 1 and Comparative Example 1 at various time points in the human wearing comfort test. Figure 3 The bar chart shows the oxygen conductivity results of Examples 1-4 and Comparative Examples 1-3 measured in the oxygen permeability test. Detailed Implementation

[0027] The technical solutions of the present invention will be clearly and completely described below with reference to the accompanying drawings of the embodiments of the present invention. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments.

[0028] In specific implementation: the liquid composition comprises: perfluorocarbon and semifluorinated alkane; the above scheme does not contain preservatives or chemical stabilizers.

[0029] This liquid composition contains no water. Neither perfluorinated carbon nor semifluorinated alkanes are miscible with water, so the system requires no water.

[0030] The perfluorinated carbon is selected from one or more of perfluorotripropylamine, perfluorotributylamine, perfluorobromooctane, perfluoron-butyltetrahydrofuran, perfluorooctane, perfluoronaphthane, perfluoron-butylnaphthane, and perfluorophenanthrene. Preferably, the perfluorinated carbon is perfluorobromooctane.

[0031] The molecular formula of semifluorinated alkane is C a H 2a+1 C b F 2b+1 Where a is selected from any integer value from 3 to 10, and b is selected from any integer value from 3 to 10. Preferably, the semifluorinated alkane is selected from C5H. 11 C4F9 (perfluorobutylpentane), C6H 13 C4F9 (perfluorobutylhexane), C6H 13 C6F 13 (Perfluorohexylhexane), C8H 17 C6F 13 (Perfluorohexyloctane), C8H 17 C8F 17 (perfluorooctyl octane), C9H 19 C6F 13 (Perfluorohexylnonane), C 10 H 21 C6F 13 One or more of (perfluorohexyldecane). Preferably C8H 17 C6F 13 (Perfluorohexyloctane).

[0032] The weight ratio of the first component to the second component in the liquid composition is from 10:1 to 1:10. Preferably, the weight ratio of the first component to the second component in the liquid composition is from 5:1 to 1:5.

[0033] Application of a liquid composition for improving the wearing performance of contact lenses, the liquid composition being used to prepare a substance that improves the lubrication and oxygen permeability of contact lenses. Oxygen is dissolved in the liquid composition, and the oxygen is introduced by means of bubbling or pressurizing into the liquid composition. Preferably, the liquid composition is a substance used to prepare artificial tears, or eye drops, or a non-aqueous contact lens lubricant.

[0034] Examples 1-4 The preparation methods of the liquid compositions in Examples 1-4 are as follows: (1) Preparation of mixed solvent: In a clean and dry environment, weigh perfluorinated carbon and semifluorinated alkane according to the prescription in Table 1 and add them to a sterile mixing tank. Turn on the electromagnetic stirrer and stir at 300~400 rpm for 5~8 minutes at room temperature (25℃±2℃) until the system is completely homogeneous and there is no layering. (2) Oxygen saturation: Take the liquid composition obtained in Example 4 and introduce medical pure oxygen at a pressure of 0.15 MPa for 30 minutes to fully dissolve the oxygen in the liquid. Other examples do not perform this step and continue with the subsequent preparation steps.

[0035] (3) Filtration and sterilization: The above liquid is filtered through a 0.22μm sterile polyethersulfone filter membrane to remove trace impurities; (4) Aseptic filling: In a Class A clean area, the filtered liquid is aseptically filled into 10mL sterile eye drop bottles and sealed to obtain the finished product.

[0036] Table 1. Content of main components in the liquid compositions of Examples 1-4

[0037] Comparative Examples 1-3 The liquid compositions of Comparative Examples 1 and 2 were obtained commercially: Comparative Example 1: Commercially available Brand A contact lens lubricant, Comparative Example 2: Commercially available Brand B contact lens lubricant, Comparative Example 3: Purified water.

[0038] Three tests were conducted on Examples 1-4 and Comparative Examples 1-3: spreadability comparison test, wearing comfort evaluation, and oxygen permeability test. Test Example I: Comparison Test Results of Spreading Performance Test materials Acrylic plate, 1mm graph paper, micropipettes and tips, counter.

[0039] Test methods Lay a clean acrylic plate flat on graph paper. Use a pipette to measure 50 μL of the liquid to be tested and add it dropwise at a uniform rate to the same position on the acrylic plate. After the drop is added, let it stand for 2 minutes. Count the number of squares on the graph paper occupied by the drop after it spreads, and convert it into the spread area. Repeat each group 6 times and take photos to record the results.

[0040] Test results Table 2. Statistics of the spread area for each test group (unit: cm) 2 ):

[0041] Results Analysis like Figure 1 As shown, the average spreading area of ​​Examples 1-4 was approximately 26-36 times that of the aqueous lubricant group, with a highly statistically significant difference (P<0.001). This indicates that the perfluorinated carbon-semifluorinated alkane binary composition of the present invention has extremely low surface tension and excellent spreading ability on solid surfaces. After being instilled into the eye, it can quickly cover the ocular surface and lens interface, achieving comprehensive lubrication.

[0042] Test Example II: Evaluation of Human Wearing Comfort Twelve healthy soft contact lens wearers (six men and six women, aged 22-35 years) were recruited using a self-controlled design. Subjects routinely wore silicone hydrogel daily disposable lenses. On test days, they were instilled with either the composition of Example 1 of this invention or the aqueous lubricant of Comparative Example 1. Eye comfort, foreign body sensation, dryness, and visual acuity were evaluated within 8 hours of wear.

[0043] Test methods Experiment duration: 2 days; Directions for use: Apply 1 drop before wearing the lenses in the morning, and apply another drop 4 hours after wearing the lenses. Evaluation criteria: The visual analog scale (VAS) was used to evaluate comfort at 2h, 4h, 6h and 8h of wear (0 points for extremely uncomfortable, 10 points for extremely comfortable).

[0044] Test results Table 3. Average comfort scores for each group:

[0045] Results Analysis like Figure 2 As shown, the comfort scores of the composition group of the present invention were significantly higher than those of the water-based lubricant group at all time points. After 8 hours of wear, the average comfort score was 7.6 points, significantly better than the 5.2 points of the water-based lubricant group. Subjects generally reported immediate moisturizing after application, no irritation, significant reduction in foreign body sensation, and no blurred vision or greasy feeling. All subjects tolerated the use during wear without experiencing adverse reactions such as eye redness, swelling, or itching.

[0046] Test Example III Oxygen Permeability Test Test methods The oxygen permeability under the contact lens cover was determined by polarography. Silicone hydrogel lenses of the same model and specification were treated with Examples 1-4 and Comparative Examples 1-3 of this invention, respectively, and then the oxygen conductivity (Dk / t value) was measured on an oxygen permeability tester.

[0047] Test results Table 4. Oxygen conductivity measured for each group:

[0048] Results Analysis Upon comparison, it was found that, such as Figure 3 As shown, the ophthalmic composition provided by the present invention has an oxygen permeability that is about 4 times higher than that of commercially available aqueous contact lens lubricants; after further oxygenation treatment, the oxygen permeability of the composition is increased by about 8 times, indicating that the composition provided by the present invention can effectively supplement the oxygen supply under the contact lens and improve the corneal hypoxia.

[0049] The above description is only a preferred embodiment of the present invention, but the scope of protection of the present invention is not limited thereto. Any equivalent substitutions or modifications made by those skilled in the art within the scope of the technology disclosed in the present invention, based on the technical solution and inventive concept of the present invention, should be covered within the scope of protection of the present invention.

Claims

1. A liquid composition for improving the wearing performance of contact lenses, characterized in that, The liquid composition comprises: Perfluorinated carbon as the first component; and semifluorinated alkane as the second component; The liquid composition is a non-aqueous system, containing no water, no salt, and no preservatives.

2. The liquid composition for improving the wearing performance of contact lenses according to claim 1, characterized in that, The perfluorinated carbon is selected from one or more of perfluorotripropylamine, perfluorotributylamine, perfluorobromooctane, perfluoron-butyltetrahydrofuran, perfluorooctane, perfluoronaphthane, perfluoron-butylnaphthane, and perfluorophenanthrene.

3. The liquid composition for improving the wearing performance of contact lenses according to claim 1, characterized in that, The semifluorinated alkane has the molecular formula C0. a H 2a+1 C b F 2b+1 , where a is selected from any integer value from 3 to 10, and b is selected from any integer value from 3 to 10.

4. The liquid composition for improving the wearing performance of contact lenses according to claim 3, characterized in that, The semifluorinated alkane is selected from C5H. 11 C4F9, C6H 13 C4F9, C6H 13 C6F 13 C8H 17 C6F 13 C8H 17 C8F 17 C9H 19 C6F 13 Or C 10 H 21 C6F 13 One or more of them.

5. The liquid composition for improving the wearing performance of contact lenses according to claim 1, characterized in that, The perfluorinated carbon is perfluorobromooctane, and the semifluorinated alkane is perfluorobutylpentane or / and perfluorohexyloctane.

6. A liquid composition for improving the wearing performance of contact lenses according to any one of claims 1-5, characterized in that, The weight ratio of the first component to the second component in the liquid composition is from 10:1 to 1:

10.

7. A liquid composition for improving contact lens wearing performance according to any one of claims 6, characterized in that, The weight ratio of the first component to the second component in the liquid composition is from 5:1 to 1:

5.

8. The liquid composition for improving the wearing performance of contact lenses according to claim 1, characterized in that, The liquid composition contains dissolved oxygen, which is introduced into the liquid composition by means of bubbling or pressurizing.

9. The application of a liquid composition for improving the wearing performance of contact lenses, characterized in that, The liquid composition is used to prepare a substance that improves the lubrication and oxygen permeability of contact lenses.

10. The application of the liquid composition according to claim 9 for improving the wearing performance of contact lenses, characterized in that, The liquid composition is a substance used to prepare artificial tears, eye drops, or non-aqueous contact lens lubricants.

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