Ophthalmic composition comprising pilocarpine

Abstract

The present invention relates to: an ophthalmic composition containing pilocarpine and having improved stability; and a use thereof.

Description

Ophthalmic composition containing pilocarpine

[0001] [Cross-reference with related applications]

[0002] This application claims the benefit of priority to Korean Patent Application No. 10-2024-0058104, filed April 30, 2024, and Korean Patent Application No. 10-2024-0170600, filed November 26, 2024, the entire contents of which are incorporated herein by reference.

[0003] The present invention relates to an ophthalmic composition comprising pilocarpine and its use.

[0004]

[0005] Pilocarpine is a type of cholinergic agonist that has the activity of reducing intraocular pressure and constricting the pupil, and is used as a treatment drug for glaucoma, ocular hypertension, presbyopia, and hyperopia.

[0006] Meanwhile, eye drops must exhibit physical and chemical properties (e.g., viscosity, pH, osmotic pressure, etc.) suitable for application to ocular tissue. Furthermore, stability is required, particularly during storage, including maintaining the appearance, physical and chemical properties, and active ingredient content. Furthermore, the generation of volatile substances can reduce drug penetration and impact safety, so stability that minimizes the generation of volatile substances is also required.

[0007] In the case of pilocarpine, it is stable at pH 6 or lower, so it is desirable to maintain the pH of eye drops containing pilocarpine at 3 to 6. In addition, since eye drops must have a certain level of viscosity so that they can remain in the eye for a long time and have a stable effect, it is desirable to include a viscosity-enhancing agent that can maintain the viscosity of the eye drops at a certain level.

[0008] Under this technical background, the present invention aims to provide a novel pilocarpine eye drop having improved physical and chemical properties, specifically pH and viscosity stability.

[0009]

[0010] The present invention aims to provide an eye drop composition containing pilocarpine with improved stability.

[0011] To achieve the above object, one aspect of the present invention provides an eye drop composition comprising pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, and xanthan gum.

[0012] The ophthalmic composition of the present invention contains pilocarpine, which has intraocular pressure lowering and vision improving activities, and thus can be used for the prevention or treatment of glaucoma and presbyopia. In addition, it contains levocarnitine and xanthan gum, which improves pH stability and viscosity stability, and thus can be usefully used as an ophthalmic composition that is easy to store for a long period of time.

[0013] In addition, the ophthalmic composition of the present invention stably maintains the content of pilocarpine and produces little volatile substances, so it can be usefully used as an ophthalmic agent.

[0014] However, the effects of the present invention are not limited to the effects mentioned above, and other effects not mentioned will be clearly understood by those skilled in the art from the description below.

[0015]

[0016] Hereinafter, the present invention will be described in detail.

[0017] One aspect of the present invention provides an eye drop composition having excellent storage stability.

[0018] The present invention provides an eye drop composition comprising pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, and xanthan gum.

[0019] The ophthalmic composition of the present invention is prepared by appropriately mixing the above ingredients and has the advantages of excellent pH stability and viscosity stability. Therefore, the ophthalmic composition of the present invention exhibits excellent storage stability even during long-term storage, is physicochemically stable, and maintains a certain level of viscosity, allowing the active ingredient, pilocarpine, to remain in the eye, thereby prolonging its efficacy. Furthermore, the ophthalmic composition of the present invention is harmless to the human body and can thus be usefully used as an ophthalmic composition.

[0020] The above pilocarpine is a type of cholinergic agonist with the chemical structure of the following chemical formula 1, and has the activity of reducing intraocular pressure and improving vision by constricting the pupil, so it can be used as a treatment drug for glaucoma, ocular hypertension, presbyopia, hyperopia, etc.:

[0021] [Chemical Formula 1]

[0022]

[0023] The above-mentioned "pharmaceutically acceptable salt" means a salt of pilocarpine that is pharmaceutically acceptable and has the desired biological or pharmacological activity of the parent compound. The salt includes, for example, an acid addition salt formed with an inorganic acid and a salt formed with an organic acid, and in particular, the salt may include, but is not limited to, pilocarpine hydrochloride. In addition, the salt may include not only a pharmaceutically acceptable salt of pilocarpine, but also all salts, hydrates, and solvates that can be prepared by conventional methods.

[0024] The ophthalmic composition of the present invention can have intraocular pressure-lowering, pupillary miosis-reducing, and vision-improving activities by containing pilocarpine or a pharmaceutically acceptable salt thereof as an active ingredient. Therefore, the ophthalmic composition of the present invention can be used for lowering intraocular pressure and / or improving vision, and can be used for the prevention or treatment of glaucoma and / or presbyopia.

[0025] The above pilocarpine or a pharmaceutically acceptable salt thereof may be contained in an eye drop composition in a therapeutically effective amount for the prevention, improvement or treatment of glaucoma or presbyopia. Specifically, the pilocarpine or a pharmaceutically acceptable salt thereof may be contained in an amount of 0.1 w / v% to 10 w / v% of the total composition. The pilocarpine or a pharmaceutically acceptable salt thereof may be contained in an amount of 0.1 w / v% or more, 0.3 w / v% or more, 0.4 w / v% or more, 0.5 w / v% or more, 0.6 w / v% or more, 0.7 w / v% or more, or 0.8 w / v% or more of the total composition, and may be contained in an amount of 10 w / v% or less, 5 w / v% or less, 3 w / v% or less, 2 w / v% or less, or 1.5 w / v% or less of the total composition. For example, the pilocarpine or a pharmaceutically acceptable salt thereof may be included in the total composition in an amount of 0.1 w / v% to 10 w / v%, 0.1 w / v% to 5 w / v%, 0.1 w / v% to 3 w / v%, 0.1 w / v% to 2 w / v%, 0.4 w / v% to 3 w / v%, 0.4 w / v% to 2 w / v%, 0.5 w / v% to 2 w / v%, or 0.6 w / v% to 2 w / v%, but is not limited thereto.

[0026] Additionally, the ophthalmic composition of the present invention comprises levocarnitine.

[0027] The levocarnitine may be included in an amount of 0.01 w / v% to 5 w / v% of the total composition to improve the pH stability of the eye drop composition. The levocarnitine may be included in an amount of 0.01 w / v% or more, 0.05 w / v% or more, or 0.1 w / v% or more, and may be included in an amount of 5 w / v% or less, 3 w / v% or less, 2 w / v% or less, 1 w / v% or less, or 0.5 w / v% or less, of the total composition. For example, the levocarnitine may be included in a content of 0.01 w / v% to 5 w / v%, 0.01 w / v% to 3 w / v%, 0.01 w / v% to 2 w / v%, 0.1 w / v% to 3 w / v%, 0.1 w / v% to 2 w / v%, or 0.1 w / v% to 1 w / v% of the total composition, but is not limited thereto.

[0028] In addition, the ophthalmic composition of the present invention includes xanthan gum. The xanthan gum is a heteropolysaccharide produced through aerobic fermentation of Xanthomonas campestris, and products such as Xantural® are sold.

[0029] The above xanthan gum can improve the viscosity stability of the ophthalmic composition by maintaining the viscosity of the ophthalmic composition stably for a long period of time.

[0030] The xanthan gum may be included in an amount of 0.01 w / v% to 2 w / v% of the total composition to improve the viscosity stability of the eye drop composition. The xanthan gum may be included in an amount of 0.01 w / v% or more, 0.05 w / v% or more, or 0.1 w / v% or more, and may be included in an amount of 2 w / v% or less, 1 w / v% or less, 0.6 w / v% or less, 0.5 w / v% or less, or 0.4 w / v% or less, of the total composition. For example, the xanthan gum may be included in an amount of 0.01 w / v% to 2 w / v%, 0.1 w / v% to 1 w / v%, or 0.1 w / v% to 0.6 w / v%, 0.1 w / v% to 0.5 w / v%, 0.1 w / v% to 0.4 w / v%, or 0.1 w / v% to 0.3 w / v% of the total composition, but is not limited thereto.

[0031] The pH of the ophthalmic composition of the present invention may be 3 to 6. In particular, the pH of the ophthalmic composition of the present invention may be 3 or more, 3.5 or more, 4 or more, and 6 or less, 5.5 or less, or 5 or less. For example, the pH of the ophthalmic composition of the present invention may be 3 to 6, 3 to 5.5, 3 to 5, 3.5 to 6, 3.5 to 5.5, 3.5 to 5, 4 to 6, 4 to 5.5, or 4 to 5, but is not limited thereto.

[0032] When the pH of the ophthalmic composition of the present invention is 3 to 6, particularly when it is 3 to 5, the efficacy of pilocarpine or a pharmaceutically acceptable salt thereof can be stably produced.

[0033] The pH of the ophthalmic composition of the present invention may be maintained even after storage at 70°C for 3 days or more. In particular, the pH of the ophthalmic composition of the present invention may be maintained even after storage at 70°C for 5 days or more, for example, 7 days or more, or 14 days or more. Furthermore, the pH of the ophthalmic composition of the present invention may be maintained even after storage at room temperature for 7 days or more. In particular, the pH of the ophthalmic composition of the present invention may be maintained even after storage at room temperature for 9 days or more, for example, 12 days or more.

[0034] The pH of the ophthalmic composition of the present invention may be stably maintained even after storage under various temperature conditions such as 25°C or 40°C for 3 days or more, 7 days or more, 10 days or more, 1 month or more, 3 months or more, 6 months or more, 12 months or more, or 24 months or more. The pH of the ophthalmic composition of the present invention may be stably maintained even after storage under high temperature conditions such as 55°C or 70°C for 3 days or more, 7 days or more, 10 days or more, 14 days or more, or 1 month or more.

[0035] The ophthalmic composition of the present invention may have a viscosity measured at 25±0.5°C of 5 cp to 2000 cp. The viscosity may be measured using a measuring method and measuring device (e.g., a single-cylinder rotational viscometer, etc.) known in the art. In particular, the ophthalmic composition of the present invention may have a viscosity measured at 25±0.5°C of 5 cp or more or 10 cp or more, and may be 2000 cp or less, 1500 cp or less, 1000 cp or less, 500 cp or less, 300 cp or less, 100 cp or less, 80 cp or less, or 50 cp or less. For example, the ophthalmic composition of the present invention may have a viscosity measured at 25±0.5°C of 5 cp to 2000 cp, 5 cp to 1500 cp, 5 cp to 1000 cp, 5 cp to 500 cp, 5 cp to 300 cp, 5 cp to 100 cp, 5 cp to 80 cp, 5 cp to 50 cp, 10 cp to 100 cp, 10 cp to 80 cp, or 10 cp to 50 cp, but is not limited thereto.

[0036] The viscosity of the ophthalmic composition of the present invention measured at 25±0.5°C may be maintained even after storage at 70°C for 3 days or more. In particular, the viscosity of the ophthalmic composition of the present invention measured at 25±0.5°C may be maintained even after storage at 70°C for 5 days or more, for example, 7 days or more, or 14 days or more. In addition, the viscosity of the ophthalmic composition of the present invention measured at 25±0.5°C may be maintained even after storage at room temperature for 7 days or more. In particular, the viscosity of the ophthalmic composition of the present invention measured at 25±0.5°C may be maintained even after storage at room temperature for 9 days or more, for example, 12 days or more.

[0037] The viscosity of the ophthalmic composition of the present invention may be stably maintained even after storage under various temperature conditions such as 25°C or 40°C for 3 days or more, 7 days or more, 10 days or more, 1 month or more, 3 months or more, 6 months or more, 12 months or more, or 24 months or more. The viscosity of the ophthalmic composition of the present invention may be stably maintained even after storage under high temperature conditions such as 55°C or 70°C for 3 days or more, 7 days or more, 10 days or more, 14 days or more, or 1 month or more.

[0038] In a specific embodiment of the present invention, an eye drop composition comprising 0.1 w / v% to 10 w / v% of pilocarpine or a pharmaceutically acceptable salt thereof, 0.01 w / v% to 5 w / v% of levocarnitine, and 0.01 w / v% to 2 w / v% of xanthan gum, having a pH of 3 to 6 and a viscosity of 5 cp to 2000 cp was prepared, and it was confirmed that the pH and viscosity of the composition can be stably maintained even after storage for 7 days or more, 10 days or more, or 14 days or more under harsh conditions of 55°C or 70°C. That is, the eye drop composition of the present invention includes levocarnitine and xanthan gum, thereby improving pH stability and viscosity stability, and can be stably stored for a long period of time, and has an appropriate viscosity, so that the active ingredient pilocarpine can stably remain in the eye when instilled, thereby allowing the medicinal effect to last for a long time.

[0039] The present invention may provide an eye drop composition comprising 0.1 w / v% to 2 w / v% of pilocarpine or a pharmaceutically acceptable salt thereof, 0.1 w / v% to 2 w / v% of levocarnitine, and 0.1 w / v% to 0.5 w / v% of xanthan gum, having a pH of 3 to 5.5 and a viscosity of 5 cp to 100 cp.

[0040] Meanwhile, the eye drop composition of the present invention may additionally include one or more additives selected from a pH adjuster, a buffer, an isotonic agent, a viscosity adjuster, a solubilizer, a stabilizer, and a preservative.

[0041] For example, the eye drop composition of the present invention may further include boric acid, glycerin, polysorbate 80, or a mixture thereof.

[0042] The present invention can provide an eye drop composition comprising pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, xanthan gum, and polysorbate 80. The present invention can provide an eye drop composition comprising pilocarpine or a pharmaceutically acceptable salt thereof at 0.1 w / v% to 10 w / v%, levocarnitine at 0.01 w / v% to 5 w / v%, xanthan gum at 0.01 w / v% to 2 w / v%, and polysorbate 80 at 0.1 w / v% to 3 w / v%, and having a pH of 3 to 6 and a viscosity of 5 cp to 2000 cp. The present invention may provide an eye drop composition comprising 0.1 w / v% to 2 w / v% of pilocarpine or a pharmaceutically acceptable salt thereof, 0.1 w / v% to 2 w / v% of levocarnitine, 0.1 w / v% to 0.5 w / v% of xanthan gum, and 0.1 w / v% to 2 w / v% of polysorbate 80, having a pH of 3 to 5.5 and a viscosity of 5 cp to 100 cp. The composition of the present invention has excellent stability, remains stably in the eye, and has excellent drug permeability, so that the efficacy can last for a long time.

[0043] The pH adjuster may include sodium hydroxide, hydrochloric acid, etc., and may be used by adding the necessary amount using a method known to those skilled in the art to obtain an appropriate pH.

[0044] Examples of the buffering agent that can be used include, but are not limited to, acetic acid and / or its salts, citric acid and / or its salts, phosphoric acid and / or its salts, boric acid and / or its salts, etc.

[0045] As the above-mentioned isotropic agent, glycerol, mannitol, sorbitol, sodium chloride, potassium chloride, boric acid, etc. can be used.

[0046] As the viscosity modifier, alginic acid or its salt, carbomer, bentonite, hydroxypropyl methylcellulose, methylcellulose, carboxymethylcellulose, gellan gum, polyvinyl alcohol, polyvinylpyrrolidone, etc. can be used, and the necessary amount can be added and used by a method known to those skilled in the art to obtain an appropriate viscosity.

[0047] As the above-mentioned dissolving aids, benzoalkonium chloride, sodium lauryl sulfate, sorbitan monopalmitate, nonoxynol 10, oxynol 9, tyloxapol, poloxamers, diethylene glycol monoethyl ether, polyethylene glycols, polyoxyl 15 hydrogenated stearic acid, polyoxyl 35 castor oil, polyoxyl 40 hydrogenated castor oil, etc. can be used.

[0048] As the above stabilizer, sodium edetate, aminocaproic acid, etc. can be used.

[0049] Examples of the preservatives that can be used include quaternary ammonium compounds including benzalkonium chloride, polyquaternium-1 (e.g., polyquad), etc.; guanidine compounds including chlorhexidine, etc.; chlorobutanol; mercury preservatives including phenylmercuric acetate, etc.; and oxidizing preservatives including stabilized oxychloro complexes (e.g., purite), paraoxyalkyl acids, etc.

[0050] Additionally, the ophthalmic composition of the present invention may further comprise an active compound. The active compound may be a drug for treating and / or preventing ophthalmic diseases such as glaucoma and / or presbyopia.

[0051] Another aspect of the present invention provides a pharmaceutical composition for preventing or treating presbyopia comprising the pilocarpine or a pharmaceutically acceptable salt thereof, the levocarnitine, and the xanthan gum.

[0052] Another aspect of the present invention provides a method for improving vision comprising administering the above ophthalmic composition to a subject.

[0053] Another aspect of the present invention provides a method for preventing or treating presbyopia comprising administering the above ophthalmic composition to a subject.

[0054] In the present invention, the term "administration" refers to introducing the ophthalmic composition of the present invention to a patient by any suitable method. The route of administration of the present invention is to administer the composition topically to the eye, given its nature as an eye drop. The method for improving vision and the method for preventing or treating presbyopia of the present invention comprise administering the ophthalmic composition of the present invention in a therapeutically effective amount. The composition of the present invention may be administered in a pharmaceutically effective amount.

[0055] Another aspect of the present invention provides a method for preparing an eye drop composition comprising the step of mixing pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, and xanthan gum.

[0056] Another aspect of the present invention provides a method for stabilizing pilocarpine, comprising the step of mixing pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, and xanthan gum.

[0057]

[0058] Hereinafter, the present invention will be described in detail through examples and experimental examples.

[0059] However, the following examples and experimental examples specifically illustrate the present invention, and the content of the present invention is not limited by the following examples and experimental examples.

[0060]

[0061] [Manufacturing Example 1]

[0062] Preparation of pilocarpine ophthalmic compositions 1 to 3

[0063] Compositions 1 to 3 were prepared according to the compositions in Table 1 below. Composition 1 was prepared by dissolving pilocarpine hydrochloride, glycerin, and boric acid in water, and then adjusting the pH to about 4 using a hydrochloric acid solution. Compositions 2 and 3 were prepared by dissolving pilocarpine hydrochloride, glycerin, boric acid, polysorbate 80, and levocarnitine in water to prepare a first solution, dissolving hydroxyethyl cellulose or xanthan gum in water, respectively, to prepare a second solution, and then mixing the first solution and each second solution, and adjusting the pH to about 4 using a hydrochloric acid solution.

[0064] Ingredient name Content (w / v%) Composition 1 Composition 2 Composition 3 Pilocarpine hydrochloride 1.06 1.06 1.06 Glycerin 11.5 1.5 Boric acid 0.10 10.1 Polysorbate 80-0.5 0.5 Levocarnitine-0.25 0.25 Hydroxyethylcellulose-0.3-Xanthan gum--0.3

[0065]

[0066] [Experimental Example 1]

[0067] Evaluation of pH stability and viscosity stability of pilocarpine ophthalmic compositions 1 to 3

[0068] The above compositions 1 to 3 were stored at 70°C for 7 days, and then the pH and viscosity were measured. The viscosity was measured at 25±0.5°C at a rotational speed of 60 rpm using a single-cylinder rotational viscometer and an S18 spindle.

[0069] As a result, in the case of Composition 1 not including levocarnitine, the initial pH was measured as 4.08, but the pH after 7 days dropped significantly to 3.44, indicating that pH stability was not maintained. On the other hand, in the case of Composition 2 not including xanthan gum, the initial viscosity was measured as 35.9 cp, but the viscosity after 7 days dropped significantly to 8.4 cp, indicating that viscosity stability was not maintained.

[0070] In contrast, in the case of Composition 3 containing both levocarnitine and xanthan gum, the pH was found to be stably maintained even under harsh conditions of 70°C, and the viscosity was also measured to be 34.8 cp after 7 days, which did not decrease significantly compared to the initial value of 38.3 cp, indicating that it was stably maintained.

[0071] Through this, it was confirmed that levocarnitine and xanthan gum can maintain the pH and viscosity of pilocarpine eye drops stably for a long period of time.

[0072]

[0073] [Manufacturing Example 2]

[0074] Preparation of pilocarpine ophthalmic compositions 4 to 7

[0075] Compositions 4 to 7 were prepared according to the compositions in Table 2 below. Specifically, a first solution was prepared by dissolving pilocarpine hydrochloride, boric acid, and levocarnitine in water, a second solution was prepared by dissolving xanthan gum in water, and then the first and second solutions were mixed and the pH was adjusted using a hydrochloric acid solution.

[0076] Ingredient name Content (w / v%) Composition 4 Composition 5 Composition 6 Composition 7 Pilocarpine hydrochloride 20.120.1 Boric acid 0.10.10.10.1 Levocarnitine 20.120.1 Xanthan gum 0.50.150.350.15

[0077]

[0078] [Experimental Example 2]

[0079] Evaluation of pH stability and viscosity stability of pilocarpine ophthalmic compositions 4 to 7

[0080] The pH and viscosity of the above compositions 4 to 7 were measured while storing them at 55°C and 70°C for 14 days. The viscosity was measured at 25±0.5°C using a single-cylinder rotational viscometer and an S18 spindle at a rotation speed of 2 rpm (composition 4), 10 rpm (composition 6), or 60 rpm (compositions 5 and 7).

[0081] As a result, it was confirmed that the pH and viscosity of all compositions 4 to 7 were stably maintained even under harsh conditions of 55°C and 70°C (Table 3).

[0082] Through this, it can be seen that the pilocarpine ophthalmic composition of the present invention is a composition with excellent pH stability and viscosity stability.

[0083] Temperature Period Composition 4 Composition 5 Composition 6 Composition 7 Viscosity (cp) - Day 0 1309 14.22 4.4 13.0 70℃ Day 10 1443 10.6 26 4.29 2 Day 141377 10.22 5 5.5 10.255℃ Day 7 1416 11.5 25 4.3 12 0 Day 141374 10.9 24 5.0 11.6 pH - Day 0 5.0 13.4 25 00 3.97 70℃ Day 104.8 13.38 4.75 3.86 Day 144.74 3.36 4.73 3.85 55℃ Day 74.9 4.35 4.89 3.87 Day 144.86 3.35 4.83 3.85

[0084]

[0085] [Manufacturing Example 3]

[0086] Preparation of pilocarpine ophthalmic compositions 8 to 12

[0087] Compositions 8 to 12 were prepared according to the compositions in Table 4 below. Specifically, a first solution was prepared by dissolving pilocarpine hydrochloride, boric acid, and levocarnitine in water, a second solution was prepared by dissolving xanthan gum in water, and then the first and second solutions were mixed and the pH was adjusted using a hydrochloric acid solution.

[0088] Ingredient name Content (w / v%) Composition 8 Composition 9 Composition 10 Composition 11 Composition 12Pilocarpine hydrochloride0.10.120.50.1Boric acid0.10.10.10.10.1Levocarnitine0.050.01210.1Xanthan gum0.150.10.40.150.15

[0089]

[0090] [Experimental Example 3]

[0091] Safety evaluation of pilocarpine ophthalmic compositions 8 to 12

[0092] The pH, viscosity, pilocarpine content, and amount of generated flexible substances of the above compositions 8 to 12 were measured while storing them at 55°C for 14 days. The viscosity was measured at 25±0.5°C using a single-cylinder rotational viscometer and an S18 spindle at a rotation speed of 10 rpm (composition 10) or 60 rpm (compositions 8, 9, 11, 12).

[0093] As a result, it was confirmed that both Compositions 8 to 12 maintained stable pH and viscosity even under harsh conditions of 55°C (Table 5). In addition, it was confirmed that the pilocarpine content was maintained stably, and the amount of flexible substances generated was low, at less than 10% (Table 5).

[0094] Through this, it can be seen that the pilocarpine ophthalmic composition of the present invention has excellent stability.

[0095] Period Composition 8 Composition 9 Composition 10 Composition 11 Composition 12 Viscosity (cp) Day 0 14.18.7 23 8.4 16.4 13.0 Day 7 11.46.7 25 0.7 15.3 12.0 Day 14.10.76.2 24 4.7 15 11.6 pH Day 0 3.48 3.43 5.0 35.46 3.97 Day 73.34 3.31 4.8 6 5.29 3.87 Day 14.36 3.33 4.8 15.19 3.85 Pilocarpine Content (%) Day 0 9.8 3.9 9.7 10.6 3.9 8.1 10.4 9.9 Day 7.95 19.7 10.3 10.1 5.9 2.9 10.2 9.9 Day 14102.6102.699.395.1101.6Flexible material generation amount (%)Day 00.60.70.40.40.7Day 72.82.83.74.92.6Day 143.13.16.38.63.5

[0096] Although representative embodiments of the present invention have been described above as examples, the scope of the present invention is not limited to the specific embodiments described above, and those skilled in the art will be able to make appropriate changes within the scope described in the claims of the present application.

Claims

1. An eye drop composition comprising pilocarpine or a pharmaceutically acceptable salt thereof, levocarnitine, and xanthan gum.

2. An ophthalmic composition according to claim 1, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is pilocarpine hydrochloride.

3. An eye drop composition according to claim 1, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is included in an amount of 0.1 w / v% to 10 w / v% of the total composition.

4. An eye drop composition according to claim 1, wherein the levocarnitine is included in an amount of 0.01 w / v% to 5 w / v% of the total composition.

5. An eye drop composition according to claim 1, wherein the xanthan gum is included in an amount of 0.01 w / v% to 2 w / v% of the total composition.

6. An eye drop composition according to claim 1, wherein the pH of the composition is 3 to 6.

7. An ophthalmic composition according to claim 6, wherein the pH is maintained even after storage at 70°C for 3 days or more.

8. An eye drop composition according to claim 1, wherein the composition has a viscosity measured at 25±0.5°C of 5 cp to 2000 cp.

9. An ophthalmic composition according to claim 8, wherein the viscosity is maintained even after storage at 70°C for 3 days or more.

10. An eye drop composition according to claim 1, wherein the composition further comprises at least one additive selected from a pH adjuster, a buffer, an isotonic agent, a viscosity adjuster, a solubilizer, a stabilizer, and a preservative.

11. An eye drop composition according to claim 1, wherein the composition is for the prevention or treatment of presbyopia.

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