Pemirolast potassium eye drops and preparation method thereof

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to pemirolast potassium eye drops and a preparation method thereof. The pemirolast potassium eye drops are composed of pemirolast potassium, hydroxypropyl ethyl cellulose, an osmotic pressure regulator, disodium hydrogen phosphate, a pH regulator and water for injection, and the prescription does not contain a bacteriostatic agent, so that the irritation of the eye drops to eye tissue cells is reduced; the pemirolast potassium eye drops provided by the invention are simple in prescription process, stable and controllable in quality and high in safety.

Description

Technical Field

[0001] The present invention belongs to the technical field of pharmaceutical preparations, and particularly relates to potassium pemirolast eye drops and a preparation method thereof. Background Art

[0002] Disclosing the information of this background art section is only intended to increase the understanding of the overall background of the present invention, and it is not necessarily regarded as an admission or an implication in any form that this information constitutes the prior art already known to those of ordinary skill in the art.

[0003] The chemical name of potassium pemirolast: 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2a]pyrimidin-4-one potassium, with the molecular formula C 10 H7KN6O, and the structural formula is as follows:

[0004]

[0005] Potassium pemirolast was first developed and synthesized in the United States by Bristol-Myers Squibb Company in 1977. It belongs to a drug that inhibits the release of allergic reaction mediators caused by antigens. Initially, it was mainly used for the treatment of asthma clinically. In 1991, it was launched in Japan by BMS Company under the trade name Pemirolastion and by Mitsubishi-Tokyo Company under the trade name Alegysal; in 1993, it was developed and launched as a drug for the treatment of allergic conjunctivitis in Japan under the name Alegysal; in 1994, the indication of allergic rhinitis was added; on September 24, 1999, the US FDA approved the listing of Pemirolast potassium eye drops (trade name: Alamast); on May 1, 2000, Japan approved Pemirolast potassium as a drug for the prevention and treatment of atopic dermatitis.

[0006] Potassium pemirolast eye drops have the effect of inhibiting allergic conjunctivitis and are applicable to the treatment of allergic conjunctivitis and vernal catarrhal conjunctivitis. Potassium pemirolast eye drops are a new type of mast cell membrane stabilizer. Only 0.1% is significantly effective, so the adverse reactions are less, and it is an ideal drug for the treatment of allergic conjunctivitis. With the development of modern industry, air pollution is becoming increasingly serious, and the number of external harmful substances is constantly increasing, resulting in an increasing incidence and mortality of various allergic and allergic reaction diseases year by year. As the most populous country in the world, China's environmental pollution is becoming increasingly serious, and the population of such diseases is constantly expanding. Therefore, the demand for this type of drug is also constantly increasing.

[0007] Benzalkonium chloride bacteriostatic agent was added to the original formulation. It was found that continuous use of eye drops for more than one month would cause corneal epithelial keratinization in brown rats, and inflammatory cell infiltration in the corneal limbus, conjunctival stroma, and epithelium. Summary of the Invention

[0008] The present invention provides potassium pemirolast eye drops with a simple prescription process, stable and controllable quality, and high safety, overcoming the defect that the bacteriostatic agent poses a potential hazard to the drug safety of the preparation. The prescription of the potassium pemirolast eye drops of the present invention does not contain a bacteriostatic agent. By optimizing the dosage ratio of hydroxypropyl ethyl cellulose and disodium hydrogen phosphate, the stability of the potassium pemirolast eye drops is higher, and the irritation of the eye drops to eye tissue cells is also reduced.

[0009] Specifically, the technical solution of the present invention is as follows:

[0010] The first object of the present invention is to provide a potassium pemirolast eye drop, and the prescription composition is: potassium pemirolast 0.05% - 0.3%, hydroxypropyl ethyl cellulose 0.8% - 2.5%, osmotic pressure regulator 0.3% - 1.0%, disodium hydrogen phosphate 0.01% - 0.5%, pH regulator, and water for injection.

[0011] Among them, the osmotic pressure regulator is one of sodium chloride, potassium chloride, boric acid, and glycerol.

[0012] Preferably, the osmotic pressure regulator is sodium chloride.

[0013] In the potassium pemirolast eye drops, the osmotic molar concentration is controlled at 0.7 - 0.9 by using the above-mentioned osmotic pressure regulator.

[0014] Among them, the pH regulator is hydrochloric acid.

[0015] In multiple embodiments, the prescription composition of the potassium pemirolast eye drops is: potassium pemirolast 0.05% - 0.3%, hydroxypropyl ethyl cellulose 0.8% - 2.5%, sodium chloride 0.3% - 1.0%, disodium hydrogen phosphate 0.01% - 0.5%, hydrochloric acid, and water for injection; the pH range adjusted by the hydrochloric acid is controlled at 7.0 - 8.6.

[0016] In one of the embodiments, the prescription composition of the potassium pemirolast eye drops is: potassium pemirolast 0.1%, hydroxypropyl ethyl cellulose 2.0%, sodium chloride 0.6%, disodium hydrogen phosphate 0.3%, hydrochloric acid and water for injection, and the pH range adjusted by the hydrochloric acid is controlled at 7.5 - 8.0.

[0017] The second object of the present invention is to provide a preparation method of the above-mentioned potassium pemirolast eye drops, which comprises the following steps:

[0018] (1) Add 85 - 95% of the total volume of water for injection to the liquid preparation tank;

[0019] (2) Add the prescription amounts of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose in sequence, and stir until completely dissolved;

[0020] (3) Add the prescribed amount of potassium pemirolast, stir until completely dissolved, then add an appropriate amount of hydrochloric acid to adjust the pH to 7.5 - 8.0, and stir evenly.

[0021] (4) Add water for injection to make up the volume to the required amount, stir evenly to prepare an intermediate liquid medicine, and conduct quality inspection.

[0022] (5) Filter the qualified intermediate liquid medicine, and use a blow - fill - seal integrated filling equipment to fill the liquid medicine into 0.2 mL low - density polyethylene plastic ampoules, with the filling volume being 0.2 ± 0.05 mL.

[0023] (6) Conduct leak detection, lamp inspection, labeling, and packaging.

[0024] Further, in the step (5): The qualified intermediate liquid medicine is filtered successively through 0.45 μm and 0.22 μm filters.

[0025] Further, in the step (6): Use a polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0026] Compared with the prior art, the technical effects of the present invention are as follows:

[0027] The present invention improves the prescription of potassium pemirolast eye drops. By optimizing the dosage ratio of hydroxypropyl ethyl cellulose and disodium hydrogen phosphate, the stability of potassium pemirolast eye drops is improved. It is shown in the accelerated test and long - term test that the impurity content of the potassium pemirolast eye drops of the present invention is low and the content of the active ingredient is stable. In addition, rabbit experiments prove that the residence time of the potassium pemirolast eye drops of the present invention in the conjunctival sac and on the cornea is extended, the corneal penetration is also improved, and the irritation of the eye drops to eye tissue cells is reduced. BRIEF DESCRIPTION OF THE DRAWINGS

[0028] Figure 1 : A physical picture of the potassium pemirolast eye drops product of the present invention. DETAILED DESCRIPTION OF THE INVENTION

[0029] In order to make the purpose and technical solutions of the present invention clearer, the following further describes the present invention with reference to the embodiments. However, the protection scope of the present invention is not limited to these embodiments, and the embodiments are only used to explain the present invention. Those skilled in the art should understand that any changes or equivalent substitutions that do not deviate from the concept of the present invention are included in the protection scope of the present invention.

[0030] Example 1 Potassium Pemirolast Eye Drops and Preparation Method

[0031] Prescription:

[0032] Material Name Prescription Quantity Pemirolast Potassium 0.1g Sodium Chloride 0.6g Hydroxypropyl Ethylcellulose 2g Disodium Hydrogen Phosphate 0.3g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.5) Water for Injection 100ml

[0033] Preparation method:

[0034] (1) Add 85 - 95% of the total volume of water for injection into the dispensing tank;

[0035] (2) Add the prescribed amounts of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose in sequence, and stir until completely dissolved;

[0036] (3) Add the prescribed amount of potassium pemirolast, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0037] (4) Add water for injection to make up the volume to the required amount, stir evenly, prepare the intermediate liquid medicine, and conduct quality inspection;

[0038] (5) Filter the qualified intermediate liquid medicine through 0.45μm and 0.22μm filters in sequence, use a blow - fill - seal integrated filling equipment to fill the liquid medicine into 0.2mL low - density polyethylene plastic ampoules, and the filling volume is 0.2 ± 0.05mL;

[0039] (6) Conduct leak detection, lamp inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0040] Example 2 Potassium Pemirolast Eye Drops and Preparation Method

[0041] Prescription:

[0042] Material Name Prescription Quantity Pemirolast Potassium 0.05g Sodium Chloride 0.3g Hydroxypropyl Ethylcellulose 0.8g Disodium Hydrogen Phosphate 0.01g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.0) Water for Injection 100ml

[0043] Preparation method:

[0044] (1) Add 85 - 95% of the total volume of water for injection into the dispensing tank;

[0045] (2) Add the prescribed amounts of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose in sequence, and stir until completely dissolved;

[0046] (3) Add the prescribed amount of potassium pemirolast, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0047] (4) Add water for injection to make up the volume to the required amount, stir evenly, prepare the intermediate liquid medicine, and conduct quality inspection;

[0048] (5) Filter the qualified intermediate liquid medicine through 0.45μm and 0.22μm filters in sequence, use a blow - fill - seal integrated filling equipment to fill the liquid medicine into 0.2mL low - density polyethylene plastic ampoules, and the filling volume is 0.2 ± 0.05mL;

[0049] (6) Perform leak detection, light inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealing packaging.

[0050] Example 3 Pemirolast potassium eye drops and preparation method

[0051] prescription:

[0052] Material Name Prescription Quantity Pemirolast Potassium 0.3g Sodium Chloride 1.0g Hydroxypropyl Ethylcellulose 2.5g Disodium Hydrogen Phosphate 0.3g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 8.6) Water for Injection 100ml

[0053] Preparation method:

[0054] (1) Add 85-95% of the total volume of water for injection into the preparation tank;

[0055] (2) Add the prescribed amount of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethylcellulose in sequence and stir until completely dissolved;

[0056] (3) Add the prescribed amount of pemirolast potassium and stir until completely dissolved. Then add an appropriate amount of hydrochloric acid to adjust the pH to 7.5-8.0 and stir evenly.

[0057] (4) Add water for injection to the required volume, stir evenly, prepare the intermediate drug solution, and perform quality inspection;

[0058] (5) The qualified intermediate drug solution was filtered through 0.45 μm and 0.22 μm filters in sequence, and filled into 0.2 mL low-density polyethylene plastic ampoules using a blow-fill-seal integrated filling equipment with a filling volume of 0.2 ± 0.05 mL;

[0059] (6) Perform leak detection, light inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealing packaging.

[0060] Example 4 Pemirolast Potassium Eye Drops and Preparation Method

[0061] prescription:

[0062] Material Name Prescription Quantity Pemirolast Potassium 0.2g Sodium Chloride 0.8g Hydroxypropyl Ethylcellulose 1.5g Disodium Hydrogen Phosphate 0.2g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 8.0) Water for Injection 100ml

[0063] Preparation method:

[0064] (1) Add 85-95% of the total volume of water for injection into the preparation tank;

[0065] (2) Add the prescribed amount of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethylcellulose in sequence and stir until completely dissolved;

[0066] (3) Add the prescribed amount of pemirolast potassium and stir until completely dissolved. Then add an appropriate amount of hydrochloric acid to adjust the pH to 7.5-8.0 and stir evenly.

[0067] (4) Add water for injection to make up to the required volume, stir evenly to prepare the intermediate liquid medicine, and conduct quality inspection;

[0068] (5) Filter the qualified intermediate liquid medicine successively through 0.45μm and 0.22μm filters, and use a blow-fill-seal integrated filling equipment to fill the liquid medicine into 0.2mL low-density polyethylene plastic ampoules, with the filling volume being 0.2 ± 0.05mL;

[0069] (6) Conduct leak detection, lamp inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0070] Control Example 1 Pemirolast Potassium Eye Drops and Preparation Method

[0071] Prescription:

[0072] Material Name Prescription Quantity Pemirolast Potassium 0.1g Sodium Chloride 0.6g Disodium Hydrogen Phosphate 0.3g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.5) Water for Injection 100ml

[0073] Preparation Method:

[0074] (1) Add water for injection accounting for 85 - 95% of the total volume to the dispensing tank;

[0075] (2) Add the prescribed amounts of disodium hydrogen phosphate and sodium chloride successively, and stir until completely dissolved;

[0076] (3) Add the prescribed amount of pemirolast potassium, stir until completely dissolved, then add an appropriate amount of hydrochloric acid to adjust the pH to 7.5 - 8.0, and stir evenly;

[0077] (4) Add water for injection to make up to the required volume, stir evenly to prepare the intermediate liquid medicine, and conduct quality inspection;

[0078] (5) Filter the qualified intermediate liquid medicine successively through 0.45μm and 0.22μm filters, and use a blow-fill-seal integrated filling equipment to fill the liquid medicine into 0.2mL low-density polyethylene plastic ampoules, with the filling volume being 0.2 ± 0.05mL;

[0079] (6) Conduct leak detection, lamp inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0080] Control Example 2 Pemirolast Potassium Eye Drops and Preparation Method

[0081] Prescription:

[0082] Material Name Prescription Quantity Pemirolast Potassium 0.1g Sodium Chloride 0.6g Hydroxypropyl Ethylcellulose 2g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.5) Water for Injection 100ml

[0083] Preparation Method:

[0084] (1) Add water for injection accounting for 85 - 95% of the total volume to the dispensing tank;

[0085] (2) Add sodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose in the prescribed amounts in sequence, and stir until completely dissolved;

[0086] (3) Add potassium pemirolast in the prescribed amount, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0087] (4) Add water for injection to make up the volume to the required volume, stir evenly, prepare an intermediate liquid medicine, and conduct quality inspection;

[0088] (5) Filter the qualified intermediate liquid medicine through 0.45μm and 0.22μm filters in sequence, use a blow - fill - seal integrated filling device to fill the liquid medicine into 0.2mL low - density polyethylene plastic ampoules, and the filling volume is 0.2 ± 0.05mL;

[0089] (6) Conduct leak detection, lamp inspection, label pasting, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0090] Comparative Example 3 Potassium Pemirolast Eye Drops and Preparation Method

[0091] Prescription:

[0092] Material Name Prescription Quantity Pemirolast Potassium 0.1g Sodium Chloride 0.6g Hydroxypropyl Ethylcellulose 3.5g Disodium Hydrogen Phosphate 0.1g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.5) Water for Injection 100ml

[0093] Preparation Method:

[0094] (1) Add 85 - 95% of the total volume of water for injection to the liquid - preparation tank;

[0095] (2) Add sodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose in the prescribed amounts in sequence, and stir until completely dissolved;

[0096] (3) Add potassium pemirolast in the prescribed amount, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0097] (4) Add water for injection to make up the volume to the required volume, stir evenly, prepare an intermediate liquid medicine, and conduct quality inspection;

[0098] (5) Filter the qualified intermediate liquid medicine through 0.45μm and 0.22μm filters in sequence, use a blow - fill - seal integrated filling device to fill the liquid medicine into 0.2mL low - density polyethylene plastic ampoules, and the filling volume is 0.2 ± 0.05mL;

[0099] (6) Conduct leak detection, lamp inspection, label pasting, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0100] Comparative Example 4 Potassium Pemirolast Eye Drops and Preparation Method

[0101] Prescription:

[0102] Material Name Prescription Quantity Pemirolast Potassium 0.1g Sodium Chloride 0.6g Methylcellulose 2g Disodium Hydrogen Phosphate 0.3g 0.1mol / L Hydrochloric Acid Solution Appropriate Quantity (pH adjusted to 7.5) Water for Injection 100ml

[0103] Preparation method:

[0104] (1) Add 85 - 95% of the total volume of water for injection into the dispensing tank;

[0105] (2) Add sodium hydrogen phosphate, sodium chloride, and methyl cellulose in the prescribed amounts in sequence, and stir until completely dissolved;

[0106] (3) Add potassium pemirolast in the prescribed amount, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0107] (4) Add water for injection to make up the volume to the required amount, stir evenly, prepare the intermediate liquid medicine, and conduct quality inspection;

[0108] (5) Filter the qualified intermediate liquid medicine through 0.45μm and 0.22μm filters in sequence, and use a blow - fill - seal integrated filling equipment to fill the liquid medicine into 0.2mL low - density polyethylene plastic ampoules, with the filling volume being 0.2 ± 0.05mL;

[0109] (6) Conduct leak detection, lamp inspection, label pasting, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0110] Potassium Pemirolast Eye Drops of Comparative Example 5 and Preparation Method

[0111] Prescription:

[0112]

[0113]

[0114] Preparation method:

[0115] (1) Add 85 - 95% of the total volume of water for injection into the dispensing tank;

[0116] (2) Add sodium citrate, sodium chloride, and hydroxypropyl ethyl cellulose in the prescribed amounts in sequence, and stir until completely dissolved;

[0117] (3) Add potassium pemirolast in the prescribed amount, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly;

[0118] (4) Add water for injection to make up the volume to the required amount, stir evenly, prepare the intermediate liquid medicine, and conduct quality inspection;

[0119] (5) Filter the qualified intermediate liquid medicine successively through 0.45μm and 0.22μm filters, and use a blow-fill-seal integrated filling and sealing device to fill the liquid medicine into 0.2mL low-density polyethylene plastic ampoules, with the filling volume being 0.2±0.05mL;

[0120] (6) Conduct leak detection, lamp inspection, labeling, and use polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

[0121] Stability test of potassium pemirolast eye drops

[0122] Take the potassium pemirolast eye drops of Examples 1-4 of the present invention, the potassium pemirolast eye drops of Comparative Examples 1-5, and the commercially available potassium pemirolast eye drops (H20130579) for accelerated stability investigation under the conditions of 40±2°C / 20±5%RH. Samples are taken at 0 day, 3 months, and 6 months respectively. The sample properties, pH, related substances, osmolarity, content, and sterility results are shown in Table 1.

[0123]

[0124]

[0125]

[0126]

[0127] Analysis of the stability data results shows that the potassium pemirolast eye drops of Examples 1-4 of the present invention do not add bacteriostatic agents, the impurity level basically does not increase during the test, the content is stable, and the stability effect of the preparation is better than that of the commercially available preparation. For the potassium pemirolast eye drops of Comparative Examples 1-5, the impurity level increases significantly and the content decreases significantly during the test.

[0128] Animal experiment

[0129] Corneal retention time

[0130] Fluorescein sodium was selected as the coloring material, and the in vivo corneal retention time of the eye drops of Example 1, Comparative Examples 1-5, and commercially available potassium pemirolast eye drops (H20130579) was studied respectively. The experiment was divided into seven groups, with 6 rabbits in each group. 100μL of the eye drops containing 0.10% fluorescein sodium solution of Example 1, Comparative Example 1, Comparative Example 2, Comparative Example 3, Comparative Example 4, Comparative Example 5, and the commercially available preparation were respectively instilled into the right conjunctival sac of the rabbits in each group. The left eyes of all rabbits were instilled with the same volume of citrate buffer solution with pH 6.30 as a control. After administration, the eyes of the rabbits were closed passively for 30 seconds. The fluorescence fading time of fluorescein sodium in the cornea and conjunctival sac was observed and recorded with a slit lamp, and the test results are shown in Table 3.

[0131] Table 3 Results of corneal residence time test

[0132]

[0133] Result analysis: Compared with Comparative Example 1-5 and commercially available pemirolast potassium eye drops, the residence time in the conjunctival sac and the retention time on the cornea of Example 1 were significantly increased.

[0134] In vitro corneal permeability test

[0135] The rabbits were sacrificed, and the intact corneas were separated. The corneas were fixed on the diffusion cell with the inner side (aqueous humor side) facing the receiving cell and the outer side facing the supply cell. 2 g of the eye drops of Example 1, Comparative Example 1-5, and commercially available pemirolast potassium eye drops were placed in the supply cell, and the corneal permeability test was carried out at 37°C. The receiving solution was completely taken out from the receiving cell at different times, and the same volume of receiving solution was replenished. The concentration of pemirolast potassium in the receiving solution was determined by HPLC, and the test results are shown in Table 4.

[0136] Table 4 Results of in vitro corneal permeability test

[0137] Group <![CDATA[Papp×10 6 (cm / s)±SD]]> Example 1 4.20±0.55 Comparative Example 1 3.05±0.29 Comparative Example 2 3.16±0.96 Comparative Example 3 3.58±0.27 Comparative Example 4 3.47±0.55 Comparative Example 5 3.61±0.65 Commercially Available Pemirolast Potassium Eye Drops 3.96±0.99

[0138] Result analysis: Compared with Comparative Example 1-5 and commercially available pemirolast potassium eye drops, the permeability of the pemirolast potassium eye drops of Example 1 increased, promoting the penetration of the drug in the cornea.

[0139] It should be noted that the present invention also conducted animal experiments on the pemirolast potassium eye drops of Examples 2-4, and tested the corneal residence time and in vitro corneal permeability of the pemirolast potassium eye drops of Examples 2-4 in rabbits. The experimental results were similar to or analogous to those of the pemirolast potassium eye drops of Example 1, with the residence time in the conjunctival sac higher than 68 min, the retention time on the cornea higher than 65 min, and the corneal permeability higher than 4.0×10 6 cm / s.

Claims

1. A potassium pemirolast ophthalmic solution, characterized in that, The prescription composition is as follows: potassium pemirolast 0.05% - 0.3%, hydroxypropyl ethyl cellulose 0.8% - 2.5%, osmotic pressure regulator 0.3% - 1.0%, disodium hydrogen phosphate 0.01% - 0.5%, pH regulator, and water for injection.

2. The potassium pemirolast eye drops according to claim 1, characterized in that, The osmotic pressure regulator is one of sodium chloride, potassium chloride, boric acid, and glycerol.

3. The potassium pemirolast eye drops according to claim 2, characterized in that, The osmotic pressure regulator is sodium chloride.

4. The potassium pemirolast eye drops according to claim 1, characterized in that, The dosage of the osmotic pressure regulator controls the osmotic molality within 0.7 - 0.

9.

5. The potassium pemirolast eye drops according to claim 1, wherein The pH regulator is hydrochloric acid.

6. The potassium pemirolast eye drops according to any one of claims 1 to 5, characterized in that, The prescription composition is as follows: potassium pemirolast 0.05% - 0.3%, hydroxypropyl ethyl cellulose 0.8% - 2.5%, sodium chloride 0.3% - 1.0%, disodium hydrogen phosphate 0.01% - 0.5%, hydrochloric acid, and water for injection; the pH range adjusted by the hydrochloric acid is controlled within 7.0 - 8.

6.

7. The potassium pemirolast eye drops according to claim 6, characterized in that, The prescription composition is as follows: potassium pemirolast 0.1%, hydroxypropyl ethyl cellulose 2.0%, sodium chloride 0.6%, disodium hydrogen phosphate 0.3%, hydrochloric acid, and water for injection, and the pH range adjusted by the hydrochloric acid is controlled within 7.5 - 8.

0.

8. A method for preparing potassium pemirolast eye drops as described in claim 6, characterized in that, The preparation method described above comprises the following steps: (1) Add 85 - 95% of the total volume of water for injection to the liquid preparation tank. (2) Sequentially add the prescribed amounts of disodium hydrogen phosphate, sodium chloride, and hydroxypropyl ethyl cellulose, and stir until completely dissolved. (3) Add the prescribed amount of potassium pemirolast, stir until completely dissolved, then add an appropriate amount of hydrochloric acid, adjust the pH to 7.5 - 8.0, and stir evenly. (4) Add water for injection to make up the volume to the required volume, stir evenly to prepare an intermediate liquid medicine, and conduct quality inspection. (5) Filter the qualified intermediate liquid medicine, and use a blow - fill - seal integrated filling device to fill the liquid medicine into 0.2 mL low - density polyethylene plastic ampoules, and the filling volume is 0.2 ± 0.05 mL. (6) Conduct leak detection, lamp inspection, labeling, and packaging.

9. The method according to claim 8, characterized in that In step (5) described above: Filter the qualified intermediate liquid medicine successively through 0.45 μm and 0.22 μm filters.

10. The method according to claim 8, wherein In step (6) described above: Use a polyester / aluminum / polyethylene pharmaceutical composite film for secondary sealed packaging.

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