Olopatadine hydrochloride tablets and preparation method thereof

Abstract

The invention provides a solid composition of olopatadine hydrochloride tablets, and relates to the field of medical technology. The solid composition of olopatadine hydrochloride tablets disclosed in the invention comprises an active component of olopatadine hydrochloride, a filler, a disintegrant, a lubricant and a polyvinyl alcohol 5-88 aqueous solution. By using 0.1%-10% polyvinyl alcohol 5-88 aqueous solution as a binder for wet granulation and tableting, and controlling the tablet hardness at 60-100N, the obtained tablet has good splitting performance, good dissolution performance and stability, a simple production process, and is suitable for industrial production and clinical use.

Description

Technical Field

[0001] The present invention relates to the field of medical technology, and in particular to an olopatadine hydrochloride tablet and a preparation method thereof. Background Art

[0002] Olopatadine hydrochloride is a second-generation antihistamine drug that has a high efficiency in antagonizing the activity of histamine H1 receptors, inhibiting the generation and release of chemical transmitters (leukotrienes, thromboxanes, PAF, etc.), and has an inhibitory effect on the release of the neurotransmitter tachykinin. It is not easy to penetrate the blood-brain barrier and has no significant central nervous system inhibitory effect. Olopatadine hydrochloride tablets are clinically used to treat allergic rhinitis, urticaria, and itchy skin diseases (eczema, dermatitis, prurigo, pruritus, psoriasis vulgaris, exudative erythema multiforme). Clinically, olopatadine hydrochloride tablets need to be quickly dissolved to ensure efficacy.

[0003] Oral solid tablets are the most commonly used dosage form in clinical practice. In order to facilitate the adjustment of dosage, reduce treatment costs, and solve the medication problems of some special groups such as the elderly and children, tablets are often artificially split (called tablet splitting in the pharmacy department) before use. Tablets with functional notches (refers to tablets with one or more notches for easy dosage splitting.

[0004] The original formulation of olopatadine hydrochloride tablets (trade name: Alok) marketed in China by Kyowa Hakko Kirin Co., Ltd. is available in only one notched 5 mg dosage form. Therefore, whether it is easy to divide is of great significance in clinical drug administration and personalized treatment for special populations.

[0005] At present, the domestically disclosed patents CN101695480A involve olopatadine hydrochloride dispersible tablets and their preparation method and quality control method, CN101632646A discloses an olopatadine hydrochloride tablet and its preparation method and detection method, and CN110882223A discloses a direct compression olopatadine hydrochloride tablet formulation. All of them only focus on the dissolution of the preparation and the related substances, but do not pay attention to the accuracy of the divided dosage as split tablets.

[0006] Scored tablets are continuous indentations across the surface of a tablet, used to divide the tablet into smaller sub-units. The problems with existing forms of scored tablets are well known. These problems include loss of active drug, imprecise tablet division, greater friability or poor stability of the divided fragments, etc., so tablet division is usually less than ideal. Moreover, for different drugs, the properties of the materials are different, resulting in different levels of difficulty in breaking. Split tablets can enhance clinical dosing compliance in patients with dysphagia, or meet the treatment of patients who require non-full tablet doses. However, achieving dosage accuracy of split tablets and dosage flexibility in clinical use are technical challenges faced by all splittable oral solid tablets: FDA guidelines require testing after breaking by hand and instrument respectively, with the mass loss after breaking less than 3.0%, the friability of the divided fragments not greater than 1.0%, and the CU of the divided fragments in compliance with USP <905> Requirements are that the dissolution of the split segments is similar to that of the intact tablets (tablets with upper and lower hardness limits are tested separately), and the split segments need to remain stable in medical storage boxes / bottles for at least 3 months, etc.

[0007] During the research process, the inventors found that when a 0.1%-10% (mass concentration) aqueous solution of polyvinyl alcohol 5-88 is used as a binder for wet granulation and tableting, and the tablet hardness is controlled at 60-100N, the resulting split tablets have higher dosage accuracy, better dissolution performance and stability, and are more convenient and safe for patients to use.

[0008] Polyvinyl alcohol is a water-soluble synthetic polymer with hydrophilic and hydrophobic groups in the molecule. The viscosity is controlled by the degree of polymerization and hydrolysis. It has good bonding and adhesion. Polyvinyl alcohol with different viscosities can be used as tablet film coating components, wet granulation adhesives, liquid preparation dispersants, etc. in the pharmaceutical field. Polyvinyl alcohol is classified according to viscosity and degree of hydrolysis. The two-digit nomenclature of different grades consists of the viscosity at 20°C (the first digit) and 4% solution and the degree of hydrolysis of the polymer (the second digit). Polyvinyl alcohol 5-88 indicates a grade of 5mPa·s viscosity and 88% hydrolysis. Its viscosity is suitable as a wet granulation adhesive. The aqueous solution has high stability. When used as an adhesive for tablets, it can affect the hardness and wear resistance of the tablets.

[0009] Hardness is the compressive strength of tablets, i.e. its radial crushing force. Hardness has an important impact on drug production and quality. The inventors found in their research that controlling the hardness of Olopatadine Hydrochloride Tablets to 60-100N can effectively improve the tablet splitting performance, and the manual splitting process is smooth, making it easier for patients to break tablets and use the drugs.

[0010] The invention uses 0.1%-10% (mass concentration) polyvinyl alcohol 5-88 aqueous solution as a binder for wet granulation and tableting, and controls the tablet hardness to be 60-100N. The obtained tablets have good splitting performance, good dissolution performance and stability, simple production process, and are suitable for industrial production and clinical use. Summary of the invention

[0011] In view of the above problems, the present invention provides a solid composition of olopatadine hydrochloride tablets and a preparation method thereof. The obtained tablets have good splitting performance, good dissolution performance and stability, a simple production process, and are suitable for industrial production and clinical use.

[0012] To achieve the above purpose, the technical solution adopted by the present invention is as follows:

[0013] In one aspect, the present invention provides a solid composition of olopatadine hydrochloride tablets, comprising an active ingredient, olopatadine hydrochloride, a filler, a disintegrant, a lubricant and a polyvinyl alcohol 5-88 aqueous solution.

[0014] Preferably, the weight proportions of the combination may be: 2-8 parts of olopatadine hydrochloride, 95-115 parts of filler, 5-12 parts of disintegrant, 1-4 parts of lubricant and 20-60 parts of polyvinyl alcohol 5-88 aqueous solution.

[0015] Further preferably, the weight proportions of the combination may be: 4-6 parts of olopatadine hydrochloride, 100-110 parts of filler, 6-10 parts of disintegrant, 1-3 parts of lubricant and 30-50 parts of polyvinyl alcohol 5-88 aqueous solution.

[0016] More preferably, the weight proportions of the combination may be: 5 parts of olopatadine hydrochloride, 105 parts of filler, 8 parts of disintegrant, 2 parts of lubricant and 40 parts of polyvinyl alcohol 5-88 aqueous solution.

[0017] Preferably, the filler comprises at least one of microcrystalline cellulose, lactose, starch and mannitol; further preferably, in some embodiments, the filler may be a mixture of microcrystalline cellulose and lactose or starch.

[0018] Preferably, the disintegrant comprises at least one of low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl cellulose, sodium carboxymethyl starch, and cross-linked polyvinylpyrrolidone; further preferably, the disintegrant may be at least one of sodium carboxymethyl starch and cross-linked polyvinylpyrrolidone.

[0019] Preferably, the lubricant comprises at least one of stearic acid, magnesium stearate, silicon dioxide and colloidal silicon dioxide; more preferably, the lubricant may be magnesium stearate.

[0020] Preferably, the mass concentration of the polyvinyl alcohol 5-88 aqueous solution may be 0.1%-10%; further preferably, the mass concentration of the polyvinyl alcohol 5-88 aqueous solution includes but is not limited to 1%, 5%, and 10%.

[0021] Preferably, the content of olopatadine hydrochloride is 5 mg.

[0022] On the other hand, the present invention also provides a method for preparing a solid composition of olopatadine hydrochloride tablets, comprising the following steps:

[0023] 1) Evenly mix olopatadine hydrochloride, filler, disintegrant and lubricant according to the formula amount;

[0024] 2) adding polyvinyl alcohol 5-88 aqueous solution for wet granulation, drying, sieving, and obtaining wet granules;

[0025] 3) Add lubricant and mix well, and use a notched die to press the granules into tablets with a tablet hardness of 60-100N.

[0026] Preferably, the specific operation of drying is: drying the wet granules in an oven at 50-70° C. for 120-180 minutes.

[0027] Compared with the prior art, the present invention has the following beneficial effects:

[0028] By adding 0.1%-10% (mass concentration) of polyvinyl alcohol 5-88 aqueous solution as a binder for wet granulation and tableting, and controlling the tablet hardness at 60-100N, the olopatadine hydrochloride split tablets prepared by the present invention have higher dosage accuracy, better dissolution performance and stability, and are more convenient and safe for patients to use. DETAILED DESCRIPTION

[0029] In order to make the technical means, creative features, purpose and effect of the present invention easy to understand, the present invention is further explained below in conjunction with specific embodiments, but the following embodiments are only preferred embodiments of the present invention, not all. Based on the embodiments in the implementation mode, other embodiments obtained by those skilled in the art without making creative work all belong to the protection scope of the present invention. It is worth noting that the raw materials used in the present invention are all common commercial products, and their sources are not specifically limited. The technology and scientific terms used in the embodiments have the meanings commonly understood by those of ordinary skill in the art to which the present invention belongs.

[0030] Example 1

[0031] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 1.

[0032] Table 1

[0033]

[0034]

[0035] Preparation process:

[0036] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose are mixed evenly, and a 5% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 60-80N.

[0037] Example 2

[0038] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 2.

[0039] Table 2

[0040] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 starch 75 Sodium carboxymethyl starch 8 Magnesium Stearate 2 5% polyvinyl alcohol 5-88 aqueous solution 40

[0041] Preparation process:

[0042] Olopatadine hydrochloride, microcrystalline cellulose, starch and sodium carboxymethyl starch are mixed evenly, and a 5% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 80-100N.

[0043] Example 3

[0044] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 3.

[0045] Table 3

[0046] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 starch 75 Sodium carboxymethyl starch 8 Magnesium Stearate 2 1% polyvinyl alcohol 5-88 aqueous solution 40

[0047] Preparation process:

[0048] Olopatadine hydrochloride, microcrystalline cellulose, starch and sodium carboxymethyl starch were mixed evenly, and 1% polyvinyl alcohol 5-88 aqueous solution was added for wet granulation. The wet granules were dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate was added and mixed evenly. The granules were pressed into tablets using a notched die, and the tablet hardness was 60-80N.

[0049] Example 4

[0050] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 4.

[0051] Table 4

[0052] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 starch 75 Crospovidone 8 Magnesium Stearate 2 10% polyvinyl alcohol 5-88 aqueous solution 40

[0053] Preparation process:

[0054] Olopatadine hydrochloride, microcrystalline cellulose, starch and cross-linked polyvinylpolypyrrolidone were mixed evenly, and 10% polyvinyl alcohol 5-88 aqueous solution was added for wet granulation. The wet granules were dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate was added and mixed evenly. The granules were pressed into tablets using a notched die, and the tablet hardness was 80-100N.

[0055] Comparative Example 1

[0056] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 5.

[0057] Table 5

[0058] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 lactose 75 Croscarmellose Sodium 8 Magnesium Stearate 2 5% Polyvinyl alcohol 4-88 40

[0059] Preparation process:

[0060] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose were mixed evenly, and 5% polyvinyl alcohol 4-88 aqueous solution was added for wet granulation. The wet granules were dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate was added and mixed evenly. The granules were pressed into tablets using a notched die, and the tablet hardness was 60-80N.

[0061] Comparative Example 2

[0062] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 6.

[0063] Table 6

[0064] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 lactose 75 Croscarmellose Sodium 8 Magnesium Stearate 2 Purified water 40

[0065] Preparation process:

[0066] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose were mixed evenly, purified water was added for wet granulation, the wet granules were dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, magnesium stearate was added and mixed evenly, and the granules were pressed into tablets using a notched die, and the tablet hardness was 60-80N.

[0067] Comparative Example 3

[0068] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 7.

[0069] Table 7

[0070] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 starch 75 Sodium carboxymethyl starch 8 Magnesium Stearate 2 5% polyvinyl alcohol 5-88 aqueous solution 40

[0071] Preparation process:

[0072] Olopatadine hydrochloride, microcrystalline cellulose, starch and sodium carboxymethyl starch are mixed evenly, and a 5% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 30-50N.

[0073] Comparative Example 4

[0074] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 8.

[0075] Table 8

[0076]

[0077]

[0078] Preparation process:

[0079] Olopatadine hydrochloride, microcrystalline cellulose, starch and sodium carboxymethyl starch are mixed evenly, and a 5% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 110-130N.

[0080] Comparative Example 5

[0081] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 9.

[0082] Table 9

[0083] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 lactose 75 Croscarmellose Sodium 8 Magnesium Stearate 2 0.01% polyvinyl alcohol 5-88 aqueous solution 40

[0084] Preparation process:

[0085] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose are mixed evenly, and 0.01% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 60-80N.

[0086] Comparative Example 6

[0087] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 10.

[0088] Table 10

[0089]

[0090]

[0091] Preparation process:

[0092] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose are mixed evenly, and 15% polyvinyl alcohol 5-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60° C. for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 60-80N.

[0093] Comparative Example 7

[0094] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 11.

[0095] Table 11

[0096] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 lactose 75 Croscarmellose Sodium 8 Magnesium Stearate 2 5% polyvinyl alcohol 8-88 aqueous solution 40

[0097] Preparation process:

[0098] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose are mixed evenly, and a 5% polyvinyl alcohol 8-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 60-80N.

[0099] Comparative Example 8

[0100] Olopatadine hydrochloride tablets were prepared using the ingredients listed in Table 12.

[0101] Table 12

[0102] Raw materials Content per tablet (mg) Olopatadine Hydrochloride 5 Microcrystalline Cellulose 30 lactose 75 Croscarmellose Sodium 8 Magnesium Stearate 2 5% polyvinyl alcohol 17-88 aqueous solution 40

[0103] Preparation process:

[0104] Olopatadine hydrochloride, microcrystalline cellulose, lactose and cross-linked sodium carboxymethyl cellulose are mixed evenly, and a 5% polyvinyl alcohol 17-88 aqueous solution is added for wet granulation. The wet granules are dried in an oven at 60°C for 150 minutes, sieved with a 24-mesh sieve, and magnesium stearate is added and mixed evenly. The granules are pressed into tablets using a notched die, and the tablet hardness is 60-80N.

[0105] Test Example 1

[0106] In vitro studies of scored tablets

[0107] With reference to the "Technical Guidelines for the Design and Research of Functional Notches for Oral Tablets of Generic Chemical Drugs (Trial)" issued by the Drug Review Center of the National Medical Products Administration on October 22, 2020, the examples, comparative examples and the original formulation of Aloko were studied by manual segmentation and blade segmentation.

[0108] (1) Weight difference

[0109] Take 30 whole tablets and weigh one divided part of each tablet. The other parts are not required to be weighed. The average weight shall be calculated. No more than one divided part shall exceed the average weight by 85%-115%. If more than one divided part exceeds the average weight by 85%-115, or one divided part exceeds the average weight by 75%-125%, the tablet shall be judged as unqualified.

[0110] Table 13 Number of tablets exceeding 85%-115% (pcs)

[0111] Split method manual blade Example 1 0 0 Example 2 0 0 Example 3 0 0 Example 4 0 0 Comparative Example 1 2 3 Comparative Example 2 3 4 Comparative Example 3 4 3 Comparative Example 4 2 3 Comparative Example 5 4 4 Comparative Example 6 2 3 Comparative Example 7 3 2 Comparative Example 8 5 4 Original research 0 0

[0112] (2) Content uniformity

[0113] Since the content of the main drug in the split part of this product is less than 25%, a content uniformity test should be conducted in accordance with the requirements of <0941 Content Uniformity Test Method> of Part IV of the 2020 edition of the Chinese Pharmacopoeia. Take 10 whole tablets and take one split part from each tablet for content uniformity test, and do not use the other parts. Use manual tablet breaking and blade cutting to measure respectively. A+2.2S should be less than 15.

[0114] Table 14 Content uniformity (A+2.2S value)

[0115] Split method manual blade Example 1 7.51 6.37 Example 2 5.26 5.68 Example 3 8.12 7.65 Example 4 7.97 6.51 Comparative Example 1 15.18 16.56 Comparative Example 2 19.22 20.23 Comparative Example 3 17.27 17.61 Comparative Example 4 18.62 19.22 Comparative Example 5 18.31 19.37 Comparative Example 6 17.56 19.62 Comparative Example 7 16.83 15.98 Comparative Example 8 23.65 20.36 Original research 13.86 14.92

[0116] (3) Weight loss

[0117] Take 15 whole tablets and weigh them accurately before splitting. Remove the scattered medicine crumbs and weigh them accurately after splitting. Compare the split parts (30 half tablets) with 15 whole tablets and calculate the weight loss. Use manual breaking and blade cutting methods to measure respectively. The weight loss should be less than 3%.

[0118] Table 15 Weight loss (%)

[0119]

[0120]

[0121] (4) Friability

[0122] Take about 6.5g of tablets and test the friability of split tablets according to the fourth part of the 2020 edition of the Chinese Pharmacopoeia <0923 Tablet friability test method>. Use manual tablet breaking and blade cutting to measure respectively. The weight loss shall not exceed 1%.

[0123] Table 16 Friability (%)

[0124] Split method manual blade Example 1 0.19 0.25 Example 2 0.15 0.20 Example 3 0.32 0.26 Example 4 0.09 0.17 Comparative Example 1 1.25 1.36 Comparative Example 2 1.53 1.62 Comparative Example 3 1.42 1.45 Comparative Example 4 1.08 0.98 Comparative Example 5 1.56 1.35 Comparative Example 6 1.21 1.08 Comparative Example 7 1.31 1.45 Comparative Example 8 0.78 1.02 Original research 0.52 0.42

[0125] (5) Dissolution

[0126] The dissolution conditions specified in the Japanese Pharmacopoeia (JP18) for Olopatadine Hydrochloride Tablets were selected: the dissolution apparatus was a paddle method using a sinker, the dissolution medium was water, the volume of the dissolution medium was 900 ml, and the dissolution temperature was 37±0.5°C. The dissolution rate of the undivided tablets was investigated, and the dissolution rate of the divided tablets produced by manual tablet breaking and blade cutting was also investigated. The dissolution rate in 15 minutes should be no less than 85%.

[0127] Table 17 Dissolution results (n=12)

[0128]

[0129]

[0130] (6) Stability study

[0131] According to the recommended inspection conditions of 25℃±2℃ / 60%RH±5%RH in the "Technical Guidelines for the Design and Research of Functional Notches for Oral Tablets of Generic Chemical Drugs (Trial)" issued by the Center for Drug Evaluation, the divided parts were placed in high-density polyethylene bottles without sealing and tightly capped for a 90-day stability inspection to examine their related substances.

[0132] Table 18 Stability test results (%)

[0133] Time 0d 90d Example 1 0.15 0.21 Example 2 0.13 0.25 Example 3 0.08 0.16 Example 4 0.11 0.18 Comparative Example 1 0.09 0.26 Comparative Example 2 0.16 0.53 Comparative Example 3 0.11 0.31 Comparative Example 4 0.10 0.35 Comparative Example 5 0.13 0.44 Comparative Example 6 0.08 0.27 Comparative Example 7 0.11 0.21 Comparative Example 8 0.12 0.19 Original research 0.15 0.27

[0134] The above results show that the weight difference, content uniformity, weight loss, friability and dissolution of the tablets obtained by using 0.1%-10% (mass concentration) polyvinyl alcohol 5-88 aqueous solution as a binder for wet granulation and tableting, and controlling the tablet hardness at 60-100N, all meet the requirements, and the split tablets are relatively stable after 90 days. And the content uniformity, weight loss and friability after splitting are better than the original preparation.

[0135] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, rather than to limit the scope of protection of the present invention. Simple modifications or equivalent substitutions of the technical solution of the present invention by ordinary technicians in this field do not deviate from the essence and scope of the technical solution of the present invention.

Claims

1. A solid composition of olopatadine hydrochloride tablets, characterized in that: The invention comprises an active ingredient, olopatadine hydrochloride, a filler, a disintegrant, a lubricant and a polyvinyl alcohol 5-88 aqueous solution; The weight proportions of the combination are: 2-8 parts of olopatadine hydrochloride, 95-115 parts of filler, 5-12 parts of disintegrant, 1-4 parts of lubricant and 20-60 parts of polyvinyl alcohol 5-88 aqueous solution; The mass concentration of the polyvinyl alcohol 5-88 aqueous solution is 1%-10%; The hardness of the solid composition of olopatadine hydrochloride tablets is 60-100N.

2. The solid composition according to claim 1, characterized in that The weight proportions of the combination are: 4-6 parts of olopatadine hydrochloride, 100-110 parts of filler, 6-10 parts of disintegrant, 1-3 parts of lubricant and 30-50 parts of polyvinyl alcohol 5-88 aqueous solution.

3. The solid composition according to claim 1, characterized in that The filler comprises at least one of microcrystalline cellulose, lactose, starch and mannitol.

4. The solid composition according to claim 1, characterized in that The disintegrant comprises at least one of low-substituted hydroxypropyl cellulose, cross-linked sodium carboxymethyl cellulose, sodium carboxymethyl starch and cross-linked polyvinylpyrrolidone.

5. The solid composition according to claim 1, characterized in that The lubricant comprises at least one of stearic acid, magnesium stearate, silicon dioxide and colloidal silicon dioxide.

6. The solid composition according to claim 1, characterized in that The content of olopatadine hydrochloride is 5 mg.

7. A method for preparing a solid composition of olopatadine hydrochloride tablets according to any one of claims 1 to 6, characterized in that: The following steps are involved: 1) Evenly mix olopatadine hydrochloride, filler, disintegrant and lubricant according to the formula amount; 2) adding polyvinyl alcohol 5-88 aqueous solution for wet granulation, drying, sieving, and obtaining wet granules; 3) Add lubricant and mix well. Use a notched die to press the granules into tablets with a tablet hardness of 60-100N.

8. The preparation method according to claim 7, characterized in that: The specific operation of the drying is: drying the wet granules in an oven at 50-70° C. for 120-180 minutes.

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