A rifampicin pharmaceutical composition for eye drops and preparation method thereof

Abstract

The present invention relates to a rifampicin pharmaceutical composition for eye drops and a preparation method thereof. The pharmaceutical composition comprises rifampicin, meglumine and polyethylene glycol 6000, and is matched with a special solvent, wherein the special solvent comprises: glycerol, citric acid, tromethamine, sodium chloride and sodium thimerosal. The preparation formula solves the problems of rifampicin drug granulation adhesion, solubility and stability. The obtained preparation can maintain good fluidity without granulation, has good dissolution and significantly improves the solubility and stability of rifampicin, and has a simple prescription process and good application value.

Description

Technical Field

[0001] The invention belongs to the technical field of medicines and relates to a rifampicin pharmaceutical composition for eye drops and a preparation method thereof. Background Art

[0002] Rifampicin, chemical name 3-[[(4-methyl-1-piperazinyl)imino]methyl]rifamycin, is an organic compound with the chemical formula C 43 H 58 N4O 12 It is a broad-spectrum antibiotic belonging to the rifamycin family. It has a strong antibacterial effect on Mycobacterium tuberculosis, and is also effective against Gram-positive or negative bacteria, viruses, etc. It is mainly used to treat tuberculosis and Staphylococcus aureus infection. It is often applied externally as eye drops. Rifampicin eye drops are an eye anti-infective drug that can play an anti-inflammatory and antibacterial role. It can be used clinically to treat trachoma, conjunctivitis, keratitis and other diseases.

[0003] Rifampicin has poor stability, is easy to degrade, and is almost insoluble in water. The preparation process in eye drops is relatively complicated. The prior art eye drops are generally made into tablets with special solvents, but bonding is easy to occur during the granulation process of the drug preparation preparation process, resulting in increased difficulty in preparation, and the dissolution has further room for improvement, while the stability after dissolution needs to be further improved. In summary, in order to solve the problems of difficulty in preparation, dissolution and poor stability of rifampicin eye drops, the prior art has limitations. The inventors have obtained rifampicin drug preparation prescriptions and preparation methods thereof in the long-term research process on rifampicin, with simple process and less amount of auxiliary materials, and the prepared rifampicin preparation has extremely high quality and stability, which increases the safety of medication; at the same time, stability and solubility are further improved compared with the prior art. Summary of the invention

[0004] The object of the present invention is to provide a rifampicin preparation with less auxiliary materials, simple preparation process, stability and good solubility and a preparation method thereof.

[0005] The solution adopted by the present invention to solve the above technical problems is:

[0006] A rifampicin pharmaceutical composition comprises rifampicin, meglumine and polyethylene glycol 6000.

[0007] Furthermore, in parts by weight, the weight ratio of rifampicin, meglumine and polyethylene glycol 6000 in the pharmaceutical composition is (5-10): (75-85): (15-25), and more preferably (5-10): 80:20.

[0008] The present invention also provides a method for preparing the above-mentioned composition, comprising the following steps:

[0009] (1) drying the raw materials comprising rifampicin, meglumine and polyethylene glycol 6000 respectively and passing them through an 80-mesh sieve to obtain raw material powders;

[0010] (2) Rifampicin, meglumine, and polyethylene glycol 6000 powder are added in order and mixed thoroughly to obtain the rifampicin pharmaceutical composition.

[0011] The present invention also provides a rifampicin pharmaceutical composition tablet, wherein the pharmaceutical tablet comprises the above pharmaceutical composition or the pharmaceutical composition obtained by the above preparation method.

[0012] Furthermore, each tablet contains 5 mg or 10 mg of rifampicin.

[0013] The present invention also provides a method for preparing the tablets, comprising the following steps: determining the tablet weight of the pharmaceutical composition comprising rifampicin, meglumine and polyethylene glycol 6000 according to specifications, and tableting the tablets on a machine.

[0014] Furthermore, the pharmaceutical composition also contains a special solvent, and the pharmaceutical composition tablets can be dissolved in the special solvent to prepare rifampicin for eye drops.

[0015] The special solvent formula is: 100g of glycerol, 5.5g of citric acid, 14g of tromethamine, dissolved in injection water and fixed to 10000ml.

[0016] Furthermore, the special solvent also contains sodium chloride in an amount of 0.04 g.

[0017] Furthermore, the special solvent also contains sodium thimerosal in an amount of 0.3 g.

[0018] The present invention also provides a method for preparing the above-mentioned special solvent, comprising the following steps:

[0019] (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution;

[0020] (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution;

[0021] (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount;

[0022] (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

[0023] The preparation formula adopted by the present invention solves the problems of granulation adhesion, dissolution and stability of rifampicin drugs. The obtained preparation can maintain good fluidity without granulation, has good dissolution and significantly improves the stability of rifampicin, and has a simple prescription process and good application value. At the same time, rifampicin for eye drops with extremely high stability can be prepared by combining with a special solvent. DETAILED DESCRIPTION

[0024] For a better understanding of the present invention, the following examples are provided to further illustrate the present invention, but the present invention is not limited to the following examples.

[0025] The rifampicin raw material of the present invention can be prepared by using existing public technology, or can be purchased as a marketed product.

[0026] Example 1 Preparation of a Rifampicin Preparation Mixed Powder According to a Prescription Quantity of 1000 Preparation Units

[0027] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0028] Example 2 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0029] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 25 g of polyethylene glycol 6000 were added and mixed uniformly.

[0030] Example 3 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0031] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 25 g of polyethylene glycol 6000 were added and mixed uniformly.

[0032] Example 4 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0033] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0034] Example 5 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0035] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 80 g of meglumine were first mixed thoroughly, and then 20 g of polyethylene glycol 6000 were added and mixed uniformly.

[0036] Example 6 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0037] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0038] Example 7 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0039] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 25 g of polyethylene glycol 6000 were added and mixed uniformly.

[0040] Example 8 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0041] Rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 25 g of polyethylene glycol 6000 were added and mixed evenly.

[0042] Example 9 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0043] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0044] Example 10 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0045] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 80 g of meglumine were first mixed thoroughly, and then 20 g of polyethylene glycol 6000 were added and mixed uniformly.

[0046] Example 11 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0047] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed evenly.

[0048] Example 12 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0049] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 73 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0050] Example 13 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0051] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 73 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed uniformly.

[0052] Example 14 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0053] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 87 g of meglumine were first mixed thoroughly, and then 27 g of polyethylene glycol 6000 were added and mixed uniformly.

[0054] Example 15 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0055] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed evenly.

[0056] Example 16 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0057] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 75 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed uniformly.

[0058] Example 17 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0059] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 73 g of meglumine were first mixed thoroughly, and then 15 g of polyethylene glycol 6000 were added and mixed uniformly.

[0060] Example 18 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0061] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 73 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed uniformly.

[0062] Example 19 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0063] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 87 g of meglumine were first mixed thoroughly, and then 27 g of polyethylene glycol 6000 were added and mixed uniformly.

[0064] Example 20 Preparation of Rifampicin Preparation Mixed Powder According to the Prescription Quantity of 1000 Preparation Units

[0065] Rifampicin, meglumine and polyethylene glycol 6000 which were dried at 70°C in advance were passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 85 g of meglumine were first mixed thoroughly, and then 13 g of polyethylene glycol 6000 were added and mixed uniformly.

[0066] The rifampicin preparation obtained in Example 1-20 was mixed and tableted, and its fluidity was observed. The results are as follows:

[0067] The powders of Examples 1-10 have good fluidity and are easy to tablet.

[0068] Examples 11-20 have poor fluidity and are not convenient for tableting.

[0069] It can be seen that adding 75g-85g of meglumine and 15g-25g of polyethylene glycol 6000 to every 5g or 10g of rifampicin can solve the problems of rifampicin sticking and poor fluidity without granulation.

[0070] Example 21 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0071] The rifampicin and polyethylene glycol 6000 dried at 70° C. in advance are passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 20 g of polyethylene glycol 6000 are mixed evenly, the content is determined, the tablet weight is determined according to the specification, the tablets are pressed on a machine, inspected, and packaged to obtain the product.

[0072] Example 22 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0073] Rifampicin and meglumine dried at 70°C in advance are passed through an 80-mesh sieve in sequence; 10 g of rifampicin and 80 g of meglumine are fully mixed and the content is determined, the tablet weight is determined according to the specification, the tablets are pressed on a machine, inspected, and packaged to obtain the product.

[0074] Example 23 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0075] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 10 g of rifampicin and 75 g of meglumine, then add 15 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package them.

[0076] Example 24 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0077] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 10 g of rifampicin and 85 g of meglumine, then add 25 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0078] Example 25 Preparation of Rifampicin Pharmaceutical Composition Tablets (10,000 Preparation Units)

[0079] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 10 g of rifampicin and 80 g of meglumine, then add 20 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package them.

[0080] Example 26 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0081] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 10 g of rifampicin and 80 g of meglumine, then add 15 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0082] Example 27 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0083] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 10 g of rifampicin and 75 g of meglumine, then add 25 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0084] Example 28 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0085] The rifampicin and polyethylene glycol 6000 dried at 70°C in advance are passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 20 g of polyethylene glycol 6000 are mixed evenly, the content is determined, the tablet weight is determined according to the specification, the tablets are pressed on a machine, inspected, and packaged to obtain the product.

[0086] Example 29 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0087] Rifampicin and meglumine dried at 70°C in advance are passed through an 80-mesh sieve in sequence; 5 g of rifampicin and 80 g of meglumine are fully mixed and the content is determined, the tablet weight is determined according to the specification, the tablets are pressed on a machine, inspected, and packaged to obtain the product.

[0088] Example 30 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0089] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 5 g of rifampicin and 75 g of meglumine, then add 15 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package them.

[0090] Example 31 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0091] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 5 g of rifampicin and 85 g of meglumine, then add 25 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0092] Example 32 Preparation of Rifampicin Pharmaceutical Composition Tablets (10,000 Preparation Units)

[0093] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 5 g of rifampicin and 80 g of meglumine, then add 20 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0094] Example 33 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0095] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 5 g of rifampicin and 80 g of meglumine, then add 15 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0096] Example 34 Preparation of Rifampicin Pharmaceutical Composition Tablets (1000 Preparation Units)

[0097] Sequentially pass rifampicin, meglumine and polyethylene glycol 6000 dried at 70°C through an 80-mesh sieve; fully mix 5 g of rifampicin and 75 g of meglumine, then add 25 g of polyethylene glycol 6000 and mix evenly, determine the content, determine the tablet weight according to the specification, press the tablets on a machine, inspect and package.

[0098] Example 35 Preparation of a solvent specifically for rifampicin pharmaceutical composition tablets

[0099] The formula is: 100g of glycerol, 5.5g of citric acid, 14g of tromethamine, 0.04g of sodium chloride, 0.3g of sodium thimerosal, dissolve in water for injection and make up to 10000ml.

[0100] The preparation method is as follows:

[0101] (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution;

[0102] (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution;

[0103] (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount;

[0104] (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

[0105] Example 36 Preparation of a solvent specifically for rifampicin pharmaceutical composition tablets

[0106] The formula is: 98g of glycerol, 5.5g of citric acid, 14g of tromethamine, 0.04g of sodium chloride, 0.3g of sodium thimerosal, dissolve in water for injection and make up to 10000ml.

[0107] The preparation method is as follows:

[0108] (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution;

[0109] (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution;

[0110] (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount;

[0111] (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

[0112] Example 37 Preparation of a solvent specifically for rifampicin pharmaceutical composition tablets

[0113] The formula is: 100g of glycerol, 5.0g of citric acid, 14g of tromethamine, 0.04g of sodium chloride, 0.3g of sodium thimerosal, dissolve in water for injection and make up to 10000ml.

[0114] The preparation method is as follows:

[0115] (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution;

[0116] (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution;

[0117] (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount;

[0118] (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

[0119] Example 38 Preparation of a solvent specifically for rifampicin pharmaceutical composition tablets

[0120] The formula is: 100g of glycerol, 5.5g of citric acid, 13g of tromethamine, 0.04g of sodium chloride, 0.3g of sodium thimerosal, dissolve in water for injection and make up to 10000ml.

[0121] The preparation method is as follows:

[0122] (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution;

[0123] (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution;

[0124] (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount;

[0125] (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

[0126] The rifampicin pharmaceutical composition tablets obtained in Examples 21-27 were subjected to a dissolution test. At 37°C ± 0.5°C, 900 mL of pH 1.0 hydrochloric acid solution and pH 3.8 acetic acid solution were used as dissolution media, respectively. The paddle method was used at a speed of 50 rpm. The dissolution of the tablets was measured after sampling at 15 min, 30 min, and 45 min, respectively. The results are shown in Tables 1 and 2.

[0127] Table 1 pH 1.0 dissolution test results

[0128]

[0129] Table 2 pH 3.8 dissolution test results

[0130]

[0131] It can be seen from the results of Table 1 and Table 2 that the addition of 75g-85g of meglumine and 15g-25g of polyethylene glycol 6000 to every 10g of rifampicin can significantly improve the solubility of rifampicin, especially the addition of 80g of meglumine and 20g of polyethylene glycol 6000 to every 10g of rifampicin has the best effect. The same test was also carried out in Examples 28-34, and similar results were obtained.

[0132] The rifampicin pharmaceutical composition tablets obtained in Example 25 and Example 32 were subjected to accelerated stability test (40°C±2°C, RH 75%±5%). The results are shown in Table 3.

[0133] Table 3 Rifampicin pharmaceutical composition tablet accelerated test results

[0134]

[0135] It can be seen from the results in Table 3 that the rifampicin drugs obtained in Examples 25 and 32 have good stability. The same test was also carried out on the rifampicin pharmaceutical preparations prepared in other Examples 23, 24, 26, 27, 30, 31, 33 and 34, and similar results were obtained.

[0136] The rifampicin pharmaceutical composition tablets prepared in Example 25 were dissolved in the special solvents prepared in Examples 35-38, respectively. Each tablet was dissolved in a special solvent, and rifampicin samples for eye drops were prepared, respectively, and the influencing factor test was carried out. The above 4 samples were subjected to the influencing factor test, and were placed at 60°C and strong light (4500lx±500lx) for 10 days. Samples were taken on the 10th day for testing, and the results were compared with those on the 0th day to investigate the stability of the samples. The results are shown in Tables 4-5:

[0137] Table 4 60℃ stability test results

[0138]

[0139] Table 5 Strong light (4500LX) stability test results

[0140]

[0141] It can be seen from the results of Table 4 and Table 5 that the special solvent formula of the rifampicin pharmaceutical composition is: 100g of glycerol, 5.0g of citric acid, 14g of tromethamine, dissolved in water for injection and diluted to 10000ml, which can significantly improve the stability of rifampicin for eye drops. Even a small change in the amount of glycerol, citric acid and tromethamine will produce a significant change in stability.

[0142] The above is only a preferred embodiment of the present invention, which certainly cannot be used to limit the scope of rights of the present invention. It should be pointed out that for ordinary technicians in this technical field, several improvements and changes can be made without departing from the principle of the present invention, and these improvements and changes are also regarded as the protection scope of the present invention.

Claims

1. A rifampicin pharmaceutical composition, characterized in that: The pharmaceutical composition comprises rifampicin, meglumine and polyethylene glycol 6000.

2. The composition according to claim 1, characterized in that In parts by weight, the weight ratio of rifampicin, meglumine and polyethylene glycol 6000 in the pharmaceutical composition is (5-10): (75-85): (15-25).

3. A method for preparing the composition according to any one of claims 1 to 2, characterized in that: The steps include: (1) Drying the raw materials of rifampicin, meglumine and polyethylene glycol 6000 at 70° C. and passing through an 80-mesh sieve to obtain raw material powders; (2) Rifampicin, meglumine, and polyethylene glycol 6000 powder are added in order and mixed thoroughly to obtain the rifampicin pharmaceutical composition.

4. A rifampicin pharmaceutical composition tablet, characterized in that: The pharmaceutical tablet comprises the pharmaceutical composition according to any one of claims 1 to 2.

5. The tablet according to claim 4, characterized in that Each tablet contains 5 mg or 10 mg of rifampicin.

6. A method for preparing a tablet according to any one of claims 4 to 5, characterized in that: The method comprises the following steps: determining the tablet weight according to the specifications of the pharmaceutical composition described in any one of claims 1 to 2 or the pharmaceutical composition obtained by the preparation method of any one of claims 3 to 4, and tableting the tablets on a machine.

7. The composition according to claim 1 or 2, characterized in that The invention also contains a special solvent for preparing rifampicin for eye drops, and the formula of the special solvent is: 100g of glycerol, 5.5g of citric acid, 14g of tromethamine, which is dissolved in injection water and fixed to 10000ml.

8. The composition according to claim 7, characterized in that The special solvent also contains 0.04 g of sodium chloride and 0.3 g of sodium thimerosal.

9. The method for preparing the special solvent according to claim 7 or 8, comprising the following steps: (1) Add glycerol to 30% of the total amount of water for injection and stir to dissolve to obtain the first solution; (2) Add citric acid, tromethamine, sodium chloride and sodium thimerosal to 30% of the total amount of water for injection in sequence, stir and dissolve to obtain the second solution; (3) Add the second liquid to the first liquid, stir evenly, and continue stirring while adding water for injection to the full amount; (4) Filter and sterilize using a 0.22 μm filter cartridge and fill into an eye drop bottle according to the specification of 10 ml.

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