A dibromohydantoin effervescent tablet and its preparation method and application

Abstract

The present invention discloses a dibromohydantoin effervescent tablet, a preparation method, and an application thereof. The dibromohydantoin effervescent tablet comprises a solubilizing factor selected from one or both of an amino group-containing compound and resorcinol. The dibromohydantoin effervescent tablet of the present invention has a fast effervescence rate and thorough dissolution, and the dissolution is not affected by water temperature or water volume. The amino group in the high-efficiency solubilizing factor can quickly form a bond with the bromine element in dibromohydantoin, thereby improving the solubility of the dibromohydantoin. At the same time, the two oxygens on the dibromohydantoin ring can form hydrogen bonds with resorcinol to increase its solubility. The simultaneous use of the two factors results in a synergistic and efficient dissolution effect of the dibromohydantoin.

Description

Technical Field

[0001] The invention relates to a dibromohydantoin effervescent tablet and a preparation method and application thereof, belonging to the field of disinfectants. Background Art

[0002] Currently, chlorine-containing disinfectants are the most widely used disinfectants, whose active ingredients include sodium dichloroisocyanurate, trichloroisocyanuric acid, hypochlorous acid, and others. However, a common problem with these chlorine-containing disinfectants is their strong odor during use. In public places such as schools, kindergartens, and train stations, this can leave an unpleasant, irritating sensation for a long time after use. Consequently, the search for milder, more user-friendly disinfectants that can overcome this odor drawback has begun. Because aqueous solutions of dibromohydantoin are non-toxic, odorless, and non-irritating, and their bactericidal efficacy is more than twice that of chlorine-containing disinfectants, disinfectants based on dibromohydantoin as a primary ingredient are well-suited to meeting these needs. However, dibromohydantoin itself is slightly soluble in water. Therefore, commercially available disinfectant tablets based on dibromohydantoin do not dissolve completely during use, or, due to its low solubility, require sufficient water and a sufficiently high temperature for dissolution. Only by overcoming the difficulty of dissolving dibromohydantoin can dibromohydantoin tablets become what everyone loves: non-toxic, odorless, non-irritating, non-corrosive, and dissolving quickly and thoroughly. Furthermore, the preparation of dibromohydantoin effervescent tablets requires stringent environmental humidity and temperature requirements, often causing mold sticking, making it difficult to form the tablets. Over time, this can lead to equipment malfunctions. Consequently, a limited number of manufacturers are capable of producing dibromohydantoin effervescent tablets, limiting their production and development.

[0003] The patent (application number: 201510327641.2) discloses a dibromohydantoin disinfectant for use in recycled paper production and its preparation method. This solution solves the solubility problem of dibromohydantoin and facilitates its use in various locations for disinfection and sterilization. However, the patent discloses a liquid dibromohydantoin disinfectant, which requires considerable storage space and requires strict light protection during storage, which limits its use to a certain extent. Therefore, a highly soluble solid dibromohydantoin disinfectant is needed to achieve ready-to-use preparation, thereby addressing the storage and long-term light decomposition issues.

[0004] Patent application number: 201110443057.5 discloses a broad-spectrum bromine-containing disinfectant, prepared from the following components and weight percentages: 20% to 60% dibromohydantoin; 30% to 50% cosolvent; 0% to 25% anhydrous sodium carbonate; and 0% to 25% dimethylhydantoin. The patent incorporates dibromohydantoin as a cosolvent, but does not provide actual dissolution and disinfection efficacy. Summary of the Invention

[0005] Purpose of the invention: The technical problem to be solved by the present invention is to provide a dibromohydantoin effervescent tablet with fast effervescence speed, thorough dissolution, dissolution not affected by water temperature, and tablet dissolution not affected by water amount, as well as a preparation method and application thereof.

[0006] Technical solution: To solve the above technical problems, the dibromohydantoin effervescent tablets provided by the present invention include the following components, in parts by weight: 30-40 parts of dibromohydantoin, 8-20 parts of a solubilizing factor, 38-45 parts of a disintegrant, 0.2-1 parts of a dispersant, 0.5-5 parts of a release agent, 0.1-8 parts of a lubricant, and 1-5 parts of a stabilizer. The solubilizing factor includes one or both of an amino group-containing compound or resorcinol.

[0007] Wherein, the amino group-containing compound includes one or more of lysine, aminobutyric acid or glucosamine.

[0008] Wherein, the disintegrant includes one or more of anhydrous citric acid, sodium bicarbonate, silica gel, sodium carboxymethyl cellulose, polyvinyl alcohol or carbomer U20.

[0009] Wherein, the dispersant includes one or more of sodium diisobutylnaphthalene sulfonate, dodecyldimethylbenzyl ammonium chloride or dodecyltrimethylammonium chloride.

[0010] Wherein, the release agent includes one or more of magnesium stearate, paraffin and magnesium silicate.

[0011] Wherein, the lubricant includes polyethylene glycol; the stabilizer includes sodium tripolyphosphate.

[0012] The dibromohydantoin effervescent tablet further comprises 0.5-2.5 parts of a filler, and the filler comprises anhydrous sodium sulfate.

[0013] The present invention provides a method for preparing the dibromohydantoin effervescent tablets, comprising the following steps: mixing dibromohydantoin, a solubility factor, a disintegrant, a dispersant, a filler, and a stabilizer, granulating, adding a release agent and a lubricant, mixing, and tableting to obtain the dibromohydantoin effervescent tablets.

[0014] Wherein, the particle size range of the particles obtained by granulation is 20-50 meshes.

[0015] The bacteria used in the sterilization of the dibromohydantoin effervescent tablets provided by the present invention include bacteria and viruses, including one or more of Escherichia coli, Staphylococcus aureus, Candida albicans, Pseudomonas aeruginosa, poliovirus or Bacillus subtilis var. niger spores.

[0016] Beneficial effects: Compared with the prior art, the present invention has the following significant advantages: (1) Fast effervescence speed: The addition of the effervescent agent and the dispersant enables the effervescent tablet to effervesce quickly within 5 minutes without stirring, and the solution is clear; (2) Complete dissolution: A solubilizing factor is added. The amino group in the high-efficiency solubilizing factor can quickly form a bond with the bromine element in dibromohydantoin, thereby changing the solubility of dibromohydantoin. At the same time, the two oxygens on the dibromohydantoin ring can form hydrogen bonds with resorcinol to increase its solubility. The simultaneous use of the two factors produces a synergistic and efficient dissolution effect of dibromohydantoin; (3) Dissolution is not affected by water temperature: The addition of the solubilizing factor causes dibromohydantoin to immediately become a water-soluble substance when it encounters water, so that its dissolution is free from the influence of temperature; (4) Tablet dissolution is not affected by the amount of water: As long as the water can cover the tablet, it can be completely dissolved, and it will not be incompletely dissolved due to a small amount of water; (5) The tableting process adopts granulation and tableting, which makes it free from the influence of the external environment, and can achieve large-scale continuous production that is not affected by the season, which can save a lot of manpower and material resources. BRIEF DESCRIPTION OF THE DRAWINGS

[0017] Figure 1 The dibromohydantoin effervescent tablets prepared in Example 1;

[0018] Figure 2 This is a diagram showing the dissolution effect of the dibromohydantoin effervescent tablets prepared in Example 1 at different temperatures;

[0019] Figure 3 This is a diagram showing the dissolution effect of the dibromohydantoin effervescent tablets prepared in Example 1 under different water amounts;

[0020] Figure 4 This is a diagram showing the dissolution effect of dibromohydantoin effervescent tablets prepared in Comparative Example 1 at different temperatures;

[0021] Figure 5 This is a diagram showing the dissolution effect of dibromohydantoin effervescent tablets prepared in Comparative Example 1 under different water amounts;

[0022] Figure 6 This is a diagram showing the dissolution effect of dibromohydantoin effervescent tablets prepared in Comparative Example 4 at different temperatures;

[0023] Figure 7 This is a diagram showing the dissolution effect of dibromohydantoin effervescent tablets prepared in comparative example 4 under different water amounts. DETAILED DESCRIPTION

[0024] The technical solution of the present invention will be further described below with reference to the accompanying drawings.

[0025] Sodium carboxymethyl cellulose: Shandong Siyang Biotechnology Co., Ltd., 20220241; Sodium diisobutylnaphthalenesulfonate: Jinan Rongzheng Chemical Co., Ltd., 20200720; Polyethylene glycol: Jinan Yuanbaolai Chemical Technology Co., Ltd., 20220411.

[0026] Example 1

[0027] formula:

[0028] 30 parts of dibromohydantoin, 8 parts of solubilizing factor aminobutyric acid, 7.5 parts of solubilizing factor resorcinol, 18 parts of anhydrous citric acid, 20 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalene sulfonate, magnesium stearate (C 36 H 70 MgO4) 1 part, polyethylene glycol (PEG 8000) 5 parts, sodium tripolyphosphate 5 parts.

[0029] Production process:

[0030] (1) 30 parts of dibromohydantoin, 8 parts of aminobutyric acid, 7.5 parts of resorcinol, 18 parts of anhydrous citric acid, 20 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalenesulfonate, and 5 parts of sodium tripolyphosphate were placed in a blender and mixed continuously for 30 minutes.

[0031] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0032] (3) Take all the granules, add 1 part of magnesium stearate and 5 parts of PEG 8000, continue to put them into the blender and mix them continuously for 30 minutes, and then prepare tablets.

[0033] (4) The tablet press pressure is adjusted to 40N, and tablets are pressed to obtain dibromohydantoin effervescent tablets ( Figure 1 The obtained dibromohydantoin effervescent tablets have a smooth surface without defects, and the production process equipment operates well and can operate continuously.

[0034] During the tableting process, samples were taken every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescent times of the five samples at 20°C water were 2'11", 3'09", 2'26", 2'25", and 2'50", respectively. The dibromohydantoin effervescent tablets in all five samples were completely dissolved within 5 minutes.

[0035] Take 5 portions of 100ml water and adjust the temperature to 5℃, 10℃, 15℃, 20℃ and 25℃ respectively. Put 5 pieces of compressed dibromohydantoin effervescent tablets into each portion. The dissolution effect is as follows: Figure 2 As shown in the figure, the dibromohydantoin effervescent tablets were completely dissolved within 5 minutes, and the solution was clear and transparent, indicating that the dissolution rate and effect of the dibromohydantoin effervescent tablets were not limited by water temperature.

[0036] Take 5 beakers, add 20ml, 50ml, 100ml, 500ml and 5L of water respectively at a water temperature of 20℃, and add 5 compressed dibromohydantoin effervescent tablets to each beaker. The dissolution effect is as follows: Figure 3The dibromohydantoin effervescent tablets were completely dissolved within 5 minutes, and the solutions were clear and transparent, indicating that the dissolution rate and effect of the dibromohydantoin effervescent tablets were not limited by the amount of water.

[0037] Example 2

[0038] formula:

[0039] 40 parts of dibromohydantoin, 11 parts of solubilizing factor glucosamine, 9 parts of solubilizing factor resorcinol, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.2 parts of sodium diisobutylnaphthalene sulfonate, 0.5 parts of magnesium stearate, 0.1 parts of PEG8000, and 1.2 parts of sodium tripolyphosphate as a stabilizer.

[0040] Production process:

[0041] (1) Place 40 parts of dibromohydantoin, 11 parts of glucosamine, 9 parts of resorcinol, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.2 parts of sodium diisobutylnaphthalenesulfonate, and 1.2 parts of sodium tripolyphosphate in a blender and mix continuously for 30 minutes.

[0042] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0043] (3) Add 0.5 parts of magnesium stearate and 0.1 parts of PEG 8000 to the granules, continue to mix them in a blender for 30 minutes, and then prepare tablets.

[0044] (4) The tablet press pressure is adjusted to 40N, and the dibromohydantoin effervescent tablets are obtained by tableting; the surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0045] During the tableting process, samples were taken every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescent times of the five samples at 20°C water were 4'17", 4'30", 5'09", 5'25", and 4'19", respectively. The dibromohydantoin effervescent tablets in all five samples were completely dissolved within 10 minutes.

[0046] Take 5 parts of 100ml of water, adjust the temperature to 5℃, 10℃, 15℃, 20℃, and 25℃ respectively, and put 5 compressed dibromohydantoin effervescent tablets into each part. The dibromohydantoin effervescent tablets are completely dissolved within 10 minutes, and the solution is clear and transparent, indicating that the dissolution rate and effect of dibromohydantoin effervescent tablets are not limited by water temperature.

[0047] Take 5 beakers and add 20ml, 50ml, 100ml, 500ml and 5L of water respectively at a water temperature of 20℃, and add 5 compressed dibromohydantoin effervescent tablets to each beaker. The dibromohydantoin effervescent tablets are completely dissolved within 10 minutes, and the solution is clear and transparent, indicating that the dissolution rate and effect of dibromohydantoin effervescent tablets are not limited by the amount of water.

[0048] Example 3

[0049] formula:

[0050] 35 parts of dibromohydantoin, 9 parts of solubilizing factor lysine, 6 parts of solubilizing factor resorcinol, 16 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.3 parts of sodium diisobutylnaphthalene sulfonate, 1 part of magnesium stearate, 3 parts of PEG8000, 4.7 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate.

[0051] Production process:

[0052] (1) 35 parts of dibromohydantoin, 9 parts of lysine, 6 parts of resorcinol, 16 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.3 parts of sodium diisobutylnaphthalenesulfonate, 4.7 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate were placed in a blender and mixed continuously for 30 minutes.

[0053] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 50 mesh.

[0054] (3) Add 1 part of magnesium stearate and 3 parts of PEG 8000 to the granules, continue to mix them in a blender for 30 minutes, and then prepare tablets.

[0055] (4) The tablet press pressure is adjusted to 40N, and the dibromohydantoin effervescent tablets are obtained by tableting; the surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0056] During the tableting process, samples were taken every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescent times of the five samples at 20°C water were 5'10", 4'59", 5'16", 5'27", and 5'35", respectively. Furthermore, the dibromohydantoin effervescent tablets in all five samples were completely dissolved within 7 minutes.

[0057] Take 5 parts of 100ml of water, adjust the temperature to 5℃, 10℃, 15℃, 20℃, and 25℃ respectively, and put 5 compressed dibromohydantoin effervescent tablets into each part. The dibromohydantoin effervescent tablets are completely dissolved within 7 minutes, and the solution is clear and transparent, indicating that the dissolution rate and effect of dibromohydantoin effervescent tablets are not limited by water temperature.

[0058] Take 5 beakers and add 20ml, 50ml, 100ml, 500ml and 5L of water respectively at a water temperature of 20℃, and add 5 compressed dibromohydantoin effervescent tablets to each beaker. The dibromohydantoin is completely dissolved within 7 minutes and the solution is clear and transparent, indicating that the dissolution rate and effect of dibromohydantoin effervescent tablets are not limited by the amount of water.

[0059] Example 4

[0060] Preferred embodiment 1 of the present invention, take the dibromohydantoin effervescent tablets obtained in Example 1, be prepared into a dibromohydantoin disinfectant with an effective bromine content of 300 ppm, and according to the requirements of the "Disinfection Technical Specification" (2002 edition), the killing effect of various bacteria required in the specification was tested by the suspension quantitative method. The experimental results are shown in Table 1:

[0061] Table 1 Sterilization effect of preferred formula products

[0062]

[0063] Conclusion: The dibromohydantoin effervescent tablets made in the preferred embodiment are prepared into a dibromohydantoin disinfectant with an effective bromine content of 300 ppm. After 10 minutes of action on Escherichia coli, Staphylococcus aureus, and Potassium aeruginosa, the killing logarithmic values ​​are all greater than 5. After 10 minutes of action on Candida albicans and poliovirus, the killing logarithmic values ​​are all greater than 4, which meets the requirements of the "Technical Specifications for Disinfection".

[0064] Comparative Example 1

[0065] formula:

[0066] 30 parts of dibromohydantoin, 15 parts of solubilizing factor aminobutyric acid, 18 parts of disintegrant anhydrous citric acid, 20 parts of disintegrant sodium bicarbonate, 5 parts of disintegrant sodium carboxymethyl cellulose, 0.5 parts of dispersant sodium diisobutylnaphthalene sulfonate, 0.5 parts of release agent magnesium stearate (C 36 H 70 MgO4) 1 part, lubricant polyethylene glycol 5 parts, filler anhydrous sodium sulfate 0.5 parts, stabilizer sodium tripolyphosphate 5 parts.

[0067] Production process:

[0068] (1) 30 parts of dibromohydantoin, 15 parts of aminobutyric acid, 18 parts of anhydrous citric acid, 20 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalenesulfonate, 0.5 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate were placed in a blender and mixed continuously for 30 minutes.

[0069] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0070] (3) Take all the granules, add 1 part of magnesium stearate and 5 parts of PEG 8000, continue to put them into the blender and mix them continuously for 30 minutes, and then prepare tablets.

[0071] (4) The tablet press pressure is adjusted to 40N, and tablets are pressed to obtain dibromohydantoin effervescent tablets. The surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0072] During the tableting process, samples were taken every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescence times of the five samples at 20°C water were 2'30", 3'11", 2'19", 3'25", and 3'25", respectively. The dibromohydantoin in the five samples completely dissolved within 20 minutes. However, it did not completely dissolve when the water volume was less than 500 ml / tablet at 20°C.

[0073] Take 5 portions of 100ml water and adjust the temperature to 5℃, 10℃, 15℃, 20℃ and 25℃ respectively. Put 5 pieces of compressed dibromohydantoin effervescent tablets into each portion. After 30 minutes, the dissolution effect is as follows: Figure 4 As shown, insoluble dibromohydantoin was deposited at the bottom of the beakers at water temperatures of 5°C, 10°C, and 15°C, while the dibromohydantoin effervescent tablets in the remaining beakers were completely dissolved.

[0074] Take 5 beakers, add 20ml, 50ml, 100ml, 500ml and 5L of water respectively at 20℃, add 5 compressed dibromohydantoin effervescent tablets to each beaker, and let it stand for 30 minutes. The dissolution effect is as follows: Figure 5 As shown, the dibromohydantoin effervescent tablets placed in 5L of water were completely dissolved, while insoluble dibromohydantoin was deposited at the bottom of the other beakers.

[0075] Comparative Example 2

[0076] formula:

[0077] 30 parts of dibromohydantoin, 20 parts of solubilizing factor glucosamine, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalene sulfonate, 1 part of magnesium stearate, 5 parts of PEG8000, 0.5 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate, a stabilizer.

[0078] Production process:

[0079] (1) 30 parts of dibromohydantoin, 20 parts of glucosamine, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalenesulfonate, 0.5 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate were placed in a blender and mixed continuously for 30 minutes.

[0080] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0081] (3) Add 1 part of magnesium stearate and 5 parts of PEG 8000 to the granules and continue mixing in a blender for 30 minutes.

[0082] (4) The tablet press pressure is adjusted to 40N, and the dibromohydantoin effervescent tablets are obtained by tableting; the surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0083] During the tableting process, samples were collected every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescence times of the five samples at 20°C water were 6'25", 6'50", 7'19", 7'25", and 6'10", respectively. The dibromohydantoin in the five samples completely dissolved within 30 minutes and did not completely dissolve when the water volume was less than 500 ml / tablet.

[0084] Take 5 portions of 100ml of water and adjust the temperature to 5℃, 10℃, 15℃, 20℃, and 25℃ respectively. Put 5 compressed tablets into each beaker. After 30 minutes, insoluble dibromohydantoin will be deposited at the bottom of the beaker in the beakers with water temperature of 5℃, 10℃, and 15℃. The dibromohydantoin effervescent tablets will be completely dissolved in the beakers with water temperature of 20℃ and 25℃.

[0085] At a water temperature of 20°C, take 5 beakers and add 20ml, 50ml, 100ml, 500ml and 5L of water respectively, and add 5 compressed dibromohydantoin effervescent tablets to each beaker. After standing for 30 minutes, the dibromohydantoin effervescent tablets in 5L of water are completely dissolved, and insoluble dibromohydantoin is deposited at the bottom of the other beakers.

[0086] Comparative Example 3

[0087] formula:

[0088] 30 parts of dibromohydantoin, 19 parts of solubilizing factor lysine, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.3 parts of sodium diisobutylnaphthalene sulfonate, 1 part of magnesium stearate, 5 parts of PEG8000, 1.7 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate.

[0089] Production process:

[0090] (1) 30 parts of dibromohydantoin, 19 parts of lysine, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalenesulfonate, and 1.7 parts of anhydrous sodium sulfate were placed in a blender and mixed continuously for 30 minutes.

[0091] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0092] (3) Add 1 part of magnesium stearate and 5 parts of PEG 8000 to the granules, continue to mix them in a blender for 30 minutes, and then prepare tablets.

[0093] (4) The tablet press pressure is adjusted to 40N, and the dibromohydantoin effervescent tablets are obtained by tableting; the surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0094] During the tableting process, samples were collected every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescence times of the five samples at 20°C were 5'17", 4'41", 5'35", 5'43", and 5'50", respectively. The dibromohydantoin in the five samples completely dissolved within 30 minutes and did not completely dissolve when the water volume was less than 500 ml / tablet.

[0095] Take 5 portions of 100ml of water and adjust the temperature to 5℃, 10℃, 15℃, 20℃ and 25℃ respectively. Put 5 compressed tablets into each beaker. After 30 minutes, insoluble dibromohydantoin will be deposited at the bottom of the beakers with water temperature of 5℃, 10℃ and 15℃, while the dibromohydantoin effervescent tablets in the other beakers will be completely dissolved.

[0096] At a water temperature of 20°C, take 5 beakers and add 20ml, 50ml, 100ml, 500ml and 5L of water respectively, and add 5 compressed dibromohydantoin effervescent tablets to each beaker. After standing for 30 minutes, the dibromohydantoin effervescent tablets in 5L of water are completely dissolved, and insoluble dibromohydantoin is deposited at the bottom of the other beakers.

[0097] Comparative Example 4

[0098] formula:

[0099] 30 parts of dibromohydantoin, 20 parts of solubilizing factor resorcinol, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalene sulfonate, 1 part of magnesium stearate, 2 parts of polyethylene glycol (PEG 8000), 3.5 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate.

[0100] Production process:

[0101] (1) 30 parts of dibromohydantoin, 20 parts of resorcinol, 18 parts of anhydrous citric acid, 15 parts of sodium bicarbonate, 5 parts of sodium carboxymethyl cellulose, 0.5 parts of sodium diisobutylnaphthalenesulfonate, 3.5 parts of anhydrous sodium sulfate, and 5 parts of sodium tripolyphosphate were placed in a blender and mixed continuously for 30 minutes.

[0102] (2) The mixed powder is placed in a granulator to obtain granules with a particle size of 20 mesh.

[0103] (3) Add 1 part of magnesium stearate and 2 parts of PEG 8000 to the granules, continue to mix them in a blender for 30 minutes, and then prepare tablets.

[0104] (4) The tablet press pressure is adjusted to 40N, and the dibromohydantoin effervescent tablets are obtained by tableting; the surface of the obtained dibromohydantoin effervescent tablets is smooth and has no defects, and the production process equipment operates well and the equipment can operate continuously.

[0105] During the tableting process, samples were collected every 5 minutes, with 10 tablets sampled at a time, for a total of 5 samplings. The average effervescent times of the five samples at 20°C water were 5'50", 5'20", 5'35", 6'08", and 6'01", respectively. The dibromohydantoin effervescent tablets in all five samples completely dissolved within 30 minutes, but remained incomplete when the water volume was less than 1 L per tablet.

[0106] Take 5 portions of 100ml water and adjust the temperature to 5℃, 10℃, 15℃, 20℃ and 25℃ respectively. Put 5 pressed tablets into each portion and let it stand for 30 minutes. The dissolution effect is as shown in the figure. Figure 6 As shown, some dibromohydantoin was deposited at the bottom of the beaker and could not be completely dissolved.

[0107] Take 5 beakers at the same temperature (20℃), add 20ml, 50ml, 100ml, 500ml and 5L of water respectively, add 5 compressed dibromohydantoin effervescent tablets to each beaker, and place them for 30 minutes. The dissolution effect is shown in the figure below. Figure 7 As shown, the dibromohydantoin effervescent tablets placed in 5L of water were completely dissolved, while insoluble dibromohydantoin was deposited at the bottom of the other beakers.

[0108] Test Case

[0109] Take the dibromohydantoin effervescent tablets obtained in Comparative Example 1 and prepare a dibromohydantoin disinfectant with an effective bromine content of 300 ppm. According to the requirements of the "Technical Specifications for Disinfection" (2002 edition), the killing effect of various bacteria required in the specifications was tested by the suspension quantitative method. The experimental results are shown in Table 2:

[0110] Table 2 Sterilization effect of the formula product of comparative example 1

[0111]

[0112] Conclusion: The dibromohydantoin effervescent tablets prepared in Comparative Example 1, when prepared into a dibromohydantoin disinfectant containing 300 ppm of available bromine, showed a logarithmic kill rate of >5 against Escherichia coli, Staphylococcus aureus, and Potassium aeruginosa after 10 minutes of action. They also showed a logarithmic kill rate of >4 against Candida albicans and poliovirus after 10 minutes of action, meeting the requirements of the Technical Specifications for Disinfection. Since resorcinol is a low-efficiency disinfectant and dibromohydantoin is a high-efficiency disinfectant, the bactericidal effect of the two after compounding is primarily due to the dibromohydantoin, while the bactericidal effect of resorcinol is not apparent. Therefore, compared with the bactericidal effect of Example 1, the presence or absence of resorcinol has almost no effect on the bactericidal effect.

[0113] Take the dibromohydantoin effervescent tablets obtained in Comparative Example 4 and prepare a dibromohydantoin disinfectant with an effective bromine content of 300 ppm. According to the requirements of the "Technical Specifications for Disinfection" (2002 edition), the killing effect of various bacteria required in the specifications was tested by the suspension quantitative method. The experimental results are shown in Table 3:

[0114] Table 3 Sterilization effect of the formula product of Comparative Example 4

[0115]

[0116] Conclusion: The dibromohydantoin effervescent tablets prepared in Comparative Example 4, when prepared into a dibromohydantoin disinfectant containing 300 ppm of available bromine, exhibited logarithmic kill rates of >5 against Escherichia coli, Staphylococcus aureus, and Potassium aeruginosa after 10 minutes of exposure. Furthermore, the logarithmic kill rates against Candida albicans and poliovirus after 10 minutes of exposure were >4, meeting the requirements of the Technical Specifications for Disinfection. Compared to the bactericidal effect in Example 1, the presence or absence of GABA had little effect on the bactericidal effect.

Claims

1. A dibromohydantoin effervescent tablet, characterized in that: The invention comprises the following components in parts by weight: 30-40 parts of dibromohydantoin, 8-20 parts of solubilizing factors, 38-45 parts of disintegrants, 0.2-1 parts of dispersants, 0.5-5 parts of release agents, 0.1-8 parts of lubricants and 1-5 parts of stabilizers, wherein the solubilizing factors comprise amino group-containing compounds and resorcinol; and the amino group-containing compounds comprise lysine, aminobutyric acid or glucosamine.

2. The dibromohydantoin effervescent tablet according to claim 1, wherein The disintegrant comprises one or more of anhydrous citric acid, sodium bicarbonate, silica gel, sodium carboxymethyl cellulose, polyvinyl alcohol or carbomer U20.

3. The dibromohydantoin effervescent tablet according to claim 1, wherein The dispersant includes one or more of sodium diisobutylnaphthalene sulfonate, dodecyldimethylbenzyl ammonium chloride or dodecyltrimethylammonium chloride.

4. The dibromohydantoin effervescent tablet according to claim 1, wherein The release agent includes one or more of magnesium stearate, paraffin and magnesium silicate.

5. The dibromohydantoin effervescent tablet according to claim 1, wherein The lubricant includes polyethylene glycol; the stabilizer includes sodium tripolyphosphate.

6. The dibromohydantoin effervescent tablet according to claim 1, wherein The dibromohydantoin effervescent tablet further comprises 0.5-4.7 parts of a filler, and the filler comprises anhydrous sodium sulfate.

7. A method for preparing the dibromohydantoin effervescent tablet according to any one of claims 1 to 6, characterized in that: The following steps are involved: Dibromohydantoin, solubility factor, disintegrant, dispersant and stabilizer are mixed and granulated, and a release agent and lubricant are added, mixed and tableted to obtain dibromohydantoin effervescent tablets.

8. The method according to claim 7, characterized in that The particle size range of the particles obtained by the granulation is 20-50 mesh.

9. Use of the dibromohydantoin effervescent tablet according to any one of claims 1 to 6 in sterilization.

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