Preparation process of water-soluble dimetridazole
By adding water-soluble carriers and spray granulation to the traditional dimenizole preparation process, the problems of low solubility and poor stability of dimenizole drugs are solved, and the effect of improving drug solubility and avoiding agglomeration is achieved.
Patent Information
- Application Number
- CN202411920578.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-12-25
- Publication Date
- 2025-03-25
AI Technical Summary
Traditional demenizole drugs have low solubility, and after mixing with feed, they are prone to problems such as difficulty in dissolution, prone to clumping and poor stability.
A water-soluble dimenizole preparation process is adopted to make water-soluble dimenizole by mixing dimenizole with nicotinamide and a water-soluble carrier (such as polyethylene glycol, polyvinylpyrrolidone, etc.), and by spray granulation.
It improves the solubility and dissolution speed of the drug, avoids the problems of agglomeration and poor stability in the feed mix state, and improves the taste of the drug and the appetite of livestock.
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Abstract
Description
Technical Field
[0001] The invention belongs to the technical field of environmental protection, in particular to a preparation process of water-soluble minidazole. Background Art
[0002] Dimetridazole, also known as dimetridazole, is an organic substance. In an anaerobic environment, dimetridazole can spontaneously reduce the complex bound to DNA, inhibit the replication of anaerobic bacterial DNA, cause rapid cell death, and play an anti-anaerobic role. It has a significant inhibitory effect on a variety of anaerobic bacteria (such as Escherichia coli, necrotic bacteria, Clostridium, Staphylococcus, Vibrio, etc.), and is also effective against spirochetes between protozoa and bacteria. It is an effective drug for the treatment of swine dysentery. Dimetridazole can inhibit the redox reaction of amoeba, break the nitrogen chain, and thus kill the protozoa. It has obvious effects on Trichomonas, Trichomonas, amoeba, flagellate, and Eperythrozoon.
[0003] However, the solubility of traditional dimetridazole drugs is low. After mixing with feed, the drug is prone to difficulty in dissolution, easy to agglomerate, and poor stability. Summary of the invention
[0004] The purpose of the present invention is to provide a process for preparing water-soluble minidazole to solve the deficiencies in the prior art.
[0005] The technical solution adopted by the present invention is as follows: A preparation process of water-soluble dimetridazole comprises the following raw material components and the mass fractions of each component: 18-22 parts of nicotinamide, 18-22 parts of dimetridazole, 55-65 parts of a water-soluble carrier, 8-12 parts of deionized water and 6-10 parts of ethanol.
[0006] Preferably, the water-soluble carrier is selected from one or more of polyethylene glycol (PEG), polyvinyl pyrrolidone (PVP), poloxamer, mannitol, and xylitol.
[0007] Preferably, a process for preparing water-soluble dimethylnidazole comprises the following steps: (1) adding dimetridazole to ethanol, mixing, adding to a homogenizer, and mixing and homogenizing to obtain a dimetridazole ethanol solution; (2) Add nicotinamide and a water-soluble carrier to deionized water, seal and stir for 31-35 minutes, heat the solution to 40-48°C, and keep warm for 2.2-2.5 hours to obtain a mixed solution for use; (3) putting the dimethylnitropropene ethanol solution prepared in step (1) and the mixed solution prepared in step (2) into a disperser and dispersing for 55-60 minutes to obtain a prepared solution; (4) The prepared liquid is granulated by a spray granulation method, and the mother liquid particles are crushed and passed through a 45-65 mesh sieve to obtain the water-soluble dimetridazole.
[0008] Preferably, the homogenization pressure in step (1) is 32-38 MPa and the homogenization time is 6-8 min.
[0009] Preferably, in step (4), the air inlet temperature is 155-165°C, the air outlet temperature is 75-85°C, and the spray air flow rate is 1.42-1.45m 3 / h, and the feed rate is 9-10g / min.
[0010] Beneficial effects of the present invention: The water-soluble carrier used in the present invention can improve the solubility of the drug by forming hydrogen bonds and other interactions with drug molecules, reduce the interfacial tension between the drug and water, thereby improving the dissolution rate and solubility of the drug, and can provide a certain sweetness or sourness, improve the taste of the drug, and increase the appetite of livestock. At the same time, it also helps to improve the solubility of the drug, and can effectively avoid agglomeration and poor stability in the feed mixing state. DETAILED DESCRIPTION Example 1
[0011] A preparation process of water-soluble dimetridazole, according to the raw material composition and the mass fraction of each component: 18 parts of nicotinamide, 18 parts of dimetridazole, 55 parts of a water-soluble carrier, 8 parts of deionized water, and 6 parts of ethanol; The water-soluble carrier is selected from one or more of polyethylene glycol (PEG), polyvinyl pyrrolidone (PVP), poloxamer, mannitol, and xylitol; A process for preparing water-soluble dimetridazole comprises the following steps: (1) adding dimetridazole to ethanol, mixing, adding to a homogenizer, and mixing and homogenizing to obtain a dimetridazole ethanol solution; (2) Add nicotinamide and a water-soluble carrier to deionized water, seal and stir for 31 minutes, heat the solution to 40°C, and keep it warm for 2.2 hours to obtain a mixed solution for use; (3) putting the dimethylnitropropene ethanol solution prepared in step (1) and the mixed solution prepared in step (2) into a disperser and dispersing for 55 minutes to obtain a prepared solution; (4) The obtained mother liquid is granulated by a spray granulation method. After the mother liquid particles are crushed, they are passed through a 45-mesh sieve to obtain the water-soluble dimetridazole.
[0012] The homogenization pressure in step (1) is 32 MPa and the homogenization time is 6 min.
[0013] In step (4), the inlet air temperature is 155°C, the outlet air temperature is 75°C, and the spray air flow rate is 1.42m 3 / h, and the feed rate is 9g / min. Example 2
[0014] A preparation process of water-soluble dimetridazole, according to the raw material composition and the mass fraction of each component: nicotinamide 20, dimetridazole 20, water-soluble carrier 60, deionized water 10, ethanol 8: The water-soluble carrier is selected from polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP); A process for preparing water-soluble dimetridazole comprises the following steps: (1) adding dimetridazole to ethanol, mixing, adding to a homogenizer, and mixing and homogenizing to obtain a dimetridazole ethanol solution; (2) Add nicotinamide and a water-soluble carrier to deionized water, seal and stir for 33 minutes, heat the solution to 45°C, and keep it warm for 2.3 hours to obtain a mixed solution for use; (3) putting the dimethylnitropropene ethanol solution prepared in step (1) and the mixed solution prepared in step (2) into a disperser and dispersing for 58 minutes to obtain a prepared solution; (4) granulating the obtained mother liquid by spray granulation, crushing the mother liquid particles, and passing through a 55-mesh sieve to obtain the water-soluble dimetridazole. The homogenization pressure in step (1) is 36 MPa and the homogenization time is 9 minutes.
[0015] In step (4), the inlet air temperature is 160°C, the outlet air temperature is 80°C, and the spray air flow rate is 1.45m 3 / h, the feed rate is 10g / min. Example 3
[0016] A preparation process of water-soluble dimetridazole, according to the raw material composition and the mass fraction of each component: nicotinamide 18-22, dimetridazole 18-22, water-soluble carrier 55-65, deionized water 8-12, ethanol 6-10: (1) Weighing the raw materials: weigh and set aside according to the raw material composition and the mass fraction of each component: calcium-based material 85, oxidant 15, catalyst 10, fluorite 20; The water-soluble carrier is selected from one or more of polyethylene glycol (PEG), polyvinyl pyrrolidone (PVP), poloxamer, mannitol, and xylitol; A process for preparing water-soluble dimetridazole comprises the following steps: (1) adding dimetridazole to ethanol, mixing, adding to a homogenizer, and mixing and homogenizing to obtain a dimetridazole ethanol solution; (2) Add nicotinamide and a water-soluble carrier to deionized water, seal and stir for 35 minutes, heat the solution to 48°C, and keep it warm for 2.5 hours to obtain a mixed solution for use; (3) putting the dimethylnitropropene ethanol solution prepared in step (1) and the mixed solution prepared in step (2) into a disperser and dispersing for 60 minutes to obtain a prepared solution; (4) The obtained mother liquid is granulated by a spray granulation method. After the mother liquid particles are crushed, they are passed through a 65-mesh sieve to obtain the water-soluble dimetridazole.
[0017] The homogenization pressure in step (1) is 38 MPa and the homogenization time is 8 minutes.
[0018] In step (4), the inlet air temperature is 165°C, the outlet air temperature is 85°C, the spray air flow rate is 1.45m3 / h, and the feed rate is 10g / min.
[0019] Comparative Example 1 Compared with Example 1, this comparative example only uses commercially available water solvent, and other method steps are the same.
[0020] Comparative Example 2 Compared with Example 2, this comparative example only selects polyethylene glycol (PEG) or polyvinyl pyrrolidone (PVP) as the water solvent, and other method steps are the same.
[0021] Comparative Example 3 Compared with Example 3, this comparative example performs simple dispersion in step (3), and other method steps are the same.
[0022] Control group Commercially available dimetridazole was used.
[0023] Sampling was performed to determine the solubility of the dimetridazole premix. Accurately weigh 100 g of aquaculture water, and the dimetridazole described in Examples 1 to 3 and Comparative Examples 1 to 3 was added. The mixture was stirred thoroughly until the drug could no longer be dissolved. The maximum solubility of the dimetridazole premix was recorded. Table 1
[0024] It can be seen from Table 1 that the maximum solubility of the embodiments is greater than the maximum solubility of the comparative example, so it can be concluded that the water-soluble dimetridazole preparation process provided by the present invention can help improve the solubility of the drug and effectively avoid agglomeration and poor stability in the feed mixing state.
[0025] The above description is only a preferred embodiment of the present invention, but the present invention does not limit the scope of implementation. Any changes made in accordance with the concept of the present invention, or modifications to equivalent embodiments with equivalent changes, which still do not exceed the spirit covered by the description and embodiments, should be within the protection scope of the present invention.
Claims
1. A process for preparing water-soluble dimethylnidazole, characterized in that: The raw material composition and the mass proportion of each component are: nicotinamide 18-22, dinitropropene 18-22, water-soluble carrier 55-65, deionized water 8-12, ethanol 6-10.
2. A process for preparing water-soluble dimethylnidazole according to claim 1, characterized in that: The water-soluble carrier is selected from one or more of polyethylene glycol (PEG), polyvinyl pyrrolidone (PVP), poloxamer, mannitol, and xylitol.
3. A process for preparing water-soluble dimethylnidazole according to claim 1, characterized in that: The steps include: (1) adding dimetridazole to ethanol, mixing, adding to a homogenizer, and mixing and homogenizing to obtain a dimetridazole ethanol solution; (2) Add nicotinamide and a water-soluble carrier to deionized water, seal and stir for 31-35 minutes, heat the solution to 40-48°C, and keep warm for 2.2-2.5 hours to obtain a mixed solution for use; (3) putting the dimethylnitropropene ethanol solution prepared in step (1) and the mixed solution prepared in step (2) into a disperser and dispersing for 55-60 minutes to obtain a prepared solution; (4) The obtained mother liquid is granulated by a spray granulation method. After the mother liquid particles are crushed, they are passed through a 45-65 mesh sieve to obtain the water-soluble dimetridazole.
4. A process for preparing water-soluble dimethylnidazole according to claim 3, characterized in that: The homogenization pressure in step (1) is 32-38 MPa and the homogenization time is 6-8 min.
5. A process for preparing water-soluble dimethylnidazole according to claim 3, characterized in that: In step (4), the air inlet temperature is 155-165°C, the air outlet temperature is 75-85°C, and the spray air flow rate is 1.42-1.45m 3 / h, and the feed rate is 9-10g / min.