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CN-122005484-A - Preparation method of amoxicillin and clavulanate potassium tablet

CN122005484ACN 122005484 ACN122005484 ACN 122005484ACN-122005484-A

Abstract

The application provides a preparation method of amoxicillin and clavulanate potassium tablets, belonging to the technical field of pharmaceutical chemistry. The application takes amoxicillin and clavulanate potassium-microcrystalline cellulose as main medicines, the mass ratio of the amoxicillin to the clavulanate potassium-microcrystalline cellulose is 1:1, the mass ratio of the amoxicillin to the clavulanate potassium is 4:1, and microcrystalline cellulose, magnesium stearate, sodium methylol starch, colloidal silicon dioxide, dry yeast and erythrosin aluminum lake as auxiliary materials.

Inventors

  • TU JIAYING
  • Qiu Shanchan
  • YU JIPING
  • Qian Bintao
  • ZHANG MINGYAN
  • DING DONGDONG
  • YANG MEIYU

Assignees

  • 浙江昂利康动保科技有限公司

Dates

Publication Date
20260512
Application Date
20260204

Claims (10)

  1. 1. The preparation method of the amoxicillin and clavulanate potassium tablet is characterized by taking amoxicillin and clavulanate potassium-microcrystalline cellulose as main medicines, wherein the mass ratio of the amoxicillin to the clavulanate potassium to the microcrystalline cellulose is 1:1, the mass ratio of the amoxicillin to the clavulanate potassium is 4:1, and microcrystalline cellulose, magnesium stearate, sodium hydroxymethylstarch, colloidal silicon dioxide, dry yeast and erythrosin aluminum lake are taken as auxiliary materials, and the preparation method comprises the following steps: Step one, dry mixing and granulating main medicine, namely placing amoxicillin, potassium clavulanate-microcrystalline cellulose, microcrystalline cellulose and magnesium stearate with prescription amounts into a single-upright lifting hopper mixer, fully and uniformly mixing, and delivering into a hopper of a dry granulator for granulating to obtain main medicine granules; Step two, granulating auxiliary materials by a wet method, namely putting the sodium carboxymethyl starch, the magnesium stearate and the microcrystalline cellulose into a groove type mixer for dry mixing, adding purified water while stirring, continuously mixing to form a soft material, sending the soft material into a swing type granulator for sieving and granulating, drying the obtained wet granules until the water content is 2.0-3.0%, and then sieving the wet granules in the swing type granulator again to obtain auxiliary material granules; And thirdly, mixing and tabletting, namely putting main medicine particles, auxiliary material particles, colloidal silicon dioxide, dry yeast and a colorant into a single-column lifting hopper mixer for full mixing, calculating tablet weight according to the feeding amount, and adopting a circular die to adjust the pressure of a tablet press for tabletting to obtain amoxicillin potassium clavulanate tablets.
  2. 2. The preparation method of the amoxicillin and clavulanate potassium tablet according to claim 1, wherein the mass ratio of the amoxicillin to the amoxicillin and clavulanate potassium tablet is 20-25%.
  3. 3. The preparation method of the amoxicillin and clavulanate potassium tablet according to claim 1, wherein the mass ratio of the magnesium stearate in the amoxicillin and clavulanate potassium tablet is 1.2-1.5%.
  4. 4. The method for preparing amoxicillin and clavulanate potassium tablet according to claim 1, wherein in the second step, the drying is performed by using circulating hot air.
  5. 5. The preparation method of the amoxicillin and clavulanate potassium tablet according to claim 1, wherein the mass ratio of the sodium hydroxymethylstarch to the amoxicillin and clavulanate potassium tablet is 20-25%.
  6. 6. The preparation method of the amoxicillin and clavulanate potassium tablet according to claim 1, wherein in the third step, the temperature of the mixed tabletting is 18-26 ℃ and the relative humidity is 45-65%.
  7. 7. The preparation method of the amoxicillin and clavulanate potassium tablet according to claim 1, wherein the mass ratio of the dry yeast in the amoxicillin and clavulanate potassium tablet is 1.0-1.5%.
  8. 8. The method for preparing amoxicillin and clavulanate potassium tablets according to claim 1, wherein the particle size of the dry yeast is 30-50 meshes.
  9. 9. The method of claim 1, wherein the round die comprises an upper punch assembly, a half-scored concave cutting edge, a middle die and a lower punch assembly.
  10. 10. The method for preparing amoxicillin and clavulanate potassium tablet according to claim 1, wherein the colorant is erythrosin aluminum lake.

Description

Preparation method of amoxicillin and clavulanate potassium tablet Technical Field The application relates to a preparation method of amoxicillin and clavulanate potassium tablets, belonging to the technical field of pharmaceutical chemistry. Background In recent years, the large-scale and intensive development of livestock and poultry breeding industry is accelerated, and infectious diseases such as respiratory tract, digestive tract and the like caused by sensitive bacteria (such as escherichia coli and Pasteurella) frequently occur, so that the growth retardation of livestock and poultry and the reduction of feed conversion rate are caused, and drug-resistant bacteria can be transmitted through animal products, thereby threatening public health safety. Therefore, a safe and efficient compound antibacterial drug is needed. The amoxicillin and clavulanate potassium tablet is widely applied to veterinary clinics as a compound antibiotic preparation, and has the action mechanism that amoxicillin inhibits bacterial cell wall synthesis to play a bactericidal role, and clavulanate potassium protects amoxicillin from being decomposed by beta-lactamase generated by bacteria, and the amoxicillin and the clavulanate potassium tablet cooperatively expand an antibacterial spectrum and enhance antibacterial activity (Chinese veterinary journal, 2025,61 (6): 67-74). However, the existing preparation process has three core pain points: Firstly, the stability of the main medicine is poor. The traditional wet granulation leads to moisture absorption and degradation of clavulanic acid components, is easy to cause loss of active ingredients, has harsh production conditions and high cost. Secondly, impurity control is difficult. The physicochemical properties of the two active ingredients are difficult to be considered in single mixed granulation (Xu Yidan. Bioequivalence study of amoxicillin and clavulanate potassium tablets in dogs [ D ], 2022.) and the total amount of impurities is easy to exceed standard after long-term storage. Third, the palatability and safety are not enough. When the medicine is directly converted into veterinary medicine, the design aiming at the taste preference of livestock and poultry is lacking, the antifeedant rate of animals is high, the intestinal mucosa is protected without special auxiliary materials, and the gastrointestinal tract irritation reaction is easy to be induced. Disclosure of Invention In view of the above, the application provides a preparation method of amoxicillin and clavulanate potassium tablets, which can give consideration to stability, impurity control and palatability. Specifically, the application is realized by the following scheme: the preparation method of the amoxicillin and clavulanate potassium tablet takes amoxicillin and clavulanate potassium-microcrystalline cellulose (mass ratio 1:1) as main medicines, microcrystalline cellulose, magnesium stearate, sodium carboxymethyl starch, colloidal silicon dioxide, dry yeast and erythrosin aluminum lake as auxiliary materials, and comprises the following steps: Step one, dry mixing and granulating main medicine, namely placing amoxicillin, potassium clavulanate-microcrystalline cellulose, microcrystalline cellulose and magnesium stearate with prescription amounts into a single-upright lifting hopper mixer, fully and uniformly mixing, and delivering into a hopper of a dry granulator for granulating to obtain main medicine granules; Step two, granulating auxiliary materials by a wet method, namely putting the sodium carboxymethyl starch, the magnesium stearate and the microcrystalline cellulose into a groove type mixer for dry mixing, adding purified water while stirring, continuously mixing to form a soft material, sending the soft material into a swing type granulator for sieving and granulating, drying the obtained wet granules until the water content is 2.0-3.0%, and then sieving the wet granules in the swing type granulator again to obtain auxiliary material granules; And thirdly, mixing and tabletting, namely putting main medicine particles, auxiliary material particles, colloidal silicon dioxide, dry yeast and a colorant into a single-column lifting hopper mixer for full mixing, calculating tablet weight according to the feeding amount, and adopting a circular die to adjust the pressure of a tablet press for tabletting to obtain amoxicillin potassium clavulanate tablets. The scheme adopts a composite flow of 'main medicine dry granulation, auxiliary material wet granulation and mixed tabletting', realizes the preparation of amoxicillin and clavulanate potassium tablets, effectively completes the synergy between the main medicine and the auxiliary material, ensures the improvement of the fluidity and the stability of the granules, and ensures the even content and the rapid disintegration of the tablets. Meanwhile, the clavulanic acid and the microcrystalline cellulose are used as one of main medicine components, and