Amoxicillin soluble powder and preparation method thereof

An amoxicillin and soluble technology, which is applied in the field of amoxicillin soluble powder and its preparation, can solve the problems of difficulty in the preparation of sustained-release preparations, affect drug efficacy, and slow release, and achieve improved physical and chemical stability and long-lasting therapeutic effects , the effect of improving solubility

Active Publication Date: 2018-07-13
四川恒通动保生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] (1) Amoxicillin is metabolized very quickly and has a short half-life, so the drug effect is not long-lasting, and repeated administration is required
[0005] (2) Amoxicillin soluble powder often forms an inhomogeneous turbid liquid when added to water, and may precipitate over time, making it impossible to ensure that animals receive an effective therapeutic dose
[0006] (3) Amoxicillin has extremely poor stability and is prone to degradation. Especially in high temperature, high humidity and other environments, the effective content is greatly reduced, especially its aqueous solution fails faster, so it is often difficult to guarantee the curative effect
[0007] The existing methods to solve the above-mentioned defects include preparing amoxicillin and sustained-release materials into sustained-release preparations to prolong the drug e

Method used

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  • Amoxicillin soluble powder and preparation method thereof
  • Amoxicillin soluble powder and preparation method thereof
  • Amoxicillin soluble powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1 prepares soluble powder with gelatin hydrolyzate of average molecular weight 1500Da-3000Da

[0058]

[0059] Pass amoxicillin and sorbitol through a 80-mesh sieve, mix evenly to obtain a mixed powder; add gelatin hydrolyzate to water to prepare an aqueous solution, then add it to the mixed powder, stir, granulate, dry, granulate, and pack, that is have to.

[0060] 1. Water solubility test and aqueous solution stability test

[0061] Take 1 g of the soluble powder of Comparative Examples 1-6 and Example 1, calculated as amoxicillin, place it in 150 ml of water with a temperature of 25°C ± 2°C, shake it for 2 minutes, observe the solution after standing for 30 minutes, and take a sample for determination content (recorded as 0h content); then place each solution at 40°C for 4h, 12h and 24h, observe and record the solution, and take a sample to measure the content, and calculate the loss rate by comparing with the 0-hour content. The results are shown in th...

Embodiment 2

[0083] Embodiment 2 prepares the gelatin hydrolyzate of average molecular weight 1500Da-3000Da

[0084] Add 1kg type A gelatin to 2kg water, heat to 55°C to dissolve, adjust the pH value of the gelatin aqueous solution to 6.5 with disodium hydrogen phosphate solution, heat to 60°C, add 0.1% w / w trypsin to the gelatin aqueous solution and stir for 2 hours Finally, 0.1% w / w Bacillus licheniformis was added to the solution, and after reacting for 2 hours, the solution was heated to 90° C. to kill enzymes, filtered, concentrated, and dried to obtain gelatin hydrolyzate. Its average molecular weight was determined to be 2488Da.

Embodiment 3

[0085] Embodiment 3 prepares the gelatin hydrolyzate of average molecular weight 1500Da-2000Da

[0086] Add 1kg type B gelatin to 2kg water, heat to 55°C to dissolve, adjust the pH value of the gelatin aqueous solution to 6.5 with disodium hydrogen phosphate solution, heat to 60°C, add 0.1% w / w trypsin to the gelatin aqueous solution and stir for 3 hours Finally, add 0.1% w / w Bacillus licheniformis to the solution, react for 3 hours, add 0.08% w / w protease from Aspergillus niger fermentation to the solution, react for 1.5 hours, heat the solution to 90°C to kill the enzyme , filtered, concentrated, and dried to obtain gelatin hydrolyzate. Its average molecular weight was determined to be 1623Da.

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Abstract

The invention relates to amoxicillin soluble powder and a preparation method thereof. The amoxicillin soluble powder is prepared from amoxicillin, gelatin hydrolysate with the average molecular weightbeing 1,500-3,000Da and a diluent, and preferably from the following components in percentage by weight: 10-30wt% of the amoxicillin, 20-50wt% of the gelatin hydrolysate with the average molecular weight being 1,500-3,000Da and 20-60wt% of sorbitol. The soluble powder can form a homogeneous liquid in water, and the solution is high in stability, more importantly, can provide effective efficacy for a long time and is durable and reliable in curative effect.

Description

technical field [0001] The invention relates to the technical field of veterinary drug preparations, in particular to a soluble amoxicillin powder and a preparation method thereof. Background technique [0002] Amoxicillin, also known as amoxycillin or amoxicillin, is the most commonly used semi-synthetic penicillin broad-spectrum β-lactam antibiotics. It has strong bactericidal effect and strong ability to penetrate cell membranes. Penicillin-sensitive gram-positive and gram-negative bacteria infections, such as Staphylococcus aureus, colibacillosis, pullorum, infectious rhinitis, calf pneumonia, bovine pasteurellosis, mastitis, porcine infectious pleura Pneumonia, fowl typhoid etc. In order to facilitate animal administration, it is usually prepared as a soluble powder, dissolved in water during use, and taken with the help of animals drinking water. [0003] However, amoxicillin soluble powder has the following defects in use: [0004] (1) Amoxicillin is metabolized ve...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/42A61K31/43A61P31/04
CPCA61K9/1658A61K31/43Y02A50/30
Inventor 郭亮刘起军黄恩龙
Owner 四川恒通动保生物科技有限公司
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