A kind of water-soluble synergistic composition containing amoxicillin and its application

A technology of amoxicillin and water solubility, which is applied in the field of water-soluble synergistic compositions, can solve the problems of amoxicillin water solubility, inconvenience of clinical medication, discount of drug effect, etc., achieve effective blood drug concentration maintenance time is short, Long maintenance time of blood drug concentration, increase the effect of dispersion and dissolution

Active Publication Date: 2019-06-21
FUJIAN AONONG BIOLOGICAL TECH GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because amoxicillin is easy to decompose in aqueous solution, it must be used up in a short time when administered with drinking water, otherwise the efficacy of the drug will be greatly reduced, which brings inconvenience to clinical medication and increases the cost of medication
[0006] 2. Amoxicillin absorbs quickly after oral administration, has low protein binding rate, short half-life, and will soon be metabolized from the body. In order to maintain the drug concentration and prolong the action time, the administration cycle must be shortened and the administration frequency increased.
Although the technical solution provided by the above-mentioned patent can effectively solve the problem of amoxicillin drug resistance, it does not solve the problems of poor water solubility, unstable aqueous solution and fast metabolism of amoxicillin
At the same time, potassium clavulanate has strong hygroscopicity, which puts forward higher requirements for the production environment and increases the production cost

Method used

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  • A kind of water-soluble synergistic composition containing amoxicillin and its application
  • A kind of water-soluble synergistic composition containing amoxicillin and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The water-soluble synergistic composition containing amoxicillin of the present embodiment comprises by mass parts:

[0032] Amoxicillin 10 parts,

[0033] 5 parts of sulbactam sodium,

[0034] Probenecid sodium 3.5 parts,

[0035] 10 parts of EDTA-2Na,

[0036] PVP-K30 2.5 copies,

[0037] PEG-6000 5 parts,

[0038] 25 copies of SDS,

[0039] Lactose 39 parts.

[0040] The above-mentioned components are pulverized into superfine powder with a particle size of 1000 mesh (that is, a particle size of 13 μm) by an ultrafine pulverizer, and then mixed uniformly with a three-dimensional mixer to obtain a soluble powder that can be directly used in veterinary clinics.

[0041] Get above-mentioned powder and carry out aqueous solution stability test:

[0042]The above-mentioned powder and conventional amoxicillin soluble powder are respectively made into a solution containing amoxicillin concentration of 100ml:10mg with drinking water, left to stand, and the amoxicillin...

Embodiment 2

[0046] The water-soluble synergistic composition containing amoxicillin of the present embodiment comprises by mass parts:

[0047] Amoxicillin 15 parts,

[0048] 7.5 parts of sulbactam sodium,

[0049] Probenecid sodium 5 parts,

[0050] 10 parts of EDTA-2Na,

[0051] PVP-K30 3.5 copies,

[0052] PEG-6000 8 parts,

[0053] 20 copies of SDS,

[0054] Lactose 31 parts.

[0055] The above-mentioned components are pulverized into superfine powders with a particle size of 1000 mesh (that is, a particle size of 13 μm) by an ultrafine pulverizer, mixed evenly with a trough mixer, and 50% ethanol solution of 1 / 10 of the total amount of components is added, and stirred to prepare The soft material is made into granules with a granulator, and dried in an oven at 45°C to make granules that can be used in veterinary clinics.

[0056] Get above-mentioned granule and carry out animal metabolism test.

[0057] Select 10 healthy pigs (about 30kg in body weight), weigh and record, and...

Embodiment 3

[0061] The water-soluble synergistic composition containing amoxicillin of the present embodiment comprises by mass parts:

[0062] Amoxicillin 20 parts,

[0063] 10 parts of sulbactam sodium,

[0064] Probenecid sodium 8 parts,

[0065] 10 parts of EDTA-2Na,

[0066] 5 copies of PVP-K30,

[0067] PEG-6000 10 parts,

[0068] 15 copies of SDS,

[0069] Lactose 22 parts.

[0070] The above-mentioned components are pulverized into superfine powder with a particle size of 2000 mesh (ie, particle size of 6.5 μm) by an ultrafine pulverizer, and then mixed uniformly with a three-dimensional mixer to obtain a soluble powder that can be directly used in veterinary clinics.

[0071] Get above powder and carry out clinical test.

[0072] The healthy weaned piglets that had just been grouped were randomly divided into three groups, one group was used as a blank group, one group was used as a control group, and one group was used as a test group, and the three groups were raised wit...

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Abstract

The invention discloses a water-soluble synergistic composition containing amoxicillin and application thereof. The water-soluble synergistic composition is prepared from the following ingredients in parts by mass: 10 to 30 parts of amoxicillin, 1 to 30 parts of sulbactam sodium, 1 to 11 parts of probenecid sodium, 1 to 15 parts of EDTA-2Na, 1 to 10 parts of PVP K30, 1 to 10 parts of PEG-6000, 1 to 30 parts of SDS and 1 to 40 parts of lactose. The composition is crashed into super micro-powder with the grain diameter being 1000 to 2000 meshes (1.3 to 6.5mum) by an ultramicro pulverization technique; then, the super micro-powder is made into powder, granules or other clinically acceptable dosage forms according to requirements for preventing and treating respiratory tract and digestive tract diseases of animals such as pigs and children. The composition has good water solubility and can realize administration in a water drinking mode. The water-soluble synergistic composition has the advantage that the clinical use effect of the amoxicillin is improved through three paths of improving the water solution stability, prolonging the plasma concentration maintaining time and enhancing the resistance on beta-lactamase.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, and in particular relates to a water-soluble synergistic composition containing amoxicillin and an application thereof. Background technique [0002] Since the advent of penicillin drugs in 1941, penicillin drugs have been irreplaceable by other drugs such as high efficiency, low toxicity, strong selectivity, broad antibacterial spectrum, and good distribution in the body, whether in human clinical or animal clinical, All of them have been widely used in the world and created huge social benefits. [0003] Amoxicillin is the most commonly used semi-synthetic penicillin broad-spectrum β-lactam antibiotics. The mechanism of action is that the β-lactam ring in the drug molecule binds to the transpeptidase in the bacteria to inactivate it and cut off the bacteria. The only way to rely on transpeptidase to synthesize glycopolypeptides to build cell walls makes bacterial cells quickly becom...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/43A61K9/00A61K47/18A61K47/32A61K47/10A61K47/20A61K47/26A61P31/04A61P11/00A61P1/00A61P13/00A61P15/00A61P17/00
CPCA61K9/0095A61K31/43A61K47/10A61K47/18A61K47/20A61K47/26A61K47/32A61K2300/00
Inventor 王庆福戴多亮周盛昌肖丽萍姜文施建成黄静梁世仁吴有林
Owner FUJIAN AONONG BIOLOGICAL TECH GRP CO LTD
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