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Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate

A technology of potassium clavulanate and amoxicillin, which is applied in the field of medicine, can solve the problems of poor drug dissolution in vitro, difficulty in industrial production, and influence on drug release, so as to improve stability and solubility, stabilize quality, and improve drug safety Effect

Inactive Publication Date: 2013-06-12
四川省惠达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The disadvantage of the above-mentioned double-layer sustained-release preparation or triple-layer sustained-release tablet is that its preparation requires too much equipment and is difficult to industrialized production, and the preparation process of the double-layer sustained-release tablet will cause the tablet hardness to be too large, which will affect drug release. It is difficult to release the drug from the connecting surface of the double-layer sheet
Moreover, because amoxicillin is slightly soluble in water, the in vitro dissolution rate of the drug is poor, resulting in low bioavailability

Method used

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  • Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate
  • Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate
  • Amoxicillin compound and pharmaceutical composition of amoxicillin compound and potassium clavulanate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] [Example 1] Preparation of Amoxicillin crystalline compound

[0048] (1) Add 100g of amoxicillin bulk drug to 1500ml of water at 12°C, adjust the pH value to 2.0 with hydrochloric acid, and obtain an aqueous solution of amoxicillin;

[0049] (2) Add 560ml of n-propanol / tetrahydrofuran mixed solution to the aqueous solution of amoxicillin, wherein the volume ratio of n-propanol to tetrahydrofuran is 1:6.2;

[0050] (3) After adding, the stirring speed is 275r·min -1 11% NH was added dropwise under stirring 3 ·H 2 O adjust the pH value to 5.0, precipitate crystals, control the temperature at 5°C, grow the crystals for 1.5 hours, then filter with suction, wash the filter cake with purified water and acetone in turn, and dry to obtain the crystalline amoxicillin compound.

[0051] The characteristic peaks in the X-ray powder diffraction pattern of the obtained amoxicillin crystalline compound obtained by Cu-Kα ray measurement are 8.0°, 12.1°, 15.4°, 17.0°, 19.8°, 21.6°, ...

preparation Embodiment 1

[0056] [Preparation Example 1] Amoxicillin and Clavulanate Potassium Tablets

[0057] Specification: Amoxicillin / clavulanic acid 875mg / 125mg

[0058] prescription:

[0059]

[0060] Preparation:

[0061] Excipients Microcrystalline cellulose, croscarmellose sodium, and micropowder silica gel were dried at 80°C for 4 hours and passed through an 80-mesh sieve; magnesium stearate was dried at 60°C for 4 hours; passed through a No. 9 sieve; set aside. Take the amoxicillin crystalline compound of Example 1 and amoxicillin-clavulanate potassium 2:1 mixed powder at a ratio of 7:1 by weight, measure the content of the two components and calculate the feeding amount. Add microcrystalline cellulose (internal addition part) and magnesium stearate (internal addition part) according to the prescription ratio, mix well, and dry press on a dry extrusion granulator to form granules under the condition that the relative humidity is not higher than 33%. The granules are mixed evenly with ...

preparation Embodiment 2

[0062] [Preparation Example 2] Amoxicillin and Clavulanate Potassium Tablets

[0063] Specification: Amoxicillin / clavulanic acid 136mg / 34mg

[0064] prescription:

[0065]

[0066] Preparation:

[0067] (a) take the amoxicillin crystalline compound of embodiment 2 (in C 16 h 19 N 3 o 5 S) 136g, potassium clavulanate (in C 8 h 9 NO 5 Total) 34g, microcrystalline cellulose (P112) 32g, croscarmellose sodium (ADS) 2g, micropowder silica gel 2g, magnesium stearate 2g, a total of 205g;

[0068] (b) After amoxicillin is granulated, it is mixed with potassium clavulanate at a mass ratio of 4:1 to form the main ingredient.

[0069] (c) Add and mix the auxiliary materials micropowder silica gel, croscarmellose sodium (ADS) and microcrystalline cellulose in equal amounts, and then add the same amount of main ingredients into the mixer and mix for 36-70 minutes.

[0070] During the whole process, the moisture content of the intermediate mixed powder is controlled to be ≤9.0%,...

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Abstract

The invention relates to an amoxicillin compound and a pharmaceutical composition of the amoxicillin compound and potassium clavulanate. The pharmaceutical composition is an oral sustained-release preparation. The amoxicillin compound is a crystalline compound which is provided with the following structural formula, wherein the characteristic peaks as shown in an X-ray powder diffraction pattern obtained by measuring through Cu-K alpha rays are displayed in 2 theta of 8.0 degrees, 12.1 degrees, 15.4 degrees, 17.0 degrees, 19.8 degrees, 21.6 degrees, 23.0 degrees, 24.3 degrees, 25.7 degrees, 27.4 degrees, 30.7 degrees and 33.5 degrees. The novel crystalline compound is improved in stability and dissolubility. The amoxicillin and clavulanate potassium prepared from the crystalline compound is higher in stability. The amoxicillin and clavulanate potassium oral sustained-release preparation prepared from the crystalline compound can be synchronously released, and is excellent in in-vitro dissolution and higher in bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an amoxicillin compound and a pharmaceutical composition of the compound and potassium clavulanate. Background technique [0002] Amoxicillin / potassium clavulanate, their chemical names are: (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-(-)-2-amino-2-(4 -Hydroxyphenyl)acetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate and (Z)-(2S,5R)-3 Potassium -(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylate. [0003] Amoxicillin / potassium clavulanate compound preparation is composed of amoxicillin and potassium clavulanate. It is a broad-spectrum enzyme-resistant and highly effective first-line anti-infective drug for severe infections commonly seen in clinical practice. Among them, amoxicillin is a broad-spectrum penicillin β-lactam semi-synthetic antibiotic, the mechanism of action is to inhibit the synthesis of bacterial cell walls, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/18A61K31/43A61K31/424A61P31/04
Inventor 闫晓晔
Owner 四川省惠达药业有限公司
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