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Cefteram pivoxil crystal and preparation method thereof and composition tablets containing crystal

A technology for cefdipram pivoxil and a composition, which is applied in the field of pharmaceutical preparations, and can solve the problems of easy decomposition, affecting drug dissolution effect and bioavailability, insoluble in water, etc.

Active Publication Date: 2012-02-15
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cefditoren axetil is insoluble in water and easily decomposes in case of acid, which greatly affects the dissolution effect and bioavailability of the drug, which greatly limits the clinical use

Method used

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  • Cefteram pivoxil crystal and preparation method thereof and composition tablets containing crystal
  • Cefteram pivoxil crystal and preparation method thereof and composition tablets containing crystal
  • Cefteram pivoxil crystal and preparation method thereof and composition tablets containing crystal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102][embodiment 1] the preparation of cefditoren neopentyl ester crystal

[0103] 1) cefditoren neopentyl powder is dissolved in an acetone solvent to form a cefditoren neopentyl solution as a dispersed phase;

[0104] 2) dissolving polyvinylpyrrolidone in water to form an aqueous solution of polyvinylpyrrolidone as a dispersion medium;

[0105] 3) Under the ultrasonic field, use a micro-injector to add the dispersed phase solution into the dispersion medium, continue ultrasonication, and centrifuge to separate the cefditoren neopentyl superpowder, remove the supernatant and add water to wash and centrifuge to remove the cephalosporin The polyvinylpyrrolidone adsorbed on the surface of telen neopentyl ester is vacuum-dried to obtain cefditoren neopentyl ester crystals.

[0106] The particle diameter of the obtained cefditoren neopentyl crystal is 1 μm, and it is measured by powder X-ray diffractometry, and the X-ray powder diffraction spectrum represented by 2θ ± 0.2 ° diff...

Embodiment 2

[0107] [embodiment 2] the preparation of cefditoren neopentyl ester crystal

[0108] 1) cefditoren neopentyl powder is dissolved in an acetone solvent to form a cefditoren neopentyl solution as a dispersed phase;

[0109] 2) Dissolve polyvinylpyrrolidone in water to make 0.05mol L -1 Polyvinylpyrrolidone aqueous solution is used as dispersion medium;

[0110] 3) Under an ultrasonic field with a power of 0.1KW, add the dispersed phase solution into the dispersion medium with a micro-injector, continue ultrasonication for 1 minute, and -1 Cefditoren neopentyl superpowder was separated by high-speed centrifugation under certain conditions, the supernatant was removed and water was added to wash and centrifuge twice to remove the polyvinylpyrrolidone adsorbed on the surface of cefditoren neopentyl, and vacuum-dried for 8 hours to obtain cephalosporin Tren pivalate crystals.

[0111] The obtained cefditoren neopentyl crystal has a particle size of 5 μm, and the X-ray powder diff...

Embodiment 3

[0112] [embodiment 3] the preparation of cefditoren neopentyl ester crystal

[0113] 1) cefditoren neopentyl powder is dissolved in an acetone solvent to form a cefditoren neopentyl solution as a dispersed phase;

[0114] 2) Dissolve polyvinylpyrrolidone in water to make 0.3mol L -1 Polyvinylpyrrolidone aqueous solution is used as dispersion medium;

[0115] 3) Under an ultrasonic field with a power of 0.3KW, add the dispersed phase solution into the dispersion medium with a micro-injector, continue ultrasonication for 3 minutes, and -1 Cefditoren neopentyl superpowder was separated by high-speed centrifugation under certain conditions, and the supernatant was removed and washed with water and centrifuged for 4 times to remove the polyvinylpyrrolidone adsorbed on the surface of cefditoren neopentyl, and vacuum-dried for 12 hours to obtain cephalosporin Tren pivalate crystals.

[0116] The obtained cefditoren neopentyl crystals had a particle size of 3 μm, and the X-ray powd...

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Abstract

The invention relates to a cefteram pivoxil crystal and a preparation method thereof and composition tablets containing the crystal. The grain diameter of the crystal is 1 to 5 microns; and the composition tablets of the crystal are obtained by coating tablets prepared from 30 to 120 grams of cefteram pivoxil crystal, 15 to 65 grams of starch, 5 to 20 grams of hydroxypropyl cellulose, 10 to 45 grams of sodium starch glycolate, 0.1 to 2 grams of magnesium stearate and a proper amount of pure water. The crystal with the grain diameter of 1 to 5 microns is prepared by using a method of compounding ultrasonic and micro emulsion; the cefteram pivoxil can be quickly released from a medicament, so that the dissolution rate of the medicament is improved and the bioavailability is improved; by using the method, separation and purification of the cefteram pivoxil and a surfactant can be realized; and because the composition contains the crystal, the dissolution rate of the medicament is improved and the bioavailability is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a cefditoren neopentyl crystal, a preparation method thereof and a composition tablet containing the crystal. Background technique [0002] Cefditoren Neopentyl Proxil, English name: Cefteram Pivoxil, synonym: Cefditoren Proxetil, trade name: Tomiron (Tomiron), chemical name (+)-(6R, 7R)-7-[(z)- 2-(2-Amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-[(5-methyl-2H-tetrazol-2-yl)-methyl]-8-oxo -5-Thia-1-azabicyclo[4.2.2]oct-2-ene-2-carboxylic acid pivaloyloxymethyl ester, molecular formula C 22 h 27 N 9 o 7 S 2 , molecular weight 593.63. This product is a solid insoluble in water, melting point: about 110°C, good photothermal stability in solid state, unstable in solution, and decomposes rapidly when encountering acid and alkali. [0003] This product is the third-generation oral cephalosporin, which is the prodrug of cefditoren modified by ester group struct...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/46C07D501/12A61K31/546A61K9/34A61P31/04
Inventor 王全园张永安王传凯
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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