Noncrystalline antibacterial composition containing cefditoren pivoxil

A kind of technology of cefditoren and composition, applied in the field of amorphous antibacterial composition, can solve problems such as inability to be administered to patients

Inactive Publication Date: 2006-11-15
MEIJI SEIKA KAISHA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since casein is a milk-derived protein, this formulation cannot be administered to patients with dairy allergies

Method used

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  • Noncrystalline antibacterial composition containing cefditoren pivoxil
  • Noncrystalline antibacterial composition containing cefditoren pivoxil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Examples 1, 6, 7 and 8: Solid Dispersions Containing Surfactants

[0044] The solid dispersion composition was obtained by dissolving crystalline cefditoren pivoxil and surfactant in a mixture of dichloromethane:methanol (1:1) at the preparation ratio shown in Table 1, and then removing the solvent by distillation . The amorphous form of cefditoren pivoxil in these compositions was confirmed by powder X-ray diffraction analysis (data omitted). Crystalline cefditoren pivoxil was prepared according to Japanese Patent No.3403206.

[0045] Surfactant

Preparation ratio

(drug: surfactant)

Example 1

fatty acid sucrose ester

100mg Potency: 5.0mg

Example 6

fatty acid sucrose ester

100mg Potency: 0.01mg

Example 7

fatty acid sucrose ester

100mg Potency: 0.1mg

Example 8

fatty acid sucrose ester

100mg Potency: 200mg

[0046] Fatty acid sucrose ester: DK Ester SS, HLB value = 20, Daiichi Kogy...

preparation Embodiment 1

[0062] A powdery formulation was prepared by mixing 130 g of the composition obtained in Example 1 with 260 g of cornstarch.

preparation Embodiment 2

[0064] 1000 capsules were prepared by mixing 130 g of the composition obtained in Example 4, 260 g of spray-dried lactose, 130 g of croscarmellose sodium and 3 g of magnesium stearate, and then filling the mixture into capsules.

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Abstract

According to the present invention, there is provided a solid dispersion composition which can maintain amorphous cefditoren pivoxil in a suspension for a long period of time. The present invention is a solid dispersion composition comprising at least 0.1 mg of a sugar ester fatty acid on the basis of an amount equivalent to 100 mg efficacy of cefditoren pivoxil.

Description

Background of the invention [0001] The present invention relates to an amorphous antibacterial composition comprising cefditoren pivoxil. [0002] The antibacterial compound cefditoren is a cephem compound represented by formula (A). [0003] [0004] Its chemical name is (+)-(6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[(Z )-2-(4-methylthiazolyl-5-yl)vinyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid . In Japanese Patent Publication No.64503 / 1991, the chemical name is 7-[2-methoxyimino-2-(2-aminothiazol-4-yl)acetamido]-3-[2-(4-methyl Thiazolyl-5-yl)vinyl]-3-cephem-4-carboxylic acid (syn-isomer, cis-isomer) is described for this compound. [0005] The pivaloyloxymethyl ester of cefditoren is known as cefditoren pivoxil, in which the carboxylic acid group at the 2-position of the cefditoren compound is esterified with pivaloyloxymethyl in order to improve its oral Absorbability through the digestive tract upon administration (hereina...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K9/00A61K9/10A61K9/14A61K47/26A61K47/32A61K47/38A61P31/04C07D501/24
CPCA61K9/0095A61K9/145A61K31/546A61P31/04A61K9/10
Inventor 近势茂横井由纪子
Owner MEIJI SEIKA KAISHA LTD
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