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Cefteram pivoxil tablet and preparation process thereof

A technology for the preparation of cefditoren and its preparation technology, which is applied in the field of preparation technology of cefditoren neopentyl pivoxil tablets, which can solve the problems of clinical use restrictions and high requirements for production control of liposome solid preparations, so as to improve dissolution behavior and bioavailability The effect that the degree, release effect improves

Active Publication Date: 2014-07-16
ZHEJIANG JUTAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This kind of liposome solid preparation has high encapsulation efficiency, uniform particle size, and long retention time of drugs in the blood circulation, but the production control requirements of liposome solid preparation are relatively high, which greatly restricts clinical use.

Method used

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  • Cefteram pivoxil tablet and preparation process thereof
  • Cefteram pivoxil tablet and preparation process thereof
  • Cefteram pivoxil tablet and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] A kind of cefditoren neopentyl tablet embodiment 1 of the present invention comprises following components, and each component is by weight:

[0032]

[0033] Wherein, the binder is an aqueous solution containing 1% hydroxypropyl cellulose and 0.5% poloxamer by mass fraction. The cefditoren neopentyl tablet prepared by this ratio, the ratio of croscarmellose sodium and microcrystalline cellulose is 2:1, the friability of the tablet is better, and the disintegration time limit and release of the tablet The effect is better, the controllability is also more ideal, and the overall dissolution rate and bioavailability of the drug are significantly improved compared with the drugs in the prior art. The binder is beneficial to mix and disperse cefditoren neopentyl pivoxil, starch, lactose, microcrystalline cellulose and croscarmellose sodium evenly, so that the prepared soft material is a uniform system. Add appropriate amount of neopentyl ester, starch, lactose, microcry...

Embodiment 2

[0038] A kind of cefditoren neopentyl tablet embodiment 2 of the present invention comprises following components, and each component is by weight:

[0039]

[0040] Wherein, the binder is an aqueous solution containing 1% hydroxypropyl cellulose and 0.5% poloxamer by mass fraction. The cefditoren neopentyl tablet prepared by this proportion, the ratio of croscarmellose sodium and microcrystalline cellulose is 1:1, the lubricating effect is better, and the overall dissolution rate and bioavailability of the medicine are also high. Compared with the medicine of the prior art, it is significantly improved.

[0041] The preparation process of this kind of Cefditoren Neopentyl Proxil Tablets is the same as in Example 1.

Embodiment 3

[0042] A kind of cefditoren neopentyl tablet embodiment 3 of the present invention comprises following components, and each component is by weight:

[0043]

[0044] Wherein, the binder is an aqueous solution containing 1% hydroxypropyl cellulose and 0.5% poloxamer by mass fraction. The cefditoren neopentyl tablet prepared according to the ratio is mainly composed of croscarmellose sodium and a small amount of microcrystalline cellulose, which has good compressibility, better tablet disintegration time limit and release effect, Moreover, the overall dissolution rate and bioavailability of the medicine are significantly improved compared with the medicines in the prior art.

[0045] The preparation process of this kind of Cefditoren Neopentyl Proxil Tablets is the same as in Example 1.

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Abstract

The invention discloses a cefteram pivoxil tablet, which comprises the following components in parts by weight: 80-120 parts of cefteram pivoxil, 80-100 parts of starch, 5-15 parts of lactose, 5-15 parts of microcrystalline cellulose, 15-30 parts of croscarmellose sodium, 0.5-2 parts of magnesium stearate and a proper amount of bonding agents. The invention further discloses a preparation process of the cefteram pivoxil tablet. In the cefteram pivoxil tablet, croscarmellose sodium is matched with microcrystalline cellulose, so that the disintegration time limit and release result of the tablet are improved unexpectedly, and a more remarkable medicinal effect is achieved. The bonding agent is low in toxicity, is absorbed easily in gastrointestinal tract, and does not interfere with the content analysis of a medicament, so that the digestion rate of the medicament can be increased remarkably, the digestion behavior of the medicament is improved remarkably, and the bioavailability of medicament is increased remarkably. Moreover, the cefteram pivoxil tablet is low in cost, simple in production process and safe.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a cefditoren neopentyl tablet and a preparation process of the cefditoren neopentyl tablet. Background technique [0002] Cefdteram neopentyl ester, the English name is Cefteram Pivoxil, the chemical name is (6R, 7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxyimino) Acetylamino]-3-[2-(5-methyl-2H-tetrazol-2-yl)methyl]-8-oxo-5-thia-1-azabicyclo[4,2,0] Oct-2-ene-2-carboxylic acid pivaloyloxymethyl ester. Cefditoren neopentyl ester belongs to the third-generation oral cephalosporins. It is a prodrug of cefditoren modified by ester group structure. Its own activity is weak. After oral absorption, it will be hydrolyzed by esterase to generate active cefditoren to produce antibacterial activity . It has spectrum antibacterial effect on Gram-negative and positive bacteria such as Citrobacter, Serratia and Enterobacter. It is mainly used clinically for infections caus...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/30A61K47/38A61K31/546A61P31/04
Inventor 王小明金晓鲁田晓英李红莲
Owner ZHEJIANG JUTAI PHARMA
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