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Tebipenem pivoxil oral preparation and preparation method thereof

A tibipenem ester and oral preparation technology, which is applied in the field of carbapenem antibiotics, can solve the problems of children's poor taking compliance, and achieve the effects of improving drug taking compliance, improving taste, and simple process

Active Publication Date: 2013-01-09
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through the dissolution test of the marketed products, it was found that most of the insoluble substances in the drug liquid were in the state of suspension. Therefore, there were still problems of gritty feeling and poor compliance for children.

Method used

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  • Tebipenem pivoxil oral preparation and preparation method thereof
  • Tebipenem pivoxil oral preparation and preparation method thereof
  • Tebipenem pivoxil oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1 Preparation of tibipenem-β-cyclodextrin inclusion compound

[0058] Weigh tibipenem 10g and β-cyclodextrin 30g, mix thoroughly, and then carry out DSC determination, the results are shown in image 3 .

[0059] The test results show that good Tibipenem-β-cyclodextrin inclusion compound can be obtained by physical mixing method.

Embodiment 2

[0060] Example 2 tibipenem granule 50mg / 0.5g

[0061] Prescription (1000 bags):

[0062]

[0063] Remarks: In the total amount of the preparation, based on tybipenem, 1g of tybipenem is equivalent to 1.3g of tybipenem. (The same below) Operation:

[0064] 1. Weigh the prescription amount of raw materials and mix them with β-cyclodextrin, and then fully mix them with other excipients;

[0065] 2. After the raw and auxiliary materials are fully mixed, add an appropriate amount of water-based soft materials containing pigments, granulate with a 16-mesh sieve and dry in a boiling dryer. The inlet air temperature is controlled at ≤60°C, and the material temperature is controlled at ≤40°C. The dry granules are granulated through a 14 mesh, and the essence is added and mixed to obtain tibipenem granules.

Embodiment 3

[0066] Example 3: tibipenem granule 50mg / 0.5g

[0067] Prescription (1000 bags):

[0068]

[0069] Operation is with embodiment 2.

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PUM

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Abstract

The invention relates to a tebipenem pivoxil-containing oral preparation and a preparation method of the tebipenem pivoxil-containing oral preparation. The preparation provided by the invention consists of tebipenem pivoxil and a pharmaceutic adjuvant as the active components. The pharmaceutic adjuvant contains beta-cyclodextrin. The tebipenem pivoxil oral preparation provided by the invention overcomes the defects that the grit feeling is produced when the tebipenem pivoxil oral preparation is taken, the patient compliance is poor and the preparation technology is complicate in the prior art, so that the tebipenem pivoxil oral preparation is an excellent preparation with good taste, high dissolvability, good stability and simple preparation technology.

Description

technical field [0001] The invention belongs to the field of carbapenem antibiotics, in particular to a tibipenem oral preparation and a preparation method thereof. Background technique [0002] Tebipenem Pivoxil, the chemical name is (1R,5S,6S)-1-methyl-6-[(1R)-1-hydroxyethyl]-2-[1-(1,3- Thiazolin-2-yl)azetidin-3-yl]thio-1-carbapenicillin-2-ene-3-carboxylic acid methyl pivalate, the structural formula is as shown in formula 1: [0003] [0004] As the first oral formulation product of carbapenem antibiotics, tibipenem was first developed and marketed by Japan Meiji Seika Co., Ltd. in August 2009. The medicine has a low inhibitory concentration, is not easy to cause the emergence of bacterial drug resistance, has few side effects, and has high drug safety, and can be used for treating children's infections. [0005] Tibipenem has an amorphous form and a crystalline form, the amorphous form of tibipenem has good solubility but poor stability, and is not suitable for the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/14A61K31/427A61K47/48A61P31/04
Inventor 张宏武陈素锐白敏马玉秀吴欢欢金晓利李园园
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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