Preparation method of tebipenem pivoxil granules

A technology of tipipenem and pivoxil, which is applied in the field of preparation of tipipenem pivoxil granules, can solve the problem of rising water content, poor stability of tipipenem pivoxil, and poor dissolution of granules and other problems, to achieve the effect of low impurities, high polymer and main drug compatibility, and good dissolution

Inactive Publication Date: 2012-12-19
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the poor stability of tipipenem pivoxate, the related substances increase greatly under high temperature and high humidity conditions, so the selection and dosage of excipients become particularly important. Random selection of excipients may make tipipenem pivoxate granules The dissolution rate of the agent becomes worse, the related substances increase, the content decreases, the polymer increases, the moisture content rises, etc., and even cannot be granulated

Method used

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  • Preparation method of tebipenem pivoxil granules
  • Preparation method of tebipenem pivoxil granules
  • Preparation method of tebipenem pivoxil granules

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the selection of preparation method

[0020] 1. Granulation method

[0021] According to the prescription of tipipenem pivoxil granules of the present invention, dry granulation and wet granulation were used respectively, and then the finished product was tested for related substances (i.e. impurities). The results are shown in Table 1.

[0022] Table 1 Test results of related substances in wet granulation and dry granulation

[0023]

[0024] It can be seen from the test results that the wet granulation process increases the impurities much more than the dry granulation process, so the dry granulation process is more suitable.

[0025] 2. Selection of dry granulation conditions

[0026] Raw material crushing particle size:

[0027] Tipipenem pivoxate is a crystalline powder. In order to mix evenly with auxiliary materials, the particle size should be kept in the same range as possible. The pulverized tipipenem pivoxate of the present invention is pa...

Embodiment 2

[0037] Embodiment 2: different proportioning tests of main and auxiliary materials

[0038] 1. Different contents of microcrystalline cellulose and sucrose

[0039] According to the prescription in Table 4, dry granulation was performed, and then the granulation condition, granule fluidity, angle of repose, granule strength, mouthfeel, and water content were used as inspection indicators for testing. The results are shown in Table 5.

[0040] Table 4 Prescriptions with different contents of microcrystalline cellulose and sucrose

[0041] Main and auxiliary materials

Prescription 1

Prescription 2

Prescription 3

Prescription 4

Prescription 5

tipipenem pivoxate

12.976g

12.976g

12.976g

12.976g

12.976g

microcrystalline cellulose

62.50g

50.00g

37.50

25.00g

12.50g

sucrose

24.524g

37.024g

49.524g

62.024g

74.424g

aspartame

1.00g

...

Embodiment 3

[0057] Embodiment 3: Preparation of tipipenem pivoxil granules of the present invention

[0058] According to the prescription of tipipenem pivoxil granule of the present invention, i.e. 32.44 parts by weight of tipipenem pivoxil, 31.25 parts by weight of microcrystalline cellulose, 183.56 parts by weight of sucrose, 2.5 parts by weight of Spartan and 0.25 parts by weight of red iron oxide (or 12.976 parts by weight of tipipenem pivoxil, 12.50 parts by weight of microcrystalline cellulose, 73.424 parts by weight of sucrose, 1.00 parts by weight of aspartame and 0.1 parts by weight red iron oxide), three batches of tipipenem pivoxil granules were prepared by dry granulation (hereinafter referred to as batch 100601, batch 100602, batch 100603), and the yields were 86.80% and 86.26% respectively , 86.60%.

[0059] Dry granulation process steps:

[0060] In an environment with a relative humidity below 60%, crush the above raw and auxiliary materials through an 80-mesh sieve, mi...

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Abstract

The invention relates to the field of chemical synthesis, and discloses a preparation method of tebipenem pivoxil granules. The preparation method comprises the following steps of: grinding the following raw materials in parts by weight: 32.44 parts of tebipenem pivoxil, 31.25 parts of microcrystalline cellulose, 183.56 parts of sucrose, 2.5 parts of aspartame and 0.25 part of red iron oxide; and mixing uniformly and feeding the mixture into a dry granulator for granulation. The method disclosed by the invention adopts four accessories with wide source and better compatibility with the primary medicine tebipenem pivoxil to prepare new granules; and the prepared granules can ensure better dissolution rate, relatively low content of impurities and polymers and the like under the condition of relatively few accessories, have good quality and can be widely applied to clinical treatment.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of tipipenem pivoxil granules. Background technique [0002] Tipipenem pivate, the chemical name is (+)-(4R,5S,6S)-6-[(1R)-hydroxyethyl]-4-methyl-7-oxo-3[[1- (2-Thiazolin-2-yl)-3-azetidinyl]sulfur]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (2,2-dimethyl -1-oxopropoxy) methyl ester belongs to carbapenem antibiotics, and its structural formula is as follows: [0003] [0004] Tipipenem pivoxil was first developed by Pfizer of the United States, and the fine-grained tipipenem pivoxil was developed by Japan Meiji Company. It was approved by Japan in February 2009 and launched in April 2009. There are listed manufacturers and related reports. Tipipenem pivoxate fine granule is used for the treatment of ear, nose, throat and upper respiratory tract infections in pediatric patients. Southern drugs. Tipipenem pivoxil has a broad antibacterial ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/427A61K47/38A61P31/04
Inventor 阮朝滨李明杰刘文芳冯长运
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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