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Micronized cefditoren pivoxil composition

A technology of cefditoren and composition, applied in the field of preparing micronized granules of cefditoren pivoxil, capable of solving the problems of low solubility of cefditoren pivoxil and inability to administer drugs

Inactive Publication Date: 2010-07-14
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this formulation has the disadvantage that it cannot be administered to patients suffering from lactose intolerance syndrome, since casein is a protein derived from milk
Despite high purity, high thermal stability and additionally satisfactory stability even when stored under high humidity conditions, crystalline cefditoren pivoxil has the disadvantage of low solubility

Method used

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  • Micronized cefditoren pivoxil composition
  • Micronized cefditoren pivoxil composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Micronization method of cefditoren pivoxil

[0052] Use air jet mill to micronize cefditoren pivoxil, and the compressed air pressure is 6PSIG to obtain 0.5 2.37μm and d 0.9 6μm powder.

Embodiment 2

[0054] Tablets containing micronized cefditoren pivoxil

[0055]

[0056] method:

[0057] (i) Sieve micronized cefditoren pivoxil, mannitol and intragranular croscarmellose sodium and mix together.

[0058] (ii) Hydroxypropyl cellulose was dissolved in purified water.

[0059] (iii) Granulating the mixture of step (i) using the binder solution of step (ii).

[0060] (iv) Drying the granules of step (iii) in a fluid bed drier.

[0061] (v) Sifting the dried granules of step (iv).

[0062] (vi) Magnesium stearate and extragranular croscarmellose sodium are sieved and blended with the granules of step (v).

[0063] (vi) Finally, the mixture of step (vi) is compressed into tablets.

Embodiment 3

[0065] With ingredients similar to Example 2, non-micronized cefditoren pivoxil (with d 0.5 greater than 100 μm) to prepare tablets comprising unmicronized cefditoren pivoxil.

[0066] Comparison of In Vitro Dissolution Profiles

[0067] Dissolution studies were performed on tablets of cefditoren pivoxil prepared according to the compositions of Examples 2 & 3 in 900 ml of 0.1N HCl at 37°C using USP Apparatus II with a paddle speed of 50 rpm. Table 1 provides a comparison of the dissolution profile of tablets comprising micronized (Example 2) and non-micronized cefditoren pivoxil (Example 3).

[0068] Table 1

[0069]

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Abstract

The invention relates to a medicament composition and method of preparing the same. The medicament composition includes micronized particles of cefditoren pivoxil, wherein the particles have the d0.5 from 1[mu]m to 40 [mu]m. The invention also relates to method for preparing micronized cefditoren pivoxil particles.

Description

field of invention [0001] The invention relates to a pharmaceutical composition comprising micronized particles of cefditoren pivoxil and a preparation method thereof. The invention also relates to a process for the preparation of micronized granules of cefditoren pivoxil. Background of the invention [0002] Cefditoren is an orally deliverable third-generation cephalosporin antibiotic. Its chemical expression is -[2-methoxyimino-2-(2-aminothiazol-4-yl)acetamido]-3-[2-(4-methylthiazol-5-yl)vinyl] - 3-cephem-4-carboxylic acid (coisomer, cis isomer). The synthesis of cefditoren is disclosed in US Patent Nos. 4,839,350 and 4,918,068. [0003] Cefditoren pivoxil is a prodrug of cefditoren, which is synthesized by esterifying the 2-carboxyl group of cefditoren with pivaloyloxymethyl (pivoxil). It exhibits improved oral absorption, and when absorbed is rapidly hydrolyzed to cefditoren by esterases. Cefditoren has low toxicity to mammals, but exhibits a very broad antibacteria...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K9/16A61P11/00A61P11/04A61P31/04
Inventor C·M·林盖姆R·瓦森A·特里汉V·阿罗拉
Owner RANBAXY LAB LTD
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