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Medicament composition of cefpodoxime proxetil and cyclodextrin and preparation method thereof

A technology of cefpodoxime axetil and composition, which is applied in the field of preparation of the composition, can solve the problems of poor disintegration of the gel, reduction of cefpodoxime absorption, slowing down of dissolution, etc.

Inactive Publication Date: 2007-06-20
RANBAXY LAB LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The formed gel disintegrates poorly, slowing down dissolution and thus greatly reducing the absorption of cefpodoxime from the gastrointestinal tract

Method used

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Examples

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Embodiment Construction

[0017] Cefpodoxime axetil is a poorly soluble drug, therefore, its dissolution rate remains limited for its absorption. The absolute bioavailability of commercially available cefpodoxime axetil tablet is only about 50% of the intravenous infusion of cefpodoxime sodium. The poor solubility of cefpodoxime axetil can also be attributed to its poor wettability, which further forms a gel when it comes in contact with aqueous media. Undoubtedly, poor solubility is still the main reason, other reasons include its poor stability due to its presystemic degradation to cefpodoxamic acid, which is poorly absorbed.

[0018] Cefpodoxime axetil should therefore be released from the pharmaceutical composition in a very soluble form to facilitate fast dissolution and reduce the chance of degradation at the site of absorption. The inclusion of cefpodoxime axetil with cyclodextrin can solve all these problems, so its bioavailability is significantly increased compared with the commercially avai...

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PUM

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Abstract

A medication compound, which include cyclodextrin and cephalosporin ester's clathrate; this invention alao related to the method to produce it.

Description

technical field [0001] The invention relates to a pharmaceutical composition comprising an inclusion complex of cefpodoxime proxetil of a cyclodextrin, and also to a process for the preparation of said composition. Background technique [0002] Cefpodoxime is a third-generation cephalosporin with the chemical name (+)-(6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-{(Z)methoxy Imino}acetylamino]-3-methoxymethyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid-1-(iso Propoxycarbonyloxy) ethyl ester. Cefpodoxime and its pharmaceutically acceptable acid addition salts are described in US Patent No. 4,486,425, which is hereby incorporated by reference in its entirety. Cefpodoxime is stable against β-lactamase-mediated hydrolysis by the most common plasmids. The drug has broad-spectrum antibacterial activity against both Gram-negative and Gram-positive bacteria, and has similar and comparable efficacy to other broad-spectrum cephalosporins in terms of the occurrence and severi...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/40A61P31/04
Inventor A·K·班塞尔K·凡苏库玛
Owner RANBAXY LAB LTD
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