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Method of stabilizing macrolide compound

一种大环内酯类、化合物的技术,应用在12员环大环内酯类化合物领域,能够解决未必提供稳定化的效果等问题

Inactive Publication Date: 2007-02-14
EISIA R&D MANAGEMENT CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cyclodextrins are not able to include any compound, and even if they can be included, they may not necessarily provide a stabilizing effect
Likewise, not all compounds have a productivity-enhancing effect in the fermentative production

Method used

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  • Method of stabilizing macrolide compound
  • Method of stabilizing macrolide compound
  • Method of stabilizing macrolide compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0060] [Stabilization method of macrolide compound]

[0061] In the stabilization method of the present invention, it is necessary to coexist the macrolide compound (1) and cyclodextrins. Cyclodextrins can be made to coexist in a solid phase or a solution containing the macrolide compound (1), especially in a solution, preferably an aqueous solution.

[0062]Representative examples of the solid phase containing the macrolide compound include conventional formulation carriers, and can be produced by conventional methods. That is, in the case of preparing an oral solid preparation, an excipient may be added to the macrolide compound (1), and further, a binder, a disintegrating agent, a lubricant, a coloring agent, a deodorizing and deodorizing Agents, etc., and then made into tablets, coated tablets, granules, powders, capsules, etc. by conventional methods. Of course, these tablets and granules may be appropriately coated with sugar coating or gelatin coating as needed.

[0...

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PUM

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Abstract

The invention provides a method of stabilizing a macrolide compound and a process for efficiently producing the compound. The method, which is for stabilizing a 12-membered cyclic macrolide compound, e.g., that represented by the formula (I), comprises causing the compound to coexist with a cyclodextrin. The process, which is for producing the macrolide compound, comprises causing a cyclodextrin to be present in a culture medium containing an actinomyces having the ability to produce the macrolide compound.

Description

technical field [0001] The present invention relates to a method for stabilizing a 12-member ring macrolide compound with antitumor activity and a method for producing the compound. Background technique [0002] Formula (I) [0003] [0004] The represented 12-membered ring macrolide compound (hereinafter referred to as macrolide compound 11107B) is an antitumor active compound found in the culture of Streptomyces sp. Mer-11107 strain , and further found that a macrolide compound with better antitumor activity can be obtained by chemically synthesizing the compound and its analogues as raw materials (refer to WO02 / 060890). However, these macrolide compounds are not sufficiently stable especially in water, and it is therefore necessary to develop a method for improving stability and an efficient production method. [0005] On the other hand, cyclodextrins are non-reducing sugars in which glucose molecules are combined into rings through β-1,4-bonds, and α-, β-, β-, and β...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D407/06C07D313/00C12P17/08C08B37/16C12N1/20C12P17/16
CPCC12P17/162C12N1/20C07D313/00C07D407/06C08B37/0012
Inventor 石原比吕之竹田晋山田智也旭义明
Owner EISIA R&D MANAGEMENT CO LTD
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