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PEG-modified echinocandin antifungal drug complex and preparation thereof

An antifungal drug, echinocandin technology, applied in antifungal agents, medical preparations of non-active ingredients, pharmaceutical formulas, etc., can solve problems such as adverse reactions and injection site irritation

Active Publication Date: 2015-10-14
南京星银药业集团有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of various emulsifiers will cause irritation at the injection site and other adverse reactions, so long-term use is not recommended.

Method used

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  • PEG-modified echinocandin antifungal drug complex and preparation thereof
  • PEG-modified echinocandin antifungal drug complex and preparation thereof
  • PEG-modified echinocandin antifungal drug complex and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The preparation of embodiment 1 PEG-MAL sample (2)

[0017] Dissolve monomethoxypolyethylene glycol PEG (5KDa, 10KDa, 20KDa) of different molecular weights in an appropriate amount of dichloromethane, add 2 equivalents of pyridine as an acid-binding agent, add 5 equivalents of maleic anhydride, and control the temperature React at 60°C for 8 hours, concentrate, and crystallize with isopropyl ether to obtain monomethoxypolyethylene glycol with a carboxyl group at one end with different molecular weights.

Embodiment 2

[0018] The preparation of embodiment 2 PEG-MAL-OSu sample (3)

[0019] Dissolve monomethoxypolyethylene glycol PEG-MAL ((5KDa, 10KDa, 20KDa) with different molecular weights and one end of carboxyl group in appropriate amount of THF, add HOSu, DCC, stir for 5h, a large amount of white solid precipitates, filter, Crystallize with isopropyl ether, filter, wash with appropriate amount of water and isopropyl ether, and dry in vacuum to obtain PEG-MAL-OSu with different molecular weights.

Embodiment 3

[0020] The preparation of embodiment 3 PEG-Mal-Caspofungin sample (5)

[0021] Use 50mM pH3.5 NaH2PO4-H3PO4 buffer solution caspofungin acetate to configure a 30mg / ml solution, respectively use different molecular weight polyethylene glycol modifiers PEG-MAL-OSu (5K Da), PEG -MAL-OSu (10K Da), PEG-MAL-OSu (20K Da) was modified, caspofungin: PEG-MAL-OSu was reacted at a molar ratio of 1:10, reacted at 4°C for 24h, added 1M glycine terminated the reaction, purified by Sephadex Superdex 200 column chromatography, concentrated, and freeze-dried to obtain the target product.

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Abstract

The present invention relates to a PEG-modified echinocandin antifungal drug complex and a preparation method thereof, wherein the preparation method is characterized in that PEG and maleic anhydride are bound to form an active ester, and then the active ester and an echinocandin antifungal drug caspofungin are subjected to two-site PEG modification so as to improve the drug stability, save the pharmaceutical activity, and increase the sustained release effect of the drug.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a PEG-modified echinocandin antifungal compound and a preparation method. Background technique [0002] With the increasing use of a large number of antibacterial drugs, antineoplastic drugs, corticosteroids and immunosuppressants, and the increasing incidence of organ transplantation, interventional surgery and acquired immunodeficiency syndrome, the incidence of deep fungal infection is also increasing year by year. Therefore, it is particularly important to develop new antifungal drugs and their preparations in the process of resisting fungal infections. So far, three main classes of drugs have been used for systemic antifungal therapy: polyenes, such as amphotericin B; triazoles, such as voriconazole, fluconazole, itraconazole, posaconazole; Mycocins, such as caspofungin, micafungin, and anidafungin. [0003] Echinocandin antifungal drugs are a new type of antifungal drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/12C08G65/48A61P31/10A61K47/60
Inventor 李小琴王俊卿
Owner 南京星银药业集团有限公司
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