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Injection use medicine composition containing water-soluble 17-allylamino-17-demethoxy geldanamycin

A technology of demethoxygeldanamycin and allylamino, which is applied in the field of injection pharmaceutical compositions of 17-allylamino-17-demethoxygeldanamycin, can solve the problem of severe side effects, Restrictions, lack of tumor cell specificity and other issues, to achieve the effect of good stability and drug safety

Inactive Publication Date: 2009-05-27
深圳生尔易美生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the tumor chemotherapy drugs commonly used clinically have the following two serious shortcomings: ① due to the lack of specificity to tumor cells, the side effects are very large
② Easy to produce tumor drug resistance
[0008] Although GA exhibited good tumor-inhibitory activity in animal models of human tumor transplantation, its clinical application was limited by its hepatotoxicity.

Method used

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  • Injection use medicine composition containing water-soluble 17-allylamino-17-demethoxy geldanamycin
  • Injection use medicine composition containing water-soluble 17-allylamino-17-demethoxy geldanamycin
  • Injection use medicine composition containing water-soluble 17-allylamino-17-demethoxy geldanamycin

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] 1. Establishment of HPLC determination method for 17-AAG influencing factors test

[0096] Use octadecylsilane bonded silica gel as filler; phosphate buffer [take sodium dihydrogen phosphate (NaH 2 PO 4 2H 2 O) 2g, add water to dissolve and dilute to make 1000ml]-acetonitrile-methanol-triethylamine (40:50:10:0.2) adjust pH to 5.0 with phosphoric acid as mobile phase; flow velocity is 1.2ml / min; detection wavelength is 303nm . The number of theoretical plates based on 17-AAG should not be less than 2000; the separation between 17-AAG peak and adjacent impurity peak should meet the requirements.

[0097] 2. Test methods and results

[0098] 1. Sample control test

[0099] Avoid light operation. Take about 15 mg of 17-AAG, weigh it accurately, put it in a 50ml measuring bottle, add an appropriate amount of mobile phase, and treat it ultrasonically for 5 minutes. 3 times of the retention time of the component peak, the total impurity is 1.26% according to the normali...

Embodiment 2

[0118] Taking different ratios of 17-AAG and excipient PEG400, the interaction between raw materials and excipients was investigated under the influence of light and temperature. Use HPLC method to check the content of 17-AAG and the changes of related substances before and after being placed, and observe the changes of drug properties such as appearance and color at the same time, so as to evaluate the compatibility of raw materials and excipients.

[0119] 1. HPLC detection method for related substances in 17-AAG preparations

[0120] Use octadecylsilane bonded silica gel as filler; phosphoric acid aqueous solution (use phosphoric acid to adjust the pH value to 3.0) as mobile phase A, and acetonitrile as mobile phase B; flow rate is 1.0ml per minute, gradient elution; detection wavelength 303nm. The number of theoretical plates based on 17-AAG should not be less than 2000; the separation between 17-AAG peak and adjacent impurity peak should meet the requirements. This HPLC...

Embodiment 3

[0136] Accurately weigh 1000 mg of 17-AAG, add it into 800 ml of PEG400 (Shanghai Pudong Gaonan Chemical Factory, batch number 040448) solution and dissolve. Sterilize and filter at room temperature in the dark. The preparation was dispensed into sterilized vials under aseptic conditions.

[0137] Add it to 0.9% sodium chloride injection or 5% or 10% glucose saline injection before clinical application to make the final concentration of PEG400 reach 30%-40% or 10%-30%. The 17- AAG remained stable within 4 hours.

[0138] For the process flow of 17-AAG injection preparation, see figure 1 .

[0139] The preparation formula of the present invention can obviously improve the water solubility of 17-AAG, and the result shows that the water solubility of 17-AAG can be increased by more than 50 times.

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Abstract

An injection of water-soluble 17-allylamino-17-demethoxy geldanamycin (17-AAG) for treating multiple kinds of cancers is prepared from 17-AAG and polyethanediol for increasing the solubility of 17-AAG in water.

Description

technical field [0001] The invention relates to a pharmaceutical composition for injection of 17-allylamino-17-demethoxygeldanamycin (17-AAG). Background technique [0002] Anticancer antibiotics are chemical substances with anticancer activity produced by microbial metabolism. There are many kinds of anticancer antibiotics reported, among which more than 10 kinds have been used clinically. Mitomycin, doxorubicin, daunorubicin, bleomycin, pingyangmycin, dactinomycin and other anticancer antibiotics of natural origin and chemically modified analogues have become more commonly used drugs for the treatment of tumors. An important component of the anticancer drug arsenal. [0003] At present, anticancer antibiotics acting on various targets have been reported one after another. The main targets include tumor blood vessels, DNA templates, matrix metalloproteinases, and heat shock protein 90 (HSP90). It has attracted attention due to its remarkable anticancer effect. Geldanamy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/395A61K9/08A61P35/00
Inventor 孔健黄颖周向阳
Owner 深圳生尔易美生物技术有限公司
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