Application of zidovudine lipid derivative in medicaments for treating virus associated diseases

A zidovudine and virus technology, which is applied in the application field of zidovudine lipid derivatives in the treatment of virus-related diseases, and can solve problems such as drug resistance or drug resistance.

Inactive Publication Date: 2009-12-02
INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after a period of treatment with many nucleoside analog drugs, drug resistance or drug resistance tends to develop in vivo, because nucleoside kinases of viruses or tumor cells no longer phosphorylate nucleoside analogs (Kimberlin DW, et al . Molecular mechanisms of antiviral resistance. AntiviralRes, 1995, 26: 369-401)

Method used

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  • Application of zidovudine lipid derivative in medicaments for treating virus associated diseases
  • Application of zidovudine lipid derivative in medicaments for treating virus associated diseases
  • Application of zidovudine lipid derivative in medicaments for treating virus associated diseases

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0033] Experimental example 1: Anti-HIV activity of cholesteryl phosphonozidovudine in vitro

[0034] Cholesterylphosphonozidovudine has strong inhibitory activity against HIV-1 IIIB virus in vitro, and has low cytotoxicity.

[0035] Materials and Methods

[0036] Routine instruments, equipment and reagents for cell and HIV virus experiments are used in the P3 laboratory. Zidovudine raw materials are purchased from pharmaceutical factories. The preparation of the cholesterol-based phosphonozidovudine self-assembly delivery system refers to the aforementioned patent (CN101244036), with an average particle size of 107 nanometers and stability. The HIV-1 IIIB virus was imported from the United States; the MT4 cell line was imported from Japan.

[0037] The concentration of zidovudine aqueous solution and self-made cholesterylphosphonozidovudine self-assembled delivery system measured by high performance liquid chromatography were 3.74mol L -1 , 3.03mol·L -1 , both were dilut...

experiment example 2

[0050] Experimental Example 2: In Vitro Anti-HIV Activity of Cholesteryl Phosphoryl Zidovudine

[0051] Cholesteryl phosphoryl zidovudine has strong inhibitory activity against HIV-1 IIIB virus in vitro, and has low cytotoxicity.

[0052] Materials and Methods

[0053] Similar to Experimental Example 1, the preparation of the cholesterol-based phosphoryl zidovudine self-assembly delivery system refers to the aforementioned patent (CN100462103), with an average particle size of 123 nanometers and stability.

[0054] The concentrations of zidovudine aqueous solution and cholesteryl phosphoryl zidovudine self-assembled delivery system measured by high performance liquid chromatography were 3.74mol L -1 , 2.22mol·L -1 , both were diluted with ultrapure water to about 50 μmol L -1 , in a 96-well cell culture plate, the three drugs were serially diluted 10 times to obtain a concentration of 50×10 3 , 5×10 3 , 500, 50, 5, 0.5nmol·L -1 Zidovudine aqueous solution, cholesterol-ba...

experiment example 3

[0063] Experimental Example 3: Pharmacokinetics and tissue distribution of cholesteryl phosphonozidovudine self-assembled delivery system after intravenous injection

[0064] Cholesterol-based phosphonozidovudine self-assembled delivery system can be quickly cleared from the blood circulation after intravenous injection to rats, targeted distribution to the mononuclear macrophage system such as liver, lung and spleen, and has a strong macrophage Cell targeting provides the basis for efficient clearance of viruses in monocytes and macrophages.

[0065] Materials and Methods

[0066] Cholesterol-based phosphonozidovudine self-assembled delivery system, concentrated to about 20 mg / ml, filtered and sterilized through a 0.22 μm sterile filter membrane before administration. Samples before administration were all accurately determined drug content by HPLC method. The rest are reagents and equipment for routine animal experiments. Healthy male Sprague-Dawley adult rats.

[0067] ...

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PUM

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Abstract

The invention discloses application of zidovudine lipid derivative in medicaments for treating virus associated diseases. The zidovudine lipid derivative comprises cholesteryl phosphono zidovudine and cholesteryl phosphinylidyne zidovudine which are amphipathic zidovudine lipid derivatives and can form a nano-scale dispersed self-assembly transmission system in water; the zidovudine lipid derivative has strong anti-HIV function in vitro and the efficacy of the derivative is 5 to 50 times that of zidovudine; moreover, the zidovudine lipid derivative is mainly distributed in a mononuclear macrophage system after in vivo medication and plays a role in treating virus infection within macrophage.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of zidovudine lipid derivatives in medicines for the treatment of virus-related diseases, wherein the zidovudine lipid derivatives include cholesteryl phosphonozidovudine and cholesteryl phosphate acyl zidovudine. Background technique [0002] Viruses are an important pathogen that endangers human health, are highly contagious, and are the cause of many other diseases such as tumors. It is a very arduous task to vigorously develop safe and effective antiviral drugs. An important criterion for antiviral drugs is to have an inhibitory effect on viruses without affecting the normal metabolism of cells. Due to the simple structure and life process of the virus, it is not easy to distinguish it from the host cell. Therefore, most antiviral drugs are highly toxic to the human body or have low antiviral effects during their action. This is one of the reasons why antiviral d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7072A61P31/12A61P1/16A61P31/18A61P31/20A61P31/14
CPCY02A50/30
Inventor 金义光李淼田瑛董俊兴邢磊
Owner INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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