Preparing method of Azidothimidine cholesterol carbonate, preparation and analytical method thereof

A technology of cholesteryl carbonate and cholesterol carbonate, which is applied in the field of pharmacokinetics research, can solve problems such as drug leakage, leakage, and reduction, and achieve the effect of improving drug safety

Inactive Publication Date: 2007-08-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In vivo distribution experiments showed that the bone marrow distribution was greatly reduced (the amount of bone marrow distribution in the solution group was about 1800 times that of the liposome group), the toxicity of AZT was greatly reduce

Method used

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  • Preparing method of Azidothimidine cholesterol carbonate, preparation and analytical method thereof
  • Preparing method of Azidothimidine cholesterol carbonate, preparation and analytical method thereof
  • Preparing method of Azidothimidine cholesterol carbonate, preparation and analytical method thereof

Examples

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example 1

[0036] Example 1. Infrared scanning detection, infrared spectrogram and data see accompanying drawing 7.

example 2

[0037]Example 2. The liquid-mass spectrometry assay, the liquid-mass spectrometry result shows that the molecular ion is M+: 679.2.

example 3

[0038] Example 3. NMR analysis, hydrogen spectrum and carbon spectrum are shown in accompanying drawings 3 and 4.

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Abstract

The invention discloses a new synthesizing method of Azidothimidine carbonic cholesterol ester (or other esters of sterol) as drug primer, which is characterized by the following: adopting Azidothimidine and cholesterol to form chloroformate cholesterol ester; fitting for multiple agents; establishing internal and external analytic method; detecting medical kinetics in the mouse; obtaining the product with half-decay time at 4.9h; lengthening AZT acting time; reducing side-effect; targeting AIDS enriched organs and tissues.

Description

Technical field: [0001] The invention relates to the technical field of medicines, in particular to a synthesis method of zidovudine cholesteryl carbonate (or other sterol esters), preparation of related preparations, in vitro and in vivo analysis methods and pharmacokinetic research. Background technique: [0002] Zidovudine is currently one of the first-choice drugs for the clinical treatment of AIDS and has been listed in the United States Pharmacopoeia. It can not only reduce the probability of opportunistic infection and neonatal occurrence, increase the number of T lymphocytes, but also cross the blood-brain barrier , achieve antiviral concentration in cerebrospinal fluid (CSF), reduce the amount of virus in CSF, improve neurophysiological function in patients with progressive encephalopathy, improve and reduce HIV-induced dementia, increase survival rate and improve quality of life, in addition, AZT can Reduce the rate of perinatal HIV mother-to-child transmission by ...

Claims

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Application Information

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IPC IPC(8): C07H19/06C07H1/00
Inventor 邓意辉陈国良毕殿洲张玲玲徐晖王绍宁王宁周欣羽赵静沈琳
Owner SHENYANG PHARMA UNIVERSITY
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