Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

6-methocy bideoxy bideoxy guanosine long circulating liposome preparation and preparing method

A liposome preparation and liposome technology, which are applied in the field of 6-methoxydideoxyguanosine long-circulating liposome preparation and its preparation, can solve the problem of short biological half-life, impact on patients' life and work, and occupation of hospital resources. And other issues

Inactive Publication Date: 2008-03-26
CHINA PHARM UNIV
View PDF0 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] 6-methoxydideoxyguanosine is used to treat viral hepatitis B, and its curative effect and many indicators are better than those of lamivudine currently on the market, but the biological half-life of 6-methoxydideoxyguanosine in the body Short, it is cleared faster in the plasma and affects the better efficacy of the drug
However, it is difficult to modify the structure of drugs, and it takes a long time; long-term clinical infusion will occupy a lot of hospital resources and have a great impact on the life and work of patients

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 6-methocy bideoxy bideoxy guanosine long circulating liposome preparation and preparing method
  • 6-methocy bideoxy bideoxy guanosine long circulating liposome preparation and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 6-Methoxydideoxyguanosine 0.051g

[0036] Hydrogenated soybean phosphatidylcholine 0.4220g

[0037] PEG5000-PG0.3645g

[0038] Cholesterol 0.1760g

[0039] After dissolving hydrogenated soybean phosphatidylcholine and cholesterol in 50ml of absolute ethanol respectively, the ethanol was removed at 50°C with a rotary evaporator, and 15ml of 6-methoxydideoxyguanosine solution (3.3mg / ml) was added to make It is fully infiltrated and stirred with a vortex mixer to prepare a liposome suspension. Add 1.21ml of a distilled aqueous solution of polyethylene glycol 5000-phosphatidylglycerol (PEG5000-PG) (equivalent to 0.475mol% of the total lipid mass of the mixed lipids) to the above-mentioned liposome suspension, heat at 60°C For 30 minutes, modify the liposome surface with PEG5000-PG. The final liposome suspension was prepared by sequentially passing through filters (0.2um filter 2 times, 0.1um filter 2 times) in a high pressure homogenizer (Niro Soavi) at 60°C.

Embodiment 2

[0041] 6-Methoxydideoxyguanosine 0.060g

[0042] Hydrogenated soybean phosphatidylcholine 0.4120g

[0043] PE63000-PE 0.3845g

[0044] Cholesterol 0.1520g

[0045] After dissolving hydrogenated soybean phosphatidylcholine and cholesterol in 25ml of ethanol at room temperature, the ethanol was removed at 50°C using a rotary evaporator, and 10ml of 6-methoxydideoxyguanosine solution (6.0mg / ml) was added to make it Fully infiltrate and stir with a vortex mixer to prepare a liposome suspension. Add a distilled aqueous solution containing polyethylene glycol 3000-phosphatidylcholine (PEG3000-PE) (equivalent to 0.475mol% of the total lipid mass of the mixed lipids) to the above-mentioned liposome suspension, and successively The final liposome suspension was prepared by passing through filters (0.2 um filter 2 times, 0.1 um filter 3 times) in a high pressure homogenizer (Niro Soavi).

Embodiment 3

[0047] 6-Methoxydideoxyguanosine 0.060g

[0048] Lecithin 0.4520g

[0049] PEG4000-PE 0.1845g

[0050] Cholesterol 0.2020g

[0051] After dissolving lecithin and cholesterol in 25ml of ethanol heated at room temperature, use a rotary evaporator to remove ethanol at 55°C, add 10ml of 6-methoxydideoxyguanosine solution (6.0mg / ml) to make it fully infiltrated, Prepare a liposome suspension by stirring with a vortex mixer. Add a distilled aqueous solution of polyethylene glycol 4000-phosphatidylethanolamine (PEG4000-PE) (equivalent to 0.475mol% of the total lipid mass of the mixed lipids) to the above liposome suspension, and pass through high pressure successively at 65°C Filters (0.2um filter 2 times, 0.1um filter 2 times) in a machine homogenizer (Niro Soavi) were used to prepare the final liposome suspension.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
The average particle sizeaaaaaaaaaa
Molecular weightaaaaaaaaaa
Login to View More

Abstract

The present invention relates to a liposome preparation containing 6-methoxydideoxy-guanosine. Said liposome is a vesicle of lipid double-layer membrane formed by using phospholipids as main membrane material, the metacawei is enveloped in the internal water phase of said liposome, and the outer surface of said liposome is modified by hydrophilic macromolecule, so that the time of that said liposome preparation is remained in the blood can be prolonged so as to raise the bioavailability and therapeutic effect of medicine.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, especially liposome preparations for changing the bioavailability of drugs and prolonging the half-life of drugs. The invention also relates to a 6-methoxydideoxyguanosine long-circulation liposome preparation and its preparation method . Background technique [0002] Many new drugs have been used to treat chronic hepatitis B over the years, but many problems have not been solved. For example, there is a lack of low-cost, safe drugs that can produce sustained responses in short-term treatment. Chronic hepatitis B patients with normal or near-normal ALT, immune tolerance or HIV infection, and HBeAg-negative patients still have great challenges for clinicians. In the coming years, new nucleoside analogs and other antiviral drugs will be approved for the treatment of chronic hepatitis B. [0003] Liposome is the fourth generation drug delivery system in pharmacy—a new dosage form of tar...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/127A61K31/708A61P1/16A61P31/12
Inventor 李战张陆勇张自强
Owner CHINA PHARM UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com