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Sophoridine nano liposome medicament and preparation of the same

A nano-liposome, sophoridine technology, applied in the directions of liposome delivery, drug combination, antipyretics, etc., can solve problems such as adverse reactions, and achieve the effects of avoiding phagocytosis, good quality and high curative effect

Inactive Publication Date: 2008-04-02
江苏德伦生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the problem of the above-mentioned adverse reactions in the existing sophoridine preparations, the present invention provides a nanoliposome drug of sophoridine, which can be used to prepare and treat adenocarcinoma, anti-inflammatory, anti-gout, anti-central nervous degenerative diseases, Analgesic and viral myocarditis drugs

Method used

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  • Sophoridine nano liposome medicament and preparation of the same
  • Sophoridine nano liposome medicament and preparation of the same
  • Sophoridine nano liposome medicament and preparation of the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The present embodiment adopts sophoridine nano liposome drug formula as follows:

[0033] Hydrogenated Soy Lecithin and Vitamin E for Injection

[0034] 350g of a mixture with a weight ratio of 9.8:0.2;

[0035] Cholesterol and β-sitosterol weight ratio 1: 1 mixture 30g;

[0036] Sophoridine 10g;

[0037] 200g of a mixture of dextran-40 and mannitol in a weight ratio of 1:7;

[0038] Reduced Glutathione 5g;

[0039] Poloxamer F-68 40g;

[0040] Phosphate buffer (0.01M, PH6.0-7.0) 2000g.

[0041] The preparation method is as follows:

[0042] (1) Sophoridine, a mixture of hydrogenated soybean lecithin for injection and vitamin E in a weight ratio of 9.8:0.2, and a mixture of cholesterol and β-sitosterol in a weight ratio of 1-3:1 were dissolved in ether and ethanol at a volume ratio of 3- In the 5:1 mixed solution, diethyl ether and ethanol were evaporated under reduced pressure in a rotary evaporator at 30-40°C to form a liposome film on the bottle wall;

[0043...

Embodiment 2

[0049] The present embodiment adopts sophoridine nano liposome drug formula as follows:

[0050] Hydrogenated Soy Lecithin and Vitamin E for Injection

[0051] 500g of a mixture with a weight ratio of 9.8:0.2;

[0052] Cholesterol and β-sitosterol weight ratio 3: 1 mixture 20g;

[0053] Sophoridine 25g;

[0054] 125g of a mixture of dextran-40 and mannitol in a weight ratio of 1:9;

[0055] Reduced glutathione 10g;

[0056] Poloxamer F-68 35g;

[0057] Phosphate buffer (0.01M, PH6.0-7.0) 1750g.

[0058] The preparation method is the same as above.

[0059] Pharmacodynamic verification experiment:

[0060] Mouse liver cancer model, the treatment group is the freeze-dried injection of the medicine of the present invention, divided into three dosage groups of 7.5mg / kg, 10mg / kg, and 12.5mg / kg, and the control group is the common water injection of 25mg / kg dosage, each group 30 mice. Carry out tail vein injection administration. Dosing once every three days, the statistic...

Embodiment 3

[0063] The present embodiment adopts sophoridine nano liposome drug formula as follows:

[0064] Hydrogenated Soy Lecithin and Vitamin E for Injection

[0065] 350g of a mixture with a weight ratio of 9.8:0.2;

[0066] Cholesterol and β-sitosterol weight ratio 1: 1 mixture 20g;

[0067] Sophoridine 10g;

[0068] 125g of a mixture of dextran-40 and mannitol in a weight ratio of 1:7;

[0069] Reduced Glutathione 5g;

[0070] Poloxamer F-68 35g;

[0071] Phosphate buffer (0.01M, PH6.0-7.0) 1750g.

[0072] The preparation method is the same as above.

[0073] Pharmacodynamic verification experiment:

[0074] Mouse liver cancer model, the treatment group is the freeze-dried injection of the medicine of the present invention, divided into three dosage groups of 7.5mg / kg, 10mg / kg, and 12.5mg / kg, and the control group is the common water injection of 25mg / kg dosage, each group 30 mice. Carry out tail vein injection administration. Dosing once every three days, the statistical ...

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PUM

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Abstract

The invention relates to a sophoridine nanoliposome drug and the preparation method. The invention provides a sophoridine nanoliposome drug and the material and the content of the material are as follows: 350-500 compound of HSPC for injection and Vitamin E with a mass ration 9.8: 0.2; 20 to 30 compound of cholesterol and Beta-sitosterol with a mass ratio 1 to 3:1; sophoridine 10 to 25; 125 to 200 compound of dextran 40 and mannitol with a mass ratio 1: 7 to 9; 5 to 10reduced glutathione; and poloxamer F-6835-40. The invention also provides the preparation method of the sophoridine nanoliposome. The drug provided in the invention can be used to treat adenocarcinoma, inflammation, gout, progressive disease of the central nervous system, to relieve pain and treat viral myocarditis.

Description

technical field [0001] The invention relates to sophoridine nano liposome medicine and its preparation. Background technique [0002] Sophocarine, molecular formula C 15 h 24 N 2 O, with a molecular weight of 248, is an alkaloid extracted from the leguminous plant Sophora sophora. [0003] The existing sophoridine preparation technology has achieved a leap from the complex Sophora sophorae extract to an effective monomer drug, which can be used to prepare and treat adenocarcinoma, anti-inflammatory, anti-gout, anti-central nervous degenerative diseases, analgesia and viral Myocarditis drugs. Adenocarcinoma refers to cancers that occur on the basis of glands, including breast cancer, nasopharyngeal cancer, lung cancer, tongue cancer, esophageal cancer, gastric cancer, intestinal cancer, liver cancer, and cervical cancer. However, the sophoridine preparations in the prior art are not ideal in the control of toxic and side effects, and there are also adverse reactions such...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K9/12A61K9/127A61K9/19A61K47/42A61P9/00A61P19/06A61P25/00A61P29/00A61P31/12A61P35/00A61K47/18
Inventor 蔡海德
Owner 江苏德伦生物制药有限公司
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