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Nanometer antiviral liposome medicine and its prepn

A nano-liposome and drug technology, which is applied in antiviral agents, liposome delivery, pharmaceutical formulations, etc., can solve the problems of adverse reactions and low oral bioavailability, so as to avoid relapse, improve blood circulation and Microcirculation, the effect of improving curative effect

Inactive Publication Date: 2007-08-22
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

[0003] However, the existing adefovir dipivoxil has gradually exposed the following deficiencies in clinical practice: the oral bioavailability is not high, adverse reactions, especially the safety issues of liver and kidney adverse reactions in patients need to be solved or improved

Method used

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  • Nanometer antiviral liposome medicine and its prepn
  • Nanometer antiviral liposome medicine and its prepn
  • Nanometer antiviral liposome medicine and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The present embodiment provides a kind of nano liposome medicine, comprises alprostadil and adefovir dipivoxil, comprises the raw material of following parts by weight:

[0030] Alprostadil and adefovir dipivoxil

[0031] Mixture 10.1 in a weight ratio of 0.1:50;

[0032] Soy lecithin 88;

[0033] Cholesterol and soybean sterol weight ratio 9: 1 mixture 40;

[0034] Equal weight mixture of polyethylene glycol 4000 and polyethylene glycol 2000 15;

[0035] Sodium Glucuronate 100;

[0036] Vitamin C 160;

[0037] Reduced Glutathione 5.

[0038] The preparation method of above-mentioned medicine, the steps are as follows:

[0039] (1) get the mixture of alprostadil and adefovir dipivoxil weight ratio 0.1-1.0: 50-300 of said amount, soybean lecithin, cholesterol and soybean sterol weight ratio 9: 1 mixture and dissolve in ethanol or ether, prepare into solution;

[0040] (2) Get the solution prepared in step (1) and evaporate to dryness in a rotary evaporator to mak...

Embodiment 2

[0052] The present embodiment provides a kind of nano liposome medicine, comprises alprostadil and adefovir dipivoxil, comprises the raw material of following parts by weight:

[0053] Alprostadil and adefovir dipivoxil

[0054]Mixture with a weight ratio of 0.65:260 56.7

[0055] Soy Lecithin 368;

[0056] Cholesterol and soybean sterol weight ratio 9:1 mixture 181;

[0057] Equal weight mixture of polyethylene glycol 4000 and polyethylene glycol 2000 31;

[0058] Sodium Glucuronate 240;

[0059] Vitamin C 723;

[0060] Reduced glutathione 7.8.

[0061] The preparation method of above-mentioned medicine refers to embodiment 1.

[0062] The curative effect verification of the medicine prepared in the present embodiment is as follows:

[0063] One-day-old Beijing female ducks were taken as a model infected with hepatitis B virus, and administered on the eighth day after infection. . Before infection, 7 days after infection, on the 5th and 10th day after administration,...

Embodiment 3

[0068] The present embodiment provides a kind of nano liposome medicine, comprises alprostadil and adefovir dipivoxil, comprises the raw material of following parts by weight:

[0069] Alprostadil and adefovir dipivoxil

[0070] Mixture 80.2 in a weight ratio of 1.0:300;

[0071] Soy Lecithin 440;

[0072] Cholesterol and soybean sterol weight ratio 9: 1 mixture 200;

[0073] Equal weight mixture of polyethylene glycol 4000 and polyethylene glycol 2000 40;

[0074] Sodium Glucuronate 280;

[0075] Vitamin C 800;

[0076] Reduced Glutathione 10.

[0077] The preparation method of above-mentioned medicine refers to embodiment 1.

[0078] The curative effect verification of the medicine prepared in the present embodiment is as follows:

[0079] One-day-old Beijing female ducks were taken as a model infected with hepatitis B virus, and administered on the eighth day after infection. . Before infection, 7 days after infection, on the 5th and 10th day after administration, ...

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Abstract

The present invention relates to one kind of nanometer antiviral liposome medicine and its preparation process. The nanometer antiviral liposome medicine includes the mixture of alprostadil and Adefovir dipivoxil in the weight ratio of 0.1-1.0 to 50-300 in 10.1-80.2 weight portions, soybean lecithin 88-440 weight portions, the mixture of cholesterol and soyasterol in the weight ratio of 9 to 1 in 40-200 weight portions, the mixture of polyglycol-4000 and polyglycol-2000 in the same ratio in 15-40 weight portions, sodium glucuronate in 100-280 weight portions, vitamin C in 160-800 and glutathione in 5-10 weight portions. The nanometer antiviral liposome medicine is used as the broad spectrum antiviral medicine.

Description

technical field [0001] The invention relates to a broad-spectrum antiviral nano-liposome medicine and a preparation method thereof. Background technique [0002] Adefovir dipivoxil (adeforir dipiroxil), chemical name [[2-(6-amino-9H-purin-9-yl) ethoxy] methyl] phosphate di-(pivaloyloxymethyl) ester, It is a nucleoside virus inhibitor developed by Gilead Sciences in the United States. It was first launched in the United States in 2002. Its trade name is Hepsera and it has broad-spectrum antiviral activity. Its antiviral spectrum includes: anti-HIV-I and HIV-II AIDS virus, anti-hepatitis B virus HBV, and has a good effect on derived HBV and lamivudine-resistant HBV, and anti-herpes virus HSV- Type I and HSV-II type herpes simplex virus, anti-HIV co-infected cytomegalovirus, anti-Epstein-Barr virus, anti-moloney mouse sarcoma virus, also has the prospect of anti-other heterogeneous viruses. It is a drug with broad market prospect. [0003] However, the existing adefovir dipi...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61K9/00A61K9/12A61K9/19A61K9/20A61K9/48A61K9/127A61K47/42A61K47/24A61P31/12A61K31/5575A61K47/20A61K47/28
Inventor 蔡海德
Owner 江苏德伦生物制药有限公司
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