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Ligustrazine microcosmic salt liposome medicine and preparing method

Ligustrazine phosphate lipid and liposome technology, which can be used in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problem of weak ability of antibody oxidation in vitro and in vivo peroxidation, obvious side effects of digestive system, stable drug Sexuality is not high, to achieve the effect of reducing the number of medications, improving curative effect, and uniform release

Inactive Publication Date: 2010-02-03
HUNAN KANGDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, in the prior art, ligustrazine phosphate medicine still has side effects, especially the side effects of the digestive system are obvious, and at the same time, the number of administrations per day is high. Even if it is intravenously dripped, it still needs to be administered twice a day, and each time takes 3-4 hours.
Inconveniencing both patients and doctors and consuming time
At the same time, the stability of the drug is still not high, especially the ability of anti-oxidation in vitro and peroxidation in vivo is not strong

Method used

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  • Ligustrazine microcosmic salt liposome medicine and preparing method
  • Ligustrazine microcosmic salt liposome medicine and preparing method
  • Ligustrazine microcosmic salt liposome medicine and preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The formula adopted in the present embodiment is as follows (consumption unit: gram):

[0031] Egg yolk lecithin, sheep brain lecithin 4:1 mixture by weight 200;

[0032] Stigmasterol and campesterol weight ratio 3: 1 mixture 170;

[0033] Reduced Glutathione 2.5;

[0034] Ligustrazine Phosphate 15;

[0035] tert-butanol, absolute ethanol, acetone weight ratio 1: 0.01: 0.02 mixture 720;

[0036] Polyethylene glycol-2000, Tween 80 weight ratio 4: 0.5 mixture 140;

[0037] Hypromellose 100.

[0038] In this embodiment, 1700 grams of 0.01 M phosphate buffer solution with a pH of 3.0-7.5 is used.

[0039] The preparation method of the present embodiment is as follows:

[0040] (1) egg yolk lecithin, sheep brain lecithin, stigmasterol, and campesterol are dissolved in the tert-butanol, dehydrated alcohol and acetone mixed solution of the amount described, fully dissolved completely;

[0041] (2) The amount of reduced glutathione, ligustrazine phosphate, polyethylene g...

Embodiment 2

[0056] The formula adopted in the present embodiment is as follows (consumption unit: gram):

[0057] Egg yolk lecithin, sheep brain lecithin 4:1 weight ratio mixture 260;

[0058]Stigmasterol and campesterol weight ratio 3: 1 mixture 200;

[0059] Reduced Glutathione 6;

[0060] Ligustrazine Phosphate 20;

[0061] tert-butanol, absolute ethanol, acetone weight ratio 1: 0.01: 0.07 mixture 1000;

[0062] Polyethylene glycol-2000, Tween 80 weight ratio 4: 1 mixture 150;

[0063] Hypromellose 110.

[0064] In this embodiment, 2500 grams of 0.01 M phosphate buffer solution with pH 3.0-7.5 is used.

[0065] The preparation method of the present embodiment is as follows:

[0066] (1) egg yolk lecithin, sheep brain lecithin, stigmasterol, and campesterol are dissolved in the tert-butanol, dehydrated alcohol and acetone mixed solution of the amount described, fully dissolved completely;

[0067] (2) The amount of reduced glutathione, ligustrazine phosphate, polyethylene glycol-...

Embodiment 3

[0082] The formula adopted in the present embodiment is as follows (consumption unit: gram):

[0083] Egg yolk lecithin, sheep brain lecithin 4:1 mixture by weight 330;

[0084] Stigmasterol and campesterol weight ratio 3: 1 mixture 280;

[0085] Reduced Glutathione 10;

[0086] Ligustrazine Phosphate 25;

[0087] tert-butanol, absolute ethanol, acetone weight ratio 1: 0.05: 0.027 mixture 1200;

[0088] Polyethylene glycol-2000, Tween 80 weight ratio 4:1 mixture 160;

[0089] Hypromellose 120.

[0090] In this embodiment, 2800 grams of 0.01 M phosphate buffer solution with a pH of 3.0-7.5 is used.

[0091] The preparation method of the present embodiment is as follows:

[0092] (1) egg yolk lecithin, sheep brain lecithin, stigmasterol, and campesterol are dissolved in the tert-butanol, dehydrated alcohol and acetone mixed solution of the amount described, fully dissolved completely;

[0093] (2) The amount of reduced glutathione, ligustrazine phosphate, polyethylene gly...

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Abstract

The invention relates to a tetramethylpyrazine phosphate liposome drug and a preparation method; wherein, the drug is characterized in that: the effective efficacy components and weight accounts of the liposome drug are as following: a mixture 200 to330 with a weight ratio 4 to 1 of egg yolk lecithin and sheep cerebral lecithin, a mixture 170 to 280 with a weight ratio 3 to 1of stigmasterol and campestrol, reduction glutathione 2.5 to 10, tetramethylpyrazine phosphate 15 to 25, a mixture 720 to 1200 with a weight ratio 1 : 0.01 to 0.05 : 0.02 to 0.07 of tert-butyl alcohol, ethanol, acetone, amixture 140 to 160 with a weight ratio 4:05 to 1 of polyethylene glycol-2000 and tween 801, and hydroxyl propyl methyl cellulose 100 to 120. The invention also provides the preparation method for theliposome drugs. The invention has the advantages of adopting the provided drugs, enabling to decrease the drug dosage by two third and once a day, and improving the efficacy above fifteen percent.

Description

technical field [0001] The invention relates to a ligustrazine phosphate liposome medicine and a preparation method thereof. Background technique [0002] Ligustrazine is the monomer component extracted from Umbelliferae Ligusticum Chuanxiong, which can be synthesized artificially. Ligustrazine phosphate is more stable than Ligustrazine and Ligustrazine hydrochloride, and it is not easy to sublimate. The medicine made from ligustrazine phosphate can treat and prevent cardiovascular and cerebrovascular diseases, and has the advantages of quick effect, good curative effect and small side effects. [0003] However, in the prior art, ligustrazine phosphate still has side effects, especially the side effects of the digestive system are obvious, and at the same time, the number of administrations per day is high. Even if it is intravenously infused, it still needs to be administered twice a day, and each time takes 3-4 hours. All bring inconvenience to patient and doctor, consum...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/34A61K31/4965A61P9/00A61K47/10A61K47/26A61K47/38
Inventor 蔡海德
Owner HUNAN KANGDU PHARMA
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