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Flexible nano realgar liposome as well as preparation method and application thereof

A nano-realgar, nano-technology, applied in liposome delivery, making medicines into special physical or taking forms of devices, sexual diseases, etc. Anti-tumor effect, poor gastrointestinal absorption, etc., to achieve strong practicability and economic significance, relieve medical resource shortage, reduce toxic and side effects

Inactive Publication Date: 2011-03-02
程艳香 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But ① there is currently no research to track and mark the anti-tumor molecular components of realgar in vitro and in vivo; ② realgar is sensitive to temperature and light, has unstable properties, and is easily converted into arsenic (that is, produced by As 4 S 4 Convert to As 2 o 3 ); ③As 4 S 4 and As 2 o 3 The anti-tumor and toxicity mechanisms are the same. As binds to the sulfhydryl group of the enzyme protein, interferes with the activity of sulfhydryl enzymes, affects cell biological metabolism, stress repair, oncogene expression, induces cancer cell apoptosis, and inhibits cancer cell cycle progression, etc. ; ④As 2+ Extremely difficult to dissolve in water, poor absorption in the gastrointestinal tract, low bioavailability, difficult to achieve anti-tumor effect; ⑤As 2 o 3 Compared with As 4 S 4 More toxic, which is the necessary basis for arsenic preparations to inhibit vigorous cancer cells in small doses and in a short-term manner

Method used

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  • Flexible nano realgar liposome as well as preparation method and application thereof
  • Flexible nano realgar liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-16

[0030] A flexible nano-realgar liposome, which contains the following main drugs and auxiliary materials in parts by weight:

[0031] Example

realgar

Sodium Deoxycholate

Natural Soy Lecithin

cholesterol

Vitamin E

gelatin

1

0.25

100

500

100

200

30

2

0.30

500

100

100

100

1

3

0.35

150

200

150

700

5

4

0.40

175

300

200

300

10

5

0.45

200

400

225

450

15

6

0.50

100

500

100

200

30

7

0.55

250

750

250

400

20

8

0.60

275

1000

275

500

25

9

0.65

300

1500

300

600

30

10

0.70

350

2000

325

675

35

11

0.75

375

2500

350

750

37

12

0.80

400

3000

375

800

40

13

0.85

425

3750

400

900

42

14

0.90

450

4500

475

950

47

[0032] 15

0.95

500

5000

500

1000

50

16

1.0

100

500

100

200

30

[0033] The preparation method is as follows:

[0034] The raw material realgar that has been crushed and passed through a 500-mesh sieve is added with distilled water at a ratio of 1g:100mL of re...

Embodiment 17

[0039] A flexible nano-realgar liposome, the preparation method is as follows: the raw material realgar powder pulverized by a ball mill is passed through a 500-mesh sieve, and 25 mg is weighed, 2500ml of distilled water is added, magnetically stirred for 30 minutes, and then added to the microjet granulator, 10 cycles , The speed of the last cycle is 5000rpm, the speed of the first 9 cycles is 30,000rpm, then ultrasonic vibration 30mim, and then sterilized by 0.22μm microporous filter, sealed and protected from light at 4℃ to obtain nano realgar suspension;

[0040] Put 50g natural soybean phospholipids, 10g cholesterol and 20g vitamin E in a round bottom flask, add absolute ethanol until the above mixture is just completely dissolved, ultrasonicate for 2min, place in a 23℃ water bath and evaporate under reduced pressure on a rotary evaporator until the organic solvent is completely volatilized , A film is formed on the bottle wall. Take the previously prepared nano realgar susp...

Embodiment 18

[0043] Realgar 50mg and distilled water 5000ml instead of the main drug dosage of Example 17 and the amount of distilled water added to the realgar after sieving, the remaining components and the preparation method are the same as in Example 17, to obtain the flexible nano realgar resin containing 50mg of the main drug realgar Plasma membrane.

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PUM

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Abstract

The invention discloses a flexible nano realgar liposome as well as a preparation method and application thereof, which is used for solving the problems of unabiding medicine potency, weak targeting performance and the like in medicines for treating cervical carcinoma in the prior art. The flexible nano realgar liposome contains the main drug of realgar and the auxiliary materials of deoxysodium cholate, natural soya lecithin, cholesterol, vitamin E and the like. In the method of the invention, the realgar is processed by using a nano Chinese medicine technique, thereby preparing the realgar into membranous flexible nano realgar liposome. The flexible nano liposome is a targeting medicine carrier with high self deformation, can penetrate through skin pore canals which are multiple times smaller than the liposome, has the characteristics of lipotropy, hydrophilicity, high permeation efficiency, high flexibility, high compatibility and the like, and has great potential in the field of targeting administration therapy for cervical carcinoma.

Description

Technical field [0001] The present invention relates to the technical field of a medicine and its preparation method and application, in particular to a flexible nano-realgar liposome and its preparation method and application. The product is suitable for cervix and other solid malignant entities capable of transdermal or mucosal administration. Tumor. Background technique [0002] The incidence of cervical cancer ranks first among malignant tumors of the female genital tract. The latest global data show that among women around the world, the number of new cases each year is 46,000, and 80% of the cases occur in developing countries. my country has 131,500 new cases each year, accounting for about 28.8% of the world’s new cases of cervical cancer. After decades of extensive gynecological surveys, the incidence and mortality of cervical cancer have been reduced by nearly 68%, but the prevalence of cervical cancer still ranks first among women in my country, and the incidence of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/36A61K9/127A61P35/00A61P15/00A61J3/00
Inventor 程艳香王晶陈滢陈干涛胡敏
Owner 程艳香
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