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Breviscapinum long-circulating nanoliposome and its preparation method

A nano-liposome and breviscapine technology, applied in the field of medicine, can solve the problems of unsafe, unfavorable treatment, low solubility of breviscapine, etc., and achieve the advantages of facilitating absorption, prolonging drug action time, and improving storage stability Effect

Inactive Publication Date: 2006-10-11
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the low solubility of breviscapine, clinically used injections are generally prepared under alkaline conditions and solubilized with surfactants such as Tween 80, which has unsafe factors
And breviscapine is eliminated very quickly in the body, which is not conducive to the treatment

Method used

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  • Breviscapinum long-circulating nanoliposome and its preparation method

Examples

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Embodiment 1

[0024] Embodiment 1, the preparation of a kind of breviscapine long circulation nano-liposome

[0025] (1) Egg yolk lecithin 1.50g, cholesterol 0.56g, polyethylene glycol derivatized phospholipid (PEG 2000 -DSPE) 0.51g and scutellarin 0.15g were added into 200ml ethanol for ultrasonic dissolution, and then the dissolving solution was placed in a 2500ml round bottom flask. (2) Evaporate the round-bottom flask under reduced pressure in a constant temperature water bath at 38°C to remove the organic solvent in the solution, so that film-forming materials such as phospholipids form a uniform film on the bottle wall, and continue to idle for 1 hour under the protection of nitrogen. (3) Add 100ml of 0.9% NaCl solution to the round bottom flask for hydration, rotate until the film formed on the wall of the flask is completely washed off, then add 1.0g of mannitol. (4) Extrude the mixture in the bottle twice through a 0.45 μm microporous membrane through an extruder to obtain brevisc...

Embodiment 2

[0042] Embodiment 2, the preparation of a kind of breviscapine long circulation nano-liposome

[0043] (1) Egg yolk lecithin 1.50g, cholesterol 0.35g, polyethylene glycol derivatized phospholipid (PEG 2000 -DSPE) 0.71g, breviscapine 0.20g, were added into 200ml ethanol for ultrasonic dissolution, and then the solution was placed in a 2500ml round bottom flask. (2) Evaporate the round-bottom flask under reduced pressure in a constant temperature water bath at 38°C to remove the organic solvent in the solution, so that film-forming materials such as phospholipids form a uniform film on the bottle wall, and continue to idle for 1 hour under the protection of nitrogen. (3) Add 100ml of 0.9% NaCl solution to the round bottom flask for hydration, rotate until the film formed on the wall of the flask is completely washed off, then add 3.0g of sucrose. (4) Continuously extruding the mixture in the bottle through a 0.45 μm microporous filter membrane through an extruder to obtain brev...

Embodiment 3

[0045] Embodiment 3, the preparation of a kind of breviscapine long circulation nano-liposome

[0046] (1) Egg yolk lecithin 1.50g, cholesterol 0.77g, polyethylene glycol derivatized phospholipid (PEG 2000 -DSPE) 0.30g, breviscapine 0.10g, were added to 200ml ethanol for ultrasonic dissolution, and then the solution was placed in a 2500ml round bottom flask. (2) Evaporate the round-bottom flask under reduced pressure in a constant temperature water bath at 38°C to remove the organic solvent in the solution, so that film-forming materials such as phospholipids form a uniform film on the bottle wall, and continue to idle for 1 hour under the protection of nitrogen. (3) Add 100ml of 0.9% NaCl solution to the round bottom flask for hydration, rotate until the film formed on the wall of the flask is completely washed off, then add 2.0g of glucose. (4) Continuously extruding the mixture in the bottle through a 0.45 μm microporous filter membrane through an extruder to obtain brevis...

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Abstract

The invention discloses a breviscapinum long-circulating nanoliposome and its preparation method, wherein the constituents include breviscapine, phosphatide, polyethylene glycol derived phosphatide (PEG2000-DSPE) and cholestrin by a molar ratio of 55:25-55:3-7:2.2-18.3, the dose type of the medicinal preparation includes injections, freeze-dried powder injections and sprays. The phospholipids can be soya bean lecithin, yolk phosphatidy icholine, hydrogenated soya bean lecithin, hydrogenated yolk lecithin, di-palmityl phosphatidyl choline or DPOG.

Description

technical field [0001] The invention relates to a medicine, in particular to a breviscapine long-circulation nano liposome and a preparation method thereof. Background technique [0002] The major issue brought about by human aging is the prevention and treatment of senile diseases. With the increase of the proportion of cardiovascular and cerebrovascular diseases, people's requirements for the quality of drugs are increasing day by day. At present, the traditional Chinese medicines used in cardiovascular and cerebrovascular diseases not only have few varieties, but also are mostly in traditional dosage forms, and the efficacy is not ideal. Breviscapine (breviscapine) is an active ingredient extracted from the chrysanthemum Breviscapine plant Breviscapine, which is a mixture of breviscapine and breviscapine. Pharmacological studies have shown that breviscapine can expand cerebral blood vessels, reduce cerebral vascular resistance, increase cerebral blood flow, improve micro...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/127A61P9/00
Inventor 罗国安田维维刘清飞王义明胡新宙
Owner TSINGHUA UNIV
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