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Liposome of Breviscapine and its preparing method

A technology of breviscapine lipid and breviscapine, which is applied in the field of medicine, can solve the problems of low bioavailability, poor absorption, and poor stability of breviscapine injection, and achieve the effect of improving curative effect and stability

Inactive Publication Date: 2003-10-01
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide breviscapine liposome and proliposome and preparation method thereof, to improve the poor oral absorption of breviscapine, low bioavailability; the defect of poor stability of breviscapine injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Preparation of breviscapine liposomes by ethanol injection

[0012] Take soybean lecithin, cholesterol, V E After adding absolute ethanol to dissolve, inject into scutellarin aqueous solution, stir at constant temperature at high speed, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane to segregate, and obtain scutellarin liposome with an encapsulation efficiency of 64.8%.

Embodiment 2

[0014] Preparation of breviscapine liposomes by film dispersion method

[0015] Take soybean lecithin, cholesterol, V E Dissolve 15ml of chloroform in a 150ml eggplant-shaped bottle, form a film under reduced pressure on a rotary thin-film evaporator and remove all organic solvents, add 10ml of scutellarin aqueous solution to hydrate, pass through a microporous membrane to granulate, and obtain scutellarin lipid body with an encapsulation efficiency of 59.2%.

Embodiment 3

[0017] Preparation of breviscapine liposomes by reverse-phase evaporation

[0018] Weigh soybean lecithin, cholesterol, V E Add 5ml of chloroform to dissolve, then add 10ml of ether, then add 15ml of breviscapine in phosphate buffer, bath ultrasonic to form a homogeneous single-phase system, evaporate under reduced pressure to remove chloroform and ether until gel is formed, continue to evaporate under reduced pressure for 5 ~10 minutes, vortex until the aqueous suspension, that is, liposomes, is formed. The encapsulation efficiency was 24.6%.

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Abstract

A liposome of breviscapine for preparing the medicines to cure cerebral thrombus and coronary heart disease is prepared from breviscapine, phosphatide, cholesterol, and supporting agent chosen from sorbitol, mannitol, cane sugar, sodium chloride, water-soluble starch, etc by different methods. Its advantages are high absorption rate, high biologic utilization rate, and high stability.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a scutellarin liposome (including proliposome) and a preparation method thereof. Background technique: [0002] Breviscapus is an active ingredient of flavonoids extracted from the Chinese herbal medicine Erigeron breriscapus (vant) Handmazz. A large number of clinical studies have shown that its therapeutic effect is significantly better than that of compound salvia miltiorrhiza. Pharmacological studies have shown that breviscapine can expand cerebral blood vessels and relax coronary arteries, reduce cerebrovascular resistance, improve blood lipid barrier permeability, significantly increase cerebral blood flow and cardiac coronary flow, improve microcirculation and resist platelet aggregation , Inhibit coagulation function in vivo, promote fibrinolytic activity. Clinically, it is mainly used to treat cardiovascular and cerebrovascular diseases such as cerebral thrombosis, c...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K47/24A61K47/26A61K47/36A61P9/10
Inventor 邓英杰钟海军
Owner SHENYANG PHARMA UNIVERSITY
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