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Strychnine composite phospholipid liposome, and preparation method thereof and use in pharmacy

A technology of complex phospholipids and strychnine, which is applied in the direction of liposome delivery, antineoplastic drugs, drug combination, etc., to achieve the effects of not easy to leak, save cost, and reduce ICSO

Inactive Publication Date: 2009-04-15
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0003] Pharmacological studies have shown that strychnine may be the most promising active ingredient in strychnine alkaloids: ①Anti-tumor experiments show that the activity of strychnine is significantly higher than that of strychnine and strychnine nitrogen oxides , Strychnine and other alkaloid components in strychnine; ②The anti-arthritis test also shows that strychnine has no therapeutic effect but strychnine has definite curative effect; ③Strychnine has an ideal sedative effect ④ The toxicity of strychnine is much lower than that of strychnine, and the toxic dose of strychnine is 71 times that of strychnine when taken orally, and 45 times when injected

Method used

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  • Strychnine composite phospholipid liposome, and preparation method thereof and use in pharmacy
  • Strychnine composite phospholipid liposome, and preparation method thereof and use in pharmacy
  • Strychnine composite phospholipid liposome, and preparation method thereof and use in pharmacy

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Embodiment 1

[0034] Embodiment 1: Preparation of strychnine complex phospholipid liposome

[0035] Weigh 1080mg of soybean lecithin, 120mg of hydrogenated soybean lecithin, and 200mg of cholesterol and dissolve them in 20ml of absolute ethanol, inject into 50ml of 0.2mol / L ammonium sulfate solution, transfer to an eggplant-shaped bottle, recover under reduced pressure to remove ethanol, add water to 50ml, Use an ultrasonic cell pulverizer to sonicate for 10 minutes, pass through a 0.22 μm microporous filter membrane, put it into a dialysis bag, and dialyze it with 20 times the volume of pH7.4 phosphate buffer for 4 times, each time for 2 hours, to remove the ammonium sulfate in the outer water phase, The blank composite phospholipid liposome was obtained. Weigh 350 mg of strychnine, add it to the blank complex phospholipid liposome, and shake in a constant temperature water bath at 60°C for 20 minutes to obtain a suspension of 7 mg / ml strychnine complex phospholipid liposome, which is a mi...

Embodiment 2

[0036] Embodiment 2: Preparation of strychnine complex phospholipid liposome

[0037] Weigh 1080mg of soybean lecithin, 120mg of hydrogenated soybean lecithin, and 400mg of cholesterol and dissolve them in 20ml of absolute ethanol, inject into 50ml of 0.2mol / L ammonium sulfate solution, transfer to an eggplant-shaped bottle, recover under reduced pressure to remove ethanol, add water to 50ml, Use an ultrasonic cell pulverizer to sonicate for 10 minutes, pass through a 0.22 μm microporous filter membrane, put it into a dialysis bag, and dialyze it with 20 times the volume of pH7.4 phosphate buffer for 4 times, each time for 2 hours, to remove the ammonium sulfate in the outer water phase, The blank composite phospholipid liposome was obtained. Weigh 100 mg of strychnine, add it to the blank complex phospholipid liposome, and shake in a constant temperature water bath at 25°C for 20 minutes to obtain a 2 mg / ml strychnine complex phospholipid liposome suspension, which is a milky...

Embodiment 3

[0038] Embodiment 3: the preparation of strychnine complex phospholipid liposome

[0039] Weigh 600mg of egg phospholipids, 600mg of dipalmitoylphosphatidylcholine, and 250mg of cholesterol and dissolve them in 30ml of absolute ethanol, inject into 50ml of 0.25mol / L ammonium sulfate solution, evaporate the ethanol at 60°C, add water to 50ml, and use high-pressure Homogenize with a homogenizer pump, pass through a 0.22 μm microporous membrane, and elute with pH 7.4 phosphate buffer on a Sephadex column to collect liposomes to obtain blank complex phospholipid liposomes. Weigh 50 mg of strychnine, add it to the blank complex phospholipid liposome, and shake in a constant temperature water bath at 25°C for 40 minutes to obtain 1 mg / ml strychnine complex phospholipid liposome suspension, which is a milky white suspension that is clear to light liquid.

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Abstract

The invention discloses a strychnine compound phospholipid liposome which is prepared by two types of phospholipids, strychnine and cholesterol in certain weight ratio. The preparation method for the strychnine compound phospholipid liposome comprises the following steps: (1) dissolving the first type phospholipid, the second class phospholipid and the cholesterol in absolute ethyl alcohol, and injecting the aqueous solution of ammonia sulfate into the mixture ; (2) removing the alcohol through heating or decompression method; (3) carrying out ultrasonic processing or high-pressure emulsion homogenization to reduce the grain size of the liposome; (4) removing the ammonia sulphate which is not encapsulated by the liposome through a dialysis method, an ultrafiltration method or a gel column chromatographic method so as to form blank liposome suspension; and (5) adding the strychnine into the suspension, and carrying out moderate incubation so as to enable the strychnine to be encapsulated by the liposome. The strychnine compound phospholipid liposome has significant characteristics of high encapsulating rate of the liposome for the strychnine, greatly improved stability, no easy leakage, and remarkably improved medicine carrying capacity. The results of tumor resisting experiments show that the cancer resisting effect of the strychnine compound phospholipid liposome is remarkably higher than that of a common single phospholipid liposome.

Description

1. Technical field [0001] The invention relates to the technical field of traditional Chinese medicine, in particular to a strychnine complex phospholipid liposome, a preparation method thereof and an application in preparation of antitumor drugs. 2. Background technology [0002] Strychnosnux vomica L., also known as Snuggle, was first recorded in "Compendium of Materia Medica Volume 18". It is the dry mature seed of Strychnosnux vomica L., which is warm in nature, bitter in taste, and highly poisonous. Return liver, spleen meridian, have the effect of dispelling stagnation and detumescence, dredging collaterals and relieving pain. Nuxychnium main active ingredient is alkaloid composition, with strychnine (strychnine, C 21 h 22 o 2 N 2 ) and strychnine (brucine, C 23 h 26 o 4 N 2 ) mainly. [0003] Pharmacological studies have shown that strychnine may be the most promising active ingredient in strychnine alkaloids: ①Anti-tumor experiments show that the activity of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/475A61K47/24A61P35/00
Inventor 蔡宝昌陈军胡敏敏王玮张婷高颖陈志鹏
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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