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Nux vomica alkaloid liposome, and its prepn. method

A technology of alkaloid lipid and strychnine, which is applied in the directions of liposome delivery, drug combination, active ingredients of heterocyclic compounds, etc. problem, to achieve the effect of high encapsulation rate

Inactive Publication Date: 2006-01-11
蔡宝昌 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are a large amount of clinical data on the treatment of cancer, Nuxychnium has large toxic and side effects, and the effective dose is close to the poisoning dose. Due to the unreasonable dosage form of the existing Nuxychnya preparations, some poisoning has been caused in clinical use. case, seriously restricting the application of Nuxyche in cancer treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Nuxychnium total alkaloids (abbreviated as total alkaloids) liposome and preparation of intravenous injection, oral liquid and external gel:

[0042] Prescription: Nuxychnium total alkaloids 5mg, soybean lecithin 300mg, cholesterol 45mg, other medicinal excipients in appropriate amount

[0043] Preparation method: (1) Preparation of total alkaloid liposome suspension of Strychnis chinensis: Weigh soybean lecithin and cholesterol dissolved in 30ml of chloroform, place in a 2000ml pear-shaped bottle, and place on a rotary evaporator with 60-100r Rotary evaporation of chloroform under the condition of rotating speed per minute and water bath constant temperature of 30°C to make the lipid evenly form a film on the inner wall of the pear-shaped bottle, and then dry in a vacuum dryer for 4-12 hours. Then add 20ml of 0.1mol / L ammonium sulfate aqueous solution, and then rotate the hydration and elute on the rotary evaporator under the conditions of 60-150r / min rotation speed, 4...

Embodiment 2

[0050] Preparation of strychnine liposomes:

[0051] Prescription: 10mg of strychnine, 600mg of soybean lecithin, 90mg of cholesterol, appropriate amount of other pharmaceutical excipients

[0052] Preparation method: Weigh soybean lecithin and cholesterol, dissolve them in 60ml chloroform, place them in a 2000ml pear-shaped bottle, and evaporate chloroform on a rotary evaporator at a speed of 60r / min and a water bath at a constant temperature of 30°C to make the lipids A film is uniformly formed on the inner wall of the pear-shaped bottle, and then dried in a vacuum desiccator for 4 to 12 hours. Then add 40 ml of 0.1 mol / L ammonium sulfate aqueous solution, rotate the hydration and elute the lipid film on the rotary evaporator under the conditions of 60-150 r / min, 40°C, and 500-600 mbar vacuum (to prevent oxidation). After all the elution, sonicate for 10 min, and squeeze out the blank liposomes with a 0.2 μm microfiltration membrane to obtain blank liposomes smaller than 20...

Embodiment 3

[0055] Preparation of strychnine liposome and its intravenous injection, oral liquid and external gel:

[0056] Prescription: 15mg of strychnine, 900mg of soybean lecithin, 135mg of cholesterol, appropriate amount of other pharmaceutical excipients

[0057] Preparation method: (1) Preparation of strychnine liposome suspension: Weigh 900 mg of soybean lecithin and 135 mg of cholesterol and dissolve them in 60 ml of chloroform, place them in a 2000 ml pear-shaped bottle, and place them on a rotary evaporator at 60 r / Under the condition of rotating speed of min and constant temperature of water bath at 30°C, the chloroform was evaporated by rotary evaporation to make the lipid evenly form a film on the inner wall of the pear-shaped bottle, and then dried in a vacuum desiccator for 4-12 hours. Then add 60 ml of 0.1 mol / L ammonium sulfate aqueous solution, rotate the hydration and elute the lipid film on the rotary evaporator under the conditions of 60-150 r / min, 40°C, and vacuum ...

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Abstract

An antineoplastic strychnos alkaloid liposome with 10w poison and high curative effect is proportionally prepared from strychnos alkaloid, phosphatide and cholesterol. Its preparing process by ammonium sulfate gradient method is also disclosed.

Description

1. Technical field [0001] The invention relates to a traditional Chinese medicine liposome and a preparation method thereof, in particular to a strychnium alkaloid liposome and a preparation method thereof. 2. Background technology [0002] Nuxychnos is the dry and mature seed of Strychnos nux-vomica L., a plant of the family Nuxaceae, which has the effects of dissipating blood heat, reducing swelling, and analgesia. Strychnine contains 2% to 5% of total alkaloids, mainly Strychnine (C 21 h 22 o 2 N 2 ), strychnine (Brucine, C 23 h 26 o 4 N 2 ) each account for about 1% to 1.4%, and also contain trace amounts of Vomicine, Pseudostrychnine, Pseudobrucine, α-Krubulin (α -Colubrine), β-Colubrine (β-Colubrine), glucoside (Loganin, C 17 h 26 o 10 ), chlorogenic acid, palmitic acid, fatty oil, protein, polysaccharide, etc. [0003] Nuxychnium was first recorded in "Compendium of Materia Medica", and since then various herbal medicines have more detailed records on the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61K9/127A61P25/02A61P25/00A61P9/10A61P21/04A61P29/00A61P19/02A61P19/08
Inventor 蔡宝昌刘陶世李彦超李伟东邓旭坤
Owner 蔡宝昌
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