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Carmustine powder injection and preparation technology thereof

A card nitrogen mustard powder and a card nitrogen mustard technology are applied in the directions of powder delivery, medical preparations with inactive ingredients, amide active ingredients, etc., which can solve the problems of influence, drug leakage, instability, etc., and achieve obvious tumor reduction, good effect

Active Publication Date: 2011-09-28
天津易诺利和科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, carmustine liposomes still have instability in the solution state, such as drug leakage, particle aggregation, oxidation and hydrolysis of phospholipids in liquid state, which affect their practical application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 100g of refined soybean lecithin, 25g of cholesterol, 12.5g of carmustine, and 412.5g of mannitol, use diethyl ether as solvent, shake in the same direction to dissolve until clear, place, filter, and spray on the mannitol crystal powder that is constantly stirring , mix well. Dry it under vacuum at 0.75-0.1Mpa to recover ether. The ether content in the obtained product cannot be detected. Packed into 100 tubes and filled with 99.99% high-purity nitrogen, sealed. Wherein in the refined soybean lecithin, the weight content of phosphatidylcholine is 66%, and the weight content of phosphatidylethanolamine is 20%.

Embodiment 2

[0027] Weigh 108g of refined soybean lecithin, 30.5g of cholesterol, 14.6g of carmustine, and 396.9g of mannitol, use ether as the solvent, shake in the same direction to dissolve completely, place, filter, and spray on the mannitol crystal powder that is constantly stirring , mix well. Dry it under vacuum at 0.75-0.1Mpa to recover ether. The product is inspected, subpackaged after passing the test, filled with 99.99% high-purity nitrogen, and sealed. Among them, in the refined soybean lecithin, the weight content of phosphatidylcholine is 70%, and the weight content of phosphatidylethanolamine is 14.3%.

Embodiment 3

[0029] Weigh 91.6g of refined soybean lecithin, 22.9g of cholesterol, 10.5g of carmustine, and 425g of mannitol, use diethyl ether as solvent, shake in the same direction to completely dissolve, place, filter, and spray on the mannitol crystal powder that is constantly stirring , mix well. Dry in vacuo to recover ether. The obtained product is subpackaged into 100 bottles after passing the test, and filled with 99.99% high-purity nitrogen gas, and sealed. Among them, in the refined soybean lecithin, the weight content of phosphatidylcholine is 67.6%, and the weight content of phosphatidylethanolamine is 17.1%.

[0030] Get a certain amount of the above-mentioned embodiment gained product, be dissolved in water and obtain carmustine injection, detect wherein free BCNU content, encapsulation rate, particle size and dispersion time etc., test result is as follows:

[0031]Test results of carmustine powder injection

[0032]

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PUM

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Abstract

The invention relates to a pro-liposome carmustine powder injection and a preparation process thereof. The carmustine powder injection mainly comprises, by weight, 1.5 to 3 % of carmustine, 15 to 20% of granulesten, 4 to 6% of cholesterol and 71.1 to 79.5% of mannitol crystalline powders, wherein the granulesten comprises, by weight, 65 to 70% of phosphatidylcholine and 14 to 20% of phosphatidylethanolamine. The carmustine powder injection prepared by the preparation process is easy to disperse in water and convenient in storage, and has an entrapment rate of 100%, a small particle size, improved stability, small toxic and side effects and enhanced safety.

Description

Technical field: [0001] The invention relates to a powder injection formulation and a preparation process in which carmustine is used as a medicine in the form of proliposome. Background technique: [0002] Carmustine (Canmustin), also known as carmustine (molecular formula C 5 h 9 Cl 2 N 3 o 2 ), referred to as CBNU, is a broad-spectrum anticancer drug with high fat solubility and easy passage through the blood-brain barrier. The curative effect is good, and its anti-cancer mechanism is to interact with DNA polymerase to inhibit the synthesis of RNA and DNA, and has a strong killing effect on brain tumor cells, and its effect is similar to that of alkylating agents. While inhibiting brain tumor cells, BCNU also kills normal cells. It mainly acts on the bone marrow hematopoietic system, and the inhibition on white blood cells and platelets is more obvious. It usually occurs within 3 to 5 weeks after administration. During the administration period, nausea, vomiting, lo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/02A61P35/00A61P35/04A61K31/17A61K47/28A61K9/14
Inventor 马淑贤
Owner 天津易诺利和科技有限公司
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