Deoxyuridine powder injection and its preparing method

A technology of deoxyfluridine and oxyfluridine powder, which is used in powder delivery, pharmaceutical formulations, and medical preparations containing active ingredients, etc. problems, to achieve the effect of convenient transportation and storage, less irritation to injection, and stable quality

Active Publication Date: 2007-04-11
JIANGSU SHENLONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

"This application stabilizes the doxifluridine aqueous solution by adding malonic acid and Tween-80 as a stabilizer. However, due to the hemolytic effect and toxicity of Tween-80, it is not recommended to use Tween-80 in general infusion formulations. 80 as an additive
[0004] In addition, the patent found that although doxifluridine is soluble in water, the dissolution rate is relatively slow
Freeze-dried formulations must be dissolved in water for injection during clinical use, and the slow dissolution rate will definitely cause inconvenience to medical staff
In addition, doxifluridine is irritating to blood vessels when injected, which will also bring additional pain to patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 5

[0041] Example 5: Weigh 100g of doxifluridine and 30g of mannitol, put them in a container, add 1600ml of water for injection, stir while adding, until completely dissolved. Add 0.3 g of activated carbon and stir for 15 minutes. The solution was decarburized by filtering through a sand filter. The filtrate was finely filtered with a microporous membrane to obtain a sterile solution. Dispense the sterile solution into sterilized vials by direct dispensing method. Pre-freeze to -27°C, turn on the condenser until the temperature of the solution drops to -50°C, turn on the vacuum system, gradually increase the temperature until the sample is dry, crimp the cap and seal, and pack it.

example 6

[0042] Example 6: Weigh 100g of doxifluridine and 40g of low-molecular-weight dextran (“low-molecular-weight dextran” refers to dextran-40, the same below), put them in a container, add 2000ml of water for injection, and stir while adding until completely dissolve. Then add 0.5 g of activated carbon and stir for 20 minutes. The solution was decarburized by filtration through a vertical sintered glass funnel. The filtrate was finely filtered with an ultrafiltration machine to obtain a sterile solution. Dispense the sterile solution into sterilized vials by direct dispensing method. Pre-freeze to -25°C, turn on the condenser until the temperature of the solution drops to -50°C, turn on the vacuum system, gradually raise the temperature until the sample is dry, crimp the cap and seal it, and pack it.

[0043] See Table 7-1 for the prescriptions and process parameters of Example 7, Example 8, Example 9, and Example 10, and see Example 5 for specific preparation methods.

example 11

[0044] Example 11: Weigh 100 g of doxifluridine and 2 g of α-cyclodextrin, put them in a container, add 100 ml of water for injection, and stir while adding until completely dissolved. Then add 0.01 g of activated carbon and stir for 1 min. The solution was decarburized by filtering through a titanium filter. The filtrate was finely filtered with a microporous membrane to obtain a sterile solution. Dispense the sterile solution into sterilized vials by direct dispensing method. Pre-freeze to -35°C, turn on the condenser until the temperature of the solution drops to -55°C, turn on the vacuum system, gradually increase the temperature until the sample is dry, crimp the cap and seal, and pack it.

[0045] See Table 7-2 for the prescriptions of Example 12, Example 13, Example 14, Example 15, Example 16, Example 17, Example 18, and Example 19, and refer to Example 11 for specific preparation methods.

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PUM

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Abstract

A process for an injection from frozen powder of doxifluridine applying to mainline and its preparation method, said injection comprise 5 parts of doxifluridine, 0.1-100 parts of excipient or 0.1-100 parts of cyclodextrin.; said product can be dissolved quickly when meeting water and convenient for clinical use.

Description

technical field [0001] The invention relates to doxifluridine powder injection and a preparation method thereof, in particular to doxifluridine freeze-dried powder injection suitable for infusion and a preparation method thereof. technical background [0002] Doxifluridine (5'-DFUR) is a nontoxic prodrug of 5-fluorouracil (5-FU). It is an anti-tumor drug developed by the American branch of Roche in the 1970s, and its trade name is Furtulon. It was first put into the market in Japan in the 1990s. In the past, the fluorinated pyrimidine series drugs were mainly enzymatically or naturally hydrolyzed into 5-FU by liver drug enzymes after oral administration. In contrast, Fluferolone can be converted into 5-FU by pyrimidine nucleoside phosphorylase (PyNPase), which shows high activity in tumor tissue. Because the enzyme is high in breast cancer, gastric cancer, colon cancer and other solid tumors, 5'-DFUR is preferentially activated in the tumor site, and the drug concentratio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/40A61K31/7072A61P35/00
Inventor 胡传良
Owner JIANGSU SHENLONG PHARMA
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