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Stable Tegafur injection and preparation method thereof

A technology of tegafur and injection, which is applied in the field of medicine, can solve the problems of unqualified foreign body inspection, yellowing of solution color, drop of pH value, etc., and achieves the effect of being convenient for promotion and clinical medication.

Active Publication Date: 2011-09-14
SICHUAN SUNNYHOPE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Through creative work, it was found that the tegafur injection is more stable, and the content of the related substance fluorouracil is greatly reduced compared with the existing technology, which solves the problem that the pH value of the tegafur injection drops during high-temperature sterilization and storage in the prior art products , the solution color turns yellow, the inspection of visible foreign matter is unqualified, and the inspection of related substances is unqualified

Method used

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  • Stable Tegafur injection and preparation method thereof
  • Stable Tegafur injection and preparation method thereof
  • Stable Tegafur injection and preparation method thereof

Examples

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Embodiment 1

[0028] A stable tegafur injection and a preparation method thereof, comprising the steps of: (1) weighing 1 g to 100 g of tegafur, 10 mg to 50 g of an antioxidant, and 10 mg to 50 g of a pH buffer; (2) taking an acid solution and / or sodium hydroxide to be prepared into solutions of any concentration, and set aside; (3) Take 500ml of water for injection below 40°C, add antioxidants, pH buffers, and tegafur in sequence, stir, and use step (2) Adjust the pH value of the prepared acid solution and / or sodium hydroxide solution to 10.5-12.0, make up water for injection below 40°C to 1000ml; (4) add activated carbon to the solution obtained in step (3), and the amount of activated carbon is 0.005g- 0.5g / 100ml, stirred for 10-60 minutes, decarburized by filtration; (5) fine-filtered the injection solution obtained in step (4) until clarified, filled with nitrogen for protection, filled, and sterilized at high temperature.

[0029] The specific components and contents thereof of the pr...

Embodiment 2

[0036] The specific components and contents thereof of the present embodiment are as follows:

[0037] Tegafur 40.0g

[0038] L-cysteine ​​2.0g

[0039] Sodium citrate 5.0g

[0040] Citric acid and / or sodium hydroxide adjust the pH of the solution.

[0041]Citric acid and / or sodium hydroxide were prepared into 10% to 20% solutions respectively for later use; take 500ml of water for injection below 40°C, add L-cysteine, sodium citrate, and tegafur in sequence, and stir. Use the citric acid solution and / or sodium hydroxide solution prepared above to adjust the pH value to 10.5-12.0, make up water for injection below 40°C to 1000ml; add activated carbon to the obtained solution, the amount of activated carbon is 0.1g / 100ml, stir for 30 Minutes, decarburized by filtration; the resulting injection was fine-filtered until clarified, filled with nitrogen for protection, filled, and autoclaved at 115°C for 30 minutes to obtain the product.

Embodiment 3

[0043] The specific components and contents thereof of the present embodiment are as follows:

[0044] Tegafur 40.0g

[0045] L-cysteine ​​5.0g

[0046] Sodium carbonate 20.0g

[0047] Hydrochloric acid and / or sodium hydroxide to adjust the pH of the solution.

[0048] Hydrochloric acid and / or sodium hydroxide were prepared into 10% to 20% solutions respectively for later use; take 500ml of water for injection below 40°C, add L-cysteine, sodium carbonate, and tegafur in sequence, stir, and use the above Adjust the pH of the prepared hydrochloric acid solution and / or sodium hydroxide solution to 10.5-12.0, make up water for injection below 40°C to 1000ml; add activated carbon to the obtained solution, the amount of activated carbon is 0.1g / 100ml, stir for 30 minutes, and filter Decarburization; the resulting injection is finely filtered until clarified, filled with nitrogen for protection, filled, and sterilized by autoclaving at 100°C for 30 minutes.

[0049] When the pres...

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Abstract

The invention discloses stable Tegafur injection and a preparation method thereof. The stable Tegafur injection is prepared mainly by the following steps of: mixing Tegafur and water for injection; adjusting the pH value to be 10.5 to 12.0 by using sodium hydroxide solution and / or acidic solution; adding an antioxidant and a pH value buffering agent and introducing nitrogen to perform protection; and performing high-temperature sterilization to prepare the injection. By the method, the Tegafur injection can be more stable; high-temperature sterilization can be performed; relative substances are greatly reduced compared with those in the prior art; particularly, the problems that the pH value is reduced, the color of the solution is changed to yellow, visible foreign matters are detected to be unqualified and relative substances are detected to be unqualified in the high-temperature sterilization and storage process of the Tegafur injection adopting the products in the prior art are solved; and the stable Tegafur injection can guarantee that the products meet the rule of the medicament quality standard and contributes to clinic administration and popularization.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a stable tegafur injection and a preparation method thereof. Background technique [0002] Tegafur is a derivative of fluorouracil, which is converted into fluorouracil by liver activation in vivo to exert its anti-tumor activity. It is mainly used clinically to treat gastrointestinal tumors, such as gastric cancer, rectal cancer, pancreatic cancer, and liver cancer. It can also be used for breast cancer. At present, the dosage forms of domestic marketed preparations mainly include injection and oral preparations. The bioavailability of oral preparations of this product is worse than that of injections, and Tegafur injections are more clinically used. [0003] In the quality standard for tegafur injection contained in the 2010 edition of the Chinese Pharmacopoeia, the pH value range of the injection is specified to be 9.5 to 10.5, and the detection methods for relate...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/513A61K47/02A61K47/10A61K47/12A61K47/16A61K47/22A61K47/26A61P35/00
Inventor 毛长兴陈开军曹原湘向先旭程亮胥勤黄筱萍李永光王昌贵李小鹏陈艳
Owner SICHUAN SUNNYHOPE PHARM CO LTD
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