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Method for stabilizing tegafur in aqueous solution

A technology of tegafur and aqueous solution, which is used in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., to achieve the effect of expanding the scope

Inactive Publication Date: 2011-06-22
山东华鲁制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of oral preparations is low bioavailability, which is even more unfavorable for patients who have difficulty swallowing
Although the small water injection preparation solves the above difficulties, it needs to be added to the sodium chloride injection for use during application, which will easily cause contamination of the liquid medicine during operation, and bring operational troubles and the possibility of making mistakes to the medical staff. Poisoning the health of medical staff
And it is easy to precipitate crystals when it is cold, which also increases the difficulty of application
[0005] Tegafur is slightly soluble in water (1g of Tegafur can be dissolved in 30-less than 100ml of water), therefore, Tegafur is made into injection, water for injection Its preferred solvent, but tegafur is unstable in water

Method used

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  • Method for stabilizing tegafur in aqueous solution
  • Method for stabilizing tegafur in aqueous solution
  • Method for stabilizing tegafur in aqueous solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0021] (3) Add sodium hydroxide to adjust the pH to 8.5~10.5, add water for injection until the volume reaches 100ml, fill and sterilize.

[0022] The amounts of sodium chloride, sodium carbonate, tegafur and sodium hydroxide in Examples 1-3 are shown in Table 1 below.

[0023] Table 1 Statistical Table of Addition of Sodium Chloride, Sodium Carbonate, Tegafur and Sodium Hydroxide in Examples 1-3

[0024]

[0025] After the solutions in Examples 1-3 were sterilized, the components therein were tested, and the test results are shown in Table 2 below.

[0026] Table 2 The solution of embodiment 1-3 is through the composition detection result after sterilization

[0027]

[0028] Tegafur content=detected tegafur amount / added tegafur amount*100% in table 2,

[0029] Sodium chloride content = detected amount of sodium chloride / added amount of sodium chloride * 100%,

[0030] Fluorouracil content = the amount of detected fluorouracil / the amount after converting the ad...

Embodiment 4-6

[0036] (3) Add sodium hydroxide to adjust the pH to 8.5~10.5, add water for injection until the volume reaches 100ml, fill and sterilize.

[0037] The amounts of sodium chloride, sodium acetate, tegafur and sodium hydroxide in Examples 4-6 are shown in Table 3 below.

[0038] Table 3 The addition statistics of sodium chloride, sodium acetate, tegafur and sodium hydroxide in Examples 4-6

[0039]

[0040] After the solutions in Examples 4-6 were sterilized, the components therein were tested, and the test results are shown in Table 4 below.

[0041] Table 4 The solution of embodiment 4-6 is through the composition detection result after sterilization

[0042]

[0043] Example 7-9

[0044] The steps of the method are as follows: (1) Take sodium chloride and prepare a 15% sodium chloride solution with water for injection;

[0045] (2) Add sodium phosphate and tegafur to the sodium chloride solution, stir to dissolve;

Embodiment 7-9

[0047] The amounts of sodium chloride, sodium phosphate, tegafur and sodium hydroxide in Examples 7-9 are shown in Table 5 below.

[0048] Table 5 The addition statistics of sodium chloride, sodium phosphate, tegafur and sodium hydroxide in Examples 7-9

[0049]

[0050] After the solutions in Examples 7-9 were sterilized, the components therein were tested, and the test results are shown in Table 6 below.

[0051] The solution of table 6 embodiment 7-9 is through the component test result after sterilization

[0052]

[0053] Comparative Examples 1-3

[0054] On the basis of embodiment 1-3, remove sodium carbonate, method step is identical with embodiment 1-3,

[0055] The amounts of sodium chloride, tegafur and sodium hydroxide in Comparative Examples 1-3 are shown in Table 7 below.

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Abstract

The invention relates to a method for stabilizing tegafur in an aqueous solution, relating to the technical field of anticarcinogen tegafur injection application. The method comprises the following steps of: taking 0.7-1.4g of sodium chloride, and preparing a 5-30% sodium chloride solution by using water for injection; adding 0.1-3.0g of sodium carbonate, sodium phosphate or sodium acetate and 0.1-2.0g of tegafur to the sodium chloride solution, stirring and dissolving; and adding 0.01-0.3g of sodium hydroxide, regulating a pH value to be 8.5-10.5, adding the water for injection till the volume reaches 100ml, filling and sterilizing. The invention solve the technical problem that the stable injection with high addition amount can not be prepared due to the unstability of the tegafur in the aqueous solution; the prepared aqueous solution of tegafur completely meets the preparation requirement on injections with small capacity and large capacity, is safe, stable, and has reliable quality; in addition, the invention enlarges the application of the tegafur raw material and lays the foundation for the development of injection formulations, in particular injections with large capacity of more than 100ml.

Description

technical field [0001] The invention relates to the technical field of application of the anticancer drug tegafur injection, in particular to a method for stabilizing tegafur in an aqueous solution. Background technique [0002] Malignant tumor (cancer) is a disease that seriously endangers human health. Drug therapy is one of the main therapies for tumors, especially for patients with tumor metastasis, drug therapy is especially important. [0003] Tegafur is a derivative of fluorouracil. It is one of the new effective anti-cancer drugs in recent years. It mainly treats gastrointestinal tumors, such as gastric cancer, colon cancer, rectal cancer and pancreatic cancer. It can also be used to treat breast cancer, bronchial lung cancer and liver cancer. The chemotherapy index is twice that of fluorouracil, and the toxicity is only 1 / 4~1 / 7 of that of fluorouracil. Tegafur is the main effective drug for clinical chemotherapy of the above tumors. In the course of chemotherap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/513A61K47/02A61K47/12A61P35/00
Inventor 于洪华
Owner 山东华鲁制药有限公司
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