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Composite fluorouracil anti-tumor medicament

A technology of fluorouracil and antineoplastic drugs, which is applied in the field of compound fluorouracil antineoplastic drugs, can solve the problems of calcium ions having no pharmacological effect, no activity, blockage of infusion catheters, etc., to achieve safe and effective treatment, reduce toxic and side effects, and grow tumors The effect of progression time

Inactive Publication Date: 2011-05-25
齐建新
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, folinic acid commonly used clinically is a calcium salt, and the active ingredient of calcium folinate is folinic acid, and calcium ions have no pharmacological effect and are not helpful for the activity
Simultaneous use of calcium folinate and 5-Fu will cause precipitation in the infusion solution, causing blockage of the infusion catheter

Method used

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Examples

Experimental program
Comparison scheme
Effect test

experiment example

[0018] Experimental example: Compatible infusion of fluorouracil for injection and sodium leucovorin for injection and the use of the two at the wrong time.

[0019] Subjects: Metastatic or inoperable colorectal cancer, no chemotherapy before, over 18 years old, physical status WHO0-2

[0020] Adopt the case of the present invention's treatment (treatment group): 25 examples,

[0021] Cases treated at the wrong time (reference group): 23 cases.

[0022] treatment method:

[0023] Treatment group: 500mg / m 2 Sodium folinate for injection and 500mg / m 2 24-hour mixed infusion of 5-FU for injection. Once a week x 6 weeks, repeated every 8 weeks, a total of 4 cycles.

[0024] Control group: sodium folinate for injection 500mg / m 2 After 2 hours of intravenous infusion, use 5-FU 500mg / m 2 24-hour infusion, once a week x 6 weeks, repeated every 8 weeks, a total of 4 cycles.

[0025] The treatment effect is shown in Table 1, and the adverse reactions are shown in Table 2.

[00...

Embodiment 1

[0035] Embodiment 1, take by weighing 100g of folinic acid of recipe quantity and add in the water for injection of 60 ℃ to make suspension, add dropwise 5% NaOH 17ml, stir to dissolve, control pH value between 8.0-9.0, add 100g of fluorouracil and 50g of mannitol, stir to dissolve, control the pH value between 8.0-9.0, add 1.2g of 0.1% activated carbon, stir for 15 minutes, filter to remove carbon, filter the filtrate through a 0.8u microporous membrane until it is clear, and then pass through a 0.22u Filter through a microporous membrane, let cool, add water for injection to 1200ml, stir, and mix well. Determine the content of intermediates, aseptically pack them into 1000 vials, determine the filling volume of each bottle according to the results of the intermediates, half-stopper, send to a lyophilizer for freeze-drying, close the rubber stoppers, roll on the aluminum caps, and pack. Each compound fluorouracil antineoplastic drug for injection contains 100mg of folinic aci...

Embodiment 2

[0036] Embodiment 2: Weigh 64.2g of sodium folinate, 50g of fluorouracil and 25g of mannitol respectively, add them into water for injection at 60°C, stir to dissolve, and add 5% NaOH solution dropwise if necessary, to adjust the pH value to 8.0 Between -9.0, add 1.2g of 0.1% activated carbon, stir for 15 minutes, filter to remove carbon, filter the filtrate through a 0.8u microporous membrane until clarified, then filter through a 0.22u microporous membrane, let it cool, and add water for injection to 1200ml, stir and mix well. Determine the content of intermediates, aseptically pack them into 1000 vials, determine the filling volume of each bottle according to the results of the intermediates, half-stopper, send to a lyophilizer for freeze-drying, close the rubber stoppers, roll on the aluminum caps, and pack. Each compound fluorouracil antineoplastic drug for injection contains 50 mg of folinic acid and 50 mg of fluorouracil.

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Abstract

The invention relates to a composite fluorouracil anti-tumor medicament, which consists of sodium folinate and fluorouracil, wherein the weight ratio of scalar-folinate of the sodium folinate to the fluorouracil is 1:(1-15), preferably 1:(1-5). A preparation is a freeze-dried injection or an injection. An auxiliary material of the preparation is one or more of mannitol, dextran, glucose, sodium hydroxide and sodium chloride. An experiment performed by Guangzhou Jiacheng Medical Science and Technology Co., Ltd. proves that composite fluorouracil can bring biological regulating effect of folinate into play better than alternate use of folinate and 5-FU, and tumor treatment is safer and more effective under the synergistic action of folinate and 5-FU. Under the condition of equal dosage, combined use of the folinate and 5-FU realizes longer tumor progress time, prolongs overall service life and lowers toxic or side reaction compared with alternate administration. Due to the reduction in toxicity, a large amount of 5-FU can be used clinically for achieving the effect of killing tumor cells.

Description

technical field [0001] The invention relates to a compound fluorouracil antineoplastic drug. Background technique [0002] The discovery of fluorouracil (5-Fu) in 1957 was a milestone in colorectal cancer chemotherapy. Early use of 5-Fu in palliative chemotherapy can significantly increase the survival time of colorectal cancer patients from an average of 4-6 months to 7.5-12 months . Since then, the anticancer drug 5-Fu has been proven to be effective against many tumors. By the late 1970s the various mechanisms of action of 5-Fu were elucidated and this was the starting point for the use of the bioregulator folinic acid to improve the original effectiveness of 5-Fu. [0003] 5-Fu is currently the most widely used anti-pyrimidine drug. 5-Fu has a broad anti-tumor spectrum. It is mainly used to treat gastrointestinal tumors, and is also commonly used to treat breast cancer, ovarian cancer, choriocarcinoma, cervical cancer, and liver cancer. , bladder cancer, skin cancer, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/513A61P35/00
Inventor 齐建新
Owner 齐建新
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