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Compound sodium levofolinate fluorouracil antineoplastic medicament

A technology of sodium levofolinate and fluorouracil, used in antitumor drugs, drug combinations and other directions, can solve the problems of calcium ions without pharmacological effects, unhelpful activity, blockage of infusion catheters, etc., to achieve safe and effective treatment, reduced toxicity, and toxic effects. The effect of reducing side reactions

Inactive Publication Date: 2011-07-20
齐建新
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, leucovorin commonly used clinically is a calcium salt, and the active ingredient of leucovorin calcium is levofolinic acid. Calcium ions have no pharmacological effects and are not helpful for activity.
Simultaneous use of calcium levofolinate and 5-Fu will cause precipitation in the infusion fluid and cause 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 injection and sodium levofolinate 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): 20 examples,

[0021] Cases treated at the wrong time (reference group): 18 cases.

[0022] treatment method:

[0023] Treatment group: Sodium levofolinate 250mg / m 2 With 5-Fu 2600mg / m 2 Mixed intravenous infusion for 24 hours, repeated every week, a total of 4 cycles.

[0024] Control group: sodium leucovorin 250mg / m 2 Intravenous infusion for 2 hours, then 5-Fu 2600mg / m 2 24-hour infusion, repeated every week, a total of 4 cycles.

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

[0026] Table 1

[0027]

Number of cases

CR

PR

SD / NC

TTP...

Embodiment 1

[0035] Example 1. Weigh 50g of the prescribed amount of levofolinic acid and add it to water for injection at 60°C to make a suspension, add 8ml of 5% NaOH dropwise, stir to dissolve, control the pH value between 8.0-9.0, and 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 0.22 u 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 sodium leucovorin antineoplastic drug for injection contains 50 mg of leucovor...

Embodiment 2

[0036] Embodiment two: take by weighing 32.1g sodium levofolinate, 50g fluorouracil and 25g mannitol respectively, add in the water for injection of 60 ℃, stir and make dissolving, if necessary, dropwise add 5% NaOH solution, to adjust the pH value at Between 8.0 and 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 injection Add water 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 sodium fluorouracil antineoplastic agent for injection contains 25 mg of leucovorin and 50 mg of fluorouracil.

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PUM

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Abstract

The invention relates to a compound sodium levofolinate fluorouracil antineoplastic medicament which comprises sodium levofolinate and fluorouracil. The weight ratio of the scalar quantity-levofolinate of the sodium levofolinate to the fluorouracil is 1:(2-30), preferably 1:(2-10). A preparation is freezing and drying injection or injection. A preparation auxiliary material is one or more of mannitol, dextran, glucose, sodium hydroxide and sodium chloride. Proved by the JiaCheng medical technology limited company of Guangzhou through experiments, the compound sodium levofolinate fluorouracil can more favorably exert the biological regulating effect of levofolinate compared with the staggered use of sodium levofolinate and 5-FU and the treatment on tumors is safer and more effective by the cooperation of the sodium levofolinate and 5-FU. The matching use has longer tumor progression time compared with staggered medicament application under same dosage, prolongs the total life cycle and reduces the toxic or side reaction. The reduction of toxicity ensures that a large dose of 5-FU can be used in clinic so as to achieve the effect of killing tumor cells.

Description

technical field [0001] The invention relates to a compound sodium levofolinate 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...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K31/513A61P35/00
Inventor 齐建新
Owner 齐建新
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