Calcium folinate composition for adjuvant treatment of colon cancer and rectal cancer

Abstract

The invention discloses a calcium folinate composition for adjuvant treatment of colon cancer and rectal cancer, and belongs to the technical field of medicine. The composition comprises calcium folinate and arginine, wherein the calcium folinate is a crystal; an X-ray powder diffraction pattern measured through using Cu-K alpha ray is described as the graph 1 (referring to the description). The novel crystal form of the calcium folinate provided by the invention is different from the crystal structure of the prior art, the test proves and discovers that compared with the prior art, the calcium folinate crystal composition provided by the invention has the following advantages: the stability is good, the content of impurities is low, and the solubility and fluidity in water are obviously improved; the problems that the calcium folinate in the prior art is poor in water solubility and stability and related substances are high in content are solved, so that convenience is provided for the preparation of a reagent, and the medicine effect is greatly improved; a powder injection prepared by using the novel crystal compound is good in stability, the stability is good after the powder injection is combined with a solvent, the content of insoluble particulates is extremely low, and the powder injection is quite suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a calcium leucovorin composition for adjuvant therapy of colon cancer and rectal cancer. Background technique [0002] Calcium folinate has a detoxifying effect on methotrexate (MTX). MTX is a folic acid antagonist. The anti-tumor mechanism of MTX is that its structure is similar to folic acid, which can inhibit the activity of dihydrofolate reductase, resulting in the lack of tetrahydrofolate (FH4) in cells, thereby affecting the synthesis of purine and pyrimidine nucleotides. Inhibits tumor cell growth. While MTX inhibits the growth of tumor cells, it also makes normal cells, especially fast-growing cells, lack FH4, resulting in greater toxicity. Therefore, the anti-tumor effect of MTX not only depends on its inhibition of tumor cells, but also the body's tolerance to MTX affects its final result. CF is a formylated derivative of folic acid reduction, which is the activated ...

AI Technical Summary

Problems solved by technology

[0004] The solubility of calcium folinate in water is not ideal. In practice, it is found that calcium folinate is not easy to dissolve when the water temperature is lower than 30°C. If the dissolution is not good, the content will decrease. It is sensitive to factors such as temperature, pH value, and oxygen, resulting in the increase of related substances. , unstable, easy to decompose when exposed to light, and poor storage stability, which limits the application and clinical application of its preparations, and increases the cost of preparations

Although calcium folinate reduces the toxic effect of the antineoplastic drug MTX, its toxic effect cannot be ignored

The existing technology solves the problems of water solubility and stability by changing the excipients and preparation methods of the preparation. It must rely on specific prescriptions and processes to achieve its stable effect, which brings certain limitations to the preparation of preparations and the selection of excipients. sex

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