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5-fluorouracil composition and its application in the preparation of anti-tumor injection

A technology of fluorouracil and composition, which is applied in the directions of antitumor drugs, drug combinations, medical preparations containing active ingredients, etc., can solve the problems of insufficient stability of 5-fluorouracil preparations and the like

Active Publication Date: 2017-11-24
CARBIOGENE THERAPEUTICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve the problem of insufficient stability of 5-fluorouracil preparations, the inventors unexpectedly found that the addition of shikonic acid can enhance the anti-cancer effect of 5-fluorouracil and reduce 5-fluorouracil toxic side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1: Test of the influence of drugs on human liver cancer cell xenograft model

[0012] 40 clean-grade healthy pure-line Kunming mice, half male and half male, weighing (20±2) g, for 6-8 weeks. They were randomly divided into 10 rats in the control group, 10 rats in the shikonic acid group, 10 rats in the 5-fluorouracil group and 10 rats in the combined treatment group. The mice pre-inoculated with H22 liver cancer ascites tumor were sacrificed, and 3.2 mL of ascites tumor was extracted from the abdominal cavity, and diluted with normal saline to 5×10 6 cells / mL, inject 0.2mL per day into the armpit of mice, and 7 days after inoculation, tumors (diameter 2-3mm) can be palpable, grouped and treated as follows: model control group: intraperitoneal injection of normal saline (0.3 mL / rat); 5-fluorouracil group: intraperitoneal injection of 5-fluorouracil (0.3mL / rat, 20mg / kg); Treatment group: Administer shikonic acid and 5-fluorouracil (0.3mL / rat, intraperitoneal...

Embodiment 2

[0020] Embodiment 2: Preparation of 5-fluorouracil injection

[0021] Prescription: 5-fluorouracil 100g

[0022] Shikonian acid 450g

[0023] Mannitol 50g

[0024] Appropriate amount of pH adjuster

[0025] Preparation process: first add 8L of water for injection into the container, add the prescribed amount of 5-fluorouracil, stir to dissolve completely, adjust the pH to 8.5 with 1mol / L sodium hydroxide solution, then add the prescribed amount of shikonic acid, stir to dissolve; Add 5g of activated carbon for injection, add water for injection to 10L, constant volume, stir and absorb for 30 minutes; the solution is decarbonized by coarse filtration, coarsely filtered through a 0.45μm cartridge filter, and then sterilized and filtered with a 0.22μm microporous filter membrane to Visible foreign matter qualified; filling, 10ml / bottle, sealing, sterilization, to obtain 5-fluorouracil injection.

Embodiment 3

[0026] Embodiment 3: Preparation of fluorouracil for injection

[0027] Prescription: 5-fluorouracil 100g

[0028] Shikonian acid 500g

[0029] Mannitol 50g

[0030] Appropriate amount of pH adjuster

[0031] Preparation process: first add 4L of water for injection into the container, add the prescribed amount of 5-fluorouracil, stir to dissolve completely, adjust the pH to 8.2 with 1mol / L sodium hydroxide solution; then add the prescribed amount of shikonic acid, stir to dissolve; Add 2.5g of activated carbon for injection, add the remaining water for injection to 5L, constant volume, stir and absorb for 30 minutes; decarbonize the solution by coarse filtration, pass through a 0.45μm cartridge filter, and then sterilize with a 0.22μm microporous membrane filter Filter until visible foreign matter is qualified; fill, 5ml / bottle, and freeze-dry to obtain fluorouracil for injection.

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Abstract

The invention relates to 5-fluorouracil containing pharmaceutical composition and an application of the 5-fluorouracil containing pharmaceutical composition in preparation of an anti-tumor injection. The injection comprises an injection solution and freeze-dried powder injection. Lithospermic acid and 5-fluorouracil can have an obvious synergistic effect, hepatocellular carcinoma growth is inhibited, side effects of chemotherapy are reduced, immunity is enhanced, and the purpose of tumor therapy is achieved finally, so that one simple and effective treatment means is provided for patients with advanced liver cancer, especially patients intolerant to a normal dose of 5-fluorouracil.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, relates to a new clinical application of an anti-tumor drug, in particular to a pharmaceutical composition containing 5-fluorouracil and its application in the preparation of an anti-tumor injection. Background technique [0002] 5-Fluorouracil (5-Fu, molecular formula: C4H3FN2O2) is a broad-spectrum anti-tumor drug, which can interfere with the nucleic acid metabolism of tumor cells through various channels and metabolites. The main mechanism of action is: fluorouracil is transformed into 5 - Fluorouracil deoxynucleoside, which forms a covalent bond with the active center of thymidine synthetase, inhibits the activity of the enzyme, reduces the generation of thymidine, and hinders the biosynthesis of DNA; in addition, it can also transform It is fluorouridine triphosphate, which is incorporated into RNA in the form of pseudo-metabolites, thereby interfering with the normal physio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/513A61P35/00A61K31/343
Inventor 杨文君
Owner CARBIOGENE THERAPEUTICS CO LTD
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