Application of ectoine and derivatives thereof in preparing medicament for preventing and treating digestive tract diseases caused by chemotherapy medicaments

A technology of ectoine and chemotherapy drugs, applied in the field of ectoine and its derivatives in the field of medicine, can solve problems such as damage to the digestive tract mucosal system, and achieve a wide range of therapeutic effects

Inactive Publication Date: 2011-10-12
江阴拉珈生物医药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, since mucosal tissue is also a fast-dividing tissue, and antineoplastic drugs have cytotoxic effects on fast-dividing tissues, gastrointestinal mucositis is also one of the key problems that limit the dosage of tumor chemotherapy drugs. Cancer patients taking chemotherapy drugs Afterwards, chemotherapeutic drugs generally have a significant destructive effect on the gastrointestinal mucosal system, such as methotrexate, 5-FU, cisplatin, etc.
Although interleukins have certain preventive and therapeutic effects on mucositis caused by chemotherapy, there is no completely effective preventive and therapeutic method at present.

Method used

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  • Application of ectoine and derivatives thereof in preparing medicament for preventing and treating digestive tract diseases caused by chemotherapy medicaments
  • Application of ectoine and derivatives thereof in preparing medicament for preventing and treating digestive tract diseases caused by chemotherapy medicaments
  • Application of ectoine and derivatives thereof in preparing medicament for preventing and treating digestive tract diseases caused by chemotherapy medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid and 1,4,5,6-tetrahydro-2-methyl-5-hydroxyl-4-pyrimidinecarboxylic acid Therapeutic effect on oral mucositis induced by chemotherapeutic drugs

[0025] Kunming mice, half male and half female, 18-28g, 6-8 weeks old, were housed in separate cages at room temperature in the animal room, and the quarantine period was 5 days. Dissolve methotrexate in normal saline, and after disinfecting the abdominal skin of mice, give methotrexate normal saline solution by intraperitoneal injection, once a day, the dose is 1.5 mg / mouse, and the administration is continuous for 3-5 days.

[0026] 30 mice with successful modeling were given intravenous injection of normal saline (NS), 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid saline solution (Ect, calculated as Ect , the dosage is 1.0mg / ml), 1,4,5,6-tetrahydro-2-methyl-5-hydroxyl-4-pyrimidinecarboxylic acid physiological saline solution (in terms of Ect-OH, the ...

Embodiment 2

[0032] Example 2 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid and 1,4,5,6-tetrahydro-2-methyl-5-hydroxyl-4-pyrimidinecarboxylic acid Therapeutic effect on small intestinal mucositis induced by chemotherapeutic drugs

[0033] Balb / C mice, 2-3 weeks old. Mix 5-Fu and irinotecan at a ratio of 1:1 and dissolve in appropriate amount of normal saline, and give 5-Fu and irinotecan intravenously at a dose of 100 mg / kg 5-Fu on the 1st, 2nd and 3rd day respectively. of physiological saline solution.

[0034] 30 rats with successful modeling were given intravenous injection of normal saline (NS), 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid saline solution (Ect, calculated as Ect, The dosage is 1.0 mg / ml), 1,4,5,6-tetrahydro-2-methyl-5-hydroxyl-4-pyrimidinecarboxylic acid physiological saline solution (in Ect-OH, the dosage is 2.0 mg / ml), amifostine normal saline solution (calculated as amifostine, the dosage is 2.0mg / ml) and interleukin 1 (IL-1, calculated as IL...

Embodiment 3

[0039] Example 3 Preparation of 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid tablets

[0040] The formula is as follows:

[0041]

[0042] Pass the prescribed 1,4,5,6-tetrahydro-2-methyl-4-pyrimidine carboxylic acid through a 150 μm sieve, and pass the excipients through a 180 μm sieve for use; now the 1,4,5,6-tetrahydro-2-methyl Base-4-pyrimidine carboxylic acid is mixed with microcrystalline cellulose, and then mixed successively with lactose, sodium carboxymethyl starch, polyvinylpyrrolidone, and magnesium stearate, and then pressed into tablets after mixing evenly.

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Abstract

The invention relates to application of ectoine and derivatives thereof in preparing medicament for preventing and treating digestive tract diseases caused by chemotherapy medicaments. The inventor is surprised to find in researches that: the ectoine and derivatives thereof have unexpected treatment effect digestive tract diseases caused by chemotherapy medicaments, contribute to relieve pains ofpatients who receive chemotherapy, and improve the tolerance dose of the patients to the chemotherapy medicaments. Therefore, the medicament prepared by the ectoine and derivatives thereof can be applied to prevention and treatment on digestive tract inflammation caused by the chemotherapy medicaments. The invention also provides a medicament for treating digestive tract diseases caused by the chemotherapy medicaments, consisting of the ectoine or derivatives thereof and medically acceptable pharmaceutic adjuvant. Compared with the conventional Mesna and other medicaments, the ectoine and derivatives thereof have wide treatment effect on the digestive tract inflammation caused by the chemotherapy medicaments.

Description

technical field [0001] The invention relates to the new application of ectoine and its derivatives in the field of medicine, specifically the application of ectoine and its derivatives in the preparation of drugs for preventing and treating digestive tract inflammation caused by chemotherapeutic drugs. Background technique [0002] Tumor is one of the common diseases that threaten human health. Research on tumors has made great progress, and various methods of radiotherapy and chemotherapy have been developed to treat tumors. However, various drugs and therapies have limitations, it is difficult to achieve the desired effect, and drug resistance is prone to occur and side effects. The mortality rate of cancer still ranks first in various diseases. [0003] Statistics show that in 2006, 3 million people died of cancer in my country, and the incidence of cancer is still on the rise. According to statistics, in less than 20 years, the incidence of cancer in my country has in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61P1/00A61P29/00
Inventor 厉凌子厉保秋
Owner 江阴拉珈生物医药有限公司
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