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Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis

A technology of ectoine and derivatives, applied in the field of cystitis, can solve the problems of cystitis without better preventive drugs, limit the dosage and long-term administration of chemotherapy drugs, lack of broad-spectrum preventive drugs, etc., and achieve a wide range of therapeutic effects Effect

Inactive Publication Date: 2011-10-12
潍坊美洛秋海洋生物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no good preventive drug for cystitis caused by mitomycin, cantharidin, camptothecin, etc.
For cystitis caused by chemotherapy drugs, except for a few narrow-spectrum preventive drugs, there is a lack of effective broad-spectrum preventive drugs or effective therapeutic drugs, which greatly limits the dosage and long-term administration of chemotherapy drugs

Method used

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  • Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis
  • Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis
  • Application of tetrahydropyrimidine and derivatives thereof in preparing medicament for treating cystitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 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 The therapeutic effect on cystitis induced by chemotherapeutic drugs

[0022] Animals: New Zealand rabbits, female, aged 3 months, weighing 1.49±0.10kg, quarantined for 7 days. After the quarantine period ended, 72 rabbits qualified for quarantine were selected, and they were given cyclophosphamide (200.0 mg / kg, given to 15 rabbits) and mitomycin (100.0 mg / kg, given to 15 rabbits) by ear vein injection respectively. ), cantharidin (86.0mg / kg, given to 15 rabbits) or camptothecin (100.0mg / kg, given to 15 rabbits).

[0023] Observation of urination frequency: Rabbits were raised in dry cages, and the iron cage was divided into two layers. The upper layer was a place for rabbits to eat and move, and the lower layer was a tray. A layer of dry crepe paper was laid flat, and the urine was taken out after getting wet. , dry the tray and rep...

Embodiment 2

[0038] Example 2 Preparation of 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinecarboxylic acid tablets

[0039] The formula is as follows:

[0040]

[0041] 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.

Embodiment 3

[0042] Example 3 Preparation of 1,4,5,6-tetrahydro-2-methyl-5-hydroxyl-4-pyrimidinecarboxylic acid tablets

[0043]

[0044] Pass the prescribed 1,4,5,6-tetrahydro-2-methyl-5-hydroxy-4-pyrimidine carboxylic acid through a 180 μm sieve for later use; pass the sieved 1,4,5,6-tetrahydro-2- Methyl-5-hydroxy-4-pyrimidinecarboxylic acid is mixed with microcrystalline cellulose, sodium carboxymethyl starch and polyvinylpyrrolidone, and then pressed into large tablets, crushed and sized to obtain smaller granules, plus lauryl Sodium sulfate and micro silica gel, mix well and press into tablets.

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Abstract

The invention discloses a new application of 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinyl carboxy and derivatives thereof in the medicine field, namely an application in preparing a medicament for treating cystitis caused by chemotherapeutics. Found by the inventors surprisingly under study, 1,4,5,6-tetrahydro-2-methyl-4-pyrimidinyl carboxy and derivatives thereof have an amazing therapeutic action on treating the cystitis caused by chemotherapeutics, and are favorable for alleviating pain of patients taking chemotherapy and for improving the tolerance dose of the patients on the chemotherapeutics, so that the tetrahydropyrimidine and derivatives thereof can be used for preparing the medicament for treating cystitis caused by chemotherapeutics. The invention also provides a medicament for treating cystitis caused by chemotherapeutics, composed of the tetrahydropyrimidine or the derivatives thereof and medically acceptable pharmaceutical auxiliary materials. Compared with the existing medicaments such as mesna and the like, the tetrahydropyrimidine and derivatives thereof have extensive therapeutic actions on the cystitis caused by chemotherapeutics rather than have limited preventive actions.

Description

technical field [0001] The invention relates to the application of ectoine and its derivatives in the preparation of medicines for treating cystitis, in particular to cystitis caused by chemotherapeutic medicines. Background technique [0002] Tumor is one of the common diseases that threaten human health. At present, the 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 prone to resistance Medication 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 increased by 69%, and the mortality rate has increased by 29.4%. Therefore, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61P13/10
Inventor 厉保秋高继友
Owner 潍坊美洛秋海洋生物科技有限公司
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