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Emulsion of n-(2-(2-amino)oxyethylthiobenzothiazole-6-)-2-carboxamide derivative and its preparation method

A technology of benzothiazole and oxyethylthio, applied in the field of medicine, can solve the problems of killing tumor cells and damaging normal cells, low selectivity, toxic and side effects, etc.

Active Publication Date: 2011-11-30
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low selectivity of existing treatment methods or drugs, some types of normal cells in the body are damaged while killing tumor cells, resulting in obvious toxic and side effects during the treatment process.

Method used

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  • Emulsion of n-(2-(2-amino)oxyethylthiobenzothiazole-6-)-2-carboxamide derivative and its preparation method
  • Emulsion of n-(2-(2-amino)oxyethylthiobenzothiazole-6-)-2-carboxamide derivative and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 CBTA emulsion

[0051] Put 12g of soybean lecithin for injection and 22g of glycerin for injection into a high-speed tissue grinder, add an appropriate amount of water for injection preheated to 80°C, and stir to make the phospholipids evenly dispersed in the water phase; another 500mg of CBTA is placed in a 200g preheated In the oil for injection, the oil phase is obtained after complete dissolution, and the temperature is lowered to 80°C for later use. Slowly add the oil phase to the water phase, and stir at high speed for 10 minutes (10000 rpm), so that the oil phase is evenly dispersed in the water phase, and white colostrum is prepared. Add water for injection to 1000ml of the colostrum, and place it in the high-pressure milk Repeated emulsification in the machine for 3 times until the average particle size is below 0.5 μm, filled with nitrogen, and sterilized by autoclaving to obtain CBTA intravenous emulsion. The measured encapsul...

Embodiment 2

[0052] The preparation of embodiment 2 CBTA emulsion

[0053] Dissolve and disperse 12g of soybean lecithin for injection, 3g of prolactin (F68) and 22g of glycerin for injection in an appropriate amount of water for injection preheated to 80°C to prepare a uniformly dispersed aqueous phase; add 100mg of CBTA to the preheated injection In 100g of oil, the oil phase is obtained after the complete dissolution, and the temperature is lowered to 80°C for later use. Slowly add the oil phase into the water phase, and stir at a high speed for 10 minutes (10000 rpm), to prepare light yellow colostrum. Add colostrum and water for injection to 1000ml, put it in a high-pressure milk homogenizer and homogenize it for 3 times until the average particle size reaches below 0.5μm, fill it with nitrogen, and sterilize it to obtain an intravenous emulsion. The measured encapsulation efficiency and particle size are: 87.47% and 324.8nm, respectively.

Embodiment 3

[0054] The preparation of embodiment 3 CBTA emulsion

[0055] Dissolve and disperse 15g of soybean lecithin for injection and 22g of glycerin for injection in an appropriate amount of water for injection preheated to 80°C to prepare a uniformly dispersed water phase; add 500mg of CBTA to 200g of preheated oil for injection, and dissolve completely to obtain Cool the oil phase to 80°C for later use. Slowly add the oil phase into the water phase, stir at high speed for 10 minutes (10000 rpm), and prepare white colostrum. Add colostrum and water for injection to 1000ml, put it in a high-pressure milk homogenizer and homogenize it for 3 times until the average particle size reaches below 0.5μm, fill it with nitrogen, and sterilize it to obtain an intravenous emulsion. The measured encapsulation efficiency and particle size are: 96.49% and 224.1nm, respectively.

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Abstract

The invention belongs to the field of medicaments, and particularly relates to an emulsion of N-(2-(2-amine) oxyethio-based benzothiazole-6-)-2-formamide derivatives and a preparation method thereof. The invention aims at providing a suitable dosage form for increasing the N-(2-(2-amine) oxyethio-based benzothiazole-6-)-2-formamide derivatives, especially for solubility and bioavailability of CBTA (carboxyl benzene triazole), and finally the inventor prepares the N-(2-(2-amine) oxyethio-based benzothiazole-6-)-2-formamide derivatives into the emulsion which is provided for clinic application.According to the prepared emulsion, the particle size of the disperse phase is 0.05mum-1mum, the average particle size is 150nm-400nm, so that the prepared emulsion belongs to submicroemulsion; the dispersion degree of liquid drops in the emulsion is large, the absorption of medicines and the acting of medicine effect are fast and the bioavailability is high.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to an emulsion of N-(2-(2-amine)oxyethylthiobenzothiazole-6-)-2-carboxamide derivatives and a preparation method thereof. Background technique [0002] Malignant tumors have become the second leading cause of human death, seriously threatening human health. In my country, according to the latest statistics, tumors have become the number one cause of death for our people. According to the latest epidemiological survey data, there are more than 3 million cancer patients in my country, and about 1.3 million patients die of malignant tumors every year. Every year, there are 1.6 to 2 million new cases of malignant tumors, and they are increasing at a rate of 3%, which poses a huge threat to the life and health of our people and brings huge pressure to society and families. To a certain extent, it restricts the sustainable economic development of our country. Traditional tumor treatment methods ar...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/14A61K9/19A61K31/428A61P35/00
Inventor 宋相容余洛汀赵瀛兰魏于全
Owner SICHUAN UNIV
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