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Cephalofruxin ester liposome, its preparation and medicinal composition containing it

A technology of cefuroxime axetil and furoxetin axetil, which is applied in the field of medicine, can solve the problems of thermal instability, slow dissolution, low solubility, etc., and achieve the effect of convenient clinical medication, rapid dissolution and stable properties

Active Publication Date: 2007-04-04
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, C in the structure of cefuroxime axetil 4 The carboxyl group on the position has a large degree of dissociation in the body, and the solubility in water is extremely small
In addition, cefuroxime axetil has a bitter taste, is unstable to heat, and is easy to absorb moisture. Therefore, the cefuroxime axetil preparation prepared by the common method has problems such as long disintegration time, slow dissolution, difficult absorption, unstable quality, and inconvenience in taking.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] a. The cefuroxime axetil required by the prescription amount is placed in acetone and dissolved in the ratio of cefuroxime axetil: soybean lecithin: cholesterol is 1: 2: 2, the volume is recorded, filtered, the filtrate is collected, and the acetone is removed by rotary evaporation into thin film, vacuum drying;

[0037] b. Add phosphate buffer with a pH value of 5.9, soak for 1.5 hours, stir at high speed, and after 3 minutes, slowly add povidone K with a concentration of 0.75 mg / ml dissolved in the same buffer solution dropwise 30 solution, and make up the buffer to the original volume;

[0038] c. Then the liposome suspension is filtered with a diameter of 0.8um microporous membrane to obtain a filtrate, which is put into a tray and freeze-dried in a lyophilizer to obtain cefuroxime axetil liposomes.

Embodiment 2

[0040] a. The cefuroxime axetil required by the prescription amount is placed in acetone and dissolved in the ratio of cefuroxime axetil: soybean lecithin: cholesterol is 1: 2: 2, the volume is recorded, filtered, the filtrate is collected, and the acetone is removed by rotary evaporation into a thin film, after vacuum drying;

[0041] b. Add phosphate buffer with a pH value of 6.2, soak for 1 hour, stir at high speed, and after 5 minutes, slowly add povidone K with a concentration of 0.75 mg / ml dissolved in the same buffer solution dropwise 30 solution, and make up the buffer to the original volume;

[0042] c. Then the liposome suspension is filtered with a diameter of 0.8um microporous membrane to obtain a filtrate, which is put into a tray and freeze-dried in a lyophilizer to obtain cefuroxime axetil liposomes.

Embodiment 3

[0044] a. The cefuroxime axetil required by the prescription amount is placed in acetone and dissolved in the ratio of cefuroxime axetil: soybean lecithin: cholesterol is 1: 2: 2, the volume is recorded, filtered, the filtrate is collected, and the acetone is removed by rotary evaporation into a thin film, after vacuum drying;

[0045] b. Add phosphate buffer with a pH value of 6.5, soak for 1 hour, stir at high speed, and after 10 minutes, slowly add povidone K with a concentration of 0.75 mg / ml dissolved in the same buffer solution dropwise 30 solution, and make up the buffer to the original volume;

[0046] c. Then the liposome suspension is filtered with a diameter of 0.6um microporous membrane to obtain a filtrate, which is put into a tray and freeze-dried in a lyophilizer to obtain cefuroxime axetil liposomes.

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Abstract

A liposome of cefuroxime axetil used to prepare the tablet with high target performance to the gastrointestinal mucosa cells is prepared from cefuroxime axetil, soybean lecithin and chlosterol in weight ration of 1:2:2. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a cefuroxime axetil liposome, a preparation method thereof and a pharmaceutical composition containing it, belonging to the technical field of medicine. Background technique [0002] Cefuroxime axetil is a second-generation cephalosporin for injection. It is a prodrug of cefuroxime with broad-spectrum antibacterial activity. After oral administration, it is rapidly hydrolyzed by non-specific esterases in the mucosal cells of the gastrointestinal tract to release cefuroxime to exert its drug effect. It has extremely low toxicity to the kidneys, and is widely used clinically for respiratory tract infections, urinary tract infections, pyelonephritis, meningitis, sepsis, and gonococcal infections. [0003] However, C in the structure of cefuroxime axetil 4 The carboxyl group on the position has a large degree of dissociation in the body, and its solubility in water is extremely small. In addition, cefuroxime axetil has a bitter ...

Claims

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Application Information

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IPC IPC(8): A61K31/46A61K9/127A61K9/28A61K47/24A61P31/04
Inventor 李国聪郭卫芹张育高志峰
Owner CSPC OUYI PHARM CO LTD
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