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Method for splitting chiral medicine of hydrochloric acid lomefloxacin

A technology for lomefloxacin hydrochloride and chiral drugs, which is applied in the field of separation of L-lomefloxacin hydrochloride and D-lomefloxacin hydrochloride, which can solve the problems of side effects, redundancy, differences in pharmacological and toxicological effects, etc.

Active Publication Date: 2009-12-23
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For drugs containing chiral centers, their isomers usually have very similar physical and chemical properties, but there are differences in pharmacological and toxicological effects. Often one of the stereoisomers has the desired biological activity, while the other has the desired biological activity. It is redundant and affects the activity of the effective substance, and even has the opposite side effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] First, ethyl acetate:methanol:water (the content of sulfonated-β-cyclodextrin in water is 0.04mol / L) was arranged in a separatory funnel according to the volume ratio of 10:1:10, shaken and then separated Floor. After balancing for a period of time, separate the upper and lower phases. A semi-preparative high-speed countercurrent chromatograph is used, equipped with an NS-1007 pump, a 20mL injection valve, a polytetrafluoroethylene column with a column volume of 148mL, an 8823A-UV ultraviolet detector, and a portable recorder. Weigh 5 mg of lomefloxacin hydrochloride crude extract and dissolve in 2 mL each of stationary phase and mobile phase for use. Before sample injection, fill the entire column with the stationary phase, adjust the speed of the main engine to 800 rpm, pump the mobile phase into the column at a flow rate of 2.0 mL / min, and inject the sample through the injection valve after the entire system reaches hydrodynamic equilibrium. Then, according to the ...

Embodiment 2

[0016] First, ethyl acetate:methanol:water (the content of sulfonated-β-cyclodextrin in water is 0.04mol / L) was arranged in a separatory funnel according to the volume ratio of 5:1:5, shaken and then separated Floor. After balancing for a period of time, separate the upper and lower phases. A semi-preparative high-speed countercurrent chromatograph is used, equipped with an NS-1007 pump, a 20mL injection valve, a polytetrafluoroethylene column with a column volume of 148mL, an 8823A-UV ultraviolet detector, and a portable recorder. Weigh 10 mg of lomefloxacin hydrochloride crude extract and dissolve in 2 mL each of stationary phase and mobile phase for later use. Before sample injection, fill the entire column with the stationary phase, adjust the speed of the main engine to 800 rpm, and pump the mobile phase into the column at a flow rate of 1.0 mL / min. After the entire system reaches hydrodynamic equilibrium, the sample is injected through the injection valve. Then, accord...

Embodiment 3

[0018] First, ethyl acetate: ethanol: water (the content of sulfonated-β-cyclodextrin in water is 0.05mol / L) was arranged in a separatory funnel according to the volume ratio of 100:1:100, shaken up and then separated Floor. After balancing for a period of time, separate the upper and lower phases. A semi-preparative high-speed countercurrent chromatograph is used, equipped with an NS-1007 pump, a 20mL injection valve, a polytetrafluoroethylene column with a column volume of 250mL, an 8823A-UV ultraviolet detector, and a portable recorder. Weigh 20 mg of lomefloxacin hydrochloride crude extract and dissolve in 2 mL of stationary phase and 2 mL of mobile phase respectively. Before sample injection, fill the entire column with the stationary phase, adjust the speed of the main engine to 800 rpm, and pump the mobile phase into the column at a flow rate of 1.0 mL / min. After the entire system reaches hydrodynamic equilibrium, the sample is injected through the injection valve. Th...

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Abstract

The invention relates to a method for splitting a chiral medicine of hydrochloric acid lomefloxacin, adopting a high-speed counter-current chromatography method to separate out levorotatory hydrochloric acid lomefloxacin and dextrorotatory hydrochloric acid lomefloxacin from a hydrochloric acid lomefloxacin crude extract. A solvent system comprises three components of ethers or normal paraffin hydrocarbon or fatty ester, acetonitrile or fatty alcohol or fatty ketone and water, the volume ratio is sequentially 5-100:1:5-100, an upper phase is used as a stationary phase, a lower phase is used as a flowing phase, sulphonation-beta-schardinger dextrin is used as a chiral splitting reagent, the content of the sulphonation-beta-schardinger dextrin in the lower phase is 0.02-0.06mol / L, and a chiral flowing phase method is adopted to split a hydrochloric acid lomefloxacin enantiomorph. The method for splitting the chiral medicine of the hydrochloric acid lomefloxacin can achieve higher separating degree, is suitable for various types of prepared type counter-current chromatography instruments and can separate and obtain the monomers of the levorotatory hydrochloric acid lomefloxacin and the dextrorotatory hydrochloric acid lomefloxacin.

Description

technical field [0001] The invention relates to a resolution method for separating L-lomefloxacin hydrochloride and D-lomefloxacin hydrochloride from the crude extract of chiral drug lomefloxacin hydrochloride by high-speed countercurrent chromatography. Background technique [0002] Chirality is one of the essential properties of nature, which vividly reflects the relationship between objects and mirror images. Due to certain asymmetric factors in the molecular structure of chiral compounds, the compounds and their solutions have a certain degree of optical rotation in polarized light. Chiral compounds are ubiquitous in nature. In addition to the optical activity of most natural amino acids and natural sugars, insect pheromones, spices, and active ingredients of some Chinese and Western medicines are also chiral compounds. In addition, the life system is a complex chiral system. The basic substances that constitute organisms, such as amino acids, sugars, and proteins, are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04C07B57/00B01D15/08
Inventor 魏芸杜世娟
Owner BEIJING UNIV OF CHEM TECH
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