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Levofloxacin Hcl Powder Usage and Synthesis.Levofloxacin is the left isomer of Ofloxacin, which is 8 times more water-soluble than Ofloxacin, easier to be made into injections, and has fewer toxic side effects. It was firstly marketed in Japan in 1994, and belongs to the third-generation of quinolone antimicrobial drugs. It is a third generation quinolone antibacterial drug. It mainly exerts antibacterial effects by inhibiting topoisomerase IV and DNA rotase (topoisomerase II), which are required for bacterial DNA replication, transcription, repair and recombination.
Levofloxacin is twice as active as ofloxacin against most clinical isolates. Because of its good activity against common respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, and Mycoplasma pneumoniae, it is also known as & ldquo; respiratory quinolone & rdquo;, and has a stronger antimicrobial activity against Pseudomonas aeruginosa than its predecessor.
Uses and functions of Levofloxacin Hcl.
Levofloxacin has excellent in vitro activity, less toxic side effects than ofloxacin, greater safety and good pharmacokinetic properties.
It can be widely used in respiratory tract infections, gynaecological infections, skin and soft tissue infections, surgical infections, biliary tract infections, sexually transmitted diseases, as well as otorhinolaryngological infections and other bacterial infections, etc. It is a broad-spectrum fluoroquinolone antimicrobial drug for oral or gastrointestinal use.
It is mainly used in the manufacture of various types of levofloxacin capsules, tablets and other antibacterial preparations.
Fully synthetic antimicrobial agent, used in the treatment of respiratory tract, urinary tract and skin tissue infections, etc.
Drug interactions of Levofloxacin Hcl.
1, and non-steroidal anti-inflammatory drugs at the same time, there is the possibility of triggering convulsions.
2、Combined with theophyllines, it may lead to the increase of theophylline blood concentration and the symptoms of theophylline poisoning.
3, and containing magnesium or aluminium antacids, aluminium sulfate, metal cations (such as iron), zinc-containing multivitamin preparations and other drugs can significantly reduce the absorption of levofloxacin.
4, with hypoglycaemic drugs, should pay attention to the monitoring of blood glucose concentration during the use of drugs.
Production Method of Bulk Levofloxacin Hcl Powder.
Method 1: Racemic ofloxacin is directly split by high performance liquid chromatography column filled with special stationary phase to obtain the levulinic acid; or oxfloxacin is treated with hydroxylamine sulphate, acidified with hydrochloric acid to obtain the hydrochloride salt by alkaline ion-exchange column, the amphoteric compounds are obtained, and added with (S)-(+)-mandelic acid, which forms crystals with the salt of the (-)-isomer, and then passes through the ion-exchange resin, and then reduced to deaminate the product. The product was obtained.
Method 2: Using 2,3,4,5-tetrafluorobenzoic acid as raw material, ethyl 2-(ethoxymethylene)-3-oxo-3-(2,3,4,5-tetrafluorophenyl)propanoate is prepared by the commonly used method, and then the asymmetric carbon atoms are introduced by reacting with (S)-2-aminopropanol, and the product is obtained by closing the ring, hydrolysing and introducing methyl piperazine.
Method 3: 2,3-difluoro-6-nitrophenol can also be used as a raw material and reacted with glycidyl p-toluenesulfonate in R configuration in the presence of a phase transfer catalyst to produce an optically active compound, which is then reduced and condensed with diethyl ethyl ethoxymethylenemalonate (EMME), and then treated with Mitsunobu's reagent, ring closure, ring closure, hydrolysis, and introduction of piperazinyl groups to obtain the product.
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