Pharmaceutical intermediate Clarithromycin Powder

CAS:81103-11-9

MF:C38H69NO13

MW:747.95

EINECS:1806241-263-5

Specification: 99% min Clarithromycin Powder

Sample:Clarithromycin Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: colorless to faint yellow

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Clarithromycin Powder Usage and Synthesis.

Clarithromycin is a semi-synthetic macrolide antibiotic, which can inhibit bacterial protein synthesis to achieve antibacterial effect, and can play a strong antibacterial effect on gram-positive bacteria, gram-negative bacteria, etc., which can significantly improve the clinical symptoms of patients.

It has a wide range of clinical applications, including soft tissue infections, skin infections, respiratory system, urinary system infections and eradication of Helicobacter pylori treatment.

The most common adverse reactions to clarithromycin are abdominal pain, diarrhoea, nausea, vomiting and abnormal taste, which are usually mild. There is also a risk of severe tip-twisting ventricular tachycardia, which should be monitored when the drug is administered.

Uses and functions of Clarithromycin.

Clarithromycin is a semi-synthetic macrolide antibiotic, which can inhibit bacterial protein synthesis to achieve antibacterial effect, and can play a strong antibacterial effect on gram-positive and gram-negative bacteria, which can significantly improve the clinical symptoms of patients.

It has a wide range of clinical applications, including soft tissue infections, skin infections, respiratory system, urinary system infections and Helicobacter pylori eradication therapy.

Macrolide antibiotics, a derivative of erythromycin, change the OH group on the 6 position of erythromycin A to OCH3, that is, clarithromycin.

It is effective against gram-positive and negative bacteria, chlamydia, and mycobacteria, and can effectively inhibit almost all respiratory pathogens. It is stable to gastric acid, well absorbed orally, with high blood concentration and long blood half-life.

Its use is similar to that of erythromycin, and it is effective against a wide range of infections in the respiratory tract, urinary tract, skin, and ear, nose and throat.

Pharmacological Effect of Clarithromycin.

Clarithromycin is a 14-membered ring macrolide broad-spectrum antibiotic. Its mechanism of action is the same as that of erythromycin, which is mainly to bind to the 50S ribosomal subunit of bacteria, and inhibit the synthesis of bacterial protein by blocking transpeptidation and mRNA shift, thus playing an antibacterial role.

Compared with erythromycin, clarithromycin has the characteristics of good oral absorption, fast peak time, high blood concentration, long half-life and small individual differences. Clarithromycin has a slightly stronger antibacterial effect than erythromycin on methicillin-sensitive staphylococci and streptococci.

The antibacterial activity of Clarithromycin is 2-4 times stronger than that of Erythromycin (its in vivo metabolite 14-hydroxyclarithromycin and Clarithromycin have synergistic antibacterial effect on E. influenzae). It is also stronger than erythromycin against Legionella pneumophila, Chlamydia trachomatis and Mycoplasma urealyticum.

Clarithromycin is bacteriostatic against Staphylococcus aureus and Streptococcus aureus, and bactericidal against Pneumococcus pneumoniae and H. influenzae.

Clarithromycin has strong antibacterial activity against Staphylococcus aureus, Streptococcus aureus, Haemophilus influenzae, Legionella, Gonococcus gonorrhoeae, Cattleya boulardii, Helicobacter pylori; it also has antibacterial effect on Mycobacterium avium, Mycobacterium avium, and Mycobacterium leprae; moreover, it is effective against Mycoplasma pneumoniae, Chlamydia trachomatis, and Mycoplasma urealyticum.

For erythromycin sensitive bacteria such as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Diplococcus pneumoniae, the effect is significantly better than erythromycin, the antibacterial effect of Streptococcus faecalis and Haemophilus influenzae and erythromycin, and erythromycin has cross-resistance.

Drug-resistant bacteria can produce an enzyme that methylates RNA, methylating the binding site of the ribosome so that the drug cannot bind to the ribosome.

In vivo antibacterial test, Clarithromycin's antibacterial effect on Staphylococcus aureus, Streptococcus pyogenes, S. pneumoniae, Haemophilus influenzae is 2-10 times stronger than that of erythromycin.

Product Method of  Bulk Clarithromycin Powder.

Erythromycin as raw material, hydrolysis to remove a methyl group on the amino group, and then react with benzyl chloroformate to protect the hydroxyl group and amino group on the tetrahydropyran ring of the 5-position side chain, and then react with iodomethane in dimethylsulfoxide and tetrahydrofuran to methylate the hydroxyl group on the 6-position, and then catalytic hydrogenolysis to remove the protective group, and then hydroxymethylation of the amino group in reaction with formaldehyde, and then finally reduced to a methyl group, that is, clarithromycin.