| Customization: | Available |
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| Powder: | Yes |
| Customized: | Non-Customized |
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Lincomycin Hydrochloride
A Lincosamides alkaline antibiotic obtained from a culture medium of Streptomyces lincolnencis. According to the anhydrate, the lincomycin should not be less than 82.5%.
Properties
White crystalline powder; slightly odorous or special odor; bitter taste. Soluble in water or mthanol, slightly soluble in ethanol. The pH of the 10% aqueous solution should be 3.0 to 3.5. Sex is more stable.
[Pharmacology]
(1) Pharmacodynamics
The antibacterial spectrum is narrower than erythromycin. Gram-positive bacteria such as Staphylococcus aureus (including penicillin-resistant strains), Streptococcus, pneumococcal, Bacillus anthracis, Mycoplasma hominis and certain mycoplasmas (Mycoplasma hyopneumoniae, Mycoplasma hyorhinis, Mycoplasma hominis), Leptospira All are sensitive to this product. Gram-negative bacteria such as Pasteurella, Klebsiella, Pseudomonas (Pseudomonas aeruginosa, etc.), Salmonella, Escherichia coli, etc. are all resistant to this product. The most important feature of lincomycin is that it has good antibacterial activity against anaerobic bacteria, such as Fusobacterium, Peptococcus, Streptococcus pneumoniae, Clostridium tetani, Clostridium perfringens and most actinomycetes. Antibiotics are sensitive. The mechanism of action of this class of drugs is the same as that of erythromycin, which mainly acts on the 50s subunit of bacterial ribosomes, and affects the synthesis of proteins by inhibiting the elongation of peptide chains. Since the action sites of erythromycin and chloramphenicol are the same, and the affinity of the first two for ribosomes is greater than the latter, this class of drugs should not be combined with erythromycin or chloramphenicol to avoid antagonistic phenomena.
Lincomycin is a bacteriostatic agent, but high concentrations also have a bactericidal effect on highly sensitive bacteria. Staphylococcus can slowly develop resistance to this product. Bacteria have complete cross-resistance to lincomycin and clindamycin, and may be partially cross-resistant with erythromycin.
(2) Pharmacokinetics
Lincomycin is poorly absorbed by the internal administration and can absorb about 30% to 40% of the dosage. Food can reduce its absorption rate and absorption. The concentration of the drug appeared in the serum 1.5 hours after oral administration, and the peak concentration of the blood drug reached 2 to 4 hours. After intramuscular injection, the absorption is rapid, and the peak concentration of blood is several times higher than that of oral administration. For example, if the pig is intramuscularly injected with llmg/kg, the peak plasma concentration is 6.25 μg/mL, while the internal dose is only 1.5 μg/mL. The absorption rate of different animals was also inconsistent. The peak concentration of blood was 13.47μg/mL after intramuscular injection of 20mg/kg for pigs; the intramuscular injection of 20mg/kg for 0.25h, and the peak concentration of blood for 0.25h; The same amount of injection takes 0.5h to reach the peak concentration of 5.83μg/mL. The product is widely distributed in the body, and its apparent distribution volume is 3.4L/kg buffalo, 1.7L/kg yellow cattle and 2.8L/kg pig. In most organizations, pleural effusion,
The ascites and joint fluid can reach an effective level, and the concentration in the bone tissue is particularly high, but it cannot penetrate the normal meninges. Even if the meninges are inflamed, it is not easy to penetrate into the cerebrospinal fluid. The plasma protein binding rate of lincomycin depends on the drug concentration and can range from 57% to 72%. The drug can pass through the placenta and can also be distributed in the milk at a concentration equal to or higher than the plasma concentration.
Lincomycin is mainly metabolized in the liver, excreted by bile and feces, and a small amount is excreted from the urine. Drugs excreted in the feces after oral administration accounted for 77%. Urinary excretion accounted for 14%. The elimination half-life of intramuscular injection was 3 to 4 hours for small animals, 6.79 hours for pigs, 2.2 hours for cows, 4.13 hours for cattle, 9.27 hours for buffaloes, and 8.1 hours for horses. Hepatic and renal dysfunction can prolong the half-life.
Use
Mainly used for various infections caused by sensitive bacteria such as pneumonia, bronchitis, sepsis, osteomyelitis, cellulitis, septic arthritis and mastitis. It also has preventive and therapeutic effects on pig's Treponema blood stasis, mycoplasma pneumonia, chicken air sac inflammation, Clostridium necrotic enteritis and acute rot disease of dairy cows. This product is more effective than spectinomycin in the infection of avian Mycoplasma and E. coli than a single drug.
medicine interactions
(1) In combination with gentamicin, it has a synergistic effect on Gram-positive bacteria such as Staphylococcus and Streptococcus.
(2) It should not be used together with anti-creeping antidiarrheal drugs, which can delay the excretion of intestinal toxins, leading to prolonged and exacerbated diarrhea. It is also not suitable to be taken orally with the kaolin earth laxative, which will reduce the absorption of lincomycin by more than 90%.
(3) Lincomycin has neuromuscular blocking effect, and should be noted when combined with other drugs with such effects, such as aminoglycosides and peptides.
(4) The combination of lincomycin and chloramphenicol or erythromycin has an antagonistic effect. Incompatibility with intravenous injection of kanamycin and novobiocin.
Note
(1) Lincomycin is banned in rabbits, hamsters, horses and ruminants because of severe gastrointestinal reactions (sudden diarrhea, etc.) and even death.
(2) Lincomycin is banned from animals that are allergic to this product or those that have been infected with candidiasis.
(3) Lincomycin can be discharged into the milk for the licking dog, and the cat may have diarrhea.
(4) The adverse reaction of dogs and cats in oral administration is gastroenteritis (vomiting, loose stools, bloody diarrhea in dogs). Intramuscular injection causes local pain in the injection. Rapid intravenous injection can cause elevated blood pressure and cardiopulmonary arrest. Gastrointestinal reactions can also occur in pigs. Large doses may cause skin erythema and anal or vaginal edema in most administered pigs.
(5) Drug withdrawal period, intramuscular injection of pigs for 2 days, oral administration of pigs for 5 days, chickens for 0 days, lactating cows, laying hens are prohibited.
| ITEM | STANDARD | RESULTS |
| Characters | White or almost white crystalline powder | meet |
| identification | conform to requirements positive |
pass pass |
| appearance of solution | clear and not more intensely conform than Y6 |
pass |
| specific rotation | +135 to +150° | +142° |
| solubility | conform to requirements | pass |
| Ph | 3.5-5.5 | 4.3 |
| Water by KF | 3.1%~4.6% | 3.5% |
| Sulfated ash | ≤0.5% | 0.07% |
| heavy metals | ≤5ppm | pass |
| related substances impurity A sum of peaks due to impurity B impurity C any other imputity total impurities: |
≤0.5% ≤0.5% ≤0.2% ≤0.10% ≤2.0% |
0.36% 0.30% 0.04% None detected 0.70% |
| Bacterial endotoxins | <0.51U/mg | <0.51U/mg |
| Residual solvents by GC: Aetone: Butanol: 2-octanol: |
≤500ppm ≤1000ppm ≤500ppm |
44ppm 263ppm 9ppm |
| Assay (anhydrous substance) Lincomycin Hydrochloride +Lincomycin B Hydrochloride Lincomycin B Hydrochloride |
96.0%-102.0% ≤5.0% |
98.9% 2.3% |
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