Colistin Sulphate
colistin sulfate
CAS: 1264-72-8
Molecular Formula: 2(C52H98N16O13).5(H2SO4)
Colistin Sulphate - Names and Identifiers
Colistin Sulphate - Physico-chemical Properties
| Molecular Formula | 2(C52H98N16O13).5(H2SO4) |
| Molar Mass | 2801.27 |
| Density | 1.26g/cm3 |
| Melting Point | 200-220°C |
| Boling Point | 1537.3°C at 760 mmHg |
| Specific Rotation(α) | -63~-73º |
| Flash Point | 883.5°C |
| Water Solubility | Soluble in water |
| Solubility | It is soluble in water, slightly soluble in ethanol, and almost insoluble in acetone, chloroform or ether. |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | White to white-like powder |
| Merck | 14,2479 |
| PH | 4.0～6.0（10g/l, 25℃） |
| Storage Condition | Inert atmosphere,2-8°C |
| Refractive Index | 1.575 |
| MDL | MFCD00146495 |
| Physical and Chemical Properties | Melting Point: 200-220°C |
| Use | Mainly used for sensitive bacterial infections, such as sepsis, acute enteritis, urinary tract infection and so on |
Colistin Sulphate - Risk and Safety
| Hazard Symbols | T - Toxic |
| Risk Codes | 25 - Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | TR1500000 |
| HS Code | 29419000 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
Colistin Sulphate - Reference
| Reference Show more | 1. Wang Honggang, Zhang Wei, Zhu Weiming, et al. Effects of polymyxin E-induced intestinal flora imbalance on intestinal barrier function and bacterial translocation [J]. Parenteral and enteral nutrition, 2012, 019(002):102-106. 2. Cen Daoji, Mai Jialin, Zhou Yuyuan, drug resistance of Escherichia coli in Guangdong goose farm and transmission characteristics of blaCTX-M genes [J]. China Animal Husbandry and Veterinary Medicine, 2020,047 (005):1571-1582. 3. Zhou Qing. Analysis of Lipid A Structure of Vibrio parahaemolyticus and Study on Related Genes [D]. Jiangnan University, 2020. 4. Chen, Bo-Chen, et al. "Phenanthrene antibiotic targets bacterial membranes and kills Staphylococcus aureus with a low propensity for resistance development." Frontiers in microbiology 9 (2018): 1593.https://doi.org/10.3389/fmicb.2018.01593 5. [IF = 4.396] Gengqi Liu et al. "A new self-immolative colistin prodrug with dual targeting functionalities and reduced toxicity for the treatment of intracellular bacterial infections." JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A |
Colistin Sulphate - Reference Information
| colistin sulfate | colistin sulfate, also known as colistin sulfate, Christian (Colistin), polymyxin E(Polymyxin E), antidixin, etc., white or nearly white powder, odorless, bitter and hygroscopic, soluble in water, slightly soluble in methanol and ethanol, almost insoluble in acetone, diethyl ether, etc., free alkali is slightly soluble in water. Stable on a PH3-7.5 scale. Colistin sulfate is produced by Polymyxa and has a strong antibacterial effect on Gram-negative bacteria. It is used to treat intestinal diseases caused by Gram-negative bacteria. It is used as a feed additive and has a significant growth-promoting effect. It is better combined with sulfadiazine. |
| pharmacodynamics | colistin sulfate is a narrow-spectrum fungicide. It has a strong antibacterial effect on gram-negative bacteria such as Escherichia coli, Salmonella, Pasteurella, Shigella, Brucella, Vibrio, Pseudomonas aeruginosa, etc. Among them, it has a strong bactericidal effect on Pseudomonas aeruginosa and Vibrio. The bactericidal mechanism is to damage the bacterial cell membrane, increase its permeability, leak amino acids, purines, pyrimidine, K, etc. in the bacteria, and can also affect the function of nucleoplasms and ribosomes, leading to bacterial death. Bacteria are not easy to develop drug resistance to this product, and there is complete cross-resistance with polymyxin B, but there is no cross-resistance with other antibacterial drugs. All Gram-positive bacteria and Proteus, Brucella and Serratia are resistant to this product. Colistin sulfate is mainly used to treat intestinal infections caused by Gram-negative bacilli, and topical to treat Pseudomonas aeruginosa infections caused by burns and trauma. As a feed drug additive, it has the effect of promoting growth. |
| pharmacokinetics | this product is rarely absorbed orally, and the drug is poorly distributed in the body after absorption and lasts for a short time. After 8 hours of oral administration, except bile, there were only trace amounts in other tissues, and there were no residues in all tissues after 16 hours. After injection, it is widely distributed in the body, reaching a peak in the main tissues at 0.5-1h, but it is not easy to penetrate into the chest cavity, joint cavity and infection foci, and it is also difficult to enter cerebrospinal fluid. 6h after blood, trachea, salivary glands, kidney, urine can not be detected, 24h after trachea, kidney, urine can not be detected. The protein binding rate of the drug is low. Mainly excreted by the kidney, renal insufficiency is easy to accumulate in the body. |
| anti-endotoxin | endotoxin is a toxin synthesized, produced and released by bacteria, consisting of O-specific side chains, core polysaccharides and lipid A. All antibiotics cause bacterial endotoxin release problems, and colistin sulfate causes the lowest bacterial endotoxin release. More importantly, colistin sulfate can neutralize endotoxin. It binds positively charged-NH2 to negatively charged phosphate on endotoxin lipid A produced by bacteria. Therefore, colistin sulfate can eliminate bacterial endotoxin and inhibit the release and vitality of bacterial endotoxin. It is a good anti-endotoxin drug. According to Lu Genfa et al. (2004) and other research reports, once endotoxin binds to receptors on the cell surface and mediates cell activation, colistin sulfate will lose its anti-endotoxin effect. Therefore, supporting colistin sulfate The direct neutralization of endotoxin is the main way to antagonize endotoxin. |
| pharmacological activity | colistin sulfate has three key active group structures in its molecular structure: fatty acid, positively charged amino acid and cyclic peptide. The lack or change of any of the above structures will greatly reduce its bactericidal activity. Colistin sulfate plays a bactericidal role, mainly positively charged free amino groups, which can combine with the negatively charged phosphate radicals in the phospholipids in the plasma membrane of bacterial cells, reducing the surface tension of the plasma membrane of bacteria and destroying the cell membrane The integrity of the cell membrane increases the permeability of the cell membrane, and makes the main components in the cell, especially purines and pyrimidines, flow out of the cytoplasm, resulting in bacterial growth being inhibited or bacterial death. Because the cell membrane of gram-negative bacteria contains a large amount of phospholipids, and the cell membrane of gram-positive bacteria contains very little phospholipids, so the antibacterial effect of colistin sulfate is mainly against gram-negative bacteria The effect is the strongest. In view of this, the antibacterial spectrum of colistin sulfate is only limited to gram-negative bacteria such as Escherichia coli, Salmonella, Pasteurella, Pseudomonas aeruginosa and Haemophilus. Moreover, these bacteria are usually resistant to commonly used aminoglycosides, penicillins, cephalosporins, fluoroquinolones, etc., which are quite common; moreover, many bacteria have multiple drug resistance. However, colistin sulfate is not easy to develop drug resistance, so far no resistance has been found against the transmission of colistin sulfate resistance plasmid. Therefore, the drug resistance of colistin sulfate spreads and spreads very slowly. At present, most gram-negative bacteria are quite sensitive to colistin sulfate. |
| characteristics of colistin sulfate | (1) strong resistance to gram-negative bacilli. Especially for Escherichia coli, Salmonella, Pseudomonas aeruginosa has a specific development hindrance. (2) has the effect of killing bacteria. By hindering the selective permeability function of cell membrane, bacteria die (3) there is almost no problem of drug resistance. No R-factor resistance was found. (4) Synergistic effect with anti-gram-positive bacteria drugs. Combined with bacitracin zinc, flavomycin, sulfonamides, semi-synthetic penicillin, gentamicin, etc., the effect is even better. (5) No residue. When administered orally, it is hardly absorbed by the intestine, but when injected intramuscularly, the blood is collected and sucked well, so there is no need to worry about residues in animal products. (6) promote the growth of livestock and poultry and prevent infectious enteritis of livestock and poultry. |
| use | is an antibiotic drug, which is used to treat intestinal diseases caused by gram-negative bacilli and has a certain growth-promoting effect mainly used for sensitive bacterial infections, such as sepsis, acute enteritis, urinary tract infection and other antibiotics. this product is produced by polymyxobacteria and has a strong antibacterial effect on gram-negative bacteria, it is used to treat intestinal diseases caused by gram-negative bacteria. Colistin sulfate is used to penetrate the cell membrane of bacteria and mannose anti-hemagglutination and antibiotic resistance of certain organisms, such as Bowman. It is also used to study the hephrotoxicity in rat kidney, MIC value, time killing kinetics, and post-antibiotic effect (PAE) of Pseudomonas aeruginosa |
Last Update：2024-04-09 21:21:28
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