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Tilmicosin phosphate
Tilmicosin is a macrolide antibiotic developed for veterinary use. It is recommended for treatment and prevention of pneumonia in cattle, sheep and pigs, associated with Pasteurella haemolytica, P. multocida, Actinobacillus pleuropneumoniae, mycoplasma species and other microorganisms found sensitive to this compound.
Tilmicosin phosphate is a macrolide antibiotic synthesized from tylosin, It developed for veterinary use only.and it has an antibacterial spectrum similar to tylosin with enhanced activity against Pasteurella haemolytica, P. multocida, Actinobacillus pleuropneumoniae, mycoplasma species and other microorganisms found sensitive to this compound. It is recommended for treatment and prevention of pneumonia in cattle, sheep, poultry and pigs, Not show resistance and cross-resistance with other antibiotic often used in clinic. Mainly used in the Pleuropneumonia and the infection caused by Pasteurellaceae , Pasteurella and mycoplasma.
Specification:
Product name | Tilmicosin Phosphate |
Items | Specification |
Appearance | light yellow powder |
Identification | IR complies with CRS |
| Test of assay retention time of peak for sample complies with standard preparation |
Water | ≤5.0% |
PH | 5.0-8.0 |
Trans-Isomer (on dry basis) | 12.0-18.0% |
Cis-Isomer (on dry basis) | 82.0-88.0% |
Assay (Tilmicosin) | ≥75.0% |
Tilmicosin, (20-deoxo-20-(3,5-dimethylpiperidin-1-yl)-desmycosin) is chemically modified long-acting macrolide antibiotic applied in the veterinary medicine. It is active mainly against Gram-positive and some Gram-negative microorganisms (streptococci, staphylococci, Pasteurella spp., mycoplasmas, etc.). Applied orally in poultry, tilmicosin reaches maximum blood levels after 3 hours and maintains high therapeutic concentrations in the target tissues. It is concentrated in the lungs, penetrating intracellularly in the alveolar macrophages. It is eliminated mainly through feces and urine. Tilmicosin induces no teratogenic and embryotoxic effect.
Indication:
For the treatment of bovine respiratory disease (BRD) and ovine respiratory disease (ORD) associated with Mannheimia (Pasteurella) haemolytica. For the control of respiratory disease in cattle at high risk of developing BRD associated with Mannheimia (Pasteurella) haemolytica.
Dosage:
Available formulations of tilmicosin include an injectable for use in cattle and sheep (Micotil 300) and premix formulations for swine (Pulmotil G40, G100 and G200). The recommended dose of the injectable formulation in both cattle and sheep is a single subcutaneous (SC) injection of 10 mg/kg BW. Recommended dose for swine in feed is 200-400 mg/kg of feed for 10 to 21 days, equivalent to 8-20 mg/kg BW per day.
Chemical name:
Tilmicosin (IUPAC name): (10E, 12E)-(3R,4S,5S,6R,8R,14R,15R)-14-(6-deoxy-2,3-di-O-methyl-b-d-allo-hexopyranosyoxymethyl)-5-(3,6-dideoxy-3-dimethylamino-b-d-gluco-hexapyranosyloxy)-6-[2-(cis-3,5-dimethyl-piperidino)ethyl]-3-hydroxy-4,8,12-trimethyl-9-oxoheptadeca-10,12-dien-15-olide
Chemical Abstracts Services Name: tylosin, 4A-O-de(2,6-dideoxy-3-C-methyl-alpha-L-ribo-hexopyranosyl)-20-deoxy-20-(3,5-dimethyl-1-piperidinyl)-(20(cis: trans))
C.A.S. number: 108050-54-0
Synonyms: 20-Deoxy-20-(3,5-dimethylpiperidin-1-yl)-desmycosin
Molecular formula: C46H80N2O13
Molecular weight: 869.15
OTHER INFORMATION ON IDENTITY AND PROPERTIES
Pure active ingredient:
Melting point: Not determined
Solubility:
Freely soluble (1500 mg/L or greater) in organic solvents (hexane, acetone, acetonitrile, chloroform, dichloromethane, ethyl acetate, methanol, tetrahydrofuran); water solubility is temperature and pH dependent, but is 566 mg/mL at pH 7 and 25°C.
Purity:
Tilmicosin consists of 82-88% cis isomer and 12-18% trans isomer, as determined by liquid chromatographic assay.
Tilmicosin Base | USP36 |
Items | Specification |
Appearance | white or almost white powder |
Identification | conform |
Water | ≤5.0% |
Cis-Isomer | 82.0-88.0% |
Trans-Isomer | 12.0-18.0% |
Total related compound (on anhydrous) | ≤10.0% |
Individual related compound(on anhydrous) | ≤3.0% |
Assay(as anhydrous) | ≥85.0% |
Heavy metal | ≤20ppm |
Butyl acetate | <0.5% |
Dosage:
Available formulations of tilmicosin include an injectable for use in cattle and sheep (Micotil 300) and premix formulations for swine (Pulmotil G40, G100 and G200). The recommended dose of the injectable formulation in both cattle and sheep is a single subcutaneous (SC) injection of 10 mg/kg BW. Recommended dose for swine in feed is 200-400 mg/kg of feed for 10 to 21 days, equivalent to 8-20 mg/kg BW per day.