Tilmicosin Raw material Tilmicosin Powder

CAS:108050-54-0

MF:C46H80N2O13

MW:869.15

EINECS:639-676-2

Specification: 99% min Tilmicosin Powder

Sample:Tilmicosin Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance: White Powder

Storage: Store at -20°C

Shelf Life: 2 Years

Test Method: HPLC

Tilmicosin Powder Usage and Synthesis.

Tilmicosin is a newer macrolide antibiotic semi-synthesised from tylosin for livestock and poultry, with the chemical name of 4A-O-de(2,6-dideoxy-3-C-methyl-L-ribose-pyranohexyl)-20-deoxy-20-(3,5-dimethyl-1-piperidinyl)-[20(cis:trans)] tylosin, molecular formula C46H80N2O13, molecular weight 869.15. The antibacterial spectrum is similar to that of Tylosin, but it can be used against haemorrhagic Pasteurellamultocida and haemorrhagic Pasteurellamultocida. 869.15.

Tilmicosin has an antimicrobial spectrum similar to that of tylosin, but with an enhanced effect against haemorrhagic septic Pasteurellamultocida (English: Pasteurellamultocida) and Pasteurella haemolytica.Developed in the 1980s, it was initially used with the designation EL-870 It was developed in the 1980s, initially using EL-870 as the code name.

Commonly used trade names are Pulmotil© and Micotil©, and formulations include tilmicosin soluble powder, premix (20%), and injection.

It was approved in most European countries in 1990 and in the United States in 1992, and is included in the United States Pharmacopoeia. There are also some domestic enterprises in China that have been approved to produce tilmicosin.

Due to its special antibacterial activity and pharmacokinetic characteristics, the drug has been approved for clinical use in the prevention and treatment of infectious diseases in cattle, goats, sheep, dairy cattle, pigs, chickens and other animals.

In particular, it is used in the treatment of respiratory diseases of livestock and poultry, such as Actinobacillus pleuropneumonia, Pasteurella and chicken mycoplasmosis, and mastitis in lactating animals.

Uses of Tilmicosin.

Mainly used for the treatment of pleuropneumonia, infections caused by Actinobacillus, Pasteurella and Mycoplasma.

Mainly used for the prevention and treatment of pneumonia (caused by Actinobacillus pleuropneumoniae, Pasteurella, Mycoplasma and other infections), avian mycoplasmosis and mastitis in lactating animals.

Synthetics of Tilmicosin.

Timicosin is a semi-synthetic macrolide antibiotic developed in 1980s for livestock and poultry, with molecular weight 869.15.The reaction of tylosin with 3,5-dimethyl piperidine produces tylosin base, and then phosphoric acid and water are added to form phosphoric acid tylosin, which is a mixture of cis-trans isomers.

Tilmicosin is a very active product obtained by the amination of aldehyde group after the study of desugarisation of tylosin, which was carried out using the Wallach reaction with formic acid as a catalyst to obtain tilmicosin in good yields.

Synthesis steps.

1, the preparation of deglycosylated tylosin Dissolve 19 g of tylosin phosphate with 100 ml of water, slowly heated to 50 ° C, while slowly adding 3 ml of concentrated sulfuric acid, heated to 30 ° C and held for 1 hour, and then cooled to room temperature, add 500 ml of butyl acetate, and finally adjusted to PH value of 13 with 0.1 mol / LNaOH, divided into the organic layer, to be used in the next step of the reaction.

2、Preparation of tilmicosin Add 4 ml of 3,5-dimethyl piperidine to the separated organic layer, heat to 70 ℃, add 3 ml of formic acid, separate the aqueous layer, then add 400 ml of water, adjust the PH value to 11 with 0.1 mol/L NaOH, precipitate precipitation, filtration, washing, vacuum drying, to obtain the product of 15.1 grams, yield 89%.

This process adopts the separation and extraction process of acid solubilisation and alkali solubilisation and acid precipitation, taking advantage of the different solubility of the target compounds in water and organic medium without distillation and heating, which is beneficial for promotion.

In vivo studies of Bulk Tilmicosin Powder.

Elimination of tilmicosin from serum and emulsion was relatively slow after subcutaneous injection, with t1/2βS of 9.3 and 41.4 h, respectively. tlmicosin had an apparent volume of distribution greater than 1 l/kg. Subcutaneous injection of 10 mg/kg resulted in a peak plasma concentration of tilmicosin of 1.56 µg/ml 6.39 h later.

Tilmicosin was widely secreted into breast milk, reaching a maximum concentration of 11.6 micrograms/ml, with an AUC milk/AUC serum ratio of approximately 12:1. 11 days after a single subcutaneous dose, tilmicosin was detectable in breast milk!