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Method for preparing amorphous tildipirosin

A new, amorphous technology of tedrol, which is applied in the field of preparation of tedrol, can solve problems such as difficulty, poor control, and high cost of industrialization

Active Publication Date: 2016-10-26
TIANJIN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

General amorphous preparation methods are spray drying, melt solidification, rapid evaporation solvent solidification or acid-base reaction precipitation method, etc. These methods have high industrialization costs and are difficult to control.

Method used

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  • Method for preparing amorphous tildipirosin
  • Method for preparing amorphous tildipirosin
  • Method for preparing amorphous tildipirosin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Add 5g of Tideroloxine raw material into 70g of isopropyl ether, stir and dissolve at 65°C, filter to obtain a clear solution, add 15mL of water dropwise, stir for 2h to obtain a white solid, and filter with suction to obtain a wet sample.

[0037] Do the XRD analysis spectrum of the wet sample as attached figure 1 As shown, there are obvious diffraction peaks at 2θ=4.70±0.2, 6.26±0.2, 8.22±0.2, 8.64±0.2, 9.56±0.2, 10.39±0.2, 10.97±0.2, 12.80±0.2, 13.42±0.2, 14.44±0.2 0.2, 15.06±0.2, 15.28±0.2, 15.78±0.2, 16.84±0.2, 17.28±0.2, 17.84±0.2, 18.35±0.2, 18.78±0.2, 19.34±0.2, 20.30±0.2, 21.08±0.2, 21.58±0.2 have characteristic peaks. The thermogravimetric weight loss map of the wet sample is attached figure 2 As shown, there is 12.6% weight loss before 100°C; the scanning electron microscope photos of wet samples are attached image 3 As shown, it is a long rod crystal form, indicating that the wet sample is an isopropyl ether solvent compound.

[0038] Place the wet sam...

Embodiment 2

[0040] Add 4 g of Tideroloxine raw materials to 60 g of isopropyl ether, stir and dissolve at a constant temperature of 50 ° C, filter to obtain a clear solution, add 10 mL of water dropwise and continue stirring for 1 h to obtain a white solid, and suction filter to obtain a wet sample. Wet sample is made XRD analysis pattern and attached figure 1 Consistent, with the same peak spectrum position and shape; thermogravimetric analysis weight loss is 12.5%. The wet sample was placed in a vacuum drying oven at 80°C and dried under normal pressure for 3 hours to obtain 3.68 g of an amorphous solid product of Tedirosin. The XRD pattern of the sample and the attached Figure 4 Same, no obvious peak shape, no weight loss by thermogravimetric analysis.

Embodiment 3

[0042] Add 2g of Tideroloxine raw material to 60g of isopropyl ether, stir to dissolve at 40°C, filter to obtain a clear solution, add 20mL of water dropwise, and continue stirring for 1h to obtain a white solid, which is obtained by suction filtration to obtain a wet sample. Wet sample is made XRD analysis pattern and attached figure 1 Consistent, with the same peak spectrum position and shape; thermogravimetric analysis weight loss is 12.3%. The wet sample was placed in a vacuum drying oven at 60°C for 3 hours to obtain 1.69 g of an amorphous solid product of Tedirosin. The XRD pattern of the sample and the attached Figure 4 Same, no obvious peak shape, no weight loss by thermogravimetric analysis.

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Abstract

The present invention relates to a method for preparing amorphous tildipirosin. The amorphous tildipirosin has an endothermic peak at 135-171 DEG C and has an exothermic peak at 186-210 DEG C in a TG-DSC spectrum and has no recognizable diffraction peak in an XPRD spectrum. The preparation method comprises steps as follows: selecting isopropyl ether as a solvent for dissolution, then adding water to precipitate solids, and drying a wet sample thoroughly after filtration to obtaining an amorphous product. The amorphous product has good stability and can be preserved for a long period without degradation. The amorphous tildipirosin is used for preparing a pharmaceutical preparation, and the dosage form of the pharmaceutical preparation can be premix, tablets, pills, powder, granules, capsules or injections. Compared with other crystal forms of tildipirosin, the amorphous tildipirosin has better solubility and higher bioavailability.

Description

technical field [0001] The invention belongs to the technical fields of medical technology and preparation of veterinary antibiotics, and in particular relates to a method for preparing tedirosine amorphous. Background technique [0002] Tedirosin is a safe and effective broad-spectrum antibiotic for the treatment of livestock and poultry respiratory infections caused by Mannheimia haemolytica, Pasteurella multocida and Haemophilus somnus. Tedirosin was developed by Intervet Schering-Plough, and in March 2011 the European Union approved the marketing of Tedirosin injection. [0003] The polymorphic state of solid drugs is an important content in the study of the existing state of drugs. For most chemical drugs, polymorphic phenomena generally exist. The polymorphism of the drug will directly affect the stability, solubility, bioavailability, safety, effectiveness and processing performance of the drug. Tiderol exists in various forms of solvent compounds and non-solvent co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08C07H1/06
CPCC07H1/06C07H17/08
Inventor 龚俊波吴送姑何林华向毅侯宝红陈小林曹建东
Owner TIANJIN UNIV
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