Ultrafine powder of macrolide drug and preparation method for ultrafine powder

Abstract

The invention relates to ultrafine powder of a macrolide drug and a preparation method for the ultrafine powder. The macrolide drugs are widely applied in clinic with definite curative effects. The drugs are wide in antibacterial spectrum, strong in antibacterial activity in vivo and long in biological half life period, and have good clinical use value. A method for preparing the ultrafine powder of the macrolide drug comprises: in a homogeneous solution containing the macrolide drug, applying ultrasound with frequency of 10kHz to 500kHz, power of 1mW to 5000W and acoustic intensity of 0.1mW / cm2 to 500W / cm2 to quickly obtain crystals of the macrolide drug; and then directly obtaining the ultrafine powder of the macrolide drug through conventional operations such as solid collection, washing and drying and the like. The ultrafine powder prepared according to the method provided by the invention does not contain a substrate, and has the advantages of high drug loading capacity, high dissolving speed and proneness to achieve better bioavailability, stability and safety, thereby meeting the requirements on bioavailability, dosage reduction and adverse effects of drugs, and having broad clinic application prospects.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an ultrafine powder of macrolide drugs and a preparation method thereof. Background technique [0002] Macrolide drugs are a class of drugs with a wide range of antibacterial activities, and are products with definite clinical efficacy. The antibacterial mechanism of these drugs is to act on the nucleoprotein 50S subunit in the bacterial 70S system, hindering the synthesis of bacterial proteins. The antimicrobial spectrum of macrolides includes Staphylococcus, Streptococcus, Diphtheria, Meningococcus, Bordetella pertussis, Legionella, Bacillus anthracis, Brucella, Campylobacter, Mycoplasma pneumoniae, Leptospira, and Chlamydia trachomatis etc. In terms of clinical application, such drugs are mainly used in respiratory tract infections, genitourinary system infections, skin and soft tissue infections, etc. At present, there are more than 50 kinds of macrolide antibiotics used ...

AI Technical Summary

Problems solved by technology

However, due to the high requirements of supercritical technology on equipment and the state of supercritical fluid is greatly affected by temperature and pressure, it is difficult to maintain the state, and the research on related application equipment still needs to be further strengthened

[0027] Anti-solvent recrystallization, solvent diffusion, solvent evaporation, reaction precipitation and other methods, due to uncontrollable crystal growth, resulting in large product size differences, and generally accompanied by high-speed stirring or high-speed centrifugation or high-pressure homogenization, while spray drying and freezing Drying is used as a drying method to collect dry particles and usually needs to be combined with other methods; the above methods are not easy to configure industrial production equipment, the operation risk factor is high, and the cost is high

[0028] The various defects of the above-mentioned ultrafine powder preparation method are the main factors that have caused no macrolide drugs to be listed in the form of ultrafine powder so far.

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