Superfine powder of Fibrates lipid-lowering drug and preparation method therefor

Abstract

The invention relates to superfine powder of a Fibrates lipid-lowering drug and a preparation method therefor. The Fibrates lipid-lowering drug is a main therapeutic drug for resisting hyperlipidemia, and due to influence resulting from factors such as relatively poor water solubility and the like, the bioavailability of the Fibrates lipid-lowering drug is not high. The method for preparing the superfine powder of the Fibrates lipid-lowering drug, provided by the invention, comprises the steps of applying ultrasonic waves, of which the frequency is 10kHz to 500kHz, the power is 1mW to 5,000W and the sound intensity is 0.1mW / cm<2> to 500W / cm<2>, to a Fibrates lipid-lowering drug containing homogeneous solution so as to rapidly obtain Fibrates lipid-lowering drug crystals, and then, carrying out normal operations such as solid collecting, washing, drying and the like, thereby directly obtaining the superfine powder of the Fibrates lipid-lowering drug. According to the superfine powder prepared by the method, the bioavailability of the drug is improved, the dosage of the drug is reduced, the solubility of the drug is improved, and the drug absorption can be enhanced, so that the application is wider.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an ultrafine powder of a fibrate lipid-lowering drug and a preparation method thereof. Background technique [0002] About 12 million people die of cardiovascular disease and cerebral apoplexy every year in the world, and atherosclerosis caused by hyperlipidemia is the main cause of coronary heart disease, hypertension and cerebrovascular disease. In 2002, the global annual sales of only atorvastatin (a blood lipid-lowering drug) was nearly 8 billion US dollars, becoming the world's best-selling drug that year. It can be seen that the research and development of blood lipid-lowering drugs has significant social benefits and market prospects. [0003] Fibrate lipid-lowering drugs are a class of synthetic ligands of peroxisome proliferator-activated receptor α (PPARα), which can effectively delay the development of atherosclerosis. Among them, fenofibrate, as a typical fibrate d...

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

[0020] The airflow milling method is to crush the material through the airflow mill, which does not require media, is not easy to produce pollution, and has a large production capacity; however, this method is suitable for drugs with a certain hardness, and slight changes in the high-speed airflow milling process can easily cause local disturbances , produce large particles, poor process stability

[0021] Anti-solvent recrystallization, solvent diffusion, solvent evaporation, reaction precipitation, spray drying 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, industrial production The equipment is not easy to configure, the operation risk factor is high, and the cost is high

[0022] The various defects of the above-mentioned ultrafine powder preparation method are the main factors that have caused few fibrate lipid-lowering drugs to be marketed in the form of ultrafine powder.

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