Ultrafine powder of HMG-CoA reductase inhibitor and preparation method of ultrafine powder

Abstract

The invention relates to ultrafine powder of an HMG-CoA reductase inhibitor and a preparation method of the ultrafine powder. The HMG-CoA reductase inhibitor is mainly used for heterozygous familial and non-familial hyperlipidemia and can also be used for hypercholesteremia caused by type-2 diabetes and nephrotic syndrome. The preparation method of the ultrafine powder of the HMG-CoA reductase inhibitor includes: in a homogeneous solution containing the HMG-CoA reductase inhibitor, applying ultrasonic wave of 10kHz-500kHz in frequency, of 1mW-5000W in power and 0.1mW / cm<2>-500W / cm<2> to quickly obtain HMG-CoA reductase inhibitor crystals; subjecting the HMG-CoA reductase inhibitor crystals to conventional operations such as solid collection, washing and drying to directly obtain the ultrafine powder of the HMG-CoA reductase inhibitor. The ultrafine powder prepared by the method does not contain matrix materials, has the characterisitics of large drug carrying capacity, high dissolving speed and easiness in realizing higher bioavailability, stability and safety and the like, meets needs on improving bioavailability of drug, lowering drug dosage and reducing adverse reaction and is wider in application range.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an ultrafine powder of an HMG-CoA reductase inhibitor and a preparation method thereof. Background technique [0002] HMG-CoA reductase inhibitors are the most widely used lipid-lowering drugs in clinical practice. With the improvement of living standards, the number of hyperlipidemic groups has increased sharply, and the market demand for lipid-lowering drugs has also increased significantly. Among the lipid-lowering drugs such as HMG-CoA reductase inhibitors, pravastatin, lovastatin, simvastatin, fluvastatin, and atorvastatin have all entered the National Basic Medical Insurance Drug List. In 2004, statin lipid-lowering drugs accounted for 86.8% of the world's lipid-lowering drug market, and statins in the domestic market are in the growth stage. [0003] Lovastatin is easily soluble in methanol and chloroform, soluble in ethanol and ethyl acetate, and almost insoluble in wa...

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

[0015] 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

[0016] The various defects of the above-mentioned ultrafine powder preparation method are the main factors leading to the absence of HMG-CoA reductase inhibitors in the form of ultrafine powder.

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