Itraconazole inhalation powder spray and preparation method thereof

Abstract

The invention discloses an itraconazole inhalation powder aerosol and its preparation method. The inhalation powder aerosol is prepared by using itraconazole and 20-80mass% of a carrier, and the carrier is at least one of lactose, mannitol, inulin and amino acids. The method comprises the following steps: mixing itraconazole with the carrier, adding the obtained mixture into a double screw hot melt extruder, setting the extrusion temperature at 150-170DEG C, starting screws after the preset temperature is reached, and carrying out strip extrusion under a screw rotating speed of 150-200r / min, cooling obtained strips in a dryer to room temperature, crushing by using a micro pulverization machine, and micronizing by using an airflow crusher to obtain the above powder. The inhalation powder aerosol has the advantages of good physical stability, good powder fluidity, high deposition amount at effective positions, high dissolution rate, fast dissolution speed, small drug dose, and low incidence rate of toxic side effects; and the method has the advantages of simple technology, no organic solvents, antiseptics or other impurities in the process, good reappearance and easy industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an itraconazole inhalation powder and a preparation method thereof. Background technique [0002] As an important drug delivery route, the pulmonary drug delivery route can be applied to local or systemic delivery of drugs to achieve safe, targeted, quick-acting, and highly effective therapeutic purposes. Local administration of the lung has significant advantages in the treatment of lung diseases, such as asthma, chronic obstructive pulmonary disease, cystic fibrosis, invasive pulmonary fungal infection and other diseases. Reduce the dosage and reduce systemic adverse reactions. Due to the special physiological structure of the lung, the surface area is large (about 100m 2 ), rich blood flow (about 5l / min), thin alveolar epithelial cells (about 0.1-0.5μm), which is conducive to the diffusion of drugs into the blood, and low enzyme activity, drug administration thr...

AI Technical Summary

Problems solved by technology

However, intravenous injection is prone to adverse reactions such as visual impairment and abnormal renal function, while oral administration is unstable, with significant individual differences, and is greatly affected by food. Due to the high permeability of oral liquid, patients are often accompanied by nausea, vomiting, abdominal pain and diarrhea And adverse reactions such as gastric mucosal bleeding

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