Itraconazole pellet as well as preparation method and preparation thereof

Abstract

The invention provides an itraconazole pellet. The itraconazole pellet is prepared by coating an itraconazole drug-containing layer and an isolated protective layer on the surface of the pellet core of the pellet in sequence, wherein the itraconazole drug-containing layer is prepared from itraconazole, a solid dispersion, a binder, an anti-sticking agent and an organic solvent; the isolated protective layer is prepared from a lubricant and a dispersion solvent. The invention further provides a preparation method of the itraconazole pellet and a preparation of a tablet or a capsule prepared by the itraconazole pellet. The itraconazole pellet disclosed by the invention can realize rapid dissolution, has dissolution rate of dissolving over 85% within 45 minutes, is remarkably superior to the existing itraconazole pellet, and can realize higher bioavailability, so that ideal medical effect is achieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an itraconazole pellet preparation and a preparation method thereof. Background technique [0002] Itraconazole is a synthetic broad-spectrum antifungal drug, a derivative of triazole, which can inhibit the synthesis of ergosterol, one of the main components of fungal cell membranes, thereby exerting antifungal effects. Good treatment for deep fungal infections, such as blastomycosis, histoplasmosis, coccidioidomycosis, and superficial fungal infections, such as pityriasis versicolor, vaginal candidiasis, tinea pedis, tinea manuum, tinea corporis, etc. It is also used for the long-term treatment of cryptococcosis in AIDS patients and the prevention of fungal infection in patients with neutropenia. Itraconazole, chemical name (±)-cis-4[4-[4-[4[2-(2,4-dichlorophenyl)-2-(1H1,2,4-triazole- 1-methyl)-1,3-dichloropentanyl]methoxy]]phenyl]-1-piperazinephenyl]-2,4...

AI Technical Summary

Problems solved by technology

[0006] Chinese patent document CN1262682A discloses a kind of itraconazole with improved solubility, its preparation method and oral pharmaceutical composition containing itraconazole, by dissolving itraconazole in an organic solvent, and carrying out dissolution-induced drying , to obtain the amorphous form of itraconazole with a diameter of 0.5-10 μm, and then make various types of oral drugs with pharmaceutical excipients. This simple method of dissolving itraconazole and then drying it is only Changing itraconazole from crystalline form to amorphous form slightly increased the dissolution rate, but it was far from meeting the requirement of more than 80% dissolution in 45 minutes in the Chinese Pharmacopoeia (2010 edition)

After the actual preparation, it was found that the oral solid preparation of the above-mentioned tablets cannot guarantee the ideal dissolution effect in a short time, and cannot achieve the drug effect well.

[0011] It can be seen that although the research on preparations containing itraconazole in the prior art is mainly focused on increasing its drug dissolution rate, the technical effects of existing multiple studies have also shown how to effectively improve the drug preparation of itraconazole. The dissolution rate problem still becomes the technical difficulty that needs to be solved urgently in this field

Images