Fluconazole pharmaceutical composition and preparation method therefor

Abstract

The invention relates to a fluconazole pharmaceutical composition. The fluconazole pharmaceutical composition is composed of fluconazole and a microcrystalline cellulose complex, wherein a weight ratio of the fluconazole to the microcrystalline cellulose complex is (1: 4) to (2: 1). According to the fluconazole pharmaceutical composition, through selecting an appropriate microcrystalline cellulosecomplex, the powder fluidity can be improved, the uniformity and dissolving rate of drugs can be improved, and the stability of fluconazole capsules can be improved remarkably.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a fluconazole pharmaceutical composition and a preparation method thereof. Background technique [0002] Fluconazole is an pyrrole broad-spectrum antifungal drug developed by Pfizer Pharmaceuticals Ltd. It highly selectively interferes with the activity of fungal cytochrome P-450, thereby inhibiting the biosynthesis of ergosterol on the fungal cell membrane, making Cellular material leaks out and dies. It is mainly used clinically for vaginal candidiasis, oral thrush, atrophic oral candidiasis, fungal meningitis, pulmonary fungal infection, abdominal infection, urinary tract infection and skin fungal infection. The molecular target is: Lanosterol 14-alpha demethylase. [0003] The chemical name of fluconazole is α-(2,4-difluorophenyl)-α-(1H-1,2,4-triazol-1-ylmethyl)-1H-1,2,4-triazole -1-yl ethanol. The structural formula is shown in the following formula...

AI Technical Summary

Problems solved by technology

But the weak point of its technical scheme is: in the process of forming particles of fluconazole and hydrophilic surfactant in this invention, because the amount of surfactant is small, uneven distribution of surfactant in the particles is prone to occur, which affects the dissolution And in vivo absorption, bioavailability is not high

[0010] After searching, most of the existing technologies aimed at improving the stability of fluconazole capsules currently use the improvement of auxiliary materials or processes, and their common disadvantages are: the prepared fluconazole pharmaceutical composition has poor fluidity and intra-batch Large variance, low dissolution rate, poor stability and other risks

For example, in the description of the Chinese invention patent with the publication number CN 101460150A, a direct compressible compound for orally disintegrating tablets is introduced, and the combination of the compound is a water-soluble excipient and a water-insoluble excipient However, the patent scheme lists many and wide-ranging drugs, and it does not indicate that it can target specific drugs (such as fluconazole); from the examples 1 to 10 listed in the patent specification, it is only known that mannitol and at least one Two kinds of water-insoluble excipients are combined into a compound and applied to aspartame tablets; therefore, how to choose the appropriate compound components can improve the stability of fluconazole capsules, and no technical inspiration can be obtained from this patent

[0012] As another example, the Chinese invention patent with the publication number CN 105520918A discloses a pregabalin capsule, which is composed of pregabalin, lactose compound, and a pharmaceutically acceptable carrier. The lactose compound is made of lactose-microcrystalline cellulose. It can significantly improve the poor stability of pregabalin capsules, but the disadvantages of this technical solution are: ①The patent adopts a direct mixing process. Since the prescription contains a high proportion of starch, it will cause problems due to the poor fluidity of the starch itself. There is a risk of fluidity in the prepared mixed powder; ②Because there are multiple varieties of starch from different sources and different models, and the properties of different varieties vary greatly, there is a risk of large differences in dissolution within the batch; ③Pregabalin The physical and chemical properties are very different from those of fluconazole, so whether the lactose-microcrystalline cellulose compound is suitable for the development of fluconazole capsules is also uncertain

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