Scutellarin nanosuspension and preparation method thereof

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a scutellarin nanosuspension and a preparation method thereof. The scutellarin nanosuspension is prepared from a stabilizer and scutellarin in a weight ratio of (1:1)-(10:1). The preparation method is implemented through dissolving the scutellarin into an alkaline solution and then adding the obtained mixture into an acid solution containing the stabilizer, so that due to the solubility difference of the scutellarin in the acid solution and the alkaline solution, the scutellarin is oversaturated and then crystallized by separating; and carrying out homogenization on the obtained product by using a high-pressure micro jet homogenizer so as to obtain the scutellarin nanosuspension, wherein the particle size of the scutellarin nanosuspension is 100-500 nm, and the polydispersity index is 0.1-0.5. The scutellarin nanosuspension and preparation method thereof disclosed by the invention have the significant advantages that the nanosuspension improves the solubility of the scutellarin and increases the oral bioavailability of the scutellarin; the scutellarin nanosuspension can be solidified through freeze drying or spray drying, and applied to dosage forms such as tablets, capsules, granules, oral suspensions and the like; and the scutellarin nanosuspension is simple in preparation process, and convenient for industrial production.

Description

technical field

[0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a scutellarin nanosuspension and a preparation method thereof. Background technique

[0002] Scutellarin is the main active ingredient of breviscapine, and its chemical name is 4',5,6-trihydroxyflavone-7-O-β-D-glucuronide. Clinically, it is mainly used to treat cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease and other diseases. Because scutellarin is almost insoluble in water, its oral absorption is poor, and its bioavailability is low, so its clinical application is greatly limited. Currently clinically used breviscapine preparations mainly include tablets, powder injections, injections and the like. The oral bioavailability of ordinary tablets is low, and the half-life of ordinary injections and powder injections is short and eliminated rapidly in the body.

[0003] In order to improve the solubility and bioavailab...

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