A kind of furatriptan succinate sustained-release microspheres and preparation method thereof

Abstract

The invention provides a frovatriptan succinate sustained-release microsphere, which consists of frovatriptan succinate and PLGA, wherein the weight ratio of the frovatriptan succinate to the PLGA is at 1: (1-15); and the frovatriptan succinate accounts for 15.9-23.7% in terms of the total weight of the microsphere, wherein in the PLGA, the molar ratio of lactic acid to glycolic acid is at (75-50): (25-50). With the application of the microsphere, an effective blood concentration can be kept for a relatively long time, the compliance of patients can be improved and a curative effect can be enhanced; and importantly, the microsphere is safe and controllable.

Description

Technical field The invention relates to a sustained-release furotriptan succinate preparation and a preparation method thereof. Background technique Furotriptan succinate, also called frovatriptan succinate, Chinese chemical name (R)-3-(methylamino)-2,3,4,9-tetrahydro-1H-carbazole-6- Formamide succinic acid. Furotriptan succinate is a new anti-migraine drug. This product mainly acts on the extracerebral arteries and intracranial arteries, and inhibits the excessive expansion of these blood vessels. As a second-generation triptan drug, it overcomes the shortcomings of the first-generation 5-HT1B / 1D receptor agonist of low oral bioavailability, short half-life and high recurrence rate. At present, there are mainly furotriptan succinate tablets and injections on the market in my country. Although conventional tablets are convenient to take, they are affected by factors such as disintegration and drug release. The absorption effect is not ideal, and they are often needed in the ...

AI Technical Summary

Problems solved by technology

As a second-generation triptan drug, it overcomes the disadvantages of low oral bioavailability, short half-life and high relapse rate of the first-generation 5-HT1B / 1D receptor agonists

At present, there are mainly furovatriptan succinate tablets and injections on the market in our country. Although conventional tablets are convenient to take, they are affected by factors such as disintegration and drug release, and the absorption effect is not ideal. multiple doses

Although the curative effect of the injection is fast, it is inconvenient to carry and use.

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