Double-layer breviscapine sustained-release tablet and preparation method thereof

Abstract

The invention relates to a double-layer breviscapine sustained-release tablet. One layer is a rapid-release layer that comprises 15-20g of breviscapine and routine tablet additives which are 0.5-4 of the weight of the breviscapine and comprise one or more of the following components: starch, lactose, microcrystalline cellulose, mannitol, CMS-Na, talcum powder, magnesium stearate L-HPC, PVPP and croscarmellose sodium; and the other layer is a sustained-release layer which comprises 45-40g of the breviscapine and skeleton matrixes which are 0.5-4 of the weight of the breviscapine and can be hydroxypropylmethyl cellulose, ethyl cellulose, carbopol or stearic acid, and auxiliary skeleton materials such as acrylics and polyvinylpyrrolidone can be also added. The preparation method of the double-layer sustained-release tablet is as follows: the components are mixed according to the proportion and compressed on a double-layer tablet machine to form the double-layer sustained-release tablet.

Description

technical field [0001] The invention relates to a breviscapine sustained-release tablet, in particular to a double-layer breviscapine sustained-release tablet with an immediate-release layer and a sustained-release layer. [0002] The present invention also relates to a preparation method of the above-mentioned breviscapine sustained-release tablet. Background technique [0003] Breviscapine is an active ingredient of flavonoids extracted from Erigeron breviscapus (Scutellaria breviscapus) (Asteraceae breviscapitalis). Reduce thrombus, reduce whole blood viscosity, significantly reduce platelet aggregation rate or platelet count; improve microcirculation disorder, accelerate blood flow; dilate cerebral blood vessels, reduce cerebral vascular resistance and peripheral blood pressure; significantly increase coronary flow and reduce the scope of myocardial infarction And anti-hypoxia and other effects, it is clinically used for the prevention and treatment of cerebrovascular d...

AI Technical Summary

Problems solved by technology

Not only that, scutellarin is also a weakly acidic drug, and the absorption becomes poor due to dissociation in the intestinal tract, so the bioavailability of breviscapine is low, and its absolute bioavailability (=AUC po / AUC iv *100%) is only 16.2%

Oral biological half-life of breviscapine (about 2 hours), the bioavailability of its ordinary granules and ordinary tablets is low, and the effective blood concentration is maintained for a short time, and its indication is cerebrovascular disease, which is a chronic disease and difficult to cure Large, its recovery period and sequelae treatment cycle is long

Therefore, it is necessary to use large doses of multiple administrations in clinical practice to achieve the therapeutic purpose, which not only causes "peak-valley" fluctuations in blood drug concentration, but also brings great troubles to patients. It is too long to maintain effective blood drug concentration and exert a continuous therapeutic effect, and there is a blind spot in the curative effect, and there is instability in the clinical curative effect. Developing it into a once-a-day sustained-release tablet can overcome the above deficiencies

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