Quetiapine fumarate film-controlled slow-release pellet capsule

Abstract

The invention relates to a quetiapine fumarate film-controlled slow-release pellet capsule. A slow-release film of the quetiapine fumarate film-controlled slow-release pellet utilizes Eurdragit RL 30D as a film-formation material. A pellet core of the quetiapine fumarate film-controlled slow-release pellet contains low-substituted hydroxypropyl cellulose having high expansibility, and also contains a pharmaceutically-acceptable common excipient for the slow-release pellet, wherein preferably, the excipient comprises microcrystalline cellulose, and the pellet core comprises 10 to 40wt% of the low-substituted hydroxypropyl cellulose. The slow-release film comprises Eurdragit RL 30D, triethyl citrate as a plasticizer and talcum powder as an antiplastering aid, wherein preferably, a ratio of Eurdragit RS 30D to triethyl citrate to talcum powder is 30: 3: 4 and a film weight increasing ratio is in a range of 19 to 35%. The quetiapine fumarate film-controlled slow-release pellet comprises the pellet core containing low-substituted hydroxypropyl cellulose having high water expansibility and thus after absorbing water, the quetiapine fumarate film-controlled slow-release pellet expands so that the slow-release film is stretched; the thickness of the slow-release film is reduced; the water-permeable micropore size is increased; and permeability is improved and the permeability reduction caused by film aging is counteracted. Therefore, in middle and later stages, the quetiapine fumarate film-controlled slow-release pellet release rate is basically constant; in the last stage, residues are less; and stable release performances can be kept in the period of validity.

Description

technical field [0001] The invention relates to a quetiapine fumarate film-controlled sustained-release pellet capsule, in particular to a quetiapine fumarate film-controlled sustained-release pellet capsule containing low-substituted hydroxypropyl cellulose in the pellet core, It belongs to the field of pharmaceutical preparations. Background technique [0002] Quetiapine fumarate is an atypical antipsychotic drug, which produces anti-schizophrenia effect by antagonizing multiple neurotransmitter receptors, and is used for the treatment of manic episodes in schizophrenia and bipolar disorder. [0003] Quetiapine fumarate is almost insoluble in water, and the earliest common preparation on the market needs to be taken twice a day, the blood concentration fluctuates greatly, the peak concentration is too high, and the adverse reactions are serious. [0004] Quetiapine Fumarate Sustained-release Tablets (trade name: Seroquel) listed by AstraZeneca is a matrix-type sustained-r...

AI Technical Summary

Problems solved by technology

[0007] In order to solve the problem of release decline caused by film aging of quetiapine fumarate film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a quetiapine fumarate that can maintain stable release performance throughout the validity period. Membrane-controlled quetiapine fumarate sustained-release pellets and capsules are characterized in that the core of the pellets contains low-substituted hydroxypropyl cellulose with high water-swellability, and the sustained-release coating film is deformed by water swelling. thereby counteracting the aging of the membrane

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