Tolterodine Tartrate Film-controlled Sustained-release Pellet Capsules

Abstract

The present invention relates to a kind of tolterodine tartrate film-controlled slow-release pellet capsule, the slow-release film of its pellet adopts the mixture of water dispersion Eurdragit RL 30D:Eurdragit RS 30D=9:1 weight ratio as film-forming material, The ball core contains low-substituted hydroxypropyl cellulose with high expansibility, and excipients commonly used in pharmaceutically acceptable sustained-release pellets. The excipients are preferably microcrystalline cellulose and lactose, wherein the low-substituted hydroxypropyl cellulose in the ball core Propylene cellulose accounts for 10-40% by weight of the ball core. The sustained-release coating film comprises a mixture of water dispersion film-forming materials Eurdragit RL 30D and Eurdragit RS 30D, plasticizer triethyl citrate and anti-sticking agent talc, the ratio of which is preferably Eurdragit RL 30D: Eurdragit RS 30D: citric acid Triethyl ester:talc powder=27:3:2:4, and the coating weight gain is preferably 19-34%. Because the ball core contains low-substituted hydroxypropyl cellulose with high water swelling, it will swell obviously after absorbing water, resulting in the expansion of the slow-release coating film, the thickness becomes thinner, the pore size of the water-permeable micropores becomes larger, and the permeability is improved. It has become better and compensated for the decrease in permeability caused by membrane aging, so that the release rate in the middle and late stages is basically constant, and the residual at the end is small, and it can always maintain a stable release performance within the validity period.

Description

technical field [0001] The invention relates to a tolterodine tartrate film-controlled sustained-release pellet capsule, in particular to a film-controlled sustained-release pellet capsule of tolterodine tartrate containing low-substituted hydroxypropyl cellulose in the pellet core, which belongs to medicine formulation field. Background technique [0002] Tolterodine tartrate is a muscarinic receptor antagonist, through selective and competitive antagonism of muscarinic receptors, inhibiting the continuous and excessive excitation of human bladder muscle, and is used to relieve urinary frequency and urgency caused by overactive bladder and urinary incontinence. [0003] Tolterodine tartrate is slightly soluble 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] The tolterodine tartrate sustained-release caps...

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem of release decline caused by film aging of tolterodine tartrate film-controlled sustained-release pellets prepared by aqueous dispersion coating, the present invention provides a film capable of maintaining stable release performance throughout the validity period Controlled tolterodine tartrate 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 absorbing water to swell to offset membrane aging

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