Sustained-release solid preparation for oral use

摘要

It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release matrix preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release matrix preparation comprising (A) a pharmacologically active drug, (B) a combination of cellulose derivatives, and (C) mannitol.

主权项

1. The sustained-release matrix preparation comprising:
(A) a pharmacologically active drug, (B) a combination of cellulose derivatives consisting of:
(i) hydroxy propyl methylcellulose acetate succinate,(ii) hydroxy propyl cellulose having a viscosity of 150 to 400 mPa·s and/or 1000 to 4000 mPa·s, and(iii) hydroxypropyl cellulose having a viscosity of 3.0 to 5.9 mPa·s, and (C) mannitol, wherein, when the preparation is subjected to a dissolution test by the paddle method at rotation rates of 50 rpm and 200 rpm at 37±0.5° C. for 2 hours in 0.01 N hydrochloric acid, the preparation exhibits a difference in average percentage dissolution (value at the rotation rate of 200 rpm in the paddle method−value at the rotation rate of 50 rpm in the paddle method) of the pharmacologically active drug in the dissolution test medium of 10% or lower, or exhibits an average percentage dissolution ratio (value at the rotation rate of 200 rpm in the paddle method/value at the rotation rate of 50 rpm in the paddle method) of the pharmacologically active drug in the dissolution test medium of 2.0 or lower.