The invention discloses a
febuxostat enteric-coated sustained-release micro-tablet
capsule as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The
capsule is a multi-unit
drug delivery system and is formed by filling a
hard capsule shell with an enteric sustained-release micro-coated
chip with the
diameter of 1.5-2.5 mm; the micro-coated
chip comprises a febux
drug-loaded tablet core and is externally coated with a functional
coating film, and the
coating film is of a single enteric-coated layer or a double-layer structure of a sustained-release layer and an enteric-coated layer. Through prescription-process cooperative control, the release rate of the preparation in 0.1 mol / L
hydrochloric acid within 2 hours is less than or equal to 10%, the release rate of the preparation in a
phosphate buffer solution with the pH value of 6.8 within 6 hours is 60-85%, and the release behavior conforms to Higuchi or zero-order
kinetics and the fitting degree Rgt; and 0.85%. In-vivo research of Beagle dogs shows that Tmax is prolonged to 4.0-8.0 h, Cmax is reduced by 35%-65%, and the
blood concentration gt; 100ng / mL is maintained for more than or equal to 12h, the peak-valley fluctuation coefficient is remarkably reduced compared with that of a
reference preparation, a
blood concentration-
time curve is more stable, and administration can be performed once a day. According to the present invention, the defects of large
blood concentration fluctuation, multi-time administration and strong
gastrointestinal tract stimulation of the rapid release preparation are solved, and the rapid release preparation is suitable for
gout and
hyperuricemia treatment, and is especially suitable for
gastrointestinal tract sensitive patients.