The invention discloses a
paliperidone release rate progressive increasing preparation and a preparation method thereof. The
paliperidone release rate progressive increasing preparation provided by the invention, from outside to inside, comprises a non-essential damp-proof beautiful
coating, a semipermeable rigid film shell which plays a vital role, and an
osmotic pump tablet core provided with one or more holes. The
osmotic pump tablet core, from top to bottom, is composed of a controlled-release layer, a
drug-containing layer and a push promoting layer; and penetration enhancers in the push promoting layer, in accordance with different
coating weight increasing degrees, include a
coating penetration enhancer I, a coating
penetration enhancer II and a coating
penetration enhancer III. The various coating penetration enhancers, which are different in coating
weight increasing degree, differ in
osmotic pressure in water. With the application of the
paliperidone release rate progressive increasing preparation disclosed by the invention, when water enters the tablet core along with an
osmotic pressure difference, the push promoting layer absorbs water to be swelled so as to push the outward release of the
drug-containing layer and the controlled-release layer, and as time varies, the isolating coating penetration enhancers are exposed in the water, so that the
osmotic pressure is continuously increased, a water-absorbing rate is increased and a
drug-release rate is increased as well, thus progressive increasing
drug release is achieved; therefore, the drug-release rate is effectively controlled, a
blood drug concentration curve is kept stable and the fluctuation of
blood drug concentration is relieved.