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.