Novel incremental release osmotic pump preparation of paliperidone and preparation method thereof

Abstract

The invention belongs to the technical field of pharmaceutical preparations and discloses a paliperidone bi-layer osmotic pump progressively-increased controlled release tablet and a preparation method thereof. The osmotic pump preparation comprises a tablet core and a semipermeable coating film, wherein the tablet core comprises a medicine containing layer and a boosting layer, the semipermeable coating film envelops the tablet core and is provided with medicine release holes, the medicine containing layer contains middle molecular polyoxyethylene (average molecular weight is 900, 000-1, 000,,000) and an osmotic active substance in a certain proportion so that the hydration rate of the medicine containing layer is proper, the release of the active medicine basically presents a progressively-increased release trend and the progressively-increased release can be kept for 14-24 hours by using the bi-layer tablet core and the single-layer coating. By adopting the preparation, the adverse reaction of the medicine can be reduced greatly, the compliance of a patient can be improved, simultaneously, the preparation is simple to prepare, the preparation process of the progressively-increased osmotic pump preparation is simplified greatly, and the preparation is more conductive to industrialized production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a novel paliperidone incremental release osmotic pump preparation with simplified process and a preparation method thereof. Background technique [0002] Osmotic pump controlled-release preparation is currently a relatively mature slow-release preparation technology, and has such advantages as: 1) It is rarely affected by factors such as the pH value of the medium environment, gastrointestinal motility, and food, with small individual differences and good correlation between in vivo and in vitro; 2) stable blood drug, less adverse reactions; 3) less frequency of medication, high patient compliance, etc. been widely developed and applied. [0003] Problems in the clinical application of central nervous system (CNS) drugs: 1. The adverse reactions are large, especially in the early stage of taking the drug, and the patient’s tolerance is poor, and it is easy ...

AI Technical Summary

Problems solved by technology

[0003] Problems in the clinical application of central nervous system (CNS) drugs: 1. The adverse reactions are large, especially in the early stage of taking the drug, and the patient’s tolerance is poor, and it is easy to stop midway; 2. Dose titration (that is, slowly increasing the dose) To reduce the occurrence of adverse reactions, but it is inconvenient to take; the steady incremental release system can solve this problem well

The preparation contains a booster layer and two drug-containing layers with different drug contents, and is covered with a semi-permeable coating film. The process is complicated, especially the three-layer tableting technology, which requires a special three-layer tableting machine, which is difficult to realize.

[0006] Chinese patent CN 200910199425 discloses a double-layer osmotic pump system that can release paliperidone incrementally in about 5 hours in the early stage. The tablet core is composed of a booster layer and a drug-containing layer, and is covered with a water-soluble isolation coat and a semi-permeable film , control the thickness of the isolation gown to control the penetration of water, so as to achieve the effect of incremental release in the early stage, but the incremental release can only last for 5h

[0007] Another Chinese patent CN201110060811 discloses an anti-aging paliperidone osmotic pump preparation. This patent studies the aging problem when cellulose acetate and polyethylene glycol are used as film-forming materials. The patent research shows that cellulose acetate and polyethylene glycol Polyethylene glycol will be combined more tightly with the prolongation of storage time, resulting in a decrease in the porosity of polyethylene glycol and a decrease in membrane permeability (the patent calls this phenomenon aging), while using ethyl cellulose and poly Vitamin ketone as a film-forming material can weaken this phenomenon

The patent mainly protects the coating process and formulation, and does not mention the issue of incremental release

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