Paroxetine hydrochloride enteric-coated and sustained-release tablet and its preparation method

Abstract

The invention discloses a paroxetine hydrochloride enteric-coated and sustained-release tablet, which comprises a tablet core, an isolating layer, a semipermeable membrane, an enteric coating and a moistureproof coat; the isolating layer is arranged between the tablet core and the semipermeable membrane, the enteric coating is arranged between the semipermeable membrane and the moistureproof coat,wherein the tablet core is prepared from paroxetine hydrochloride, penetrating agent, filling agent, binding agent and lubricant; the penetrating agent comprises one or more drug release hole. The invention further provides a preparation method of the paroxetine hydrochloride enteric-coated and sustained-release tablet, which includes steps of preparing tablet core grains and performing compression moulding to obtain the tablet core; making the tablet core pass through the isolating layer, the emipermeable membrane, the enteric coating and moistureproof coat, drying to obtain the paroxetine hydrochloride enteric-coated and sustained-release tablet. The paroxetine hydrochloride enteric-coated and sustained-release tablet can effectively control the drug release rate, and keep stable blooddrug concentration and durable drug effect, increase the safety, effectiveness and compliance of patients after taking drugs; the production preparation technique is simple, and the cost is low.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a paroxetine hydrochloride enteric-coated sustained-release tablet and a preparation method thereof. Background technique [0002] Paroxetine is a selective serotonin reuptake inhibitor (SSRI) type antidepressant used to treat depression, obsessive-compulsive disorder, panic disorder or social anxiety disorder. [0003] The earliest common preparation of this product on the market has serious adverse reactions in the gastrointestinal tract and poor compliance. Therefore, an enteric-coated sustained-release preparation that is taken once a day has been launched abroad. Paroxetine hydrochloride enteric-coated sustained-release tablets are developed by GlaxoSmithKline (GSK), under the trade name CR is marketed and clinically used for the treatment of severe depression, panic disorder (with or without place phobia), social anxiety disorder and premenstrual anxiety disorder. Ent...

AI Technical Summary

Problems solved by technology

[0004] Because the Paroxetine Hydrochloride Sustained-release Preparation developed by GlaxoSmithKline (GSK) adopts a skeleton erosion structure, the release and absorption rate of the drug are also affected by factors such as the gastrointestinal fluid in the patient's body, so its blood drug concentration remains the same. There are large fluctuations, difficult to control and predict, and have a certain degree of uncertainty. The duration of effective effects and the magnitude of side effects also vary from person to person, with large individual differences and uncontrollable

[0005] Osmotic pump-type controlled-release preparations use osmotic pressure as the driving force for drug release and are characterized by zero-order release kinetics. The most widely used is the dual-chamber osmotic pump controlled-release tablet, but most of the dual-chamber osmotic pump tablets are currently on the market. Type osmotic pump controlled-release tablets have the following defects: (1) The preparation process is special, and the production cost is relatively high

(2) The thermal stability of the main auxiliary materials of the tablet core is poor

Polyoxyethylene is used as the main auxiliary material for dual-chamber osmotic pump controlled-release tablets. It has poor thermal stability and a low glass transition temperature (62-67°C). After granulation, the drying temperature should not exceed 40°C, which is prone to excessive solvent residues. , and in the tableting process, it is necessary to install a special device to cool down the tableting machine. At the same time, the storage conditions of the preparation are relatively high, and improper storage is prone to changes in the stability of the storage process.

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