Paroxetine sustained release preparation and preparation method thereof

Abstract

The invention relates to a paroxetine sustained release preparation and a preparation method thereof. The sustained release preparation is a paroxetine double-layer osmotic pump tablet, wherein one layer contains most of paroxetine and a permeation enhancing substance in labelled amount, and the other layer contains an osmotic substance; the a tablet core is wrapped by a semipermeable membrane containing polymer; the semipermeable membrane on the side containing a pharmacological active ingredient layer is provided with a small hole. Besides, the preparation also comprises a medicine-containing coating layer.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical preparation, in particular to a paroxetine sustained-release preparation and a preparation method thereof. Background technique [0002] Paroxetine is a selective serum reuptake inhibitor (SSRI) type antidepressant, and its drug form is Paroxetine hydrochloride. It is commonly used in the treatment of depression and obsessive-compulsive disorder in clinical practice. Sexually inhibits the reuptake of 5-HT by the presynaptic membrane. It leads to the accumulation of 5-HT in the synaptic gap, thereby enhancing the transmission efficiency of 5-HT. It is the most effective inhibitor of 5-HT reuptake among several SSRIs. The ability to inhibit the reuptake of NE is much smaller, it is insensitive to dopamine and histamine receptors, and has only a weak affinity to M receptors. EEG shows that taking this product does not cause sedation, but clinical use can significantly improve sleep. Regardless ...

AI Technical Summary

Problems solved by technology

Another problem of this type of tablet is that the active ingredient of the drug is released incompletely, about 15% cannot be released, so it is necessary to increase the dose of the drug in the drug layer, that is, the layer of the drug contains more than 15% of the active ingredient on the label to be compatible with the drug layer. Bioequivalence of regular tablets or extended-release tablets with other sustained-release mechanisms

To solve the defect that the active ingredient in the osmotic pump double-layer tablet cannot be completely released, the method of using 15% more actual content than the labeled amount is currently used. However, the osmotic pump preparation still cannot solve the problem of this type of tablet in the human body and in vivo. The release shows a hysteresis problem of 1 to 3 hours. In the prior art, in order to solve this problem, Chinese patent CN 101856339A adopts a layer of gastric-soluble coating layer containing an appropriate amount of drugs to solve the hysteresis problem of 1 to 3 hours. , but the plan is to prevent the drug from being exposed to the natural environment and cause instability, so a layer of gastric-soluble coating is added to the outermost layer, resulting in too thick a film coating layer of the tablet, and the surface finish becomes poor during the tablet collision process. The surface layer is easy to absorb water, the storage time is reduced, and the stability is poor.

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