A kind of venlafaxine sustained-release preparation and preparation method thereof

Abstract

The invention relates to a sustained-release preparation of venlafaxine and a preparation method thereof. The sustained-release preparation is a double-layer osmotic pump tablet of venlafaxine, wherein one layer contains most of the marked amount of venlafaxine and osmotic enhancement Substance, another layer contains osmotic substances, the tablet core is wrapped by a semipermeable membrane containing a polymer, and there is a small hole on the semipermeable membrane on the side of the layer containing the active ingredient of the drug, and there is also a coating layer containing the drug.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical preparation, in particular to a venlafaxine sustained-release preparation and a preparation method thereof. Background technique [0002] The structural formula of venlafaxine is: 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol, and its hydrochloride is commonly used in medicine. It is called venlafaxine hydrochloride. The drug belongs to 5-hydroxytryptamine (5-HT)-norepinephrine (NE) reuptake inhibitors, and exerts antidepressant effect by significantly inhibiting the reuptake of 5-HT and NE. It is different from tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MAOIs) in that it has a unique chemical structure and neuropharmacological effects. The drug mainly exerts dual antidepressant effects by simultaneously blocking the reuptake of NE and 5-HT, increasing the concentration of NE and 5-HT, and has only a slight inhibitory effect on the reuptake of dopamine (D...

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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