Osmotic pump controlled release tablet with milnacipran selected-time delayed controlled release function and method for preparing osmotic pump controlled release tablet

Abstract

The invention discloses an osmotic pump controlled release tablet with a milnacipran selected-time delayed controlled release function and a method for preparing the osmotic pump controlled release tablet. The osmotic pump controlled release tablet comprises a tablet core and a semi-permeable membrane with medicine release holes. The tablet core comprises a medicine containing layer and a propulsion layer, the medicine containing layer comprises hot-melt extrusion substances, the hot-melt extrusion substances are prepared from milnacipran and hot-melt excipients, the hot-melt excipients preferably are compositions of PVP (polyvinyl pyrrolidone) and PEG (polyethylene glycol), and a weight ratio of the PVP to the PEG is 4:1-10:1; the propulsion layer comprises polyoxyethylene, osmotic pressure active substances, povidone and the like; the medicine containing layer and the propulsion layer are compressed to obtain a double-layer tablet, then the semi-permeable membrane wraps the double-layer tablet, and the semi-permeable membrane is perforated. According to the technical scheme, the osmotic pump controlled release tablet and the method have the advantages that medicines can be effectively released in a controlled manner, medicine onset blanking periods can be shortened, the osmotic pump controlled release tablet which is prepared by the aid of hot-melt extrusion processes can becompletely released in an in-vitro manner and effectively conforms to zero-order release characteristics, and the bioavailability and the stability of the osmotic pump controlled release tablet whichis a product can be improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a milnacipran time-delayed controlled-release osmotic pump controlled-release tablet and a preparation method thereof. Background technique [0002] Milnacipran (milnacipran, trade name is Ixel, chemical name is 1-phenyl-2-aminomethylcyclopropane-N, N-diethylformamide,) is developed by French Pierre Fabre pharmaceutical company A drug for the treatment of depression developed and launched in 1997, milnacipran belongs to the serotonin and norepinephrine reuptake inhibitor (SNRI), the drug is the fourth generation of antidepressants, can simultaneously Inhibiting the reabsorption of serotonin and norepinephrine by neurons with similar strength, this product can also be used for the treatment of diseases such as fatigue, pain, fibromyalgia and irritable bowel syndrome. However, some formulations and compositions of milnacipran have problems such as poor stabilit...

AI Technical Summary

Problems solved by technology

However, some preparations and compositions of milnacipran have poor stability and low bioavailability.

[0003] For example, the invention patent application with the application number CN1232387A discloses a galenic preparation for prolonged release of milnacipran. Resin coating, in which the acrylic resin and the components of milnacipran microparticles work separately, this preparation cannot achieve the same release behavior in gastric juice and intestinal juice

And with the application of large-scale production, some problems have also appeared: the loss rate is relatively large; the production efficiency is low (the output is only 60-100kg per day); it is mainly based on membrane control, and the stability is not good; the requirements for workers to operate Higher, requiring longer training sessions to master

Although it has been improved compared with the known process scheme, it is difficult to achieve effective controlled release of the drug, and there may be a blank period of drug onset

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