Penfluridol polyanhydride pellets and penfluridol long-acting controlled-release tablets and preparation method thereof

Abstract

The invention discloses a penfluridol polyanhydride pellet and a penfluridol long-acting controlled release tablet as well as a preparation method of the penfluridol long-acting controlled release tablet. The penfluridol long-acting controlled release tablet is prepared from the following components in percentage by weight: 50-60 % of penfluridol polyanhydride pellets, 15-20 % of starch, 10-16 % of sucrose powder, 5-10 % of polysaccharide, 0.2-1.0 % of magnesium stearate, and 1-3 % of hydroxypropylcellulose, wherein the penfluridol polyanhydride pellets are mixture particles composed of (fumaric acid--sebacic acid) polyanhydride [P(FA--SA)] (FA:SA=0.25:1) and penfluridol, and the weight percentage of penfluridol is 15-25 %. The penfluridol long-acting controlled release tablet has the long-acting controlled release effect, and is orally taken twice per month, 2 tablets each time, or the tablets are increased or decreased according to the diseases, or the administration is carried out following the doctor's advice, so that the untoward effects of penfluridol can be greatly reduced, the clinical efficacies can be improved, the home treatment for psychopaths is conveniently maintained, and the hospitalization expenses and other treatment cost of the psychopaths are reduced. Compared with the other clinical medicines for treating schizophrenia, the penfluridol long-acting controlled release tablet has better economic applicability and better clinical efficiency.

Description

technical field [0001] The present invention relates to penfluridol preparations. Background technique [0002] Penfluridol is a commonly used antipsychotic drug in clinical practice. At present, long-acting sugar-coated tablets are taken orally in clinical practice. The usual dosage is to take 1-3 tablets orally once a week, 20 mg per tablet. It has definite curative effect on the treatment of various types of acute and chronic schizophrenia [1] , becoming one of the first-line antipsychotic drugs in psychiatry. [0003] However, it is worth noting that since the drug has been used in clinical practice for decades, many patients with mental illness have experienced various adverse reactions of varying degrees. Parkinson's syndrome-like symptoms such as tremor and salivation; ②Acute dystonia: such as compulsive mouth opening, tongue protruding, torticollis, respiratory movement disorder, and dysphagia; ③Akathisia: such as restlessness and repeated wandering; ④Delayed onset...

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Problems solved by technology

[0003] However, it is worth noting that since the drug has been used in clinical practice for decades, many patients with mental illness have experienced various adverse reactions of varying degrees. Parkinson's syndrome-like symptoms such as tremor and salivation; ②Acute dystonia: such as compulsive mouth opening, tongue protruding, torticollis, respiratory movement disorder, and dysphagia; ③Akathisia: such as restlessness and repeated wandering; ④Delayed onset Sexual dyskinesia: mouth-tongue-buccal triad, such as sucking, tongue licking, chewing, etc., the most common ones are tremor, akinesia, tachycardia, etc., the incidence rate is as high as 40%, and it may even cause a transient Once serious adverse reactions occur, the normal life of mentally ill patients will be greatly disturbed. In severe cases, there are many cases of suicide to get rid of pain.

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