Ziprasidone hydrochloride pharmaceutical composition and preparation method thereof

Abstract

The invention discloses a ziprasidone hydrochloride pharmaceutical composition and a preparation method thereof. The ziprasidone hydrochloride pharmaceutical composition comprises ziprasidone hydrochloride, glutamic acid, sodium acetate trihydrate, lactose and hydroxypropyl methylcellulose. The preparation method comprises the following steps: adding the ziprasidone hydrochloride into a solvent, heating the mixture at 40-60 DEG C, and continuously stirring the mixture to enable the medicine to be in a suspension state to prepare a suspension A; dissolving the rest components in appropriate amount of water to obtain a solution B; slowly adding the solution B into the solution A under stirring, continuously heating the mixture to keep the temperature at 40-60 DEG C during the process, and continuously stirring the mixture until the medicine is completely dissolved to prepare a transparent or reddish mixed solution C; carrying out vacuum rotary evaporation to dryness on the mixed solutionC at 40-60 DEG C to obtain a material D; and (3) placing the material D in a vacuum drying oven, carrying out vacuum-drying at 40-60 DEG C for 12-24 hours, carrying out crushing and sieving to obtainziprasidone hydrochloride pharmaceutical granules, and preparing the granules into tablets or capsules and other dosage forms by adopting conventional methods.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical compositions, and in particular relates to a pharmaceutical composition of ziprasidone hydrochloride and a preparation method thereof. Background technique [0002] Worldwide, about 1% of people are troubled by schizophrenia. Ziprasidone hydrochloride is a second-generation atypical broad-spectrum antipsychotic drug developed by Pfizer in the United States. It is clinically used to treat schizophrenia and bipolar disorder. Disorder manic episodes and agitation symptoms in the acute phase of schizophrenia. This product is well tolerated and rarely causes extrapyramidal adverse reactions. [0003] The chemical name of ziprasidone hydrochloride is 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3- Dihydro-2H-indol-2-one hydrochloride monohydrate is a white to light pink powder with a solubility in water of about 0.3 μg / ml. It is an insoluble drug, and its solubility has obv...

AI Technical Summary

Problems solved by technology

It belongs to class II in the classification system of biopharmaceuticals, and its low solubility leads to low oral bioavailability. The oral bioavailability of its commercially available preparations is about 30%. Under the premise of taking it with food with more than 500Kcal calories at the same time, the drug The bioavailability is 60%. Fasting and full stomach have a great influence on the absorption and curative effect of the drug

[0004] However, patients taking ziprasidone hydrochloride have poor drug compliance, and it is difficult to control whether the patient takes the drug on an empty stomach or on a full stomach, and it is difficult to ensure good absorption of the drug, resulting in a decline in the efficacy of the drug, which brings huge harm to patients and their families. Mental stress and financial loss

[0005] Therefore, in order to meet the needs of the market and improve the compliance of patients taking the medicine, improve the safety and effectiveness of the medicine, a simple, stable and easy-to-industrial production of ziprasidone hydrochloride that can solve the poor solubility of the medicine has been developed. The pharmaceutical composition and its preparation method are one of the new problems to be solved urgently in this medicine

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