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Ziprasidone hydrochloride solid dispersible tablets and hot melt extrusion method thereof

A technology of hot-melt extrusion of ziprasidone hydrochloride, which is applied in the direction of pharmaceutical formulations, organic active ingredients, and medical preparations of non-effective ingredients, etc. It can solve the problem of limited application range, high experiment cost, and large production input volume, etc. problem, to achieve the effect of improved performance in vivo and in vitro, good reproducibility, and simple production process

Active Publication Date: 2018-05-29
江苏省药物研究所有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantage is firstly that drugs with poor thermal stability cannot use this technology, and the scope of use is limited
Secondly, the scale-up production of the pilot scale has a large amount of feed material and the cost of the experiment is high.

Method used

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  • Ziprasidone hydrochloride solid dispersible tablets and hot melt extrusion method thereof
  • Ziprasidone hydrochloride solid dispersible tablets and hot melt extrusion method thereof
  • Ziprasidone hydrochloride solid dispersible tablets and hot melt extrusion method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] prescription:

[0053]

[0054] Preparation method: After fully mixing ziprasidone hydrochloride, CopovidoneS630, EudragitEPO, Soluplus, extrude strips through a twin-screw hot-melt extruder, after cooling and solidifying, crush them for 90 seconds to obtain a solid dispersion, and then add Filler microcrystalline cellulose, disintegrant croscarmellose sodium and lubricant magnesium stearate, after mixing again, use a single-punch tablet machine to directly compress the powder into tablets, and the weight of the tablet is 3-4kg Within 1-2min, the disintegration time limit is sufficient.

Embodiment 2

[0056] prescription:

[0057]

[0058] Preparation method: After fully mixing ziprasidone hydrochloride, CopovidoneS630, EudragitEPO, Soluplus, extrude strips through a twin-screw hot-melt extruder, after cooling and solidifying, crush them for 90 seconds to obtain a solid dispersion, and then add Filler microcrystalline cellulose, disintegrant croscarmellose sodium and lubricant magnesium stearate, after mixing again, use a single-punch tablet machine to directly compress the powder into tablets, and the weight of the tablet is 3-4kg Within 1-2min, the disintegration time limit is sufficient.

Embodiment 3

[0060] prescription:

[0061]

[0062] Preparation method: After fully mixing ziprasidone hydrochloride, CopovidoneS630, EudragitEPO, Soluplus, extrude strips through a twin-screw hot-melt extruder, after cooling and solidifying, crush them for 90 seconds to obtain a solid dispersion, and then add Filler microcrystalline cellulose, disintegrant croscarmellose sodium and lubricant magnesium stearate, after mixing again, use a single-punch tablet machine to directly compress the powder into tablets, and the weight of the tablet is 3-4kg Within 1-2min, the disintegration time limit is sufficient.

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Abstract

The invention discloses ziprasidone hydrochloride solid dispersible tablets and a hot melt extrusion method thereof. Based on ziprasidone hydrochloride as a main component, one or two of mixed carriers of copolyvidone S630 or HPMCAS-HF (hydroxypropyl methylcellulose acetate succinate) as a base, a coating material is added, and the glass transition temperature of an extruded mixture can also be reduced; then, a surfactant is added. The ziprasidone hydrochloride solid dispersible tablets are prepared through steps as follows: the raw and auxiliary materials are evenly mixed by a three-dimensional mixing machine, extruded by a hot melt extruder at a high temperature and ground into powder with proper size; the powder is then mixed with a fixed quantity of filler, disintegrant and lubricant sufficiently and uniformly, and direct tableting is preformed, and the ziprasidone hydrochloride solid dispersible tablets are prepared. The prepared ziprasidone hydrochloride solid dispersible tabletshave the advantages that the problem of poor in-vitro dissolution of ziprasidone hydrochloride is solved, bioavailability of ziprasidone hydrochloride under the condition of empty stomach is improved, and the treatment effect of the tablets is improved finally.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a hot-melt extrusion method for preparing ziprasidone hydrochloride solid dispersion. Background technique [0002] Ziprasidone hydrochloride (Formula 1) is a kind of second-generation atypical antipsychotic drugs. It is clinically used to treat schizophrenia, manic episodes of bipolar disorder and agitation symptoms of polar phase in patients with schizophrenia. Unlike typical antipsychotics, research suggests that it acts through antagonism of D2, 5-HT2A, 5-HT2C, and 5-HT1 receptors. Due to its relatively high affinity for 5-HT2A receptors, the probability of extrapyramidal systemic reaction ESP is greatly reduced. [0003] [0004] Formula 1: Ziprasidone hydrochloride. [0005] However, ziprasidone hydrochloride belongs to class II in the biopharmaceutical classification system, and is a poorly water-soluble drug with low solubility, which leads to a decrease in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/496A61K47/32A61K47/38A61P25/18
CPCA61K9/2027A61K9/2054A61K9/2095A61K31/496
Inventor 薛序任丽莉陈国广
Owner 江苏省药物研究所有限公司
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