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Ziprasidone controlled release preparation and preparation method thereof

A kind of technology of ziprasidone and sustained-release agent, applied in the field of medicinal chemistry

Inactive Publication Date: 2018-02-23
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, how to reduce the maximum blood concentration after taking ziprasidone to reduce the possibility of QTc interval prolongation caused by taking ziprasidone remains to be studied

Method used

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  • Ziprasidone controlled release preparation and preparation method thereof
  • Ziprasidone controlled release preparation and preparation method thereof
  • Ziprasidone controlled release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] In this embodiment, ziprasidone is provided in the form of dispersion, the solvent in the dispersion is methanol, the skeleton material is HPMC K100M, the content is 20.89%, and the viscosity is 100000 mP·s.

[0109] 1. Preparation of solid dispersion

[0110] (1) Use an electronic balance to weigh ziprasidone hydrochloride monohydrate and HPMCAS-HG in a mass ratio of 1:3, and dissolve it in an appropriate amount of methanol (solid content 1% w / w) to obtain a mixed liquid.

[0111] (2) The mixed solution was placed in a Shanghai Okawahara SCL-12 spray drying apparatus, and spray-dried to obtain a solid dispersion.

[0112] Among them, the spray drying process parameters are shown in Table 1-1.

[0113] Table 1-1: Process parameters

[0114] Intake air temperature setting value (℃)

120

Outlet temperature setting value (°C)

60

Atomizer speed(Hz)

15

Peristaltic pump speed (rpm)

50

[0115] 2. Preparation of Ziprasidone Sustained...

Embodiment 2

[0139] In this embodiment, ziprasidone is provided in the form of dispersion, the solvent in the dispersion is ethanol-water solution, the skeleton material is HPMC K100M, the content is 20.89%, and the viscosity is 100000mP·s.

[0140] 1. Preparation of solid dispersion

[0141] (1) Use an electronic balance to weigh ziprasidone hydrochloride monohydrate and HPMCAS-HG according to a mass ratio of 1:3, and dissolve it in an appropriate amount of ethanol-water solution (8:2) (solid content 7.4%) w / w) to obtain a mixed solution.

[0142] (2) The mixed solution was placed in a Shanghai Okawahara SCL-12 spray drying apparatus, and spray-dried to obtain a solid dispersion.

[0143] Among them, the spray drying process parameters are shown in Table 2-1.

[0144] Table 2-1: Process parameters

[0145] Intake air temperature setting value (℃)

140

Outlet temperature setting value (°C)

70

Atomizer speed(Hz)

35

Peristaltic pump speed (rpm)

30 ...

Embodiment 3

[0171] In this embodiment, ziprasidone is provided in the form of ziprasidone hydrochloride, and the skeleton materials are HPMC K100M and HPMC K4M, wherein the content of HPMC K100M is 20%, the viscosity is 4000mP·s, and the content of HPMC K4M is 10.89%. The viscosity is 100000mP·s.

[0172] 1. Preparation of Ziprasidone Sustained Release Tablets

[0173] (1) Wet granulation, the binder is 250g water, the specific prescription is shown in Table 3-1;

[0174] A. Weigh the materials and pre-mix them for 5 minutes in the Gladt granulator, the speed of the stirring blade is 200rpm, and the speed of the cutting knife is 2000rpm.

[0175] B. Add liquid after premixing, nozzle type 4, peristaltic pump speed 100rpm, stirring blade speed 200rpm, cutter speed 2000rpm. The liquid addition amount is 250g, and the liquid addition time is 210s.

[0176] C. Granulate after adding liquid, the time is 2min, the rotation speed of the stirring blade is 150rpm, and the rotation speed of the ...

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Abstract

The invention discloses a ziprasidone controlled release preparation and a preparation method thereof. The ziprasidone controlled release preparation is prepared from ziprasidone, a framework materialand pharmaceutically acceptable auxiliary materials, wherein a weight ratio of the ziprasidone to the framework material is 1 to (1 to 6). The ziprasidone disclosed by the invention has a better controlled release effect, so that drug administration times of patients are reduced, medication compliance of the patients is improved, the maximum plasma concentration is reduced, and the possibility ofQTc interval prolongation, caused by taking the ziprasidone, of the patients is reduced. The preparation method of the ziprasidone disclosed by the invention has the advantages of convenience in operation, safety, controllability, higher yield and suitability for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to a ziprasidone sustained-release agent and a preparation method thereof. Background technique [0002] Ziprasidone is an atypical antipsychotic drug with good curative effect. It can be used as intramuscular injection in emergency cases, and oral capsules are often used for long-term treatment. The specifications are 20mg, 40mg, 60mg and 80mg. times, with food. Ziprasidone is currently the only atypical antipsychotic that can inhibit the reuptake of norepinephrine and 5-HT, and has a good effect. Clinically, this drug has certain advantages. Compared with some other atypical antipsychotic drugs and traditional antipsychotic drugs, the overall adverse reactions are relatively mild, well tolerated, less likely to cause weight gain, and metabolism-related adverse reactions are small (such as diabetes, dyslipidemia, etc.). [0003] However, a more obvious p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/22A61K47/38A61K31/496A61P25/18
CPCA61K9/0002A61K9/2054A61K9/2866A61K31/496
Inventor 许玉珍仇海镇黄心游劲松黄芳芳
Owner SUNSHINE LAKE PHARM CO LTD