Composition of amorphous vortioxetine or amorphous vortioxetine salt and pharmaceutical adjuvants, and preparation method thereof

A technology of pharmaceutical excipients and vortioxetine, which is applied in the direction of drug combination and nervous system diseases, can solve the problems of difficulty in the development of pharmaceutical formulations and the limitation of the total amount of excipients, and achieve low price, increased stability, and good solubility Effect

Inactive Publication Date: 2017-03-15
CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmaceutical preparations must use a variety of pharmaceutical excipients, and the total amount of excipients is also limited. For example, when a single excipient is used in a large amount, it will also bring certain difficulties to the development of pharmaceutical formulations.

Method used

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  • Composition of amorphous vortioxetine or amorphous vortioxetine salt and pharmaceutical adjuvants, and preparation method thereof
  • Composition of amorphous vortioxetine or amorphous vortioxetine salt and pharmaceutical adjuvants, and preparation method thereof
  • Composition of amorphous vortioxetine or amorphous vortioxetine salt and pharmaceutical adjuvants, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Dissolve vortioxetine hydrobromide (50 mg), D-mannitol (50 mg) and povidone K30 (50 mg) in methanol (800 microliters), heat to 60°C and stir to dissolve. The above solution was rapidly cooled to -10°C, a white solid was precipitated, filtered, and dried to obtain a composition of amorphous vortioxetine hydrobromide, D-mannitol and povidone K30, the X-ray of the composition Powder diffraction pattern as figure 1 As shown, there is no characteristic peak of the vortioxetine hydrobromide crystal form in the X-ray powder diffraction pattern after deducting the background peak of the pharmaceutical excipient.

Embodiment 2

[0048] Vortioxetine (50 mg), polyacrylic acid resin Eudragit L100 (50 mg) and polyethylene glycol 4000 (200 mg) were dissolved in ethanol (600 μl) and water (600 μl) at -40 °C Stir down to mix well. The above solution is slowly concentrated to dryness in a rotary evaporator to obtain a white solid, which is a composition of amorphous vortioxetine, polyacrylic acid resin Eudragit L100 and polyethylene glycol 4000, and the X-ray powder diffraction pattern of the composition Among them, there were no characteristic peaks of vortioxetine crystal form after deducting the background peaks of pharmaceutical excipients.

Embodiment 3

[0050] Add vortioxetine hydrochloride (2 g), lactose (2 g) and polyethylene glycol 8000 (10 g) into water (300 ml), heat to 60°C and stir to dissolve. The above solution was dried with JISL micro-spray dryer LSD-48, and the inlet temperature was maintained at 60°C and the outlet temperature was 50°C. The composition of ethylene glycol 8000, in the X-ray powder diffraction diagram of the composition, there is no characteristic peak of vortioxetine hydrochloride crystal form after deducting the background peak of pharmaceutical excipients.

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Abstract

The invention relates to a composition of vortioxetine or pharmaceutically acceptable vortioxetine salt and pharmaceutical adjuvants, and a preparation method thereof. The composition includes vortioxetine or pharmaceutically acceptable vortioxetine salt and two or more pharmaceutical adjuvants, and a weight ratio of the vortioxetine or pharmaceutically acceptable vortioxetine salt to all the pharmaceutical adjuvants is 1:(0.1-100), wherein the vortioxetine or pharmaceutically acceptable vortioxetine salt in the composition has an amorphous form, and no characteristic peak of the vortioxetine or pharmaceutically acceptable vortioxetine salt exists in an X-ray powder diffraction spectrum of the composition, subtracting the background peaks of the pharmaceutical adjuvants. The composition of vortioxetine or pharmaceutically acceptable vortioxetine salt and pharmaceutical adjuvants has good stability and dispersibility, increases the dissolvability of the vortioxetine or pharmaceutically acceptable vortioxetine salt, is in favor of improving the bioavailability of a medicinal preparation and the medicine absorption of bodies, and keeps good physical stability and chemical stability under accelerated test conditions. The preparation method of the amorphous composition has the advantages of simplicity in operation, low cost, good reappearance, easiness in realization, and suitableness for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a composition of vortioxetine or a pharmaceutically acceptable salt thereof and pharmaceutical auxiliary materials and a preparation method thereof. Background technique [0002] Vortioxetine, chemically named 1-[2-(2,4-methylphenylthio)phenyl]piperazine, trade name Brintellix, is an antidepressant developed by Lundbeck, Denmark disease drugs. Vortioxetine was approved by the US Food and Drug Administration on September 30, 2013 for the treatment of severe depression. The world's leading research and consulting company on pharmaceutical and healthcare issues - Decision Resources (Decision Resources) released a report predicting that by 2022, Vortioxetine will be sold in the five major markets of the United States, Japan, and the European Union (France, Germany, Italy, Spain) , UK) will become a blockbuster drug. Based on the data obtained to date, Vortiox...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P25/24
Inventor 张席妮熊志刚王颖奇资春鹏
Owner CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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