Pharmaceutical composition containing amorphous vortioxetine hydrobromide and preparation method thereof

A technology of vortioxetine hydrobromide and composition, which is applied in the field of composition and preparation of vortioxetine hydrobromide and pharmaceutical excipients, which can solve the impact of the release of active pharmaceutical ingredients and the development of pharmaceutical formulations Difficulties and other problems, to achieve industrialized production, avoid the risk of toxic and side effects, and easy to achieve

Inactive Publication Date: 2018-01-05
SHANGHAI FANGNAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This will have a great impact on the release of the active ingredients of the drug in the human body, so it will also bring certain difficulties to the development of pharmaceutical formulations

Method used

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  • Pharmaceutical composition containing amorphous vortioxetine hydrobromide and preparation method thereof
  • Pharmaceutical composition containing amorphous vortioxetine hydrobromide and preparation method thereof
  • Pharmaceutical composition containing amorphous vortioxetine hydrobromide and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0045] Any solid form of vortioxetine hydrobromide can be used in the preparation of the pharmaceutical composition of the present invention.

[0046] The calculation method of the load rate of vortioxetine hydrobromide in the pharmaceutical composition is as follows:

[0047] Loading rate=(feeding weight of vortioxetine hydrobromide-the loss weight of vortioxetine hydrobromide in filtrate) / the gross weight of pharmaceutical composition

[0048] Vortioxetine hydrobromide (50 mg) and povidone K30 (30 mg) were added to methanol (900 microliters), heated to 60 ° C and stirred to dissolve, then added colloidal silicon dioxide Aerosil 200 ( 30 mg). The above mixture was rapidly cooled to -10°C, a white solid was precipitated, filtered, and dried to obtain 102 mg of a composition of amorphous vortioxetine hydrobromide, povidone K30 and colloidal silicon dioxide Aerosil 200, the active ingredient The load factor is 47.2%. The X-ray powder diffraction pattern of this composition is...

Embodiment 2

[0050] Vortioxetine (50 mg) and hydroxypropyl methylcellulose HPMC E3 (30 mg) were added to methanol (800 microliters) and dichloromethane (800 microliters), stirred and dissolved at 40 ° C, and then added Colloidal silicon dioxide Aerosil 200 (30 mg). The above mixture was slowly concentrated to dryness in a rotary evaporator, and further vacuum-dried to obtain a white solid, namely 110 mg of a composition of amorphous vortioxetine, hydroxypropylmethylcellulose HPMC E3 and colloidal silicon dioxide Aerosil 200 , the loading rate of the active ingredient was 45.4%. The X-ray powder diffraction pattern of this composition is as follows figure 2 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 3

[0052] Vortioxetine hydrobromide (2 g) and polyethylene glycol 8000 (1.2 g) were added to methanol (50 ml), heated to 60°C and stirred to dissolve, then magnesium aluminum silicate Neusilin UFL2 (0.6 gram). The above mixture was slowly concentrated to dryness in a rotary evaporator, and further vacuum-dried to obtain a white solid, which was further vacuum-dried to obtain a mixture of amorphous vortioxetine hydrobromide, polyethylene glycol 8000 and aluminum magnesium silicate Neusilin UFL2 The composition is 3.8 grams, and the loading rate of the active ingredient is 52.6%. In the X-ray powder diffraction pattern of the composition, there is no characteristic peak of the crystal form of vortioxetine hydrobromide after deducting the background peak of the pharmaceutical excipient.

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PUM

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Abstract

The invention provides a pharmaceutical composition containing amorphous vortioxetine hydrobromide and a preparation method thereof. The pharmaceutical composition comprises vortioxetine hydrobromide,at least one organic carrier and at least one adsorbent, wherein a weight ratio of vortioxetine hydrobromide to all the organic carriers is 1: 0.1-10, and a weight ratio of vortioxetine hydrobromideto all the adsorbents is 1: 0.1-10; vortioxetine hydrobromide in the composition is in an amorphous state; and after deduction of the background peaks of pharmaceutical adjuvants, the X-ray powder diffraction spectrum of the composition is free of characteristic peaks of the crystal of vortioxetine hydrobromide. The composition of vortioxetine hydrobromide and the pharmaceutical adjuvants has goodstability and dispersibility; the dissolution rate of vortioxetine hydrobromide is improved; the bioavailability of a medicinal preparation and body absorption of vortioxetine hydrobromide are improved; and under accelerated test conditions, the composition can maintain good physical stability and chemical stability. The preparation method for the amorphous composition of the invention has the advantages of simple operation, low cost, good reproducibility, easy realization and suitability for industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a composition of vortioxetine hydrobromide and pharmaceutical excipients and a preparation method thereof. Background technique [0002] Vortioxetine, whose chemical name is 1-[2-(2,4-methylphenylsulfanyl)phenyl]piperazine and whose trade name is 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. Decision Resources, the world's leading research and consulting company on pharmaceutical and healthcare issues, 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, Vortioxetine is expected to be the most success...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61P25/24A61P25/22A61P25/28A61P25/00C07D295/096
Inventor 张席妮熊志刚资春鹏熊理查
Owner SHANGHAI FANGNAN PHARMA
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