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Novel medicinal composition containing amorphous vortioxetine hydrobromide and preparation method of novel medicinal composition

A technology of vortioxetine hydrobromide and its composition, which is applied in the field of pharmaceutical preparations, can solve the problems of affecting the bioavailability and curative effect of the drug, the improvement of the dissolution rate is not obvious, and the difficulty in developing tablet prescriptions, so as to inhibit the crystallization Occurrence, enhanced bioavailability, good dispersion and effect of amorphous state

Inactive Publication Date: 2018-01-30
SHANGHAI FANGNAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The adsorbent has a strong adsorption capacity for the active ingredient, which will have a great impact on the release of the drug, and the improvement of the dissolution rate is not obvious; at the same time, the inorganic adsorbent requires other organic excipients to be bonded together for granulation and tablet compression. A large number of adsorbents will require a larger amount of organic excipients, which will cause certain difficulties in the formulation development of tablets
affect the bioavailability and efficacy of the drug

Method used

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  • Novel medicinal composition containing amorphous vortioxetine hydrobromide and preparation method of novel medicinal composition
  • Novel medicinal composition containing amorphous vortioxetine hydrobromide and preparation method of novel medicinal composition
  • Novel medicinal composition containing amorphous vortioxetine hydrobromide and preparation method of novel medicinal composition

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Experimental program
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Effect test

Embodiment 1

[0050] Any solid form of vortioxetine hydrobromide can be used in the preparation of the pharmaceutical composition of the present invention.

[0051] The calculation method of the load rate of vortioxetine hydrobromide in the pharmaceutical composition is as follows:

[0052] Loading rate=(feeding weight of vortioxetine hydrobromide-the loss weight of vortioxetine hydrobromide in filtrate) / the gross weight of pharmaceutical composition

[0053] 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) and microcrystalline cellulose (20 mg). The above mixture was rapidly cooled to -10°C, a white solid was precipitated, filtered, and dried to obtain a composition of amorphous vortioxetine hydrobromide, povidone K30, microcrystalline cellulose and colloidal silicon dioxide Aerosil 200 121 mg, the loading rate of the active ingredient is...

Embodiment 2

[0055] 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) and Mannitol (50 mg). The above mixture was slowly concentrated to dryness in a rotary evaporator, and further dried in vacuum to obtain a white solid, namely a combination of amorphous vortioxetine, hydroxypropylmethylcellulose HPMC E3, mannitol and colloidal silicon dioxide Aerosil 200 160 mg, the loading rate of the active ingredient is 31.2%. 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

[0057] 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 grams) and lactose (2 grams). 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 amorphous vortioxetine hydrobromide, polyethylene glycol 8000, lactose and magnesium aluminum silicate Neusilin The composition of UFL2 is 5.8 g, and the loading rate of active ingredient is 34.4%. 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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Abstract

The invention relates to a medicinal composition containing vortioxetine hydrobromide. The medicinal composition contains a solid dispersion (formed by vortioxetine hydrobromide and an organic carrier), at least one adsorbent, and at least one medicinal adjuvant, wherein vortioxetine hydrobromide is amorphous, in the X-ray powder diffraction spectrum of the composition, after the background peak of the organic carrier, the adsorbent and the medicinal adjuvant is deducted, the characteristic peak of crystal of vortioxetine hydrobromide does no exist. The invention further relates to a preparation method of the medicinal composition of the amorphous vortioxetine hydrobromide. The medicinal composition of vortioxetine hydrobromide provided by the invention is good in stability and dispersibility, the dissolution rate of vortioxetine hydrobromide is increased, the bioavailability of the medicinal preparation and the absorption of the body for the medicine can be improved, and under the condition of acceleration test, good physical stability and chemical stability can be kept. The preparation method provided by the invention is easy to operate, low in cost, good in reproducibility, easyto realize, and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a pharmaceutical composition containing amorphous vortioxetine hydrobromide, a preparation method thereof, and an application of the composition for treating emotional disorders. Background technique [0002] Vortioxetine, the chemical name is 1-[2-(2,4-methylphenylsulfanyl)phenyl]piperazine hydrobromide, the trade name is Brintellix, and it is a product of Lundbeck, Denmark. A 5-HT reuptake inhibitor developed by Lundbeck and Takeda. Vortioxetine hydrobromide 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/495A61K9/14A61P25/18A61P25/22A61P25/24A61P25/28A61P25/04A61P25/00
Inventor 张席妮熊志刚资春鹏熊理查
Owner SHANGHAI FANGNAN PHARMA
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