Dripping pill containing vortioxetine and preparation method of dripping pill

Abstract

The invention discloses a dripping pill containing vortioxetine and a preparation method of the dripping pill. The dripping pill is prepared from hydrobromic acid vortioxetine, water / ethanol water, penetrant, pH modifier and a carrier matrix. Hydrobromic acid vortioxetine exists in the penetrant and the carrier matrix in the solid dispersion state. Vortioxetine is prepared into the dripping pill, and therefore the influences of the smashing, particle preparation and tabletting steps on the crystal form of the dripping pill can be avoided, and relative stability of the crystal form of the medicine is ensured. The prepared dripping pill never generates hydrobromic acid vortioxetine characteristic absorption peaks, and no obvious new characteristic peaks are generated. The problem of crystal form conversion is solved in a sense; meanwhile, because the dripping pill is not constrained by crystal lattices, free energy is large, dissolution and release of the product can be more easily achieved, and the bioavailability of the product is easily improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a drop pill containing vortioxetine and a preparation method thereof. Background technique [0002] Vortioxetine was first jointly developed by Lundbeck and Takeda Pharmaceuticals in the United States. It was approved by the Food and Drug Administration (FDA) for marketing in the United States on September 30, 2013. The trade name is Brintellix, and the dosage form is oral tablets. Dosage, the specifications are 5, 10, 15 and 20mg, respectively, for the treatment of major depressive disorder in adults. [0003] Vortioxetine is a white to off-white powder; it is not stable to light. According to the original research patent patent, the vortioxetine hydrobromide raw material of this product has crystal forms of α, β, and γ, and the FDA approved the original formulation to use the β crystal form raw material as the active ingredient of this product, and the β crystal form is It i...

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Problems solved by technology

[0008] CN104887624A provides an oral solution of vortioxetine and its preparation process patent. The biggest problem of this product is that it is prepared as an oral solution, and its stability is not as good as oral solid preparations. During the long-term stability process, related impurities will increase significantly , and the bioavailability of the oral solution of this product is no different from that of ordinary oral tablets

[0009] CN104873458A provides a vortioxetine freeze-dried orally disintegrating tablet and a preparation method thereof. The orally disintegrating tablet is prepared by a freeze-drying method, which has certain novelty. The effect of oral absorption into the blood is not obvious, and there is no significant increase in the bioavailability of this product

[0010] CN104146953A provides a patent for the prescription and preparation process of vortioxetine hydrobromide injection. The biggest advantage of this product is its fast onset of action and high bioavailability. However, due to the characteristics of the injection, the degradation of impurities is particularly unfavorable The long-term stability of the storage of the drug, and the injection has high requirements for sterility, and the patient's tolerance is poor. Combined with the indications of this product, the promotion of this injection has great limitations.

[0011] CN104644594A provides a kind of vortioxetine hydrobromide stomach-dissolving tablet and its preparation method, its actual prescription composition has no obvious difference compared with the original preparation, that is, it is a common oral tablet, the dosage form and process design have no novelty, and the prescription adopts The excipients are also conventional excipients, and the product quality has not been significantly improved compared with the original research

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