103 results about "Vortioxetine" patented technology

The invention discloses a preparation method of vortioxetine (I). The preparation method comprises the following steps: subjecting a compound shown in a formula (II) as a raw material and 2,4-dimethylthiophenol (III) to condensation to generate 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV) or 2-(2,4-dimethylphenylthioalkyl)aniline (V) which is obtained by reducing the 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV), and subjecting the 2-(2,4-dimethylphenylthioalkyl)aniline (V) and a compound shown in a formula (VI) to cyclization under alkaline conditions to obtain the vortioxetine (I). The preparation method is accessible in raw materials, is concise in process, is economical and environment-friendly and is suitable for industrial production.

The invention discloses a preparation method of vortioxetine (I). The preparation method comprises the following steps: subjecting 2-substituted thiophenol shown in a formula (II) and 2,4-dimethylphenyl halide shown in a formula (III) to condensation to generate 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV) or 2-(2,4-dimethylphenylthioalkyl)aniline (V) which is obtained by reducing the 2-(2,4-dimethylphenylthioalkyl)nitrobenzene (IV), and subjecting the 2-(2,4-dimethylphenylthioalkyl)aniline (V) and a compound shown in a formula (VI) to cyclization under alkaline conditions to obtain the vortioxetine (I). The preparation method is accessible in raw materials, is concise in process, is economical and environment-friendly and is suitable for industrial production.

The invention relates to an orally disintegrating pharmaceutical composition and a preparation method thereof and belongs to the field of pharmaceutical preparations. Considering the characteristic of bitter taste of hydrobromic acid vortioxetine, the invention provides a method for preparing orally disintegrating tablets which are small in particle size and can cover the bitter taste. The method is realized by mainly adopting the technical scheme, namely the composition is prepared by granulating or directly tabletting pharmaceutical microcapsules, 20-80 weight percent of filling agent, 5-10 weight percent of disintegrating agent, 0.5-2 percent of flavoring agent and 1-2 percent of lubricating agent. The orally disintegrating tablets do not have a grit feeling, sweetening agents such as saccharin sodium salt and Aspartame are not needed to be added into a subsequent tablet prescription, or the flavor of the tablets can be increased by adding a small amount of sweetening agent or essence and flavor according to market requirements, and the medicine content and encapsulation efficiency can meet the industrial large-scale production requirements.

The invention relates to the technical field of medicines and in particular relates to a hydrobromic acid vortioxetine gastric-soluble tablet and a preparation method thereof. The hydrobromic acid vortioxetine gastric-soluble tablet comprises the following components in percentage by weight: 4.24% of hydrobromic acid vortioxetine, 1.0-5.0% of a lubricating agent, 81-91% of a filling agent, 2-5% of a binding agent and 2-15% of a disintegrating agent. Dissolution rate of the hydrobromic acid vortioxetine gastric-soluble tablet is similar to the foreign original standard, so that the hydrobromic acid vortioxetine gastric-soluble tablet has good application prospect and market prospect.

The invention discloses a preparation method and intermediate of vortioxetine. The preparation method of vortioxetine includes the following steps that 1, a compound V is prepared according to a preparation method of the compound V; 2, the compound V and dichloro ethylamine or salt of dichloro ethylamine are subjected to a cyclization reaction in a high-boiling-point solvent to prepare vortioxetine, wherein the boiling point of the high-boiling-point solvent is above 120 DEG C at normal pressure. The preparation method is low in cost, easy to implement, safe, environmentally friendly, high in yield and suitable for industrial production, and reaction conditions are mild.

A process for the manufacture of vortioxetine is provided in which a compound of formula I, formula I is reacted with optionally substituted piperazine and 2,4-dimethylthiophenol(ate) followed by de-cmplexation.

The invention discloses a preparation method of vortioxetine. A benzothiazole derivative (II) is dissociated into o-aminothiophenol (III) under the condition of alkali, and then the o-aminothiophenol(III) reacts with 2,4-dimethyl halogeno benzene under the catalysis of copper or a copper salt to generate 2-(2,4-dimethylphenylsulfanyl)aniline (V), the 2-(2,4-dimethylphenylsulfanyl)aniline (V) andbis(2-hydroxybenzenesulfonic acid)-4-methylbenzenesulfonamide (VI) are cyclized to obtain Ts-protected vortioxetine (VII), and the Ts-protected vortioxetine (VII) is converted into the vortioxetine (I) under the effect of Mg. The synthesis method has the advantages of easily available raw materials, simple process, low cost, high purity and suitability for industrial production.

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.

Pharmaceutical compositions comprising vortioxetine and donepezil are provided and the use of such composition for the treatment of cognitive dysfunctions.

The present invention relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine of formula (I), also known as vortioxetine, salts thereof, and intermediates useful for its synthesis.

The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.

The invention discloses vortioxetine sustained-release capsules as well as a preparation method and application of the vortioxetine sustained-release capsules. The vortioxetine sustained-release capsules are prepared by loading vortioxetine sustained-release micro-pills into hollow capsules. Each vortioxetine sustained-release micro-pill is composed of a medicine-carrying pill core, an isolation type coating layer, a sustained-release coating layer and a protective coating layer from inside to outside, wherein the medicine-carrying pill core is composed of vortioxetine, an adhesive and a sucrose hollow pill core, and the specific weight percent is as follows: 0.1 percent to 10 percent of the vortioxetine, 10 percent to 30 percent of the adhesive and 10 percent to 60 percent of the sucrose hollow pill core. A sustained-release preparation can be used for prolonging the holding time of treatment concentration of the vortioxetine in a body to 12h and reducing the side effect caused by the fact that the fluctuation of plasma drug concentration is too great; meanwhile, the number of times of orally taking drug is reduced, and the vortioxetine sustained-release capsules have remarkable effect on patients with depressive disorder, who need to be treated, and are convenient to use.

The present invention discloses a hydrobromic acid vortioxetine crystal that has diffraction peaks at 8.55+ / -0.2, 13.05+ / -0.2, 13.44+ / -0.2, 14.46+ / -0.2, 15.20+ / -0.2, 16.63+ / -0.2, 16.94+ / -0.2, 17.22+ / -0.2, 17.85+ / -0.2, 19.83+ / -0.2, 20.43+ / -0.2, 21.33+ / -0.2, 23.14+ / -0.2, 23.60+ / -0.2, 24.77+ / -0.2, 26.25+ / -0.2, 26.72+ / -0.2, 26.96+ / -0.2, 29.69+ / -0.2, 30.52+ / -0.2, 33.33+ / -0.2, 33.89+ / -0.2, 34.89+ / -0.2, 35.54+ / -0.2, 37.03+ / -0.2, and 38.33+ / -0.2 in a powder X-ray diffraction diagram represented with 2 theta. In addition, the present invention further discloses a preparation method for the crystal. The hydrobromic acid vortioxetine crystal and the preparation method therefor in the present invention have good repeatability, easy operation, good product stability, and high yield and purity, and are suitable for industrial production.