49 results about "Vilazodone Hydrochloride" patented technology

The invention relates to a vilazodone hydrochloride composition and a preparation method thereof. The composition includes vilazodone hydrochloride, a microcarrier and pharmaceutically acceptable excipients for an oral solid preparation. The preparation method is as below: mixing and crushing vilazodone hydrochloride and the microcarrier, and evenly mixing the mixture with pharmaceutically acceptable excipients for oral solid preparation. The obtained composition preparation has greatly improved dissolution in vitro, and in vivo bioavailability reaching bioequivalence to VIIBRYD.

The invention discloses a preparation method and application of a 5-(4-(4-(5-cyano-3-indolyl)butyl)-1-piperazinyl)benzofuran-2-formamide hydrochloride IV crystal. The method comprises the steps of: 1) under certain temperature, dissolving 5-(4-(4-(5-cyano-3-indolyl)butyl)-1-piperazinyl)benzofuran-2-formamide in an organic solvent to obtain a solution; 2) heating the solution obtained in step 1) to a reflux temperature of 40DEG C; 3) slowly adding concentrated hydrochloric acid dropwise; 4) subjecting the system obtained in step 3) to heat preservation reaction for 0.5-12 hours; 5) conducting filtering to obtain an IV crystal form wet product; and 6) conducting vacuum drying to the wet product obtained in step 5) at 80-140DEG C to a constant weight, thus obtaining the IV crystal. By adopting the technical scheme, the process is simplified, a complex preparation process of the existing IV crystal is overcome, and a mixed crystal can be avoided. The method provided by the invention can achieve high crystal purity, stable volume production and high yield, and is easy to realize industrialized production.

The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of form I of vilazodone free base.

The invention relates to a vilazodone hydrochloride crystal form. The powder X-ray powder diffraction pattern of the crystal form has characteristic peaks when a diffraction angle 2theta is 9.019+ / -0.2 DEG, 14.481+ / -0.2 DEG, 18.839+ / -0.2 DEG, and 24.580+ / -0.2 DEG, 27.271+ / -0.2 DEG, the relative intensity of the diffraction angle 2theta at 24.580+ / -0.2 DEG is 100%, the relative intensity of the diffraction angle 2theta at 18.839+ / -0.2 DEG is no less than 70%, the relative intensity of the diffraction angle 2theta at 14.481+ / -0.2 DEG is no less than 30%, the relative intensity of the diffraction angle 2theta at 9.019+ / -0.2 DEG is no less than 20%, and the relative intensity of the diffraction angle 2theta at 27.271+ / -0.2 DEG is no less than 18%. The invention also relates to a preparation method of the vilazodone hydrochloride crystal form, a pharmaceutical composition and the vilazodone hydrochloride crystal form in preparation of medicine for treating depression.

The present invention relates to an improved process for the preparation of vilazodone hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.

Disclosed herein is a stable amorphous form of vilazodone hydrochloride substantially free of crystalline forms, a process for the preparation, pharmaceutical compositions, and methods of treating thereof. Disclosed also herein are stable amorphous co-precipitates of vilazodone hydrochloride and a pharmaceutically acceptable excipient, methods for the preparation, pharmaceutical compositions, and method of treating thereof.

The invention discloses a compound composition for treatment of depression and a preparation method thereof. The compound composition takes a novel antidepressant vilazodone hydrochloride and vitamin K as active components. Vitamin K participates in vilazodone hydrochloride to treat severe depression, on the one hand, the clinical dosage of vilazodone hydrochloride can be reduced, a very good antidepressant effect can be generated while maintaining a low dosage, more serious side effects caused by dosage fluctuation similar to gradual dosage increase and gradual dosage decrease during drug withdrawal, and on the other hand, the adverse reaction of abnormal bleeding generated after use of vilazodone hydrochloride can be reduced. Combined use of the two drugs can show stronger antidepressant activity. The compound composition has good application prospects.

The invention relates to a preparation method of 3-(4-chlorobutyl)-1H-5-cyanindole. The above compound is an important intermediate for preparing an antidepressant vilazodone hydrochloride. The method comprises the following steps: dispersing sodium borohydride in a solvent, adding a trichloroacetic acid organic solution, and adding 3-(4-chlorobutylacyl)-1H-5-cyanindole in batches. The preparation method of the vilazodone hydrochloride intermediate 3-(4-chlorobutyl)-1H-5-cyanindole has the advantages of simple operation, low device requirements, high yield, good purity, suitableness for industrial production, and obvious creativity and practical application values. The reaction equation of the method is shown in the specification.

The present invention relates to a new crystal form of vilazodone hydrochloride. The 2θ angles of the crystal form on the powder X-ray diffraction pattern are 9.019±0.2°, 14.481±0.2°, 18.839±0.2°, 24.580±0.2°, There is a characteristic peak at 27.271±0.2°, and the relative intensity of the characteristic peak at the 2θ angle of 24.580±0.2° is 100%, the relative intensity of the characteristic peak at the 2θ angle of 18.839±0.2° is not less than 70%, and the 2θ angle is at 14.481±0.2 The relative intensity of the characteristic peak at ° is not less than 30%, the relative intensity of the characteristic peak at the 2θ angle of 9.019±0.2° is not less than 20%, and the relative intensity of the characteristic peak at the 2θ angle of 27.271±0.2° is not less than 18%. The invention also relates to a preparation method, a pharmaceutical composition and a medicine for treating depression of the vilazodone hydrochloride crystal form.

The invention provides a preparation route for a vilazodone hydrochloride crystal form XI: vilazodone hydrochloride with the crystal form XI is obtained by a series of operations such as dilution, pHregulation, crystallization and drying, and the problem that the crystal form XI cannot be obtained by the route of the prior patent. The drug is used for treating or preventing depression, anxiety, bipolar disorder, mania, dementia, mental disorders associated with psychoactive substances, sexual dysfunction, eating disorder, obesity, fibromyalgia, sleep disorder, psychosis-like mental disorders,cerebral infarction, tension, side effects in hypertension treatment, brain diseases, chronic pain, acromegaly, hypogonadism, secondary amenorrhea and premenstrual syndrome.