52 results about "Dapoxetine-N-oxide" patented technology

The present invention relates to a time-delayed sustained release pharmaceutical composition for oral administration, which comprises an immediate release phase and a prolonged sustained release phase, wherein said immediate release phase and prolonged sustained release phase respectively comprise dapoxetine therein as an active ingredient.; The pharmaceutical composition of the present invention comprises dapoxetine, which is an agent for treating premature ejaculation, in both the immediate release phase and the prolonged sustained release phase thereof, to thereby immediately exhibit the effectiveness of the pharmaceutical composition of the present invention in order to enable a patient to achieve sexual satisfaction during the early stage of administration, as well as to reduce side effects by means of the time-delayed sustained release of the prolonged sustained release phase during the early stage of administration and enable a continuous in vivo absorption of dapoxetines, to thereby lengthen the duration of the effectiveness of the pharmaceutical composition of the present invention.; Further, agents for treating erectile dysfunction, such as sildenafil, tadalifil or the like can be added to the immediate release phase so as to allow for a coincidence of the durations of the effectiveness of a premature ejaculation treatment agent and erectile dysfunction treatment agents, even though a half-life difference exists between the two types of treatment agents, thus maximizing patient satisfaction.

The invention discloses a method for preparing a dapoxetine intermediate (S)-3-chloro-N, N-dimethyl-1-phenyl-1-propylamine, and preparation of dapoxetine hydrochloride by using the intermediate through condensation and salification. The preparation of dapoxetine hydrochloride is shortened in reaction steps, reduced in cost, simple in operation and is applicable to industrial production.

The invention relates to a crystal form A of dapoxetine hydrochlorate which is a drug for treating male premature ejaculation, and a preparation method thereof; the crystal form A is characterized in that the crystal form A has characteristic diffraction peaks corresponding to positions with 2theta values of about 8.9 degrees, 14.4 degrees, 15.1 degrees, 16.3 degrees, 16.6 degrees, 18.9 degrees, 20.7 degrees, 22.7 degrees, 23.8 degrees, 25.3 degrees, 29.0 degrees, and 29.5 degrees on an X-ray powder diffraction pattern, and the new crystal form has the characteristics of high purity, good stability, and the like.

The invention discloses a preparation process for preparing a dapoxetine hydrochloride beta-isomer impurity shown as formula I and an enantiomer shown as formula II. The method comprises the following steps: taking optically pure Boc-(S) or (R)-3-amino-3-phenylpropanol as a raw material, performing condensation reaction with 2-fluoronaphthalene or 1-fluoronaphthalene, performing methylation reaction with formic acid-formaldehyde, and performing HCl salification reaction to obtain a target product dapoxetine hydrochloride beta-isomer or enantiomer impurity. Meanwhile, a detection method of isomer impurities is developed.

The invention discloses a dapoxetine hydrochloride monohydrate and a preparation method thereof, a composition containing the dapoxetine hydrochloride monohydrate, and uses of the composition in preparation of drugs for treatment of sexual dysfunction, wherein the dapoxetine hydrochloride monohydrate is represented by a formula I. According to the present invention, the dapoxetine hydrochloride monohydrate overcomes the disadvantages of easy moisture absorption, poor stability, high requirements on storage conditions and difficult long-term preservation of the existing crystal form or the amorphous form of dapoxetine hydrochloride, and is suitable for industrial scale-up and preparation production. The formula I is defined in the specification.