A kind of dapoxetine hydrochloride tablet

Abstract

The invention relates to a dapoxetine hydrochloride tablet. The invention belongs to the field of new technologies for pharmaceutical manufacturing, and in particular to a dapoxetine hydrochloride tablet and a preparation method thereof. The tablet uses dapoxetine hydrochloride as the main component. It is formed by direct compression of dapoxetine hydrochloride solid dispersion particles and auxiliary materials; the described dapoxetine hydrochloride solid dispersion particles are prepared as follows: dapoxetine hydrochloride and an organic solvent form a clear solution, Then add to dextrin for granulation. The weight ratio of dapoxetine hydrochloride to dextrin is 1: 2-15. The organic solvent is selected from one or more of ethanol, acetic acid, ethyl acetate and acetone. The dapoxetine hydrochloride tablet of the invention solves the influence of crystal form differences on preparations, and provides a safe and stable dapoxetine hydrochloride tablet with good in vitro dissolution.

Description

technical field [0001] The invention belongs to the field of new medicine manufacturing technology, and in particular relates to a dapoxetine hydrochloride tablet and a preparation method thereof. Background technique [0002] Dapoxetine (INN, trade name Priligy), is dedicated to the treatment of premature ejaculation (PE) in men, which is an on-demand treatment drug, and is the first oral drug of this type approved for the treatment of premature ejaculation in the world so far. The medicine (tablet) is a product of Menarini, a century-old pharmaceutical company and the number one pharmaceutical company in Italy. The applicable population is men aged 18-64. The recommended first dose for all patients is 30 mg, which needs to be taken about 1 to 3 hours before sexual intercourse. If the effect after taking 30mg is not satisfactory and the side effects are still within the acceptable range, the dosage can be increased to the maximum recommended dosage of 60mg. The maximum r...

AI Technical Summary

Problems solved by technology

Crystal form C has good stability and is not easily converted into crystal forms A and B, but has poor solubility and is insoluble in water

[0009] CN103130661B discloses a crystal, an amorphous substance of dapoxetine hydrochloride and a preparation method thereof. It has discovered an amorphous substance of dapoxetine hydrochloride. The amorphous substance has good solubility and is slightly soluble in water, but the amorphous substance is stable Poor resistance, crystal form A after one month at room temperature

CN103735525B uses micronization technology and adds a large amount of surfactant in the preparation to avoid the influence of the difference in crystal form on the dissolution rate of the preparation. By controlling the particle size of dapoxetine hydrochloride at 0.5-20um and adding sodium lauryl sulfate, Successfully eliminated the influence of crystal form differences on the dissolution rate of preparations, but the dissolution rate of dapoxetine hydrochloride tablets made by the CN103735525B method has dropped to the limit during the long-term test (25°C, 40RH%) for 12 months

At the same time, the addition of a large amount of surfactant sodium lauryl sulfate increases the gastrointestinal reactions when taking dapoxetine hydrochloride tablets orally. Large doses of poloxamers can easily cause the reversal of the water-oil environment of the gastrointestinal mucosa, thereby causing nausea and vomiting. Vomit

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