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Sildenafil citrate composition and preparation method thereof

A technology of sildenafil citrate and its composition, which is applied in the field of sildenafil citrate composition and its preparation, and can solve the problems of low water and impurity content, insufficient drug dissolution rate, and uneven mixing. , to achieve the effect of saving the drying step, easy operation and less process steps

Inactive Publication Date: 2021-01-12
广州汇元医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of sildenafil citrate composition and preparation method thereof for the treatment of urology class disease medicine, the sildenafil citrate sheet or capsule obtained by hot-melt extrusion technology, after testing It is found that the preparation method is simple to operate, environmentally friendly, and the obtained preparation has a high dissolution rate, good stability, low moisture and impurity content, improves the safety of clinical application, and solves the problem of complex processes and insufficient drug dissolution in the prior art. , Mixing is not uniform enough, etc.

Method used

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  • Sildenafil citrate composition and preparation method thereof
  • Sildenafil citrate composition and preparation method thereof

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Experimental program
Comparison scheme
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Embodiment 1

[0027] The present embodiment provides a sildenafil citrate composition, which is a tablet, and consists of the following raw materials in terms of weight percentage:

[0028]

[0029] The preparation method comprises the following steps:

[0030] (1) Processing of raw and auxiliary materials: crushing sildenafil citrate through a 100-mesh sieve, and passing povidone K30 and crospovidone through a 80-mesh sieve;

[0031] (2) Weighing: Weigh sildenafil citrate, povidone K30, crospovidone and triethyl citrate respectively according to the prescription;

[0032] (3) Mixing: add sildenafil citrate, povidone K30 and crospovidone into the three-dimensional mixer, set the mixing speed to 15 rpm, and the mixing time is 10 minutes to obtain the mixed powder;

[0033] (4) Hot-melt extrusion: Add triethyl citrate dropwise to the mixed powder in step (3), set the extrusion temperature to 150°C, when the screw temperature reaches the set temperature and stabilizes, start the screw, and...

Embodiment 2

[0035] The present embodiment provides a sildenafil citrate composition, which is a tablet, and consists of the following raw materials in terms of weight percentage:

[0036]

[0037] The preparation method comprises the following steps:

[0038] (1) Processing of raw and auxiliary materials: crush sildenafil citrate and pass through a 100-mesh sieve, and vinylpyrrolidone-vinyl acetate copolymer and croscarmellose sodium pass through a 80-mesh sieve;

[0039] (2) Weighing: Weigh sildenafil citrate, vinylpyrrolidone-vinyl acetate copolymer, croscarmellose sodium and dibutyl sebacate respectively according to the prescription;

[0040] (3) Mixing: Add sildenafil citrate, vinylpyrrolidone-vinyl acetate copolymer and croscarmellose sodium into the three-dimensional mixer, set the mixing speed to 15 rpm, and the mixing time is 10 minutes, obtain mixed powder;

[0041] (4) Hot-melt extrusion: Add dibutyl sebacate dropwise to the mixed powder in step (3), set the extrusion temp...

Embodiment 3

[0043] The present embodiment provides a sildenafil citrate composition, which is a capsule and consists of the following raw materials in weight percentage:

[0044]

[0045] The preparation method comprises the following steps:

[0046] (1) Processing of raw and auxiliary materials: crushing sildenafil citrate through a 100-mesh sieve, and passing povidone K30 and croscarmellose sodium through a 80-mesh sieve;

[0047] (2) Weighing: Weigh sildenafil citrate, povidone K30, croscarmellose sodium, tributyl citrate and magnesium stearate respectively according to the prescription;

[0048] (3) Mixing: Add sildenafil citrate, povidone K30 and croscarmellose sodium into a three-dimensional mixer, set the mixing speed to 15 rpm, and the mixing time to 10 minutes to obtain a mixed powder;

[0049](4) Hot-melt extrusion: Add tributyl citrate dropwise to the mixed powder in step (3), set the extrusion temperature to 140°C, when the screw temperature reaches the set temperature an...

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Abstract

The invention discloses a sildenafil citrate composition and a preparation method thereof, and belongs to the technical field of medicines. The sildenafil citrate composition takes sildenafil citrateas a main drug, and takes povidone K30, crospovidone, a vinyl pyrrolidone-vinyl acetate copolymer, xanthan gum, crosslinked carboxyl cellulose sodium, hydroxypropyl cellulose, triethyl citrate, tributyl citrate, dibutyl sebacate, diethyl phthalate, magnesium stearate and the like as auxiliary materials. Compared with those in the prior art, sildenafil citrate tablets or capsules obtained by adopting a hot-melt extrusion technology are simple and convenient to operate, environment-friendly, simple in prescription and suitable for large-scale production and application; and compared with preparations in the market, the obtained sildenafil citrate tablets or capsules are high in dissolution rate, good in stability, low in impurity content and high in clinical application safety.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a sildenafil citrate composition and a preparation method thereof as medicine for treating urological diseases. Background technique [0002] Sildenafil is an oral drug for the treatment of erectile dysfunction (ED). It is a selective inhibitor of phosphodiesterase type 5 (PDE5) specific for cyclic guanosine monophosphate (cGMP). Mechanism of action: The physiological mechanism of penile erection involves the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. The activation of guanylate cyclase by NO leads to an increase in the level of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle in the cavernous body and fills the blood. Sildenafil is currently the drug of choice for the clinical treatment of various types of erectile dysfunction. It is a white crystalline powder with a solubility in water of 3.5mg / ml. The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/519A61K47/38A61K47/36A61K47/32A61K47/14A61P15/10
CPCA61K9/205A61K9/2027A61K9/2054A61K9/4866A61K9/4858A61K31/519A61P15/10
Inventor 黎永诚凌永峰许桂浩谭银合王雪峰张龙辉
Owner 广州汇元医药科技有限公司
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