Sildenafil citrate composition granules for treating urologic diseases

A sildenafil citrate, urology technology, applied in the field of medicine, can solve the problems of great influence on the stability of the drug and the difficulty in preparation of preparations, and achieve low moisture and impurity content, good stability, and low impurity content. Effect

Inactive Publication Date: 2015-11-18
QINGDAO HUAZHICAO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Sildenafil citrate has strong hygroscopicity, and it is easy to absorb moisture and deteriorate under normal conditions. Therefore, the water content has a great influence on the stability of the drug. It is necessary to strictly control the product quality, which brings great difficulties to the preparation of the preparation.

Method used

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  • Sildenafil citrate composition granules for treating urologic diseases
  • Sildenafil citrate composition granules for treating urologic diseases
  • Sildenafil citrate composition granules for treating urologic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: the preparation of sildenafil citrate crystal

[0024] Dissolving sildenafil citrate in a mixed solvent of methanol and acetonitrile whose volume is 10 times the weight of sildenafil citrate at 35°C, the volume ratio of methanol and acetonitrile is 3:1, after the dissolution is completed, Add volume and be the mixed solvent of 6 times of sildenafil citrate weight hexane, propanol, the volume ratio of hexane, propanol is 4.5:1, temperature is dropped to 0 ℃ in 2 hours, at 0 ℃ for 3 hours, then further lowered to -5 ℃, and then placed at -5 ℃ for 3 hours, crystals were precipitated, and sildenafil citrate crystals were obtained.

[0025] The prepared sildenafil citrate crystal uses Cu-Kα ray to measure the X-ray powder diffraction pattern obtained as figure 1 shown.

Embodiment 2

[0026] Embodiment 2: the preparation of sildenafil citrate granule

[0027] Prescription: the sildenafil citrate crystalline form compound that the embodiment 1 of 10 parts by weight makes, the sorbitol of 17.5 parts by weight, the croscarmellose sodium of 3.3 parts by weight, the magnesium carbonate of 7 parts by weight, 0.5 parts by weight of aspartame, 14 parts by weight of 95% ethanol.

[0028] Preparation:

[0029] (1) Processing of raw and auxiliary materials: sieve sildenafil citrate to 100 mesh, and magnesium carbonate to 80 mesh;

[0030] (2) Weighing: Weighing according to the prescription;

[0031] (3) Granulation: Add sildenafil citrate, sorbitol, croscarmellose sodium, magnesium carbonate, and aspartame into the wet mixing granulator, dry mix for 10 minutes, and 95% ethanol is added to the wet mixing granulator for wet mixing and cutting, and 18 mesh granulation is selected to make soft materials;

[0032] (4) Drying and sieving: distribute the wet granules ob...

Embodiment 3

[0035] Embodiment 3: the preparation of sildenafil citrate granule

[0036] Prescription: the sildenafil citrate crystalline form compound that the embodiment 1 of 10 weight parts makes, the sorbitol of 17.7 weight parts, the croscarmellose sodium of 3.35 weight parts, the magnesium carbonate of 8 weight parts, 0.6 parts by weight of aspartame, 15 parts by weight of 95% ethanol.

[0037] Preparation:

[0038] (1) Processing of raw and auxiliary materials: sieve sildenafil citrate to 100 mesh, and magnesium carbonate to 80 mesh;

[0039] (2) Weighing: Weighing according to the prescription;

[0040] (3) Granulation: Add sildenafil citrate, sorbitol, croscarmellose sodium, magnesium carbonate, and aspartame into the wet mixing granulator, dry mix for 10 minutes, and 95% ethanol is added to the wet mixing granulator for wet mixing and cutting, and 18 mesh granulation is selected to make soft materials;

[0041] (4) Drying and sieving: distribute the wet granules obtained from...

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Abstract

The invention discloses sildenafil citrate composition granules for treating urologic diseases, belonging to the technical field of medicines. The composition is prepared from sildenafil citrate, sorbitol, croscarmellose sodium, magnesium carbonate, aspartame and 95% ethanol. The sildenafil citrate is a novel crystal-form compound; an x-ray powder diffraction diagram obtained by measuring by using cu-kalpha rays is shown in the figure 1 and is different from the prior art; experiments find that the compound with the novel crystal-form structure is improved in moisture absorbability, good in stability and low in impurity content; and granules prepared from the novel crystal-form compound of sildenafil citrate are good in stability, low in water and impurity contents, high in bioavailability and capable of improving the safety of clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a sildenafil citrate composition granule for treating urological diseases. Background technique [0002] Sildenafil is an effective drug for the treatment of erectile dysfunction caused by objective and subjective reasons. It was approved by the FDA as a prescription drug in the United States in March 1997. Sildenafil is a highly selective phosphodiesterase 5 (PDE5 ) inhibitor, PDE5 is highly expressed in the corpus cavernosum, while its expression is low in other tissues (including platelets, blood vessels, visceral smooth muscle, and skeletal muscle). Sildenafil selectively inhibits PDE5, enhances the nitric oxide (NO)-cGMP pathway, and increases the level of cGMP to cause the relaxation of the smooth muscle of the cavernous body of the penis, so that patients with erectile dysfunction can produce a natural erectile response to sexual stimulation. Erectile response generally inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/519C07D487/04A61P13/00A61P15/10A61K47/38
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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