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Sidenafil citrate composition particle preparation for treating urology diseases

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

Inactive Publication Date: 2015-11-11
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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  • Sidenafil citrate composition particle preparation for treating urology diseases
  • Sidenafil citrate composition particle preparation for treating urology diseases
  • Sidenafil citrate composition particle preparation for treating urology diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of Sildenafil Citrate Crystals

[0024] Prepare 35 ℃ of sildenafil citrate crude product saturated methanol solution, then add the mixed solvent that volume is 8 times of isobutanol and hexane of saturated methanol solution volume, the volume ratio of described isobutanol, hexane is 2:3. After stirring evenly, stir while cooling down. The cooling rate is 10°C / hour, and the stirring speed is 105 rpm. After reaching -5°C, the stirring was stopped, and the crystal was grown for 3 hours, filtered, and dried under reduced pressure to obtain a crystalline compound of sildenafil citrate.

[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] Example 2: Preparation of Sildenafil Citrate Granules:

[0027] Prescription: in parts by weight as shown in Table 1.

[0028] Table 1 sildenafil citrate composition prescription

[0029]

[0030] Preparation:

[0031] 1) Processing of raw and auxiliary materials: pass calcium sulfate and sildenafil citrate through a 100-mesh sieve with a vibrating sieve;

[0032] 2) Weighing: Weigh each raw and auxiliary material according to the prescription amount;

[0033] 3) Granulation: Add the prescribed amount of sildenafil citrate, lactose, calcium sulfate, tartaric acid, and aspartame into the high-speed mixing granulator, turn on the stirring motor and mix at low speed for 10 minutes, then add the prescribed amount of purified water , Wet mix for 150-180 seconds to make soft materials, choose 18 mesh stainless steel mesh and install it in the spinning granulator to granulate;

[0034] 4) Drying and sieving: Control the inlet air temperature of the boiling dryer at 55...

Embodiment 3

[0037] Example 3: Preparation of Sildenafil Citrate Granules:

[0038] Prescription: in parts by weight as shown in Table 2.

[0039] Table 2 sildenafil citrate composition prescription

[0040]

[0041] Preparation:

[0042] 1) Processing of raw and auxiliary materials: pass calcium sulfate and sildenafil citrate through a 100-mesh sieve with a vibrating sieve;

[0043] 2) Weighing: Weigh each raw and auxiliary material according to the prescription amount;

[0044] 3) Granulation: Add the prescribed amount of sildenafil citrate, lactose, calcium sulfate, tartaric acid, and aspartame into the high-speed mixing granulator, turn on the stirring motor and mix at low speed for 10 minutes, then add the prescribed amount of purified water , Wet mix for 150-180 seconds to make soft materials, choose 18 mesh stainless steel mesh and install it in the spinning granulator to granulate;

[0045] 4) Drying and sieving: Control the inlet air temperature of the boiling dryer at 55...

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Abstract

The invention discloses a sidenafil citrate composition particle preparation for treating urology diseases, and belongs to the technical field of Chinese medicine. The composition preparation is prepared by sidenafil citrate, lactose, calcium sulfate, tartaric acid, aspartame, purified water and magnesium stearate. The sidenafil citrate is a novel crystal-form composition, Cu-K alpha rays are used for obtaining an X-ray powder diffraction diagram showed as in figure 1 through measurement, and the sidenafil citrate is different from sidenafil citrate reported in the prior art. The experiment finds that the composition of the novel crystal-form structure has the advantages of improving hygroscopicity and being good in stability and low in content of impurities. The particle preparation prepared by the sidenafil citrate composition of the novel crystal form is good in stability, low in content of water and impurities and high in bioavailability and improves 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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IPC IPC(8): A61K31/519A61K9/16A61P13/00C07D487/04
Inventor 曹正霞
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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