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Sildenafil citrate compound and pharmaceutical composition thereof

A technology of sildenafil citrate and compound, applied in the field of sildenafil citrate compound and pharmaceutical composition thereof, can solve problems such as slow drug dissolution rate, problems in drug absorption rate or degree, poor water solubility and the like , to achieve the effect of improving solubility and hygroscopicity

Active Publication Date: 2015-08-12
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the water solubility of sildenafil citrate is poor, and the absorption rate of the drug in the body is often determined by the speed of dissolution. Before the drug in the solid preparation is absorbed, it must go through the process of disintegration and dissolution and then turn into a solution. , if the drug is not readily released from the formulation or dissolves very slowly, there may be a problem with the rate or extent of drug absorption in the formulation

Method used

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  • Sildenafil citrate compound and pharmaceutical composition thereof
  • Sildenafil citrate compound and pharmaceutical composition thereof
  • Sildenafil citrate compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] [Example 1] Preparation of Sildenafil Citrate Compound

[0057] 1) Sample dissolution: Dissolve 1 kg of sildenafil citrate in a mixed solution of 5L dimethylformamide and acetone at 45°C (the volume ratio of dimethylformamide and acetone in the mixed solution is 3: In 1), solution I was obtained, and the temperature of solution I was kept at 38° C.;

[0058]2) Crystallization: take solution I and press filter to remove insoluble matter to obtain solution II, keep the temperature of solution II at 38°C, under stirring, add 1 / 4 of the volume of solution II pure water dropwise continuously, and control the addition within 1.5 hours; After 1.5 hours of crystallization, continue to add 3 / 4 of the volume of solution II pure water dropwise under stirring, control the addition within 1 hour, and stir until crystallization; after 1 hour of crystal growth, cool down to 15°C and keep it warm for 3 hours. Centrifuge to collect the sildenafil citrate wet product;

[0059] 3) Water...

preparation Embodiment 1

[0069] [Preparation Example 1] Sildenafil Citrate Tablets

[0070] Prescription: 25mg

[0071]

[0072] Preparation:

[0073] 1. Screening: the raw and auxiliary materials are all passed through a 100-mesh sieve;

[0074] 2. Weigh sildenafil citrate, microcrystalline cellulose, lactose, calcium hydrogen phosphate, and croscarmellose sodium according to the prescription, and mix well;

[0075] 3. Granulation: make soft material with 2.5% hypromellose aqueous solution, granulate with 18 mesh sieve, dry at 55℃~65℃ for 3.0-3.5h, granulate with 18 mesh sieve;

[0076] 4. Total blending: add croscarmellose sodium and magnesium stearate according to the prescription amount;

[0077] 5. Intermediate product detection: determine the content of sildenafil, and calculate the weight of the tablet to be compressed;

[0078] 6. Tablet pressing: use Φ6.5mm / Φ8.5mm / Φ11mm shallow concave punching die to press the tablet respectively;

[0079] 7. Film coating, coating weight gain 2-4%; ...

preparation Embodiment 2

[0081] [Preparation Example 2] Sildenafil Citrate Tablets

[0082] Prescription: 50mg

[0083]

[0084]

[0085] Preparation method: same as preparation example 1.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a sildenafil citrate compound and a pharmaceutical composition thereof. The molecular formula of the sildenafil citrate compound disclosed by the invention is C22H30N6O4S.C6H8O7.3 H2O, the sildenafil citrate compound is determined by using a powder X-ray diffraction determination method, and an X-ray powder diffraction spectrum expressed by using a diffraction angle of 2theta+ / -0.2 degrees is shown in figure 1. Compared with sildenafil citrate in the prior art, the sildenafil citrate compound provided by the invention has significantly improved solubility and hygroscopicity.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a sildenafil citrate compound and a pharmaceutical composition thereof. Background technique [0002] Sildenafil citrate, the chemical name is 1-methyl-3-n-propyl-5-[2-ethoxy-5-(4-methylpiperazine-1-sulfonyl)phenyl]- 1,6-dihydro-7H-pyrazolo[4,2-d]pyrimidin-7-one citrate, the structural formula is as follows: [0003] [0004] Sildenafil citrate was developed by Pfizer Pharmaceuticals of the United States and entered clinical research as a 5-phosphodiesterase inhibitor for the treatment of cardiovascular diseases, but in March 1998 it was used to treat male penile erectile function Indications for disorders are approved by the U.S. Federal Food and Drug Administration. In recent years, studies have shown that sildenafil citrate can also be used to treat pulmonary hypertension. [0005] CN1586483 discloses an orally disintegrating tablet of sildenafil ci...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61P9/00A61P15/10
CPCC07D487/04
Inventor 刘延珍朱玉青马荣伟王立志
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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