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Aildenafil citrate crystal form O, preparation method and application thereof

A technology of citric acid and amorphous form, which is applied in the field of edenafil citrate crystal form O and its preparation and application, and can solve problems not related to edenafil citrate crystal form and its preparation method

Inactive Publication Date: 2012-07-04
HONG KONG GOLDEN WISDOM MEDICAL PRODN LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent (application number 02100198.7) discloses edenafil citrate and its preparation method, etc., but does not involve edenafil citrate crystal form and preparation method

Method used

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  • Aildenafil citrate crystal form O, preparation method and application thereof
  • Aildenafil citrate crystal form O, preparation method and application thereof
  • Aildenafil citrate crystal form O, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] In a 1000ml reaction bottle, add 20 grams of edenafil citrate, 450ml of distilled water, and 50ml of tetrahydrofuran, start stirring, heat up to reflux, filter while it is hot after 15 minutes, stir the filtrate and cool it down to room temperature, and keep stirring for 25 hours. Precipitate crystals, filter, place indoors for 1 hour, then move to a vacuum drying oven, and vacuum dry for 3 hours to obtain 18.8 g of aldenamorph citrate crystal form O, with a purification rate of 94%, measured by HPLC area normalization method The content is 99.96%. Detected by X-ray diffractometer and infrared spectrometer (see figure 1 , figure 2 ), showing the characteristics of Aldenafil Citrate Form O.

Embodiment 2

[0059] In a 2000ml reaction bottle, add 40 grams of edenafil citrate, 900ml of distilled water, and 95ml of tetrahydrofuran, start stirring, heat up to reflux, filter while it is hot after 20 minutes, stir the filtrate and cool it down to room temperature, and keep stirring for 25 hours. Precipitate crystals, filter, place indoors for 1 hour, then move to a vacuum drying oven, and vacuum dry for 4 hours to obtain 37.6 g of aldenafil citrate crystal form O, with a purification rate of 94%, measured by HPLC area normalization method The content is 99.96%. Detected by X-ray diffractometer and infrared spectrometer (see figure 1 , figure 2 ), showing the characteristics of Aldenafil Citrate Form O.

Embodiment 3

[0061] Granules containing Aldenafil Citrate Form O

[0062] Prescription: 50 grams of Aldenafil Citrate Form O, 650 grams of lactose, 100 grams of crospovidone, 90 grams of PEG-4000, 135 grams of hydroxypropyl methylcellulose, appropriate amount of distilled water, made into 1000 bags.

[0063] Process: PEG-4000 and aldenafil citrate crystal form O are pulverized together, passed through an 80-mesh sieve, mixed with other materials, made into soft materials with distilled water, granulated, dried at low temperature, and then packed into granules.

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Abstract

The invention relates to 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazol[4,3-d] pyridine-5-group)-4-ethoxybenzene sulfonyl]-cis-3,5-lupetazin citrate or aildenafil citrate crystal form O and a preparation method thereof. The invention also relates to a medicine compound containing aildenafil citrate crystal form O and the application thereof in preparing the medicine for treating erectile dysfunction (ED). The aildenafil citrate crystal form O is formed by the steps of: solving citrate in the distilled water and tetrahydrofuran, stirring, rising temperature, filtering, stirring filtrate, decreasing temperature, crystallizing and filtering. The aildenafil citrate crystal form O is prepared into the medicine together with the medical excipients and is applied in treating the erectile dysfunction disease.

Description

Technical field: [0001] The present invention relates to 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)- Crystal form O of 4-ethoxybenzenesulfonyl]-cis-3,5-dimethylpiperazine citrate (Aildenafil citrate) and its preparation method, containing the present invention The pharmaceutical composition of the obtained crystal form O and the application of the crystal form O in the manufacture of a drug for treating male erectile dysfunction (male erectile dysfunction, ED). Background technique: [0002] Male erectile dysfunction (male erectile dysfunction, ED) is a common disease, which can be defined as the inability to erect the penis, ejaculate or both. According to statistics, its incidence rate accounts for 1.9% in men over 40 years old, and the incidence rate is 1.9% in men over 65 years old. For men it reaches 65%. There are about 125 million men in the world suffering from different degrees of erectile dysfunction, and it is expected to reach 3...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P15/10
CPCA61K9/1652A61K9/2054A61K9/2018C07D487/04A61K9/1641A61K9/2027A61K9/1623A61K9/2031A61K9/1635A61P15/10C07B2200/13A61K31/519C07C51/43C07C59/265
Inventor 刘桂坤
Owner HONG KONG GOLDEN WISDOM MEDICAL PRODN LTD
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