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Crystal form V of Aildenafil citrate and preparation method and application thereof

A citric acid and amorphous technology, which is applied to the citrate aldenafil crystalline form V and the fields of its preparation and use, and can solve the problems that do not involve the citrate aldenafil crystalline form and its preparation method.

Inactive Publication Date: 2012-07-25
刘桂坤
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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 and its preparation method, etc., but does not involve the crystal form of edenafil citrate and its preparation method

Method used

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  • Crystal form V of Aildenafil citrate and preparation method and application thereof
  • Crystal form V of Aildenafil citrate and preparation method and application thereof
  • Crystal form V of Aildenafil citrate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] In a 3000ml reaction bottle, add 30 grams of edenafil citrate and 870ml of distilled water, start stirring, heat up to reflux, filter while it is hot after 15 minutes, the filtrate drops to 45°C-50°C, add 1740ml of acetone, and continue stirring After 1 hour, crystals were precipitated, filtered, and placed indoors for 1 hour, then moved to a vacuum drying oven, and dried in vacuum for 2 hours to obtain 27.3 g of the above-mentioned aldenafil citrate crystal form V, with a purification rate of 91%. The content measured by normalization method is 99.95%. Detected by X-ray diffractometer and infrared spectrometer (see Figure 1, Figure 2), it shows the characteristics of Aldenamorph citrate crystal form V.

Embodiment 2

[0059] In a 1000ml reaction bottle, add 10 grams of edenafil citrate and 250ml of distilled water, start stirring, heat up to reflux, filter while it is hot after 15 minutes, the filtrate drops to 45°C-50°C, add 500ml of acetone, and continue stirring After 1 hour, crystals were precipitated, filtered, and placed indoors for 1 hour, then moved to a vacuum drying oven, and dried in vacuum for 3 hours to obtain 9.2 g of the above crystalline form V of aldenafil citrate, with a purification rate of 92%. The content measured by normalization method is 99.95%. Detected by X-ray diffractometer and infrared spectrometer, (see Figure 1, Figure 2) shows the characteristics of Aldenamorph citrate crystal form V.

Embodiment 3

[0061] Granules Containing Aldenafil Citrate Form V

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

[0063] Process: PVG-4000 and aldenafil citrate crystal form V are crushed 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 packaged into granules.

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Abstract

The invention relates to a crystal form V of 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H- pyrazolo[4,3-d] 5-pyrimidinyl)-4-ethyoxylbenzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or Aildenafil citrate, and a preparation method thereof. The preparation method comprises the following steps: dissolving raw materials of the Aildenafil citrate in distilled water, stirring, and raising temperature to a reflux temperature; and adding acetone solution, and stirring and raising temperature continuously. The prepared product meets product requirements after being tested by an X-ray powder diffractometer and an infrared spectrometer. The invention also relates to a medicinal composition comprising the crystal form V of the Aildenafil citrate, and application of the crystal form V of the Aildenafil citrate in preparing medicaments for treating erection disturbance (ED).

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)- 4-ethoxybenzenesulfonyl]-cis-3,5-dimethylpiperazine citrate (Aildenafil citrate) crystal form V and its preparation method, containing the present invention The pharmaceutical composition of the crystal form V and the application of the crystal form V in the manufacture of a medicament 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 322 milli...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04A61K31/519A61P15/10
Inventor 刘桂坤
Owner 刘桂坤
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