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Ilaprazole sodium compound and pharmaceutical composition thereof

A technology of ilaprazole sodium and compounds, applied in the field of pharmaceutical compositions containing said ilaprazole sodium compounds, capable of solving problems such as unmentioned key quality attributes of crystal form stability

Inactive Publication Date: 2016-04-06
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Five different crystal forms are disclosed in the prior art, but the stability critical quality attribute of the above crystal forms is not mentioned

Method used

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  • Ilaprazole sodium compound and pharmaceutical composition thereof
  • Ilaprazole sodium compound and pharmaceutical composition thereof
  • Ilaprazole sodium compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Embodiment 1: Preparation of B crystal form of ilaprazole sodium

[0080] Method 1: Add 2.5g of ilaprazole sodium raw material drug into 100ml of methanol, stir and dissolve at 25°C, filter to remove insoluble matter, rotate the filtrate at 25°C for crystallization, filter, and dry to obtain ilaprazole sodium type B crystal 2.2 g. Yield 88%.

[0081] Method 2: Add 2.5g of ilaprazole sodium crude drug into 50ml of methanol, stir and dissolve at 50°C, filter to remove insoluble matter, and the filtrate is crystallized by rotary evaporation at 50°C, filter, and dry to obtain ilaprazole sodium type B crystal 2.24 g. Yield 89.6%.

[0082] Method 3: Add 2.5g of ilaprazole sodium raw material drug into 100ml of ethanol, stir and dissolve at 50°C, filter to remove insoluble matter, rotate the filtrate at 50°C for crystallization, filter, and dry to obtain ilaprazole sodium type B crystal 2.3 g. Yield 92%.

[0083] Method 4: Add 2.5g of ilaprazole sodium crude drug into a ...

Embodiment 2

[0088] Embodiment 2: Preparation of C crystal form of ilaprazole sodium

[0089] Method 1: Suspend 2.5 g of ilaprazole sodium crude drug in 100 ml of ethyl acetate, stir at 25°C for 24 hours, filter, and dry to obtain 2.22 g of ilaprazole sodium type C crystals. Yield 88.8%.

[0090] Method 2: Suspend 2.5 g of ilaprazole sodium crude drug in 100 ml of acetonitrile, stir at 25°C for 24 hours, filter, and dry to obtain 2.28 g of ilaprazole sodium type C crystals. Yield 91.2%.

[0091] Method 3: Suspend 2.5 g of ilaprazole sodium crude drug in 50 ml of ethyl acetate, stir at 50° C. for 24 hours, filter, and dry to obtain 2.26 g of ilaprazole sodium type C crystals. Yield 90.4%.

[0092] Method 4: Suspend 2.5 g of ilaprazole sodium crude drug in 60 ml of acetonitrile, stir at 50° C. for 24 hours, filter, and dry to obtain 2.3 g of ilaprazole sodium type C crystals. Yield 92%.

[0093] Method 5: Add 2.5g of ilaprazole sodium crude drug into a beaker filled with 30ml of isoprop...

Embodiment 3

[0103] Embodiment 3: Preparation of D crystal form of ilaprazole sodium

[0104] Method 1: Suspend 2.5 g of ilaprazole sodium crude drug in 100 ml of chloroform, stir at 25°C for 24 hours, filter, and dry to obtain 2.45 g of ilaprazole sodium type D crystals. Yield 98%.

[0105] Method 2: Suspend 2.5 g of ilaprazole sodium crude drug in 50 ml of chloroform, stir at 50° C. for 24 hours, filter, and dry to obtain 2.25 g of ilaprazole sodium type D crystals. Yield 90%.

[0106] Polarized photos show that the above-mentioned ilaprazole sodium compound D-type crystals are powdery crystals, and the XRPD spectrum measured by Cu-Kα radiation is basically as follows: Figure 13 As shown, the spectral data are listed in Table 4 below. The TGA spectrum is basically as Figure 14 As shown, the crystal form has a weight loss of about 17.2% at 30-200°C, and the corresponding DSC has an endothermic peak at about 74.7°C. The IR spectrum is basically as Figure 15 shown. The Raman spect...

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Abstract

The invention provides various crystal forms of an ilaprazole sodium compound. In tests with influence factors of illuminance, high temperature and high moisture and an acceleration test, the crystal forms are good in stability, wherein the crystal form C is more stable and is suitable for preparing injections and enteric solid preparations. The various crystal forms are simple in preparation method and are suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a polymorph of ilaprazole sodium compound, a preparation method thereof, and a pharmaceutical composition containing the ilaprazole sodium compound. Background technique [0002] Peptic ulcer is a common chronic and recurrent disease. Its mortality rate is very small, but it brings great pain to patients and increases the economic burden of the country and patients. Peptic ulcer is a well-defined mucosal disorder that penetrates the muscularis mucosa and occurs in areas of the gastrointestinal tract that come into contact with gastric juices and can be seen in the lesser curvature of the stomach (gastric ulcer), pyloric duct (pyloric duct ulcer), twelve Duodenal bulb (duodenal ulcer), duodenal retrobulbar (retrobulbar ulcer), lower esophagus (reflux esophagitis), and marginal anastomotic or jejunal ulcers from gastrojejunostomy. At present, acid suppressants are the main drug...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61K31/4439A61P1/04
Inventor 陈庆财赵俊赵小伟王孝雯潘迅
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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