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Amorphous pinaverium bromide

An amorphous form, pinaverium bromide technology, applied in the direction of medical preparations containing active ingredients, organic chemistry, pharmaceutical formulations, etc., can solve instability and other problems, achieve good stability, promote bioavailability, and simple steps Effect

Active Publication Date: 2016-02-10
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention provides a stable pinaverium bromide in an amorphous form. The inventor unexpectedly found that the amorphous form not only exhibits good solubility and can promote the absorption and bioavailability of pinaverium bromide, but also has Good stability overcomes the defect that amorphous drugs are easily affected by external factors and is unstable, and lays a good foundation for transforming into pharmaceutical dosage forms and putting them into industrial production

Method used

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  • Amorphous pinaverium bromide
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  • Amorphous pinaverium bromide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh 1.0 g of pinaverium bromide in a round-bottomed flask, add 33 mL of dichloromethane, stir and dissolve under heating and reflux, wait for the solution to be clarified, and suction filter while it is hot. g pinaverium bromide in amorphous form, with a yield of 90.5% and a purity of 99.4%.

[0039] After measurement, the X-ray powder diffraction pattern of its gained amorphous form pinaverium bromide is as follows figure 1 shown.

Embodiment 2

[0041] Weigh 1.0g of pinaverium bromide in a round-bottomed flask, add 38mL of methanol, stir and dissolve under heating and reflux, wait for the solution to be clarified, and suction filter while it is hot. The resulting filtrate is quickly removed by a rotary evaporator and dried to obtain 0.873g The finalized form of pinaverium bromide has a yield of 87.3%, a purity of 99.2%, and its X-ray powder diffraction pattern is the same as in Example 1.

Embodiment 3

[0043] Weigh 1.0g of pinaverium bromide in a round-bottomed flask, add 34mL of water and 14mL of dioxane as a mixed solvent, stir and dissolve under heating and reflux, wait for the solution to be clarified, suction filter while it is hot, and obtain the filtrate by rotary evaporation Quickly remove, dry, obtain 0.854g amorphous pinaverium bromide, yield 85.4%, purity 99.2%, its X-ray powder diffraction pattern is the same as embodiment 1.

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Abstract

The invention relates to an amorphous pinaverium bromide. The amorphous pinaverium bromide has good dissolvability, can promote drug absorption and improve the bioavailability of drugs, and also has unexpected stability, so the morphous pinaverium bromide can be well applied in the preparation of medicinal preparations. The invention also provides a method for preparing the morphous pinaverium bromide. The method has the advantages of simple steps, easy operation, and suitableness for industrial large-scale production.

Description

technical field [0001] The invention relates to an amorphous form of medicine for treating irritable bowel syndrome, in particular to an amorphous form of calcium antagonist pinaverium bromide. Background technique [0002] Pinaverium bromide, developed by Solvay Pharmaceuticals of France, is a calcium antagonist with highly selective antispasmodic effects on the gastrointestinal tract and is used for the treatment of irritable bowel syndrome, pain associated with intestinal dysfunction, bowel motility Abnormalities and discomforts and other diseases. The mechanism of action of pinaverium bromide on smooth muscle is the same as that of other calcium antagonists, but it has a highly selective effect on colonic smooth muscle. Pinaverium bromide achieves antispasmodic effect by blocking calcium ions from flowing into intestinal wall smooth muscle cells and preventing excessive muscle contraction. It can eliminate the hyperresponsiveness of intestinal smooth muscle and increase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/096A61K31/5375A61P1/00
Inventor 周浩辉林国良耿玉先产运霞范宝成刘宇凡郝艳山
Owner BEIJING WINSUNNY PHARMA CO LTD