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Pharmaceutical composition containing pyridyl dicyandiamide as well as preparation method and application thereof

A technology of pyridylguanidine and composition, applied in the field of pharmaceutical compositions of pyridylcyanoguanidine, can solve the problems of insoluble compounds, the compliance of weak patients with cancer patients, etc., and achieve the effect of improving solubility

Inactive Publication Date: 2015-06-10
TIANJIN HEMAY BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although as mentioned above, pyridyl cyanoguanidine is a promising antitumor drug with very noteworthy antitumor activity, but they have a high degree of lipophilicity and are insoluble compounds. CN01819244.0 discloses N -(6-(4-Chlorophenoxy)-hexyl)-N'-cyano-N"-(4-pyridyl)-guanidine has a solubility of 0.0002mg / ml in water and is usually only available for oral administration
However, many cancer patients are so debilitated by their disease that there are great problems in patient compliance when administering drugs orally

Method used

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  • Pharmaceutical composition containing pyridyl dicyandiamide as well as preparation method and application thereof
  • Pharmaceutical composition containing pyridyl dicyandiamide as well as preparation method and application thereof
  • Pharmaceutical composition containing pyridyl dicyandiamide as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0268] Embodiment 1, the HP-β-CD composition of compound 1 (1: 2 molar ratio)

[0269] Weighed 2.5mg of compound 1, added 0.5ml of 0.1N hydrochloric acid solution to dissolve, and added 21mg of HP-β-CD to dissolve to obtain a clear solution, which was freeze-dried to remove the solvent to obtain the target composition 1.

Embodiment 2

[0270] Embodiment 2, the HP-β-CD composition of compound 1 (1: 2 molar ratio)

[0271] Weigh 2.5mg of compound 1, add 0.5ml of 0.1N hydrochloric acid solution to dissolve, add 21mg of HP-β-CD to dissolve to obtain a clear solution, adjust the pH with 0.1N sodium hydroxide until the precipitate is just about to form, freeze-dry to remove the solvent , to obtain the target composition 2.

Embodiment 3

[0272] Example 3. Weigh 2.5 mg of compound 1, add 0.5 ml of 0.1N hydrochloric acid solution to dissolve to obtain a clear solution, add the same amount of sodium hydroxide solution as in Example 2, freeze-dry to remove the solvent, and obtain the target composition 3.

[0273] The compositions in Example 4-Example 24 were prepared by the preparation method of Example 2.

[0274] Weigh 2 mg of compound 1 and dissolve it with 2 ml of methanol and 0.5 ml of DMSO to obtain control solution 1;

[0275] Weigh 2 mg of compound 2 and dissolve it with 2 ml of methanol and 0.5 ml of DMSO to obtain a control solution 2;

[0276] Weigh 2 mg of compound 3 and dissolve it with 2 ml of methanol and 0.5 ml of DMSO to obtain control solution 3;

[0277] After dissolving the compositions obtained in Examples 2, 4-10 with water, take the control solution 1 as a contrast, and use HPLC to measure the concentration of the obtained composition solutions in each embodiment;

[0278] After the compo...

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Abstract

The invention discloses a composition formed by the pyridyl dicyandiamide and the cyclodextrin derivatives. The solubility of the pyridyl dicyandiamide in a water solution is greatly increased. The preparation method of the composition disclosed by the invention comprises the following steps: mixing a pyridyl dicyandiamide compound solution, the cyclodextrin derivatives or a solution containing the cyclodextrin derivatives and removing the solvent. The invention further discloses application of the composition in preparation of a medicine for treating the disease caused by the abnormality of cell proliferation.

Description

field of invention [0001] The invention relates to a pharmaceutical composition of pyridyl cyanoguanidine, its preparation method and application. Background of the invention [0002] Pyridylcyanoguanidines such as pinacidil (N-1,2,2-trimethylpropyl-N'-cyano-N"-(4-pyridyl)guanidine) were initially found to be potassium channel openers, And therefore be developed into antihypertensive drug.If the side chain of pinacidil is replaced by longer side chain containing aryl group, then lose antihypertensive activity, but find that this compound is administered orally when having Antitumor activity in a rat model of Yoshida ascites tumor. [0003] Different classes of pyridylcyanoguanidines with antiproliferative activity are disclosed in, for example, EP660823, WO98 / 54141, WO98 / 54143, WO98 / 54144, WO98 / 54145, WO00 / 61559 and WO00 / 61561, WO98 / 54146, WO2002 / 094813, in US5696140. The structure-activity relationship (SAR) of this class of compounds is discussed in C. Schou et al., Bio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4409A61K31/4406A61K31/444A61K31/4439A61K31/4709A61K31/506A61P35/00A61P35/02
Inventor 张和胜陈英伟霍爱红
Owner TIANJIN HEMAY BIO TECH CO LTD