Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal

Active Publication Date: 2015-06-25
POLA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a way to prevent the formation of an isomer of luliconazole caused by factors like humidity and light. This means that the stability of the product is improved.

Problems solved by technology

However, in the present circumstances, any effective measure should be inevitably found out by means of trial and error.

Method used

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  • Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal
  • Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal
  • Use of surface free energy for differential evaluation of crystal, crystal evaluated on basis of surface free energy as index, and pharmaceutical composition prepared by containing the crystal

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0072]Luliconazole was recrystallized under various conditions to obtain crystals in different states. The powder X-ray diffraction measurement was performed for these crystals (machine type of apparatus: XRD-DSCII, manufacturer: Rigaku Corporation, Condition: X-ray source: CuKα, measurement temperature: room temperature, tube voltage: 40 kV, tube current: 40 mA, 2θ: 5 to 35°, step angle: 0.05°). As a result, the positions of the diffraction angle 2θ of the diffraction peaks were identical in relation to all of them (see FIG. 1). Further, the peak was also single in DSC (machine type of apparatus: DSC7, manufacturer: PerkinElmer), and the melting point was observed in the vicinity of 149° C. (see FIG. 2, crystal recrystallized with water-containing ethanol (25%), crystal recrystallized with water-containing ethanol (50%), crystal recrystallized with water-containing ethanol (75%), and crystal recrystallized with ethyl acetate / n-hexane are shown from the top). According to these resu...

production example 1

[0079]Luliconazole was dissolved in ethanol while being heated, to which water in an amount of ⅓ of that of ethanol was gradually added, followed by being gently cooled to obtain Crystal 1 (ethanol / water (75:25) not pulverized).

production example 2

[0080]Crystal 1 was ground or pulverized with an agate mortar for 3 minutes to obtain Crystal 2 (ethanol / water (75:25) pulverized for 3 minutes).

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Abstract

An object is to provide means for suppressing the formation of any isomer of luliconazole on account of any influence of, for example, the humidity and the light and improving the stability. Disclosed is a method for differential evaluating a crystal of luliconazole, comprising differential evaluating the crystal by using, as indexes, surface free energy of the crystal of luliconazole and a ratio of a polar component of the surface free energy, wherein the crystal is evaluated to be stable on condition that the surface free energy is smaller and the ratio of the polar component is lower.

Description

TECHNICAL FIELD[0001]The present invention relates to a crystal of luliconazole having a useful crystal habit as an active pharmaceutical ingredient for a pharmaceutical composition, and pharmaceutical compositions which contain the crystal as the active pharmaceutical ingredient.BACKGROUND ART[0002]Luliconazole is an antifungal agent which is excellent in the action on fungi. At present, luliconazole is widely used as a pharmaceutical or medicine for tinea pedis and tinea corporis, and it is going to be applied to tinea unguium as well. Further, luliconazole has an extremely high suppressing effect on Aspergillus. Therefore, it is also expected to be applied to profound mycosis (fungal disease) in a form of a pharmaceutical preparation (medicament preparation) for inhalation or the like for pneumonia and a vaginal agent for vaginitis. In relation to the pharmaceutical preparation of luliconazole, it is known as problems which should be solved that luliconazole is converted to stere...

Claims

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Application Information

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IPC IPC(8): G01N33/15C07D409/06
CPCG01N33/15C07B2200/13C07D409/06A61P31/10
InventorMASUDA, TAKAAKIKANEDA, HIDEO
OwnerPOLA PHARMA