Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Pharmaceutical composition

a pharmaceutical composition and composition technology, applied in the field of skin agents, can solve the problems of not having a definite law for maintaining not knowing how to achieve the maintenance and not having a definite law for the maintenance property of the steric structur

Inactive Publication Date: 2010-08-12
POLA PHARMA +1
View PDF37 Cites 35 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016]The present invention may provide a formulation in which the compound represented by the general formula (1) stably exists. Such formulation may be usefully used for seborrheic dermatitis.

Problems solved by technology

Therefore, it is restricted to use a solvent such as methyl ethyl ketone from the viewpoints of possibility of causing an irritation, flammability, and the like.
Because the compound represented by the general formula (1) has restricted water solubility, one problem is how to prepare a formulation in a form of a single-phase solution without impairing the solubility of the compound.
In particular, in a compound having an asymmetric carbon in the molecule, the maintenance of a steric structure becomes a critical issue in addition to the solubility.
However, there is no definite law for maintenance property of such steric structure.
In a formulation containing the compound represented by the general formula (1), there has been no finding about whether or not the maintenance of the steric structure of the compound becomes a problem, and further, it is not known how to achieve such maintenance of the steric structure.
It is known that those ingredients may cause hydrolysis or the like to affect the stability of an active ingredient.
However, there has been no finding that the ingredients have a preferred contribution to the stability in a specified mixing ratio.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pharmaceutical composition
  • Pharmaceutical composition
  • Pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0030]Luliconazole was dissolved by adding an appropriate amount of ethanol. To the resulting solution, POE (20) sorbitan monostearate (“NIKKOL TS-10MV”; manufactured by Nihon Surfactant Kogyo K.K.) was gradually added, water was further added, and homogenization was performed (Table 1). The resultant was named as Skin agent A for external use. Further, Skin agent B for external use as a control was prepared in the same manner as in Skin agent A for external use except that ethanol was added in place of water.

TABLE 1Prescription of Skin agent A for external useIngredientmass %Luliconazole1.2POE (20) sorbitan monostearate7.5Water23.3Ethanol68Total100

[0031]Form of formulation: a form of a single-phase and homogeneously dissolved solution was confirmed through a visual check.

No irritating sensation of the formulation was confirmed.

[0032]For Skin agent A for external use and Skin agent B for external use, the time-dependent stability of luliconazole was evaluated 1 week after preparatio...

example 2

[0033]In the same manner as in Example 1, luliconazole was dissolved in ethanol. To the resulting solution, POE (20) sorbitan monooleate (“NIKKOL TO-10MV”; manufactured by Nihon Surfactant Kogyo K.K.) was gradually added, water was further added, and homogenization was performed to prepare Skin agent C for external use. Further, Skin agent D for external use as a control was prepared in the same manner as in Skin agent C for external use except that ethanol was added in place of water.

TABLE 3Prescription of Skin agent C for external useIngredientmass %Luliconazole1.2POE (20) sorbitan monooleate9.3Water23.3Ethanol66.2Total100

[0034]Form of formulation: a form of a single-phase and homogeneously dissolved solution was confirmed through a visual check.

No irritating sensation of the formulation was confirmed.

[0035]For Skin agent C for external use and Skin agent D for external use, the time-dependent stability of luliconazole was evaluated 1 week after preparation under a preservation co...

example 3

[0036]In the same manner as in Example 1, luliconazole was dissolved in ethanol. To the resulting solution, polyoxyethylene hydrogenated castor oil 40 (“NIKKOL HCO-40”; manufactured by Nihon Surfactant Kogyo K. K.) was gradually added, water was further added, and homogenization was performed to prepare Skin agent E for external use. Further, Skin agent F for external use as a control was prepared in the same manner as in Skin agent E for external use except that ethanol was added in place of water.

TABLE 5Prescription of Skin agent E for external useIngredientmass %Luliconazole1.2Polyoxyethylene hydrogenated1.4castor oil 40Water23.7Ethanol73.7Total100

[0037]Form of formulation: a form of a single-phase and homogeneously dissolved solution was confirmed through a visual check.

No irritating sensation of the formulation was confirmed.

[0038]For Skin agent E for external use and Skin agent F for external use, the time-dependent stability of luliconazole was evaluated 1 week after preparat...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
mass %aaaaaaaaaa
mass %aaaaaaaaaa
mass %aaaaaaaaaa
Login to View More

Abstract

Disclosed is an antifungal agent for external use, which is characterized by containing a compound represented by the general formula (1) below, 50-95% by mass of an alcohol, and 0.1-35% by mass of water and / or an anionic surfactant.

Description

TECHNICAL FIELD[0001]The present invention relates to a skin agent for external use, and more specifically, to an antifungal agent for external use.BACKGROUND ART[0002]For diseases such as athlete's foot and candidiasis to be caused by fungi, medicaments such as bifonazole, butenafine, and terbinafine have been developed and prescribed as skin medicines for external use.[0003]Of those, there may be exemplified, as a particularly promising medicament, a compound represented by a general formula (1) having an effect of shortening a therapeutic period for diseases derived from fungi, which has been reported in recent years as a novel imidazole compound having an antifungal activity, especially, luliconazole, which is an optically active substance (see JP 3278738 B). Further, such compound is also useful for onychomycosis, and a formulation for onychomycosis has also already been known (for example, see WO 03 / 105841). That is, the compound represented by the general formula (1) may be s...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4178A61P31/10
CPCA61K31/4178A61K9/0014A61P17/00A61P17/08A61P31/10
Inventor MASUDA, TAKAAKIKOBAYASHI, NAOKOSASAGAWA, HIDEAKI
Owner POLA PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com