Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1995-11-16
1998-03-10
Bawa, Raj
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424447, 424448, 424449, 424401, 424 45, 514937, 514944, 514945, 514969, A61F 1300
Patent
active
057258740
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a solubilizing agent or solubilizer for a pharmaceutically effective ingredient and an external preparation containing the solubilizer. In particular, the present invention relates to a solubilizer for an efficacious ingredient used in a percutaneously absorbable preparation such as poultice or for a fat-soluble powder used in a pack, the solubilizer being excellent in solubilization of such an effective ingredient as well as in safety, stability, compatibility, non-odorousness and refreshing, effect, and also relates to an external preparation containing the solubilizer.
BACKGROUND ART
Up to this time, many attempts have been made to attain desirable curative effects by the percutaneous absorption of drugs. It is a significant problem in such percutaneously absorbable preparations how efficiently the drug (active ingredient as a drug) is released from the base, i.e., how efficiently the drug migrates from the base to the skin. In general, when attempting to design a preparation using some drug therein, there frequently occurs a case that the drug crystallizes in the base because of its insufficient dissolution therein, resulting in poor drug release so that a sufficient curative effect is not achieved. Accordingly, the selection of an optimum solubilizer for a drug is an important factor in designing such a preparation. If an unsuitable solubilizer is selected for a drug, the release of the drug from the base is lowered due to the insufficient dissolution of the drug in the base, which leads to poor migration of the drug to an affected part so that poor curative effect results.
Solubilizers currently used for drugs include alcohols, glycols, several surfactants, essential oils such as peppermint oil, crotamiton, methyl salicylate, glycol salicylate and fatty acid esters such as isopropyl myristate.
For example, Japanese Pat. Appln. Laid-Open Gazette No. 154413/1981 discloses an anti-inflammatory agent for external use which comprises both an oil-in-water emulsion containing a solution of flurbiprofen in a terpene or in a fatty acid ester and an aqueous base, and Japanese Pat. Appln. Laid-Open Gazette No. 98209/1982 discloses another anti-inflammatory agent for external use which is prepared by dissolving indomethacin in a mono- or polyhydric alcohol or the like.
However, these solubilizers have problems because they have poor solubilizability (capability of solubilization) to cause the crystallization of a drug, they are limited in use due to their odors, they bleed from the base with the lapse of time due to their poor compatibility with the base, they are poor in stability to cause decomposition or discoloration with the lapse of time and they cause undesirable side effects due to their stimuli to the skin, resulting in unsatisfactory effects in many cases.
Meanwhile, attempts have been made to get a powder which is soluble in fat or difficultly soluble in water (hereinafter referred to as "fat-soluble powder") to be contained in a pack for its practical use. However, a pack generally comprises a water-soluble base which exhibits extremely poor solubilizability for a fat-soluble powder, so that many of the above attempts were accompanied by the problems that the solubilization of the powder in the base was difficult and/or that the resulting pack was poor in stability to cause crystallization of the powder with the lapse of time even when the powder could be solubilized in the base in the preparation stage.
SUMMARY OF THE INVENTION
The present invention aims at solving the above problems to provide a solubilizer which exhibits excellent solubilizability for a pharmaceutically effective ingredient and is excellent in safety, stability and compatibility, and provides an external preparation containing the solubilizer.
The above object of the present invention can be attained by using 3-l-menthoxypropane-1,2-diol as the solubilizer for a pharmaceutically effective ingredient.
Namely, the present invention resides in a solubilizer for a pharmaceuticall
REFERENCES:
patent: 4459425 (1984-07-01), Amano et al.
Chemical Abstracts, vol. 110, No. 18, May 1, 1989, Columbus, Ohio, US; Abstract No. 160412, XP002014010.
Hirano Munehiko
Nakagawa Akira
Oda Hideshi
Shoho Koki
Tateishi Tetsuro
Bawa Raj
Hisamitsu Pharmaceutical Co. Inc.
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