Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1997-03-31
1999-04-06
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514625, A61K 31165, A61K 4716
Patent
active
058919201
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to a drug solubilizer and a drug-absorption accelerator which are for use in administration by percutaneous absorption of the drug in a preparation for external use, and also to a percutaneously absorbable preparation. More particularly it relates to (1) a drug solubilizer which consists of an N-substituted-o-toluidine derivative and is excellent in drug solubility, safety, stability, compatibility with a base and feeling at the time of use, (2) a drug-absorption accelerator which contains said toluidine derivative as an absorption acceleration effective ingredient, increases the drug in permeability and transmittability through the skin and is low in irritation to the biomembranes and (3) a percutaneously absorbable preparation containing said solubilizer and said absorption accelerator.
BACKGROUND ART
There have conventionally been developed ointments, poultices, tape-aids, lotions, suppositories, eye lotions and the like in the field of preparations for external use. Among these preparations, percutaneously absorbable preparations have recently attracted public attention and are arousing an increasing interest in themselves. The reasons for this are that in cases where a drug, the pharmacological action of which is expected, is administered locally or systemically so as to be percutaneously absorbed, it is advantageously possible to keep the efficacy of the drug, adjust the rate of absorption thereof easily thereby enabling the prevention of medicinal side effects caused by overdosing the drug, lessen the influence of metabolism exerted by the effect of the drug caused by the initial passage thereof through the liver as is experienced in case of oral administration, thereby enabling the drug to be effectively utilized, and administer comparatively safe even such a drug as to cause liver troubles and the like. In addition to the above preparations, there has now been developed a form of preparation, called "TTS", having a high function to control the release thereof.
(1) In these externally usable preparations attempted to be percutaneously absorbed, it is important to release a drug from a base which contains it, that is, it is necessary for the drug to be efficiently transferred from the base to the skin. To this end, generally importance is placed in the state of dissolution of the drug in the base at the stage of designing these preparations. In other words, how the drug exists in the base will have remarkable effects on not only its physicochemical stability but also its release from the base, percutaneous absorption efficiency and consequent medicinal efficacy. Thus, it comes to be very important when designing preparations, to select a solubilizer which is excellent in solubilization of the drug and exerts an effect on uniform dispersion of the drug into the base.
Solubilizers now used for drugs include fatty acids such as oleic acid and myristic acid, fatty acid esters such as isopropyl myristate and isopropyl palmitate, essence oils such as limonene, peppermint oil and eucalyptus oil, polyhydric alcohols such as polyethylene glycol and propylene glycol, surface-active agents, glycol salicylate and crotamiton, among which crotamiton is frequently used as a solubilizer for difficultly soluble drugs. For example, crotamiton is used as a solubilizer for indomethacin in Japanese Patent Gazette No. Hei 3-3368 (or No. 3368/91), as a solubilizer for steroids in Japanese Pat. Appln. Laid-Open Gazette No. Sho 51-73115 (No. 73115/76) and as a precipitation preventer for valeric acid dexamethasone in Japanese Patent Gazette No. Hei 2-36572. In addition, Japanese Pat. Appln. Laid-Open Gazette No. Sho 59-116212 discloses an indomethacin-containing creamy preparation comprising crotamiton as a solubilizer for the drug.
These solubilizers, however, raise problems as to precipitation of a drug in the crystal form because of shortage of their solubilizability (capability of solubilization), limitation of their use because of their odor, their bleeding with time due to th
REFERENCES:
patent: 4752612 (1988-06-01), Saito et al.
patent: 5162315 (1992-11-01), Rajadhyaksha et al.
Database WPI Week 8748, Derwent Publications Ltd., AN 87-337226, XP 002046755 Japanese Publication No. 62-240628A, Publication Date: Oct. 21, 1987.
Hirano Munehiko
Kido Mitsuhiko
Kuribayashi Mitsuru
Hisamitsu Pharmaceutical Co. Inc.
Spivack Phyllis G.
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