Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1997-01-17
1999-01-12
Schofer, Joseph L.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424682, A61K 914
Patent
active
058584080
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a sustained-release oral ointment which is intended for use in the remedy of oral diseases, such as periodontal disease and the like. More particularly, the present invention relates to a sustained-release oral ointment which comprises a hydrophobic ointment base, an adhesive substance, an aluminum compound and a drug.
BACKGROUND ART
As ointment bases applied on oral mucosa, there are generally and widely used those ointments comprising a hydrophobic ointment base (e.g. petrolatum or plastibase) and an adhesive substance (e.g. sodium carboxymethyl cellulose or sodium polyacrylate) in consideration of the of SQUIBB JAPAN INC.; Aphtasolon for Dental Use (or for Use in Oral Cavity, trade name), a product of Showa Yakuhin Kako Co., Ltd.; and Dexarutin Ointment (trade name), a product of Nippon Kayaku Co., Ltd.!. These ointments, however, have been insufficient as sustained-release ointments. The inventors of the present application have previously filed JP-A-4-13616 in which they have disclosed a sustained-release oral ointment which comprises a hydrophobic ointment base, an adhesive substance, a polyhydric alcohol and a drug. However, there has not yet been known an ointment base which comprises a hydrophobic ointment base, an adhesive substance and an aluminum compound.
Therefore, it has been desired to develop a sustained-release oral ointment which has applicability to an oral mucosa, particularly to a periodontal pocket, sustained-release properties to supply a drug to affected part over a long period of time while maintaining the concentration thereof at a sufficiently high level, and enhanced ratio of utilization of drug (the ratio of the total amount of drug released to affected part to the total amount of drug in the composition applied).
Hence, in order to solve the above problems, the present invention has an object of providing a novel sustained-release oral ointment.
DISCLOSURE OF THE INVENTION
Under the above-mentioned situation, the inventors of the present application made an intensive study. As a result, the present inventors found that a sustained-release oral ointment which comprises a hydrophobic ointment base, an adhesive substance, an aluminum compound and a drug can achieve the above object, and completed the present invention.
The present invention is hereinafter described in detail.
The drug used in the present invention is not particularly restricted. Specific examples thereof includes antibacterial agents such as compounds ##STR1## wherein R.sup.1 represents a substituted or unsubstituted alkyl, alkenyl, cycloalkyl, aryl or heterocyclic group; R.sup.2 represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a protected or unprotected hydroxyl, amino or alkylamino group, or a dialkylamino group; R.sup.3 represents a substituted or unsubstituted cycloalkyl, vinyl or cyclic amino group; ##STR2## represents a group ##STR3## wherein X.sup.1 represents a hydrogen atom or a halogen atom, or alternatively, forms, together with R.sup.1, a group represented by the formula: ##STR4## wherein R.sup.4 represents a hydrogen atom or an alkyl group, and D represents an oxygen atom or a sulfur atom; and ##STR5## represents a group represented by ##STR6## wherein X.sup.2 represents a hydrogen atom or a halogen atom, salts thereof, tetracycline, oxytetracycline, fradiomycin sulfate, chloramphenicol and the like; bactericidal disinfectants such as chlorhexidine hydrochloride, cetylpyridinium chloride, benzethonium chloride, decalinium chloride, benzalkonium chloride and the like; antiphlogistics such as dexamethasone, triamcinolone acetonide, sodium azulenesulfonate and the like; antiphlogistic enzyme preparation such as .alpha.-amylase and the like; local anesthetics such as lidocaine, ethyl aminobenzoate and the like; and so forth.
In the specification of the present application, unless otherwise specified, "halogen atom" refers to a fluorine atom, a chlorine atom, a bromine atom or an iodine atom; "alkyl group" refers to C.sub
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Kato Shosaku
Sotani Sadao
Takakura Isamu
Watanabe Yasuo
Sarofin N.
Schofer Joseph L.
Toyama Chemical Co., Ltd.
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