Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-06-12
1995-06-06
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514396, 514418, 514419, 514423, 514424, 514887, 514937, 514938, A61K 31415, A61K 3140
Patent
active
054223610
DESCRIPTION:
BRIEF SUMMARY
This invention relates to cosmetically elegant, chemically and physicially stable topical cream and lotion bases and lipophilic drug compositions containing an amount of N-methyl-2-pyrrolidone effective to enable penetration through the skin of lipophilic drugs, such as steroids and antimicrobials.
Topical application of drugs is the preferred mode of administration in many instances to avoid side effects often found with systemic application of such drugs. Topical pharmaceutical compositions should possess the following characteristics: sensitization;
One of the most serious problems which must be overcome in developing an effective topical base for a pharmaceutical composition is penetration of the drug into the skin. Good skin penetration is a particularly difficult problem for lipophilic drugs exhibiting low water solubility, such as steroids and antimicrobials, especially antifungals and pentrants for such drugs are often added to lipophilic drug-containing compositions.
Penetrants for drugs are known. U.S. Pat. No. 3,551,554 discloses use of dimethyl sulfoxide and U.S. Pat. No. 4,316,893 discloses use of 1-lower alkyl substituted azacyclopentan-2-ones to enhance percutaneous adsorption of drugs. N-methyl-2-pyrrolidone is also a known penetrant for drugs, but it has been found in our laboratories that N-methyl-2-pyrrolidone breaks down emulsion systems such as creams and lotions. Thus, we are aware of no successful cream or lotion systems containing N-methyl-2-pyrrolidone. Creams and lotions, e.g., oil-in-water emulsions, are particularly desirable bases for such lipophilic drugs. In the course of developing the bases and pharmaceutical compositions of the present invention, we prepared numerous creams containing known drug penetration agents such as dimethyl sulfoxide and N-methyl pyrrolidone, but most of these creams did not have all of the desired characteristics necessary for an acceptable topical pharmaceutical formulation for a lipophilic drug.
Thus, there is still a need for a chemically and physically stable, cosmetically elegant topical cream and/or lotion base for a lipophilic drug-containing pharmaceutical composition which allows effective penetration of the lipophilic drug through the skin with minimal skin irritation and/or sensitization.
SUMMARY OF THE INVENTION
We have surprisingly discovered that a chemically and physically stable, cosmetically elegant topical cream and lotion base for lipophilic drug-containing pharmaceutical compositions which incorporates an amount of N-methyl-2-pyrrolidone effective to allow penetration of a lipophilic drug through the skin with minimal skin irritation. Thus, this invention provides a base in the form of an oil-in-water emulsion for use in cream and lotion lipophilic drug-containing pharmaceutical compositions containing at least one lipophilic drug comprising (a) an amount of N-methyl-2-pyrrolidone effective to enable a lipophilic drug to penetrate through the skin, (b) an aqueous phase comprising water and an amount of propylene glycol sufficient to at least partially solibilize a lipophilic drug in the aqueous phase; and (c) an oil phase comprising an amount of mineral oil or diethyl sebacate effective to at least partially solubilize a lipophilic drug in the oil phase, (d) an amount of a surfactant system effective to stablize the emulsion formed from the oil phase and aqueous phase, (e) an occlusive agent, (f) a preservative, and optionally a silicon oil and wherein the pH of said base is in the range of about 4.0 to 7.0.
This invention also provides a topical cream and/or lotion pharmaceutical composition in the form of an oil-in-water emulsion containing at least one lipophilic drug and a base comprising (a) an amount of N-methyl-2-pyrrolidone effective to enable a lipophilic drug to penetrate through the skin, (b) an aqueous phase comprising water and an amount of propylene glycol sufficient to at least partially solubilize a lipophilic drug in the aqueous phase; and (c) an oil phase comprising an amount of diethyl sebacate or mineral o
REFERENCES:
patent: 4039664 (1977-08-01), Stoughton et al.
patent: 4316893 (1982-02-01), Rajadhyaksha
patent: 4424234 (1984-01-01), Alderson et al.
patent: 4537776 (1985-08-01), Cooper
Chemical Abstracts (1977) vol. 87: 157098g (Vazquez et al.).
Chemical Abstracts (1991) vol. 105: 30084j (Naito).
Munayyer Farah J.
Sequeira Joel A.
Cintins Marianne M.
Criares T. J.
Hoffman Thomas D.
Schering Corporation
LandOfFree
Stable cream and lotion bases for lipophilic drug compositions does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Stable cream and lotion bases for lipophilic drug compositions, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Stable cream and lotion bases for lipophilic drug compositions will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-987953