Merck + Co., Inc.

Boehringer Ingelheim Animal Health USA Inc.

Interx Research Corporation

Jacob A Zupan

Deborah L Steinbrenner

Novel aqueous oxytetracycline compositions comprising oxytetracycline, polyethylene glycol with a mean molecular weight of 400, and magnesium oxide. These compositions have good clarity and low viscosity.

Novel oxytetracycline compositions

Eucalyptol is used to enhance skin permeation of bio-affecting agents.

Use of eucalyptol for enhancing skin permeation of bio-affecting agents

Greatly enhanced delivery of a wide variety of bio-affecting agents is provided by formulations for topical application comprising at least one bio-affecting agent and eucalyptol. Optionally, the formulation can further comprise a non-toxic topical carrier and/or an additional penetration enhancer. The eucalyptol acts as a unique transport agent which readily delivers the active bio-affecting agent across the stratum corneum to the target area. Cosmetic and therapeutic dermatological agents as well as systemically effective therapeutic agents can be easily formulated with eucalyptol and effectively delivered through the skin to the desired site, i.e., to the underlying tissues of the epidermis and dermis or to the general circulation.

The invention relates to a novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protected aromatic amine; and removing the N-protecting group therefrom.

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St. Joseph, MO, United States of America

Jacob A Zupan