The present invention relates to pharmacological active preparations, especially local anesthetic preparations and deals with the problem of i a obtaining a solution of a local anesthetic agent in the form of its base, where the concentration is higher than otherwise possible. This problem has been dissolved according to the present invention thereby that one local anesthetic agent in the form of its base and as such having a melting point of 30.degree. to 50.degree. C., preferably prilocaine or tetracaine, is provided with one other local anesthetic agent in the form of its base and as such having a melting point of above 30.degree. C., preferably above 40.degree. C., preferably bensocaine, lidocaine, bupivacaine, mepivacaine, etidocaine or tetracaine which agents when brought and heated together form a homogenous oil having a melting of preferably below 40.degree. C., more preferably below 25.degree. C.
A topical, transdermal anesthetic comprising a eutectic mixture of, preferably, lidocaine and prilocaine in a ratio of about 3:1 by weight, incorporated within a lipophilic base. In addition to the property of rapid-onset, the formulation of the present invention has high storage stability and is less restricted by dosage limitations of other prilocaine-containing transdermal anesthetics and is, advantageously, not dependent upon occlusive dressing for optimal transdermal absorption.
The present invention relates to stabilized topical pharmaceutical preparations. More specifically the present invention relates to a stabilized topical pharmaceutical preparation, based on the solubilization of a eutectic mixture of local anesthetic agents, in base form, which when combined in the presence of a surfactant and water produce a single phase hydrated polymer to be used in obtaining topical anesthesia and also relates to a stabilized antimicrobial topical pharmaceutical preparation.
The present invention relates to a delivery system which includes a bioactive drug or cosmetic substance presented in the form of submicron oil spheres alone, or drugs or cosmetic substances in a combination with the oil spheres in an aqueous suspension or emulsion. Optionally, a skin penetration enhancer may be included in such formulations. Such preparations achieve improved bioavailability and exert larger pharmacological effects than an equivalent dose of the drug or cosmetic formulated in conventional creams, lotions or oleaginous bases.
The present invention relates to a delivery system which includes a bioactive drug or cosmetic substance presented in the form of submicron oil spheres alone, or drugs or cosmetic substances in a combination with the oil spheres in an aqueous suspension or emulsion. Optionally, a skin penetration enhancer may be included in such formulations. Such preparations achieve improved bioavailability and exert larger pharmacological effects than an equivalent dose of the drug or cosmetic formulated in conventional creams, lotions or oleaginous bases.
A novel topical anesthetic preparation is characterized by improved transdermal absorption and efficacy. In a preferred embodiment, the topical preparation contains at least one local anesthetic agent and at least two melting point depressing agents. Also provided is a two-phase liquid composition that contains aqueous and oil phases, the oil phase having a relatively high concentration of a local anesthetic agent to enhance transdermal absorption and efficacy when incorporated into a topical anesthetic preparation. A preferred topical anesthetic preparation includes lidocaine or tetracaine, thymol or menthol, and ethyl alcohol or isopropyl alcohol. The preparation is expected to be safe and effective in obtaining transdermal anesthesia on intact skin and mucous membrane of adults, children, infants and newborns.
