Process for preparing acylated esters of hydroxy carboxylates
申请人:THE PROCTER & GAMBLE COMPANY
公开号:EP0002872A1
公开(公告)日:1979-07-11
A process for esterifying and acylating hydroxycarboxylate compounds in an organonitrile reaction medicine comprising the steps of contacting said compounds with an esterification agent-and thereafter acylating by adding an acylating agent to the reaction medium.
A large group of lipophilic, pharmacologically active compounds can be effectively delivered across intact skin by applying them topically in a binary, penetration-enhancing vehicle containing (1) a C3-C4 diol, diol ester, or diol ether and (2) a cell envelopedisordering compound. This vehicle provides surprising enhancement of skin penetration for the pharmacological active, compared to either component alone.
Skin conditioning compositions are described which comprise an emulsion of petrolatum; water; an unsaturated monoglyceride emulsifier; and a skin conditioning agent, preferably glycerine. As a result of the novel cubic, viscous isotropic dispersed phase of these water-in-oil emulsions, they possess the ability to incorporate and deliver relatively high levels of glycerine while retaining high cosmetic acceptance.
Topical pharmaceutical compositions are described which comprise an emulsion of petrolatum; water; an unsaturated monoglyceride emulsifier; and a pharmaceutical agent. The dispersed phase of these water-in oil emulsions exists in a cubic, viscous isotropic phase. These compositions are useful for delivery of a large group of pharmaceutical agents through the skin for local and/or systemic action.
Improved topical pharmaceutical compositions containing a pharmaceutically-active agent and the penetration enhancing agent 1-dodecylazacycloheptan-2-one are disclosed. This agent is used at selected levels in combination with certain C3-C4 diols or a 1-substituted azacycloalkyl-2-one. This composition provides marked transepidermal and percutaneous delivery of the selected pharmaceutically-active agent. A method of treating certain pathologies and conditions responsive to the selected active, systemically or locally, is also disclosed.