FIELD: pharmaceuticals.
SUBSTANCE: group of inventions relates to a topical composition containing tacrolimus and a method for production thereof. Composition for topical application includes: a first disperse phase containing first oil and tacrolimus; a second disperse phase comprising a second oil; a dispersed aqueous medium and a surfactant. First oil differs from the second oil and the phase is chemically and physically different. First oil contains diisopropyl adipate and/or isopropyl myristate and/or triglycerides of caprylic acid. Second oil includes oil selected from a group consisting of mineral oil, dimethicone, cyclomethicone, hydrogenated polyisobutane, heptamethylnonane and mixtures of two or more of them. Composition has total content of surfactant less than 5 wt % of composition weight. Polar miscible with water, if present, in amount of less than 5 wt % of composition weight. Method of preparing the composition involves: (i) providing a first oil containing tacrolimus; (ii) providing a second oil; (iii) providing an aqueous component and (iv) dispersing the first oil and the second oil in the aqueous component to form said composition for local use.
EFFECT: use of two different oil phases of said composition provides effective penetration through skin and solvation of tacrolimus without using high levels of polar water-miscible liquids, such as alcohols and glycols, in a dispersed aqueous medium, which, in turn, minimizes skin irritation caused by the composition; composition of the composition shows better penetration through the skin in vivo than existing preparations in the form of an ointment, such as ProtopicTM, with the same concentration of tacrolimus in the composition of the agent.
13 cl, 12 tbl, 9 ex, 9 dwg
