Composition for promoting vascular smooth muscle relaxation

摘要

A composition for topical application to a part of the body comprises a local anaesthetic and optionally a vasodilator as active ingredient dissolved in a blend of volatile and non-volatile solvents of different solvating capacities for the active ingredient. The vasodilator may comprise glyceryl trinitrate and the local anaesthetic may comprises an anaesthetic of the aminoamide or aminoester type. The volatile solvent may comprise a mixture of water with a C1-C5 alcohol and the non-volatile solvent may comprise a polyhydric alcohol and optionally a glycol. A low-concentration vasodilator-containing composition is also described. The compositions allow a “virtual injection” of the active ingredient to be delivered transdermally without general systemic uptake.

主权项

1. A spreadable gel or cream for topical application to a part of the body comprising a vasodilator as an active ingredient dissolved in a blend of volatile and non-volatile solvents of different solvating capacities for the active ingredient, wherein the volatile solvent comprises a mixture of water and a C1-C5 alcohol in a ratio by weight of 1.6:1 to 2.5:1, the non-volatile solvent comprises glycerol in a concentration from 5 to 40% by weight of the total solvent content, and the spreadable gel or cream comprises between 0.015 mg and 5 mg of glyceryl trinitrate in a unit-dosage form, wherein the concentration of the vasodilator present in the total solvent system is at or slightly below a saturated concentration such that super-saturation occurs upon loss of volatile components.