초록 ▼

A local anesthetic microsuspension system is disclosed that includes lipospheres, that are solid, water-insoluble microparticles that have a layer of a phospholipid embedded on their surface. The core of the liposphere is a solid anesthetic such as lidocaine or marcaine, or an anesthetic dispersed i

A local anesthetic microsuspension system is disclosed that includes lipospheres, that are solid, water-insoluble microparticles that have a layer of a phospholipid embedded on their surface. The core of the liposphere is a solid anesthetic such as lidocaine or marcaine, or an anesthetic dispersed in an inert solid vehicle, such as a wax. Anesthetic lipospheres provide a controlled delivery of local anesthetics to achieve extended, effective relief from pain by slowly releasing the anesthetic from the solid hydrophobic core. This is highly preferred over the situation in which an aqueous solution of local anesthetic must be frequently administered because it is quickly systemically absorbed.

대표청구항 ▼

A liposphere comprising: a core formed of a hydrophobic material existing as a solid at a temperature of 30°C. having anesthetic activity as a result of an anesthetic compound, and a phospholipid coating surrounding the core, wherein the hydrophobic ends of the phospholipid are embedded in the solid

A liposphere comprising: a core formed of a hydrophobic material existing as a solid at a temperature of 30°C. having anesthetic activity as a result of an anesthetic compound, and a phospholipid coating surrounding the core, wherein the hydrophobic ends of the phospholipid are embedded in the solid core and the hydrophilic ends of the phospholipid are exposed on the surface of the liposphere, the combination forming a spherical structure having an average particle diameter between 0.35 and 250 microns, wherein the core may contain a vehicle for the anesthetic compound, and the anesthetic compound, vehicle, and phospholipid coating are in a ratio of anesthetic compound to vehicle to phospholipid between 1:0:0.01 and 1:100:100.