Synergistic mixed poloxamer systems for the solubilisation of drugs
AssigneeIS Pharmaceuticals Limited
InventorsJohn Meadows, Colum Martin Dwyer
Life of this patent
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Abstract
Drugs which are difficult to solubilise in water, and especially those which otherwise cause pain on injection, can be readily formulated and typically administered with substantially less pain when solubilised in synergistic, aqueous micellar preparations of poloxamers. Such preparations may also be prepared with less, or without, co-solvents.
Claims23
A method for making an homogeneous aqueous preparation comprising preparing a synergistic mixture of two poloxamers in water, and adding lidocaine thereto;
- wherein the ratio of poloxamers is between 7:3 and 3:7 by weight, and
- wherein the poloxamers are selected from the group consisting of P188, P234, P237, P338 and P407.
A method of making an homogeneous aqueous preparation comprising mixing lidocaine with a synergistic mixture of two poloxamers, and adding water thereto;
- wherein the ratio of poloxamers is between 7:3 and 3:7 by weight, and
- wherein the poloxamers are selected from the group consisting of P188, P234, P237, P338 and P407.
The method according to claim, 11, wherein said synergistic mixture of poloxamers comprises micelles.
An homogeneous aqueous preparation comprising lidocaine as the only active anaesthetic ingredient, solubilized in water and a synergistic mixture of two poloxamers, wherein said mixture of poloxamers, together with water, solubilize more of said lidocaine than an equivalent amount of any individual poloxamer of the mixture under the same conditions;
- wherein the ratio of poloxamers is between 7:3 and 3:7 by weight, and
- wherein the poloxamers are selected from the group consisting of P188, P234, P237, P338 and P407.
An homogeneous aqueous anaesthetic preparation comprising the freebase form of lidocaine solubilized in water and a synergistic mixture of two poloxamers, wherein said mixture of poloxamers, together with water, solubilize more of said lidocaine than an equivalent amount of any individual poloxamer of the mixture under the same conditions;
- wherein the ratio of poloxamers is between 7:3 and 3:7 by weight, and
- wherein the poloxamers are selected from the group consisting of P188, P234, P237, P338 and P407.
An homogeneous aqueous preparation consisting essentially of:
- lidocaine, solubilized in water, and
- a synergistic mixture of two poloxamers, wherein said mixture of poloxamers, together with water, solubilize more of said lidocaine than an equivalent amount of any individual poloxamer of the mixture under the same conditions, wherein the ratio of poloxamers is between 7:3 and 3:7 by weight, and wherein the poloxamers are selected from the group consisting of P188, P234, P237, P338 and P407, and
- optionally, one or more of a suitable co-solvent, sterilizing agent, stabilizing agent, bacteriostat, antioxidant, tonicity, or pH modifying agent.
Dependencies are inferred from the claim text.