DICLOFENAC PARENTERAL COMPOSITIONS
The present application provides parenteral compositions of diclofenac or its pharmaceutically acceptable salt and methods for making and using such compositions. Some of the compositions of the present application has one or more following properties: (1) ready to be injectable, (2) in the form of an oil-water emulsion, (3) stable under appropriate storage conditions, (4) containing therapeutically effective amount of diclofenac or its pharmaceutically acceptable salt, (5) sterilizable by filtration (6) containing components acceptable by regulatory agencies (e.g. the FDA), (7) containing low oil content and thus not exacerbating hyperlipidemia, and (8) is neither hypoallergenic nor vein irritating.
1 . A parenteral composition in the form of oil-in-water emulsion that comprises:
(a) diclofenac or its pharmaceutically acceptable salt,
(b) an oil component,
(c) a phospholipid component, and
(d) water.
2 . The composition of claim 1 , wherein the oil component comprises a monoglyceride, a diglyceride, a triglyceride, or a mixture thereof.
3 . The composition of claim 2 , wherein the triglyceride is medium chain triglycerides.
4 . The composition of claim 1 , wherein the oil component comprises combination of vegetable oil and a medium chain triglyceride.
5 . The composition of claim 1 , further comprises a cryoprotectant.
6 . The composition of claim 1 , wherein the phospholipid component comprises a phosphatidyl choline, lecithin, phosphatidylethanolamine, phosphatidylglycerol, phosphatidic acid, or a mixture thereof.
7 . The composition of claim 6 , wherein the lecithin comprises soy lecithin and egg lecithin.
8 . The composition of claim 1 , wherein the composition optionally comprise additives such as acidifying, alkalizing, antioxidant, buffering, chelating, complexing and solubilizing agents, antioxidants and antimicrobial preservatives, suspending and/or viscosity modifying agents, tonicity modifying agents, and other biocompatible materials or therapeutic agents.
9 . The composition of any of the claims 1 - 8 , wherein the composition has an osmolality of at least 250 mOsm.
10 . The composition of any of the claims 1 - 9 , comprises at least one tonicity modifying agent.
11 . The composition of any of the claims 1 - 10 , is vein non-irritable.
12 . The composition of any of the claims 1 - 11 , is filter sterilizable.
13 . The composition of claim 5 , wherein the cryoprotectant is sucrose.