Sustained release formulations - Patents

Sustained release formulations

Agent: U.s. Patent Operations/rnm Dept. 4300, M/s 27-4-a - Thousand Oaks, CA, US
Inventors: Merrill S. Goldenberg, Jian Hua Gu
Class: 424468000 (USPTO), A61K038/08 (Intl Class)
#20050271722
12/08/05
The present invention relates broadly to the field of sustained release formulations. More specifically, the invention describes compositions and methods relating to formulating proteins and/or peptides with purified gallic acid esters. In one example, the gallic acid ester is PentaGalloylGlucose (PGG) and in anther example the gallic acid ester is epigallocatechin gallate (EGCG).
FIELD OF THE INVENTION
[0002] The present invention relates broadly to the field of sustained release formulations. More specifically, the invention describes compositions and methods relating to formulating proteins and/or peptides with purified gallic acid esters. In one example, the gallic acid ester is PentaGalloylGlucose (PGG), where gallic acid is also known as 3,4,5 trihydroxybenzoic acid and in another example the gallic acid ester is epigallocatechin gallate (EGCG).
SUMMARY OF THE INVENTION
[0011] The present invention provides pharmaceutical compositions comprising a stable sustained release complex composed of a protein and/or peptide and a gallic acid ester that allow for sustained delivery of the protein or peptide in vivo upon administration of the complex. Accordingly, the complex of the invention can permit continuous delivery of a pharmaceutically active peptide to a subject for periods of time less than about one or two weeks.
[0012] The complex of the invention is formed by combining a protein or peptide and a gallic acid ester under conditions such that a complex is formed. In a preferred embodiment, the complex is a salt of the gallic acid ester and protein or peptide. The complex is typically poorly soluble in water and can be purified from various aqueous solutions. As the complex is in the form of a solid (e.g., a paste, granules, a powder or a lyophilizate), the complex can be prepared for administration to a subject as a stable liquid suspension or semi-solid dispersion.
[0013] In one embodiment of the invention, the group suitable for use in forming a complex with a peptide or protein is a gallic acid ester. Preferably, the ester itself is formed by a linkage of the acid group of gallic acid to an alcohol moiety on another compound such as a sugar. In a particular embodiment, the gallic acid ester is PentaGalloylGlucose (PGG), where the gallic acid is also known as 3,4,5-trihydroxybenzoic acid. In another embodiment, the gallic acid ester is Epigallocatechin Gallate (EGCG).
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