Pharmaceutical compositions of water soluble peptides with poor solubility in isotonic conditions and methods for their use
AssigneeStrongbridge Dublin Limited
InventorMichel Afargan
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Abstract
The present invention provides compositions comprising water soluble peptides with poor solubility in isotonic solutions which exhibit enhanced bioavailability with reduced adverse effects including injection site reactions. Methods are also disclosed for using such compositions for the treatment of diseases including, but not limited to, cancer, type 2 diabetes, acromegaly, metabolic disorders, endocrine disorders, exocrine tumors, and hormone-related tumors. Methods to reduce adverse injection site reactions and improve bioavailability are also disclosed.
Claims21
A pharmaceutical composition comprising:
- veldoreotide or a pharmaceutically acceptable salt thereof;
- and a polymeric microsphere, wherein veldoreotide or the pharmaceutically acceptable salt thereof is encapsulated in the polymeric microsphere, and wherein the surface area of the polymeric microsphere is from about 7 m2/g to about 12 m2g.
A process for manufacturing polymeric microspheres comprising the steps of:
- (i) mixing an excipient comprising a hydrophobic scavenger, a sugar, an amino acid, or nicotinamide, and veldoreotide or a pharmaceutically acceptable salt thereof in water to form a first aqueous mixture;
- (ii) mixing a polymer in organic solvent to form a polymeric solution;
- (iii) mixing the first aqueous mixture in the polymeric solution to form a first dispersion mixture comprising a water-in-oil primary emulsion;
- (iv) mixing polyvinyl alcohol (PVA) in phosphate buffered saline or in saline to form a second aqueous mixture;
- (v) mixing the primary emulsion in the second aqueous mixture of PVA to form a water-in-oil-in-water double emulsion thereby providing a secondary dispersion mixture;
- and
- (vi) allowing the organic solvent in the secondary dispersion mixture to evaporate to form polymeric microspheres comprising veldoreotide or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.