FORMULATIONS OF GROWTH HORMONE RELEASING FACTOR (GRF) MOLECULES WITH IMPROVED STABILITY

摘要

Stabilized solid and liquid pharmaceutical formulations comprising a GRF molecule as active ingredient, such as GRF analogs including those comprising an N-terminal-attached hydrophobic moiety, such as [trans-3-hexenoyl]hGHRH (1-44) amide, are disclosed. The formulation comprises a GRF molecule or a pharmaceutically acceptable salt thereof and a β-cyclodextrin which is not conjugated to the GRF molecule or salt thereof. Also disclosed is the use of the formulation for the treatment of various conditions, methods of preparing the formulation, as well as kits containing it. Methods of stabilizing (e.g., with respect to chemical stability) such GRF molecules, as well as methods of inhibiting their deamidation at Asn8, are also disclosed.

主权项

1. A liquid pharmaceutical formulation comprising:
[trans-3-hexenoyl]hGRF(1-44) amide (SEQ ID NO: 7) or a pharmaceutically acceptable salt thereof, in an amount of about 1 mg/ml to about 10 mg/ml; and a modified β-cyclodextrin at a concentration of about 5% to about 10% (w/v), wherein said formulation is isotonic and has a pH of about 5.5 to about 6.5, and wherein said modified β-cyclodextrin is not conjugated to said [trans-3-hexenoyl]hGRF(1-44) amide or pharmaceutically acceptable salt thereof.