Progesterone freeze-dried systems in sublingual dosage form

Various polymer matrices were tested to enhance progesterone bioavailability as part of an emergency therapy. Among the different polymers used, i.e. poly(N-vinylpyrrolidone) (PVP), poly(ethylene oxide) (PEO), Dextran T70 and partially saponified poly(methyl glyoxylate) (PMGz), the latter gives the fastest solubilization rate. The best results were obtained with the lyophilized dosage form instead of a simple mixture of the drug within the polymer matrix. A nearly instantaneous solubilization was observed with PMGz copolymers bearing 10-40% of carboxylic groups and containing up to 20% of the drug. The instantaneous solubilization of the PMGz matrix is due to the hydrophilic moieties, and the presence of hydrophobic zones in PMGz promotes good affinity with the drug and optimal dispersion into the matrix.