abstract |
The present invention provides compositions and methods for extending the release time and reducing toxicity of pharmacologically active compounds. The compound contains a pharmacologically active compound, a salt of a lipophilic counterion and a pharmaceutically acceptable water-soluble solvent, which are mixed to form an injectable composition. The lipophilic counterion may be a C 8 -C 22 saturated or unsaturated fatty acid, preferably a C 10 -C 18 saturated or unsaturated fatty acid. When injected into a mammal, at least a portion of the composition precipitates, releasing the active compound over a period of time. Thus, the composition becomes a sustained release drug depot of the active compound in mammals. Thus, the present invention allows for dose-controlled administration of the active compound for a period of up to 15 days or longer. Many compounds can be administered according to the present invention, including but not limited to tilmicosin, oxytetracycline, metoprolol, fluoxetine, roxithromycin, and terbinafine. |