Solvent system enhancing the solubility of pharmaceuticals for e

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...

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252364, 424 80, 424455, 424456, 5147729, A61K 31765

Patent

active

050716433

ABSTRACT:
This invention relates to a solvent system for enhancing the solubility of an acidic, basic, or amphoteric pharmaceutical agent to produce a highly concentrated solution suitable for softgel filling or two piece encapsulation. The solvent system comprises polyethylene glycol containing 0.2-1.0 mole equivalents of an ionizing agent per mole equivalent pharmaceutical agent and 1-20% water. Glycerin or polyvinylpyrrolidone may be added to further enhance the solubility of certain drugs. The disclosed solvent system is capable of enhancing solubilities of pharmaceutical agents 40-400%.
The ionizing agent functions by causing partial ionization (neutralization) of the free pharmaceutical agent. When the pharmaceutical agent is acidic, the ionizing agent is preferably a hydroxide ion species, whereas when the pharmaceutical agent is basic, the ionizing agent is preferably a hydrogen ion species. For amphoteric pharmaceutical agents, either hydroxide ion or hydrogen ion sources may be utilized to effect partial ionization.
The disclosed solvent system is useful because it not only provides for the enhancement or improvement of bioavailability of acidic, basic and amphoteric pharmaceutical agents by delivering them already in solution, but it also provides for a highly concentrated solution capable of encapsulation in a small enough vessel to permit easy swallowing.
The highly concentrated solid solutions of the present invention are also useful for conversion into tablets and as veterinary spot and pour on preparations.

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