Dispersions for the formulation of slightly or poorly soluble agents

Supersaturated dispersions in form of an oil-in-water emulsion comprising:

• an oil phase;
• a water phase;
• one or more surfactants or stabilizers;
• and
• one or more drugs being only slightly or poorly soluble in the water and in the oil, the dispersions are supersaturated and contain an incorporated amount of the drug in dispersion that is at least 5 times higher than the additive solubility calculated from the drug solubility in the oil and water phases of the dispersion, and the dispersions are organic solvent-free, said dispersion obtained by combining;
• the aqueous phase,
• the oily phase, which oily phase is not or only partially miscible with the aqueous phase,
• the surfactant or stabilizer, and
• a solid phase, which comprises the one or more drugs, to form a pre-dispersion, wherein the active ingredient is suspended in at least a portion of the aqueous phase before contacting the active ingredient with the oily phase,
• which pre-dispersion of liquid and solid phases is subjected to a high-energy homogenization process wherein no toxicologically dangerous solvents are used, and wherein at least one of the one or more drugs is incorporated as solid particles into the liquid phases of the dispersion without previously being dissolved,
• the one or more drugs is pulverized to form particles, the particles of drug are triturated or mixed with an oil-in-water emulsion or a water-in-oil emulsion to form the pre-dispersion, or
• the one or more drugs is pulverized to form particles, the particles of drug are added to a surfactant solution, said surfactant solution is homogenized and mixed with an oil-in-water emulsion or a water-in-oil emulsion to form the pre-dispersion.

A method for the production of a dispersion comprising:

• an oily phase;
• an aqueous phase, in the form of an oil-in-water emulsion or a water-in-oil emulsion;
• and
• at least one active ingredient that is only slightly or with difficulty soluble in the oily phase and the aqueous phase, wherein the dispersion is free from toxicologically dangerous organic solvents and the dispersion is supersaturated containing the active ingredient dissolved in a quantity that is at least 5 times greater than the quantity which results additively from its maximum solubility in the oily and the aqueous phase of the emulsion, the method comprising:
• suspending the active ingredient in at least a portion of the aqueous phase to form a suspension and mixing the suspension with said oily phase to form a mixture;
• subjecting the mixture of liquid and solid phases to a high-energy homogenization process with a homogenizer without using toxicologically dangerous organic solvents, wherein one of:
• (a) incorporating the active ingredient as a solid into the liquid phases of the dispersion without previously being dissolved,
• (b) pulverizing the active ingredient, triturating or mixing the pulverized active ingredient with an oil-in-water emulsion or a water-in-oil emulsion to form a pre-dispersion, and subjecting the pre-dispersion to the homogenization or high pressure homogenization process, or
• (c) pulverizing the active ingredient, dispersing the pulverized active ingredient in a surfactant solution, homogenizing the dispersion to form a homogenized dispersion, then mixing the homogenized dispersion with an oil-in-water emulsion or a water-in-oil emulsion to form a pre-dispersion, and subjecting the pre-dispersion to the homogenization or high pressure homogenization process.