Non-aqueous compositions for oral delivery of insoluble bioactive agents
OwnerDoron Friedmaninventor
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Abstract
The present invention provides a composition of low water solubility drug, dissolved or dispersed in a non crystalline or low crystalline form in an emulsion type composition of internal oily-solvent and external non-hydrous and water soluble solvent, whereas 1) emulsifying stabilizer comprises low fraction of the composition, and 2) emulsions of mean droplets size below one micron is obtained upon dilution with physiological fluids, and 3) facilitated dispersion of biologically active agents in body fluids is obtained, and more particularly to facilitating biological availability or improving clinical performance.
Claims20
A pharmaceutical composition of oily solvent dispersed in non-hydrous hydrophilic solvent, composed of:
- a) a low-solubility drug dissolved or dispersed in the composition, whereas majority of drug is non crystalline in the composition, and
- b) At least one oily solvent comprising the internal phase of the emulsion dispersion, and
- c) at least one emulsifying stabilizer, and
- d) a continuous non-hydrous and hydrophilic solvent phase,
- Wherein, sub-micron mean droplets size is obtained upon dilution with physiological fluids.
A process for producing homogeneous amorphous dispersion of hydrophobic drug in non-aqueous nano size droplets semi-solid emulsion;
- A—Heating and co-melting the drug and selected oils and emulsifying stabilizers until clear solution devoid of solid material is obtained.
- B—Heating non-aqueous hydrophilic phase to 80° C.-100C.
- C—Adding the hot non-aqueous phase (B) to hot oily phase (A) in increments under stirring and mixing.
- D—Homogenizing the emulsion (C) until the hot liquids cools into semi-solid state.
A method for facilitating the dissolution and the oral availability of a pharmacologically active agent having low or poor water solubility, wherein the method comprises oral administering of the patient undergoing treatment a mixture of the pharmacologically active agent composed of:
- A. a low-solubility drug dissolved or dispersed in the composition, whereas majority of drug is non crystalline in the composition, and
- B. At least one oily solvent comprising the internal phase of the emulsion dispersion, and
- C. at least one emulsifying stabilizer, and
- D. a continuous non-hydrous and hydrophilic solvent phase,
- Wherein, sub-micron mean droplets size is obtained upon dilution with
Dependencies are inferred from the claim text.