Novel solid pharmaceutical dispersions
OwnerIsaac Ghebre-Sellassie, Robert Reisch JR. +3inventors
InventorsIsaac Ghebre-Sellassie, Robert Reisch JR., Riten Parikh, Mahdi B. Fawzi, Russell U. Nesbitt
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Abstract
A novel solid pharmaceutical dispersion that improves the bioavailability of poorly water soluble drugs is produced by combining the drug with a polymer carrier such as polyvinylpyrrolidone. The drug is combined with the carrier without the need for using organic solvents or melting temperatures (fusion) through the use of a transition compound such as polyethylene glycol which partially solubilizes the drug and/or plasticizes the polymer.
Claims19
A process for the preparation of a poorly water soluble drug in solid dispersion comprising
- a) blending the drug with a carrier;
- b) dissolving a surfactant and a plasticizer/solubilizer in water;
- c) spraying the surfactant-plasticizer/solubilizer solution onto the drug/carrier mixture in a fluid bed granulator;
- d) extruding the resulting granulation through a twin screw extruder with at least one heating zone;
- and,
- e) milling the extrudate to a powdery mass of the solid drug dispersion.
A solid pharmaceutical dispersion with improved solubility characteristics consisting essentially of a poorly water soluble drug and;
- a) a carrier selected from the group consisting of polyvinyl pyrrolidone, high molecular weight polyethylene glycol, urea, citric acid, Eudragit® acrylic polymers, succinic acid and mixtures thereof and,
- b) a solubilizer/plasticizer selected from the group consisting of polyols, phthalate esters, glycerol esters, citrate esters, sugar alcohols and mixtures thereof.
A solid pharmaceutical dispersion with improved solubility characteristics comprised of a poorly water soluble drug and a carrier produced by the process consisting of:
- a) mixing said drug and the carrier in a ratio of approximately 1:9 to about 5:1 respectively, on a percent weight basis;
- b) spraying onto said mixture a solution consisting of a plasticizer/solubilizer, and optionally, a surfactant;
- c) extruding the resultant granulation in a twin screw extruder with at least one heating zone;
- and
- d) milling the extrudate to a powdery mass.
Dependencies are inferred from the claim text.