Embedded micellar nanoparticles
AssigneeSolvay Pharmaceuticals GmbH
InventorJan Peter Möschwitzer
Life of this patent
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Abstract
The present invention relates to a thermostable solid composition containing nanosized micelles, the micelles containing a poorly soluble chemical substance, such as a biologically active substance, dissolved in an auxiliary material, and the micelles being embedded in a water soluble carrier. The invention further relates to a process for preparing a thermostable solid composition and to a process for preparing pharmaceutical dosage forms comprising the same.
Claims22
A solid composition comprising nanosized micelles, wherein said micelles comprise a poorly soluble active substance dissolved in an auxiliary material or a mixture of auxiliary materials,
- wherein said auxiliary material or said mixture of auxiliary materials is chosen from polyoxyethylene stearates, Polyoxyethylene sorbitan fatty acid esters, Polyoxyethylene Castor Oil Derivatives, Vitamin E TPGS, nonionic polyoxyethylene-polyoxypropylene block co-polymers, water-soluble long chain organic phosphate esters, and inulin lauryl carbamate,
- wherein said micelles are embedded in a water-soluble carrier, wherein said water-soluble carrier is chosen from:
- alkylcelluloses;
- hydroxyalkylcelluloses;
- hydroxyalkyl-alkylcelluloses;
- carboxyalkylcelluloses;
- alkali metal salts of carboxyalkylcelluloses;
- carboxyalkylalkylcelluloses;
- starches;
- pectines;
- chitin derivates;
- polysaccharides, alkali metal and ammonium salts thereof;
- carrageenans, galactomannans, tragacanth, agar-agar, gummi arabicum, guar gummi, and xanthan gummi;
- polyacrylic acids and the salts thereof;
- polymethacrylic acids and the salts thereof, methacrylate copolymers;
- polyvinylalcohol;
- polvinylpyrrolidone, copolymers of polyvinylpyrrolidone with vinyl acetate;
- polyalkylene oxides;
- and
- copolymers of ethylene oxide and propylene oxide;
- and
- wherein the composition is a powder that remains free flowing when heated above the melting point of the main auxiliary material.
A process for preparing a solid pharmaceutical composition, comprising:
- A) combining a poorly soluble active substance, an auxiliary material or a mixture of auxiliary materials, optionally one or more additional auxiliary materials, a matrix forming material, and water to form nanosized micelles;
- and
- B) drying the mixture obtained in (A) to obtain a solid pharmaceutical composition, wherein the micelles are embedded in the matrix forming material, and wherein the composition is a powder that remains free flowing when heated above the melting point of the main auxiliary material;
- wherein said auxiliary material or said mixture of auxiliary materials is chosen from polyoxyethylene stearates, Polyoxyethylene sorbitan fatty acid esters, Polyoxyethylene Castor Oil Derivatives, Vitamin E TPGS, nonionic polyoxyethylene-polyoxypropylene block co-polymers, water-soluble long chain organic phosphate esters, and inulin lauryl carbamate;
- and
- wherein said water-soluble carrier is chosen from:
- alkylcelluloses;
- hydroxyalkylcelluloses;
- hydroxyalkyl-alkylcelluloses;
- carboxyalkylcelluloses;
- alkali metal salts of carboxyalkylcelluloses;
- carboxyalkylalkylcelluloses;
- starches:
- pectines;
- chitin derivates;
- polysaccharides, alkali metal and ammonium salts thereof;
- carrageenans, galactomannans, tragacanth, agar-agar, gummi arabicum, guar gummi, and xanthan gummi;
- polyacrylic acids and the salts thereof;
- polymethacrylic acids and the salts thereof, methacrylate copolymers;
- polyvinylalcohol;
- polvinylpyrrolidone, copolymers of polyvinylpyrrolidone with vinyl acetate:
- polyalkylene oxides;
- and
- copolymers of ethylene oxide and propylene oxide.
Dependencies are inferred from the claim text.