초록 ▼

A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tgand Tsis at least about 10° C. (i.e. Tg-Tsis greater than 1

A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tgand Tsis at least about 10° C. (i.e. Tg-Tsis greater than 10° C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier. It is particularly valuable in unit dosage form having a moisture barrier, in combination with appropriate labelling instructions. A process for producing a powdered dispersible composition is also provided, wherein the process comprises removing the solvent from a solution comprising a solvent, a glass former and a pharmacologically active material under conditions sufficient to form a glassy matrix having the pharmacologically active material within the matrix.

대표청구항 ▼

A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tgand Tsis at least about 10° C. (i.e. Tg-Tsis greater than 1

A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tgand Tsis at least about 10° C. (i.e. Tg-Tsis greater than 10° C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier. It is particularly valuable in unit dosage form having a moisture barrier, in combination with appropriate labelling instructions. A process for producing a powdered dispersible composition is also provided, wherein the process comprises removing the solvent from a solution comprising a solvent, a glass former and a pharmacologically active material under conditions sufficient to form a glassy matrix having the pharmacologically active material within the matrix. t 5 percent by weight. 19. The method of claim 1, wherein said powder has a moisture content of less than about 2% by weight. 20. The method of claim 1, wherein said storing is carried out at a storage temperature that is at least 30° C. less than the Tg of said powder. 21. The method of claim 1, wherein the Tg of said powder in step (ii) is greater than 45° C. 22. The method of claim 1, wherein the Tg of said powder in step (ii) is greater than 55° C. 23. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of carbohydrates, carbohydrate derivatives, carbohydrate polymers, organic carboxylic acid salts, synthetic organic polymers, proteins, peptides, amino acids, and mixtures thereof. 24. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of carbohydrates, peptides, and amino acids. 25. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of sodium citrate, raffinose, lactose, trehalose, maltotriose, maltodextrin, maltose, glucopyranosyl-sorbitol, glucopyranosyl-mannitol, polydextrose, sucrose, cyclodextrin, casein, human serum albumin, hydroxyethyl starch, stachyose, magnesium gluconate, cellobiose, and mixtures thereof. 26. The method of claim 1, further comprising aerosolizing said powder. 27. The method of claim 26, wherein said aerosolizing is carried out by actuating a dry powder inhaler.