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US 5,723,269 AGranted
Microparticle preparation and production thereof
AssigneeTakeda Chemical Industries, Ltd.
InventorsYasaburo Akagi, Nobuyuki Takechi, Muneo Nonomura
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AssigneeTakeda Chemical Industries, Ltd.
InventorsYasaburo Akagi, Nobuyuki Takechi, Muneo Nonomura
Estimating the term…
A novel microparticle preparation comprising microparticles of a polymer which contain a drug and are at least partially or wholly coated with a water-soluble inorganic salt, a water-soluble organic acid or a water-soluble salt of an organic acid, which acts as an agent for preventing aggregation of the microparticle preparation is disclosed. The preparation is produced by spraying a polymer solution containing a drug and a solution or dispersion of a water-soluble inorganic salt, a water-soluble organic acid or a water-soluble salt of an organic acid from different nozzles and contacting them with each other in a spray dryer. In this procedure, if desired, a non-ionic surfactant may be added to the solution of the water-soluble inorganic salt, the water-soluble organic acid or the water-soluble salt of organic acid, or a solution of non-ionic surfactant may be sprayed from the other nozzle simultaneously.
A method for producing a microparticle preparation which comprises spraying a solution of polymer containing a drug and a solution of a water-soluble inorganic salt, a water-soluble organic acid or a water-soluble salt of an organic acid separately from different nozzles and contacting the solution sprays with each other in a spray dryer to produce microparticles of the polymer which contains the drug and are coated at least partially or wholly with the water-soluble inorganic salt, the water-soluble organic acid or the water-soluble salt of the organic acid, wherein the organic acid is selected from the group consisting of citric acid, tartaric acid, malic acid, succinic acid, benzoic acid, chondroitin sulfuric acid, alginic acid and peptic acid, and wherein the polymer is a poly fatty acid ester selected from the group consisting of homopolymers of .alpha.-hydroxycarboxylic acid, copolymers of two or more .alpha.-hydroxycarboxylic acid, and a mixture thereof.
A method for producing a microparticle preparation which comprises spraying (a) a solution of a lactic acid/glycolic acid copolymer containing a drug selected from the group consisting of leuprorelin acetate and thyrotropin-releasing hormone and (b) a solution of a water-soluble inorganic salt separately from different nozzles and contacting them with each other in a spray dryer to produce microparticles of the copolymer which contain the drug and are coated at least partially or wholly with the water-soluble inorganic salt.
Dependencies are inferred from the claim text.