Details for Patent: 8,871,273
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Title: | Method for producing granules |
Abstract: | In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50.degree. C. or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm.sup.2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced. |
Inventor(s): | Nagahara; Naoki (Osaka, JP), Asakawa; Naoki (Hikari, JP), Nonomura; Muneo (Osaka, JP) |
Assignee: | Takeda Pharmaceutical Company Limited (Osaka, JP) |
Filing Date: | Feb 24, 2006 |
Application Number: | 11/884,498 |
Claims: | 1. A coated granule comprising a biologically active substance, obtained by a method that comprises steps of: (a) providing a granule comprising the biologically active substance and low substituted hydroxypropyl cellulose, wherein the biologically active substance is a benzimidazole proton pump inhibitor, (b) coating the granule comprising the biologically active substance with a coating material comprising a polymer base selected from the group consisting of low substituted hydroxypropyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, polyvinyl pyrrolidone, polyvinyl alcohol, methyl cellulose, and hydroxyethylmethyl cellulose, so as to provide an intermediate coating layer on the granule (c) coating the granule obtained in the step (b) with a coating material comprising a mixture of two or more kinds of polymers selected from the group consisting of methyl methacrylate methacrylic acid copolymers, so as to provide a controlled release coating film on the granule, and (d) heating the granule comprising the biologically active substance to a temperature about 50.degree. C. or higher, and then maintaining the granule heated at the temperature for about 1 minute to about 1 hour, wherein the heating step is performed during the step (a), or during, before, or after the step (b) or the step (c), wherein the coated granule dissolves or elutes the biologically active substance, pH-dependently; and controls a release of the biologically active substance from the coated granule depending on pH to which the coated granule is exposed. 2. The coated granule according to claim 1, wherein the heating temperature of the granule is about 60.degree. C. or higher. 3. The coated granule according to claim 1, wherein the heating temperature of the granule is about 65.degree. C. or higher. 4. The coated granule according to claim 1, wherein the granule is maintained heated at the temperature for about 3 minutes to about 1 hour. 5. The coated granule according to claim 1, wherein the step of heating and maintaining the heat is performed before the coating step (b). 6. The coated granule according to claim 1, wherein the step of heating and maintaining the heat is performed during either of the coating steps (b) or (c). 7. The coated granule according to claim 1, wherein the step of heating and maintaining the heat is performed after either of the coating steps (b) or (c). |