Suspension for oral administration containing amorphous tolvaptan
A technology of tolvaptan and suspension, which is applied in the field of suspensions for oral administration containing amorphous tolvaptan, can solve problems such as reduced solubility and absorption, and achieve excellent absorption, high solubility, The effect of retarding crystallization
Active Publication Date: 2019-05-10
OTSUKA PHARM CO LTD
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Problems solved by technology
When tolvaptan is prepared as a solid preparation using a common preparation technology, tolvaptan becomes crystals, and there is a problem that solubility and absorption from the gastrointestinal tract are reduced
Method used
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preparation example 1B
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Abstract
The present invention provides a suspension for oral administration, the suspension for oral administration comprises granules containing amorphous tolvaptan, capable of inhibiting or delaying the dissolution of amorphous tolvaptan in the suspension over time crystallization, and stably maintain high solubility of tolvaptan and excellent absorbability from the gastrointestinal tract; and a solid preparation for oral administration, which can be suspended when used so that Suspensions for oral administration are prepared. The present invention relates to a suspension for oral administration, especially a syrup, comprising (a) granules containing amorphous tolvaptan, (b) hydroxypropylmethylcellulose (HPMC) and (c) a solvent, wherein, Based on the total weight of the suspension for oral administration, the compounding amount of the HPMC (b) is 0.1 to 25% by weight.
Description
technical field The present invention relates to suspensions (especially syrups) for oral administration containing amorphous tolvaptan and methods for their manufacture. Background technique Tolvaptan (tolvaptan) is 7-chloro-5-hydroxyl-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2 shown in formula (I), 3,4,5-Tetrahydro-1H-benzazepine is a vasopressin antagonist having aquaretic activity (Patent Document 1). Tolvaptan is marketed as a therapeutic drug against hyponatremia, fluid retention in heart failure, and fluid retention in cirrhosis. When tolvaptan is prepared as a solid preparation using a common preparation technique, tolvaptan becomes a crystal, and there is a problem that the solubility and the absorbability from the gastrointestinal tract are lowered. As a means to solve the above problems, Patent Document 2 reports a means of dissolving tolvaptan and hydroxypropyl cellulose in an organic solvent, and then powdering them by spray drying to form a Compositions...
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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/26A61K47/38A61K9/16A61K31/55
CPCA61K9/0095A61K47/26A61K47/38A61K9/1652A61K31/55A61P1/00A61P1/16A61P13/00A61P3/12A61P7/10A61P9/00A61P9/04A61K9/0053A61K9/10
Inventor 赤木亮之铃木海中村笃哉西林彻
Owner OTSUKA PHARM CO LTD
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