Targeted-release rifaximin composition
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- バウシュ ヘルス アイルランド リミテッド
- Filing Date
- 2026-02-24
- Publication Date
- 2026-06-09
AI Technical Summary
【0024】 一実施形態では、本明細書中に記載される発明は、開示された標的化放出組成物を患者に投与するステップを含む、鎌状赤血球症(SCD)の処置をそれを必要とする患者において実施する方法を含む。一部の実施形態では、鎌状赤血球症(SCD)を処置する方法は、患者における循環加齢性好中球(CAN)のレベルの上昇を減少させるステップを含む。一部の実施形態では、患者における鎌状赤血球症(SCD)を処置する方法は、患者において血管閉塞性クリーゼ(VOC)を処置するステップを含む。一部の実施形態では、患者において血管閉塞性クリーゼ(VOC)を処置することは、(1)患者においてVOCの1つ以上の症状を緩和するステップ;(2)患者においてVOCの発生を低減するか又は防止するステップ;(3)患者においてVOCの持続時間又は重症度を減少させるステップ;及び/又は(4)VOC中の患者のオピオイドの利用(usage)を仲介する(mediate)、そうでない場合その利用を減らすステップを含む。一部の実施形態では、患者において鎌状赤血球(SCD)を処置する方法は、患者において血管閉塞性クリーゼ(VOC)の1つ以上の症状を緩和するステップを含む。一部の実施形態では、患者において鎌状赤血球症(SCD)を処置する方法は、患者において血管閉塞性クリーゼ(VOC)の発生を低減するか又は防止するステップを含む。一部の実施形態では、鎌状赤血球症(SCD)を処置する方法は、患者においてVOCの持続時間又は重症度を減少させるステップを含む。一部の実施形態では、患者において鎌状赤血球症(SCD)を処置する方法は、患者において血管閉塞性クリーゼ(VOC)中患者のオピオイドの利用を仲介する、そうでない場合、その利用を減らすステップを含む。
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Abstract
Claims
1. A rifaximin bead composition comprising multiple beads, Each bead, A substantially spherical sugar base, A first coating comprising rifaximin and hydroxypropyl methylcellulose acetate succinate (HPMC-AS), wherein HPMC-AS is present in an amount of about 20% to about 60% by weight based on the total weight of rifaximin in the composition, or about 1% to about 12% by weight based on the total weight of the composition, and A second coating, where the second coating is an enteric coating that substantially covers the first coating, A rifaximin bead composition containing the above.
2. The rifaximin bead composition according to claim 1, wherein HPMC-AS is present in an amount of about 20% to about 50% by weight, based on the total weight of rifaximin in the composition.
3. The rifaximin bead composition according to claim 1 or 2, wherein HPMC-AS is present in an amount of about 25% to about 45% by weight, or about 43% to about 47% by weight, based on the total weight of rifaximin in the composition.
4. The rifaximin bead composition according to any one of claims 1 to 3, wherein HPMC-AS is present in an amount of about 30% to about 35% by weight, or about 44% to about 45% by weight, based on the total weight of rifaximin in the composition.
5. The rifaximin bead composition according to claim 1, wherein HPMC-AS is present in an amount of about 1% to about 4% by weight, or about 8% to about 11% by weight, based on the total weight of the composition.
6. The rifaximin bead composition according to claim 1 or 5, wherein HPMC-AS is present in an amount of about 1% to about 3% by weight, or about 8% to about 10% by weight, based on the total weight of the composition.
7. The rifaximin bead composition according to claim 1, 5, or 6, wherein HPMC-AS is present in an amount of about 2% to about 3% by weight, or about 9% to about 10% by weight, based on the total weight of the composition.
8. The rifaximin bead composition according to any one of claims 1 to 7, wherein HPMC-AS is HPMC-AS grade M.
9. A rifaximin bead composition according to any one of claims 1 to 8, further comprising a surfactant.
10. A rifaximin bead composition according to any one of claims 1 to 9, further comprising at least one pharmaceutically acceptable plasticizer, and / or at least one agent selected from the group consisting of ascorbyl palmitate, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), citric acid, sodium metabisulfite, cysteine, potassium metabisulfite, propyl gallate, sodium thiosulfate, vitamin E (e.g., vitamin E TPGS), and 3,4-dihydroxybenzoic acid.
11. The rifaximin bead composition according to any one of claims 1 to 10, wherein an enteric coating surrounds a substantially spherical sugar base coated with a first coating comprising rifaximin and HPMC-AS.
12. The rifaximin bead composition according to any one of claims 1 to 11, wherein the enteric coating comprises a methacrylic acid-acrylate copolymer.
13. The rifaximin bead composition according to any one of claims 1 to 12, wherein the enteric coating comprises an anionic methacrylate copolymer.
14. The rifaximin bead composition according to any one of claims 1 to 13, wherein the enteric coating comprises a copolymer of methacrylic acid and ethyl acrylate.
15. The rifaximin bead composition according to any one of claims 1 to 14, wherein rifaximin is present in an amount of about 1% to about 30% by weight, based on the total weight of the composition.
16. A rifaximin bead composition according to any one of claims 1 to 15, wherein the composition is intended to cause release into the mid-gastrointestinal tract of a subject requiring it.
17. A pharmaceutical composition used to treat one or more disorders in a subject requiring such treatment, comprising a therapeutically effective amount of the rifaximin bead composition according to any one of claims 1 to 16.
18. The pharmaceutical composition according to claim 17, wherein one or more disorders are selected from irritable bowel syndrome (IBS), diarrhea, microbial-associated diarrhea, infectious diarrhea, Clostridium difficile infection and symptoms, traveler's diarrhea, small intestinal bacterial overgrowth (SIBO), Crohn's disease, sickle cell disease, diverticular disease, pancreatitis, pancreatic insufficiency, enteritis, colitis, antibiotic-associated colitis, hepatic encephalopathy, gastric dyspepsia, cirrhosis, polycystic liver disease, cystitis, peritonitis, short bowel syndrome, inflammatory bowel disease, rosacea, H. pylori infection, Parkinson's disease, Alzheimer's disease, autism, and acute myeloid leukemia.
19. The pharmaceutical composition according to claim 17 or 18, wherein one or more disorders are selected from Clostridium difficile-associated diarrhea, chronic pancreatitis, ulcerative colitis, microscopic colitis, alcoholic cirrhosis, and atherosclerotic cardiovascular disease.