JP2023036678A5 - - Google Patents

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Publication number

JP2023036678A5

JP2023036678A5 JP2022197348A JP2022197348A JP2023036678A5 JP 2023036678 A5 JP2023036678 A5 JP 2023036678A5 JP 2022197348 A JP2022197348 A JP 2022197348A JP 2022197348 A JP2022197348 A JP 2022197348A JP 2023036678 A5 JP2023036678 A5 JP 2023036678A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

particles

carrier

lactose monohydrate

powder base

Prior art date

2022-12-09

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Pending

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• 239000008194 pharmaceutical composition Substances 0.000 claims 26
• 239000002245 particle Substances 0.000 claims 11
• WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 6
• 229960001021 lactose monohydrate Drugs 0.000 claims 6
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 5
• 229940079593 drug Drugs 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 229960001375 lactose Drugs 0.000 claims 5
• 239000008101 lactose Substances 0.000 claims 5
• 239000000203 mixture Substances 0.000 claims 5
• 239000000843 powder Substances 0.000 claims 5
• FBCDRHDULQYRTB-UHFFFAOYSA-N 2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1h-imidazo[5,1-f][1,2,4]triazin-4-one;trihydrate;hydrochloride Chemical compound O.O.O.Cl.CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 FBCDRHDULQYRTB-UHFFFAOYSA-N 0.000 claims 3
• 102000007637 Soluble Guanylyl Cyclase Human genes 0.000 claims 2
• 108010007205 Soluble Guanylyl Cyclase Proteins 0.000 claims 2
• 239000003795 chemical substances by application Substances 0.000 claims 2
• 238000009472 formulation Methods 0.000 claims 2
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
• 238000000034 method Methods 0.000 claims 2
• 229960001540 vardenafil hydrochloride Drugs 0.000 claims 2
• 229940124549 vasodilator Drugs 0.000 claims 2
• 239000003071 vasodilator agent Substances 0.000 claims 2
• HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 claims 1
• IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims 1
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
• 102000008100 Human Serum Albumin Human genes 0.000 claims 1
• 108091006905 Human Serum Albumin Proteins 0.000 claims 1
• ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
• ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
• 229930195725 Mannitol Natural products 0.000 claims 1
• 108010039918 Polylysine Proteins 0.000 claims 1
• 229920002472 Starch Polymers 0.000 claims 1
• HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
• SECKRCOLJRRGGV-UHFFFAOYSA-N Vardenafil Chemical compound CCCC1=NC(C)=C(C(N=2)=O)N1NC=2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(CC)CC1 SECKRCOLJRRGGV-UHFFFAOYSA-N 0.000 claims 1
• HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
• CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
• 235000013539 calcium stearate Nutrition 0.000 claims 1
• 239000008116 calcium stearate Substances 0.000 claims 1
• 229940112141 dry powder inhaler Drugs 0.000 claims 1
• 235000010445 lecithin Nutrition 0.000 claims 1
• 229940067606 lecithin Drugs 0.000 claims 1
• 239000000787 lecithin Substances 0.000 claims 1
• 235000005772 leucine Nutrition 0.000 claims 1
• 150000002613 leucine derivatives Chemical class 0.000 claims 1
• 235000019359 magnesium stearate Nutrition 0.000 claims 1
• 239000000594 mannitol Substances 0.000 claims 1
• 235000010355 mannitol Nutrition 0.000 claims 1
• 229920000724 poly(L-arginine) polymer Polymers 0.000 claims 1
• 108010011110 polyarginine Proteins 0.000 claims 1
• 229920000656 polylysine Polymers 0.000 claims 1
• 208000002815 pulmonary hypertension Diseases 0.000 claims 1
• WXXSNCNJFUAIDG-UHFFFAOYSA-N riociguat Chemical group N1=C(N)C(N(C)C(=O)OC)=C(N)N=C1C(C1=CC=CN=C11)=NN1CC1=CC=CC=C1F WXXSNCNJFUAIDG-UHFFFAOYSA-N 0.000 claims 1
• 229960000529 riociguat Drugs 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 229940127296 soluble guanylate cyclase stimulator Drugs 0.000 claims 1
• 239000008107 starch Substances 0.000 claims 1
• 235000019698 starch Nutrition 0.000 claims 1
• 229960002381 vardenafil Drugs 0.000 claims 1
• 229960004573 vardenafil hydrochloride trihydrate Drugs 0.000 claims 1