JP2021512876A - 抗ムスカリン薬又は抗コリン作動薬及びリポ酸の組合せ物並びにその使用 - Google Patents
抗ムスカリン薬又は抗コリン作動薬及びリポ酸の組合せ物並びにその使用 Download PDFInfo
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- JP2021512876A JP2021512876A JP2020542141A JP2020542141A JP2021512876A JP 2021512876 A JP2021512876 A JP 2021512876A JP 2020542141 A JP2020542141 A JP 2020542141A JP 2020542141 A JP2020542141 A JP 2020542141A JP 2021512876 A JP2021512876 A JP 2021512876A
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- Prior art keywords
- acid
- formula
- compound
- lipoic
- pharmaceutically acceptable
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- 235000019136 lipoic acid Nutrition 0.000 title claims abstract description 151
- 229960002663 thioctic acid Drugs 0.000 title claims abstract description 100
- 230000001022 anti-muscarinic effect Effects 0.000 title claims abstract description 57
- AGBQKNBQESQNJD-UHFFFAOYSA-M lipoate Chemical compound [O-]C(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-M 0.000 title abstract 4
- 239000003814 drug Substances 0.000 title description 48
- 229940079593 drug Drugs 0.000 title description 37
- 230000001078 anti-cholinergic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 230
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 137
- 150000003839 salts Chemical class 0.000 claims abstract description 103
- 239000006069 physical mixture Substances 0.000 claims abstract description 93
- 239000000812 cholinergic antagonist Substances 0.000 claims abstract description 66
- 239000003149 muscarinic antagonist Substances 0.000 claims abstract description 65
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims abstract description 58
- 239000000203 mixture Substances 0.000 claims description 266
- 239000002253 acid Substances 0.000 claims description 187
- AGBQKNBQESQNJD-UHFFFAOYSA-N lipoic acid Chemical compound OC(=O)CCCCC1CCSS1 AGBQKNBQESQNJD-UHFFFAOYSA-N 0.000 claims description 114
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims description 90
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 claims description 72
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 claims description 72
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims description 72
- 238000011282 treatment Methods 0.000 claims description 59
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 58
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 57
- 238000000034 method Methods 0.000 claims description 57
- AGBQKNBQESQNJD-SSDOTTSWSA-N (R)-lipoic acid Chemical compound OC(=O)CCCC[C@@H]1CCSS1 AGBQKNBQESQNJD-SSDOTTSWSA-N 0.000 claims description 55
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 54
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 54
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- 239000000651 prodrug Substances 0.000 claims description 48
- -1 undecylene Chemical group 0.000 claims description 45
- 206010013781 dry mouth Diseases 0.000 claims description 44
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 38
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 38
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims description 38
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 38
- 235000021355 Stearic acid Nutrition 0.000 claims description 37
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 37
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 37
- 239000008117 stearic acid Substances 0.000 claims description 37
- YWWVWXASSLXJHU-AATRIKPKSA-N (9E)-tetradecenoic acid Chemical compound CCCC\C=C\CCCCCCCC(O)=O YWWVWXASSLXJHU-AATRIKPKSA-N 0.000 claims description 36
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 claims description 36
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 claims description 36
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- 239000005639 Lauric acid Substances 0.000 claims description 36
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- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 36
- 235000021314 Palmitic acid Nutrition 0.000 claims description 36
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 36
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- YZXBAPSDXZZRGB-DOFZRALJSA-N arachidonic acid Chemical compound CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O YZXBAPSDXZZRGB-DOFZRALJSA-N 0.000 claims description 36
- JXTHNDFMNIQAHM-UHFFFAOYSA-N dichloroacetic acid Chemical compound OC(=O)C(Cl)Cl JXTHNDFMNIQAHM-UHFFFAOYSA-N 0.000 claims description 36
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 36
- ZQPPMHVWECSIRJ-MDZDMXLPSA-N elaidic acid Chemical compound CCCCCCCC\C=C\CCCCCCCC(O)=O ZQPPMHVWECSIRJ-MDZDMXLPSA-N 0.000 claims description 36
- 239000010440 gypsum Substances 0.000 claims description 36
- 229910052602 gypsum Inorganic materials 0.000 claims description 36
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims description 36
- KQNPFQTWMSNSAP-UHFFFAOYSA-N isobutyric acid Chemical compound CC(C)C(O)=O KQNPFQTWMSNSAP-UHFFFAOYSA-N 0.000 claims description 36
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 36
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims description 36
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 claims description 36
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims description 36
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid Chemical compound OC(=O)CCCCCCCCC(O)=O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 claims description 36
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 36
- 208000005946 Xerostomia Diseases 0.000 claims description 34
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 30
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 30
- 208000030533 eye disease Diseases 0.000 claims description 30
- 229960002989 glutamic acid Drugs 0.000 claims description 30
- 235000013922 glutamic acid Nutrition 0.000 claims description 30
- 239000004220 glutamic acid Substances 0.000 claims description 30
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 26
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 25
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 25
- 239000001630 malic acid Substances 0.000 claims description 25
- 235000011090 malic acid Nutrition 0.000 claims description 25
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- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 24
- 229960005261 aspartic acid Drugs 0.000 claims description 24
- 150000002148 esters Chemical class 0.000 claims description 24
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 22
- RNAICSBVACLLGM-GNAZCLTHSA-N pilocarpine hydrochloride Chemical compound Cl.C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C RNAICSBVACLLGM-GNAZCLTHSA-N 0.000 claims description 21
- 229960002139 pilocarpine hydrochloride Drugs 0.000 claims description 21
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 21
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 claims description 20
- 239000005711 Benzoic acid Substances 0.000 claims description 19
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 19
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 19
- 229960000583 acetic acid Drugs 0.000 claims description 19
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- 235000010323 ascorbic acid Nutrition 0.000 claims description 19
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- 235000014655 lactic acid Nutrition 0.000 claims description 19
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 19
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- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 claims description 18
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 18
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- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 claims description 18
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- 239000007939 sustained release tablet Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- KKEYFWRCBNTPAC-UHFFFAOYSA-L terephthalate(2-) Chemical compound [O-]C(=O)C1=CC=C(C([O-])=O)C=C1 KKEYFWRCBNTPAC-UHFFFAOYSA-L 0.000 description 1
- 238000002076 thermal analysis method Methods 0.000 description 1
- 229930003799 tocopherol Natural products 0.000 description 1
- 239000011732 tocopherol Substances 0.000 description 1
- 235000019149 tocopherols Nutrition 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- VMPHSYLJUKZBJJ-UHFFFAOYSA-N trilaurin Chemical compound CCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCC)COC(=O)CCCCCCCCCCC VMPHSYLJUKZBJJ-UHFFFAOYSA-N 0.000 description 1
- 235000019871 vegetable fat Nutrition 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 229920003169 water-soluble polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
- QUEDXNHFTDJVIY-UHFFFAOYSA-N γ-tocopherol Chemical class OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-UHFFFAOYSA-N 0.000 description 1
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- A—HUMAN NECESSITIES
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Abstract
【選択図】なし
Description
本出願は、2018年2月5日出願のインド仮特許出願第201841004306号及び2018年3月5日出願のインド仮特許出願第201841008091号の利益を主張するものであり、その開示全体があらゆる目的に依拠し、引用することにより本出願の一部をなす。
治療有効量の抗ムスカリン薬又は抗コリン作動薬又はそれらの薬学的に許容可能な塩又は立体異性体と、
治療有効量のリポ酸又はその薬学的に許容可能な塩又は立体異性体又はプロドラッグと、
を含む、医薬組成物を提供する。
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である。
(式中、RHは、H、ヨウ素、塩化物、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である。
本明細書において使用される以下の用語及び語句は、以下に記載の意味を有するものとする。他に定義されない限り、本明細書において使用される全ての技術用語及び科学用語は、当業者により通常理解されるものと同じ意味を有する。
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である。
(式中、RHは、H、塩化物、ヨウ素、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である。
DSC(2℃/分)、開始(℃)
装置:TA Q100又は同等物
試料調製:2.0mg〜5.0mgの試験試料を秤量し、アルミニウム製密閉パンに移して、蓋を閉めてクリンパーで密封した。それを試料区画内に把持する。
炉内温度プログラム:
2℃/分で30℃から150℃((R)−リポ酸ピロカルピン)
2℃/分で30℃から300℃(塩酸ピロカルピン及び(R)−リポ酸の物理的混合物)
装置:天秤、pH計及び100ml容のメスフラスコ
試料調製:1gの試験試料を秤量し、100ml容のメスフラスコに移し、容量を補うために50mlの水を加えた。試料のpHをpH計で確認した。
比旋光度(SOR)は、R−リポ酸及び塩酸ピロカルピンの物理的混合物の旋光度分析である。
装置:天秤、旋光計及び50mL容のメスフラスコ
手順:0.5gの試料を50ml容のメスフラスコ中に正確に秤量し、メタノールで溶解し、容量を補った。
1.きれいなスライドガラスに少量の顕微鏡用オイルを取り、少量の試料の粒子を加えた。十分に混合して均質な混合物を形成した。
2.気泡が形成しないようにカバースリップを混合物の上に静かに置いた。
3.準備したスライドをNikon社の偏光顕微鏡のステージ上に置き、適宜4倍及び10倍で顕微鏡写真を記録した。
4.試験の完了後に、準備したスライドを廃棄した。
解釈:
1.これらのバッチの結晶は異方性である。
2.結晶形態は不規則であった。
3.粒子サイズは均一ではなく、これは凝集を原因とし得る。
4.複屈折は、結晶の様々な空間に多色の斑点として現れた。
5.交差偏光の存在下で、黒色の背景に結晶が輝いているように見えたことから、材料の結晶性が確認された。
本出願は、2018年2月5日出願のインド仮特許出願第201841004306号及び2018年3月5日出願のインド仮特許出願第201841008091号の利益を主張するものであり、その開示全体があらゆる目的に依拠し、引用することにより本出願の一部をなす。
治療有効量の抗ムスカリン薬又は抗コリン作動薬又はそれらの薬学的に許容可能な塩又は立体異性体と、
治療有効量のリポ酸又はその薬学的に許容可能な塩又は立体異性体又はプロドラッグと、
を含む、医薬組成物を提供する。
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である。
(式中、RHは、H、ヨウ素、塩化物、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である。
本明細書において使用される以下の用語及び語句は、以下に記載の意味を有するものとする。他に定義されない限り、本明細書において使用される全ての技術用語及び科学用語は、当業者により通常理解されるものと同じ意味を有する。
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である。
(式中、RHは、H、塩化物、ヨウ素、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である。
DSC(2℃/分)、開始(℃)
装置:TA Q100又は同等物
試料調製:2.0mg〜5.0mgの試験試料を秤量し、アルミニウム製密閉パンに移して、蓋を閉めてクリンパーで密封した。それを試料区画内に把持する。
炉内温度プログラム:
2℃/分で30℃から150℃((R)−リポ酸ピロカルピン)
2℃/分で30℃から300℃(塩酸ピロカルピン及び(R)−リポ酸の物理的混合物)
装置:天秤、pH計及び100ml容のメスフラスコ
試料調製:1gの試験試料を秤量し、100ml容のメスフラスコに移し、容量を補うために50mlの水を加えた。試料のpHをpH計で確認した。
比旋光度(SOR)は、R−リポ酸及び塩酸ピロカルピンの物理的混合物の旋光度分析である。
装置:天秤、旋光計及び50mL容のメスフラスコ
手順:0.5gの試料を50ml容のメスフラスコ中に正確に秤量し、メタノールで溶解し、容量を補った。
1.きれいなスライドガラスに少量の顕微鏡用オイルを取り、少量の試料の粒子を加えた。十分に混合して均質な混合物を形成した。
2.気泡が形成しないようにカバースリップを混合物の上に静かに置いた。
3.準備したスライドをNikon社の偏光顕微鏡のステージ上に置き、適宜4倍及び10倍で顕微鏡写真を記録した。
4.試験の完了後に、準備したスライドを廃棄した。
解釈:
1.これらのバッチの結晶は異方性である。
2.結晶形態は不規則であった。
3.粒子サイズは均一ではなく、これは凝集を原因とし得る。
4.複屈折は、結晶の様々な空間に多色の斑点として現れた。
5.交差偏光の存在下で、黒色の背景に結晶が輝いているように見えたことから、材料の結晶性が確認された。
参照化合物 (R)−リポ酸プロドラッグ
両方のR−リポ酸プロドラッグ−(参照製剤)、ピロカルピン及び(R)−リポ酸(試験製剤)は、以下(表4 試験製剤、表5 参照製剤)に例示されるように製剤された:
パイロットスタディ:
さまざまな時点での(R)−リポ酸とピロカルピンの濃度、および房水中の薬物動態プロファイルを以下の表にまとめる。
・ピロカルピン:試験製剤で処理された動物の房水中のピロカルピンの濃度は、0.5時間で高く、1時間で減少することが観察された。
様々な時点での濃度および房水中の(R)−リポ酸の薬物動態プロファイルを以下に要約する。
・房水における(R)−リポ酸の濃度は、0.5時間でより高くなり、これらの濃度は、試験製剤および参照製剤で処理された動物では1時間で減少した。
・房水中の(R)−リポ酸の濃度は、試験製剤で処理された動物で2〜4時間まで検出可能であった。しかし、これらの濃度は、参照製剤で処理された動物のグループで1時間までしか検出できなかった。
・房水中のピロカルピンの濃度は、試験製剤で処理された動物で4時間まで検出可能であった。
Claims (21)
- a)治療有効量の抗ムスカリン薬又は抗コリン作動薬又はそれらの薬学的に許容可能な塩又は立体異性体と、
b)治療有効量のリポ酸又はその薬学的に許容可能な塩又は立体異性体又はプロドラッグと、
を含む、医薬組成物。 - 前記抗ムスカリン薬又は抗コリン作動薬は、
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
から選択される、請求項1に記載の医薬組成物。 - 前記リポ酸は、式IV:
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である、又は、
前記リポ酸のプロドラッグは、式V:
(式中、RHは、H、塩化物、ヨウ素、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である、請求項1に記載の医薬組成物。 - 前記抗ムスカリン薬又は抗コリン作動薬又はそれらの薬学的に許容可能な塩又は立体異性体は、0.1mg〜200mgの治療的有効用量範囲で存在する、請求項1に記載の医薬組成物。
- 前記リポ酸又はそれらの薬学的に許容可能な塩又は立体異性体は、10mg〜2gの用量で存在する、請求項1に記載の医薬組成物。
- 前記化合物の前記有効用量は、約0.01mg/kg(体重)/日〜約100mg/kg(体重)/日の範囲である、請求項1に記載の医薬組成物。
- 治療有効量の抗ムスカリン薬又は抗コリン作動薬又はそれらの薬学的に許容可能な塩又は立体異性体と、治療有効量のリポ酸又はその薬学的に許容可能な塩又は立体異性体又はプロドラッグとを含む物理的混合物。
- 前記抗ムスカリン薬又は抗コリン作動薬は、
式I:
(式中、RHは、
式II:
(式中、RHは、
式III:
(式中、RHは、
から選択される、請求項7に記載の物理的混合物。 - 前記リポ酸は、式IV:
(式中、RHは、なし、H、ナトリウム、カリウム、マグネシウム、カルシウム、アルギニン、グルタミン酸、リジン、グリシン、プロリン、ピリドキシン、ピリドキサミン、コリン、タウリン、リンゴ酸、PHMB、ポリヘキサニド又はグアニジンである)の化合物又はその薬学的に許容可能な塩又は立体異性体である、又は、
前記リポ酸のプロドラッグは、式V:
(式中、RHは、H、塩化物、ヨウ素、グルタミン酸、アスパラギン酸、リジン、ケトロラク、ケトプロフェン、ナプロキセン、臭素、ジクロフェナク、ネパフェナク、ブロムフェナク又はグリシンである)のコリンエステルプロドラッグ化合物又はその薬学的に許容可能な塩又は立体異性体である、請求項7に記載の物理的混合物。 - 式Iの化合物と、式IV又は式Vの化合物とを含む、請求項7に記載の物理的混合物。
- 式IIの化合物と、式IV又は式Vの化合物とを含む、請求項7に記載の物理的混合物。
- 式IIIの化合物と、式IV又は式Vの化合物とを含む、請求項7に記載の物理的混合物。
- 前記式Iの化合物は塩酸ピロカルピンであり、前記式IVの化合物はR−(+)−リポ酸である、請求項10に記載の物理的混合物。
- 式Iの化合物及び式IVの化合物又はそれらの物理的混合物を含む医薬組成物。
- 前記式Iの化合物は0.01mg〜200mgの治療的有効用量範囲で存在し、前記式IVの化合物は5mg〜4gの治療的有効用量範囲で存在する、請求項15に記載の医薬組成物。
- 前記式Iの化合物は塩酸ピロカルピンであり、前記式IVの化合物はR−(+)−リポ酸である、又はそれらの物理的混合物である、請求項14に記載の医薬組成物。
- 少なくとも1種の薬学的に許容可能な賦形剤を更に含む、請求項1〜6又は請求項14〜16のいずれか一項に記載の医薬組成物。
- 前記組成物は、経口投与、経鼻投与、皮膚投与、眼内投与、局所投与、直腸投与、経膣投与、エアロゾル投与又は非経口投与用に製剤化されている、請求項17に記載の組成物。
- 前記組成物は、口腔乾燥症及び口腔内灼熱症候群又はそれらの合併症の処置用である、請求項18に記載の組成物。
- 前記組成物は、老眼、緑内障及びその関連する状態からなる群より選択される眼疾患又は眼障害の処置用である、請求項18に記載の組成物。
- 処置を必要とする被験体における口腔乾燥症及びその合併症を処置する方法であって、前記被験体に、治療有効量の請求項1〜6又は請求項14〜20のいずれか一項に記載の組成物を投与することを含む、方法。
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