JP2021506971A - イソキサゾリン系寄生虫駆除剤及び眼瞼炎を治療する方法 - Google Patents
イソキサゾリン系寄生虫駆除剤及び眼瞼炎を治療する方法 Download PDFInfo
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- 239000007940 sugar coated tablet Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000002344 surface layer Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000271 synthetic detergent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
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- 238000007910 systemic administration Methods 0.000 description 1
- 229960001685 tacrine Drugs 0.000 description 1
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 description 1
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- 238000012360 testing method Methods 0.000 description 1
- 239000004308 thiabendazole Substances 0.000 description 1
- WJCNZQLZVWNLKY-UHFFFAOYSA-N thiabendazole Chemical compound S1C=NC(C=2NC3=CC=CC=C3N=2)=C1 WJCNZQLZVWNLKY-UHFFFAOYSA-N 0.000 description 1
- 229960004546 thiabendazole Drugs 0.000 description 1
- 235000010296 thiabendazole Nutrition 0.000 description 1
- NWWZPOKUUAIXIW-FLIBITNWSA-N thiamethoxam Chemical compound [O-][N+](=O)\N=C/1N(C)COCN\1CC1=CN=C(Cl)S1 NWWZPOKUUAIXIW-FLIBITNWSA-N 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 125000002640 tocopherol group Chemical group 0.000 description 1
- 239000012929 tonicity agent Substances 0.000 description 1
- 229940100611 topical cream Drugs 0.000 description 1
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- 229940100617 topical lotion Drugs 0.000 description 1
- 229940126702 topical medication Drugs 0.000 description 1
- 229960000323 triclabendazole Drugs 0.000 description 1
- JLEXUIVKURIPFI-UHFFFAOYSA-N tris phosphate Chemical group OP(O)(O)=O.OCC(N)(CO)CO JLEXUIVKURIPFI-UHFFFAOYSA-N 0.000 description 1
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- QUEDXNHFTDJVIY-DQCZWYHMSA-N γ-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1 QUEDXNHFTDJVIY-DQCZWYHMSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
Abstract
Description
Claims (62)
- 患者の眼瞼炎を治療する方法であって、
眼瞼炎の治療を必要とする患者の一方又は両方の眼の眼表面に対して直接、眼用組成物に製剤化した有効量のイソキサゾリン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記イソキサゾリン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記組成物の総重量に対して約0.01%〜約1%の前記イソキサゾリン系寄生虫駆除剤を投与する、ことを特徴とする請求項1に記載の方法。
- 前記組成物の総重量に対して約0.03重量%の前記イソキサゾリン系寄生虫駆除剤を投与する、ことを特徴とする請求項1に記載の方法。
- 前記組成物の総重量に対して約0.10重量%の前記イソキサゾリン系寄生虫駆除剤を投与する、ことを特徴とする請求項1に記載の方法。
- 前記眼用組成物は点眼剤である、ことを特徴とする請求項1に記載の方法。
- 前記眼用組成物は精油を含まない、ことを特徴とする請求項1に記載の方法。
- 前記イソキサゾリン系寄生虫駆除剤は、フルララネル、サロラネル、ロチラナー、アフォキソラネル及びフルキサメタミドからなる群から選択される、ことを特徴とする請求項1に記載の方法。
- 前記眼表面は、前記患者の一方又は両方の眼の結膜又は角膜の少なくとも一方を含む、ことを特徴とする請求項1に記載の方法。
- 前記眼用組成物はポリソルベートを含む、ことを特徴とする請求項1に記載の方法。
- 患者の眼瞼炎を治療する方法であって、
眼瞼炎の治療を必要とする患者の一方又は双方の眼、眼瞼又は一つ又は複数のまつ毛に対して直接、眼用組成物に製剤化した有効量のイソキサゾリン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記イソキサゾリン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記眼用組成物を局所的に投与する際、前記組成物が前記患者のマイボーム腺の開口及び前記患者の眼瞼辺縁の外側に接触するように前記患者の眼が閉じられる、ことを特徴とする請求項10に記載の方法。
- 前記まつ毛及び前記まつ毛の毛包に前記組成物を適用するステップをさらに含む、ことを特徴とする請求項11に記載の方法。
- アプリケータにより前記まつ毛及び前記まつ毛の毛包に前記組成物を適用するステップをさらに含む、ことを特徴とする請求項11に記載の方法。
- 前記組成物の総重量に対して約0.001%〜約1%の前記イソキサゾリン系寄生虫駆除剤を投与する、ことを特徴とする請求項10に記載の方法。
- 前記組成物の総重量に対して約0.001%〜約1%の前記イソキサゾリン系寄生虫駆除剤を投与する、ことを特徴とする請求項10に記載の方法。
- 少なくとも約2週間の間、少なくとも1日1回、前記眼用組成物を局所的に投与するステップを含む、ことを特徴とする請求項10に記載の方法。
- 少なくとも約4週間の間、少なくとも1日1回、前記眼用組成物を局所的に投与するステップを含む、ことを特徴とする請求項10に記載の方法。
- 患者のデモデックス眼部寄生を治療する方法であって、
デモデックス眼部寄生の治療を必要とする患者の一方又は双方の眼、一方又は双方の眼の眼瞼又はまつ毛に対して直接、眼用組成物に製剤化した有効量のイソキサゾリン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記イソキサゾリン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記患者の解剖学的構造におけるデモデックスダニの量について第1の評価を受けるステップと、
前記デモデックスダニの量が所定値よりも多い場合に、前記眼用組成物を局所的に投与するステップと、
をさらに含む、ことを特徴とする請求項18に記載の方法。 - 前記眼用製剤は、前記患者に寄生するデモデックスダニの頭胸部と比較して、前記デモデックスダニの腹部及び尾部の動きをより迅速に停止させる、ことを特徴とする請求項18に記載の方法。
- 眼瞼炎及び/又は酒さを治療する方法であって、
一つ又は複数のまつ毛の近傍にイソキサゾリン系寄生虫駆除剤を局所的に適用するステップを含み、
前記局所的に適用するステップは、デモデックスダニの頭部に対する当該デモデックスダニの胴体の動きの低下に十分な前記デモデックスダニによる摂取に関して前記デモデックスダニの胴体に優先的に吸収させるため治療的に有効であり、
前記まつ毛の近傍におけるデモデックスダニの減少又は排除に十分であり、眼瞼炎及び/又は酒さの症状を改善する、ことを特徴とする方法。 - 患者の眼瞼炎を治療するための局所眼用製剤であって、
有効量のイソキサゾリン系寄生虫駆除剤及び薬学的に許容された溶剤を含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記イソキサゾリン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする局所眼用製剤。 - 前記組成物の総重量に対して約0.01%〜約1%の前記イソキサゾリン系寄生虫駆除剤が投与される、ことを特徴とする請求項22に記載の局所眼用製剤。
- 前記組成物の総重量に対して約0.03重量%の前記イソキサゾリン系寄生虫駆除剤が投与される、ことを特徴とする請求項22に記載の局所眼用製剤。
- 前記組成物の総重量に対して約0.10重量%の前記イソキサゾリン系寄生虫駆除剤が投与される、ことを特徴とする請求項22に記載の局所眼用製剤。
- 前記眼用組成物は点眼剤である、ことを特徴とする請求項22に記載の局所眼用製剤。
- 前記眼用組成物は精油を含まない、ことを特徴とする請求項22に記載の局所眼用製剤。
- 前記イソキサゾリン系寄生虫駆除剤は、フルララネル、サロラネル、ロチラナー、アフォキソラネル及びフルキサメタミドからなる群から選択される、ことを特徴とする請求項22に記載の局所眼用製剤。
- 眼表面疾患の治療に使用するための局所製剤であって、
イソキサゾリン系寄生虫駆除剤と、
ペムレン及びHPMCの少なくとも一方と、
ポリソルベート80と、
グリセリンと、
緩衝剤と、
ラウラルコニウムクロリドと、
を含み、
まつ毛の近傍におけるデモデックスダニの減少又は排除に治療的に有効であり、眼瞼炎及び/又は酒さの症状を改善する、ことを特徴とする局所製剤。 - 眼瞼炎の治療に使用する、ことを特徴とする請求項29に記載の局所製剤。
- 前眼瞼炎の治療に使用する、ことを特徴とする請求項29に記載の局所製剤。
- 後眼瞼炎の治療に使用する、ことを特徴とする請求項29に記載の局所製剤。
- 眼性酒さの治療に使用する、ことを特徴とする請求項29に記載の局所製剤。
- 患者の眼瞼炎を治療する方法であって、
眼瞼炎の治療を必要とする患者の一方又は双方の眼の眼表面に対して直接、眼用組成物に製剤化した有効量のホルムアミジン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記ホルムアミジン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記組成物の総重量に対して約0.01%〜約1%の前記ホルムアミジン系寄生虫駆除剤を投与する、ことを特徴とする請求項34に記載の方法。
- 前記組成物の総重量に対して約0.03重量%の前記ホルムアミジン系寄生虫駆除剤を投与する、ことを特徴とする請求項34に記載の方法。
- 前記組成物の総重量に対して約0.10重量%の前記ホルムアミジン系寄生虫駆除剤を投与する、ことを特徴とする請求項34に記載の方法。
- 前記眼用組成物は点眼剤である、ことを特徴とする請求項34に記載の方法。
- 前記眼用組成物は軟膏又はクリームである、ことを特徴とする請求項34に記載の方法。
- 前記眼用組成物は精油を含まない、ことを特徴とする請求項34に記載の方法。
- 前記ホルムアミジン系寄生虫駆除剤は、アミトラズ、N−(2,4−ジメチルフェニル)−N−メチルホルムアミジン(DPMF)及び2,4−ジメチルアナリンからなる群から選択される、ことを特徴とする請求項34に記載の方法。
- 前記眼表面は、前記患者の一方又は両方の眼の結膜又は角膜の少なくとも一方を含む、ことを特徴とする請求項34に記載の方法。
- 前記眼用組成物はポリソルベートを含む、ことを特徴とする請求項34に記載の方法。
- 患者の眼瞼炎を治療する方法であって、
眼瞼炎の治療を必要とする患者の一方又は双方の眼、眼瞼又は一つ又は複数のまつ毛に対して直接、眼用組成物に製剤化した有効量のホルムアミジン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記ホルムアミジン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記眼用組成物を局所的に投与する際、前記組成物が前記患者のマイボーム腺の開口及び前記患者の眼瞼辺縁の外側に接触するように前記患者の眼が閉じられる、ことを特徴とする請求項44に記載の方法。
- 前記まつ毛及び前記まつ毛の毛包に前記組成物を適用するステップをさらに含む、ことを特徴とする請求項44に記載の方法。
- アプリケータにより前記まつ毛及び前記まつ毛の毛包に前記組成物を適用するステップをさらに含む、ことを特徴とする請求項44に記載の方法。
- 前記組成物の総重量に対して約0.001%〜約1%の前記ホルムアミジン系寄生虫駆除剤を投与する、ことを特徴とする請求項44に記載の方法。
- 前記組成物の総重量に対して約0.001%〜約1%の前記ホルムアミジン系寄生虫駆除剤を投与する、ことを特徴とする請求項44に記載の方法。
- 少なくとも約2週間の間、少なくとも1日1回、前記眼用組成物を局所的に投与するステップを含む、ことを特徴とする請求項44に記載の方法。
- 少なくとも約4週間の間、少なくとも1日1回、前記眼用組成物を局所的に投与するステップを含む、ことを特徴とする請求項44に記載の方法。
- 患者のデモデックス眼部寄生を治療する方法であって、
デモデックス眼部寄生の治療を必要とする患者の一方又は双方の眼、一方又は双方の眼の眼瞼又はまつ毛に対して直接、眼用組成物に製剤化した有効量のホルムアミジン系寄生虫駆除剤を局所的に投与するステップを含み、
前記眼用組成物は、薬学的に許容された溶剤をさらに含み、
前記眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記ホルムアミジン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする方法。 - 前記患者の解剖学的構造におけるデモデックスダニの量について第1の評価を受けるステップと、
前記デモデックスダニの量が所定値よりも多い場合に、前記眼用組成物を局所的に投与するステップと、
をさらに含む、ことを特徴とする請求項52に記載の方法。 - 前記眼用製剤は、前記患者に寄生するデモデックスダニの頭胸部と比較して、前記デモデックスダニの腹部及び尾部の動きをより迅速に停止させる、ことを特徴とする請求項52に記載の方法。
- 眼瞼炎及び/又は酒さを治療するための方法であって、
一つ又は複数のまつ毛の近傍にホルムアミジン系寄生虫駆除剤を局所的に適用するステップを含み、
前記局所的に適用するステップは、デモデックスダニの頭部に対する当該デモデックスダニの胴体の動きの低下に十分な前記デモデックスダニによる摂取に関して前記デモデックスダニの胴体に優先的に吸収させるため治療的に有効であり、
前記まつ毛の近傍における前記デモデックスダニの減少又は排除に十分であり、眼瞼炎及び/又は酒さの症状を改善する、ことを特徴とする方法。 - 患者の眼瞼炎を治療するための局所眼用製剤であって、
有効量のホルムアミジン系寄生虫駆除剤及び薬学的に許容された溶剤を含み、
眼用組成物は、無菌であり、眼に対して非刺激性であり、
前記ホルムアミジン系寄生虫駆除剤は、前記眼用組成物の唯一の有効成分である、ことを特徴とする局所眼用製剤。 - 前記組成物の総重量に対して約0.01%〜約1%の前記ホルムアミジン系寄生虫駆除剤が投与される、ことを特徴とする請求項56に記載の局所眼用製剤。
- 前記組成物の総重量に対して約0.03重量%の前記ホルムアミジン系寄生虫駆除剤が投与される、ことを特徴とする請求項56に記載の局所眼用製剤。
- 前記組成物の総重量に対して約0.10%重量%の前記ホルムアミジン系寄生虫駆除剤が投与される、ことを特徴とする請求項56に記載の局所眼用製剤。
- 前記眼用組成物は点眼剤、クリーム又は軟膏である、ことを特徴とする請求項56に記載の局所眼用製剤。
- 前記眼用組成物は精油を含まない、ことを特徴とする請求項56に記載の局所眼用製剤。
- 前記ホルムアミジン系寄生虫駆除剤は、アミトラズ、N−(2,4−ジメチルフェニル)−N−メチルホルムアミジン(DPMF)及び2,4−ジメチルアナリンからなる群から選択される、ことを特徴とする請求項56に記載の局所眼用製剤。
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EP3829569A4 (en) | 2018-07-27 | 2022-04-27 | Aperta Biosciences, LLC | SPINOSYN FORMULATIONS FOR THE TREATMENT OF DEMODEX-INDUCED EYE AND FACIAL DISORDERS |
AU2020251960A1 (en) | 2019-04-04 | 2021-11-11 | Tarsus Pharmaceuticals, Inc. | Systemic isoxazoline parasiticides for vector-borne and viral disease treatment or prophylaxis |
US20220249445A1 (en) | 2019-06-19 | 2022-08-11 | Tarsus Pharmaceuticals, Inc. | Isoxazoline parasiticide formulations and methods for treating blepharitis |
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