JP2021523183A - 非ヒト哺乳動物における鉄欠乏症を制御するための獣医用組成物およびその使用 - Google Patents
非ヒト哺乳動物における鉄欠乏症を制御するための獣医用組成物およびその使用 Download PDFInfo
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- JP2021523183A JP2021523183A JP2020563763A JP2020563763A JP2021523183A JP 2021523183 A JP2021523183 A JP 2021523183A JP 2020563763 A JP2020563763 A JP 2020563763A JP 2020563763 A JP2020563763 A JP 2020563763A JP 2021523183 A JP2021523183 A JP 2021523183A
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- Prior art keywords
- iron
- veterinary composition
- complex
- sodium
- concentration
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- 206010022971 Iron Deficiencies Diseases 0.000 title claims abstract description 28
- 150000004698 iron complex Chemical class 0.000 claims abstract description 32
- 208000007502 anemia Diseases 0.000 claims abstract description 25
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract description 25
- 239000004480 active ingredient Substances 0.000 claims abstract description 18
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- -1 glycerol formal Chemical compound 0.000 claims description 46
- 229910052742 iron Inorganic materials 0.000 claims description 30
- 235000002639 sodium chloride Nutrition 0.000 claims description 29
- 239000004094 surface-active agent Substances 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 23
- 238000002347 injection Methods 0.000 claims description 18
- 239000007924 injection Substances 0.000 claims description 18
- VTLYFUHAOXGGBS-UHFFFAOYSA-N Fe3+ Chemical compound [Fe+3] VTLYFUHAOXGGBS-UHFFFAOYSA-N 0.000 claims description 16
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 15
- 229920002307 Dextran Polymers 0.000 claims description 13
- 239000003960 organic solvent Substances 0.000 claims description 13
- 229920001282 polysaccharide Polymers 0.000 claims description 13
- 239000005017 polysaccharide Substances 0.000 claims description 13
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 12
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- 238000010255 intramuscular injection Methods 0.000 claims description 7
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- WSHYKIAQCMIPTB-UHFFFAOYSA-M potassium;2-oxo-3-(3-oxo-1-phenylbutyl)chromen-4-olate Chemical compound [K+].[O-]C=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 WSHYKIAQCMIPTB-UHFFFAOYSA-M 0.000 claims description 7
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
- 241000283690 Bos taurus Species 0.000 claims description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 6
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 6
- 241001494479 Pecora Species 0.000 claims description 6
- 239000011734 sodium Substances 0.000 claims description 6
- 229910052708 sodium Inorganic materials 0.000 claims description 6
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- 241000282326 Felis catus Species 0.000 claims description 5
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- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
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- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 claims description 4
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- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 4
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 4
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 4
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- OKPYIWASQZGASP-UHFFFAOYSA-N n-(2-hydroxypropyl)-2-methylprop-2-enamide Chemical compound CC(O)CNC(=O)C(C)=C OKPYIWASQZGASP-UHFFFAOYSA-N 0.000 claims description 3
- 150000003904 phospholipids Chemical class 0.000 claims description 3
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- AEQDJSLRWYMAQI-UHFFFAOYSA-N 2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline Chemical compound C1CN2CC(C(=C(OC)C=C3)OC)=C3CC2C2=C1C=C(OC)C(OC)=C2 AEQDJSLRWYMAQI-UHFFFAOYSA-N 0.000 claims description 2
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 claims description 2
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- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 claims description 2
- ATRRKUHOCOJYRX-UHFFFAOYSA-N Ammonium bicarbonate Chemical compound [NH4+].OC([O-])=O ATRRKUHOCOJYRX-UHFFFAOYSA-N 0.000 claims description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 claims description 2
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 claims description 2
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- HLCFGWHYROZGBI-JJKGCWMISA-M Potassium gluconate Chemical compound [K+].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O HLCFGWHYROZGBI-JJKGCWMISA-M 0.000 claims description 2
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 2
- 239000001099 ammonium carbonate Substances 0.000 claims description 2
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- NEEHYRZPVYRGPP-UHFFFAOYSA-L calcium;2,3,4,5,6-pentahydroxyhexanoate Chemical compound [Ca+2].OCC(O)C(O)C(O)C(O)C([O-])=O.OCC(O)C(O)C(O)C(O)C([O-])=O NEEHYRZPVYRGPP-UHFFFAOYSA-L 0.000 claims description 2
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- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 claims description 2
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Abstract
Description
およびAnaemex(登録商標)の商標の下で商品化されている。Ceva Sante Animale、SerumWerk、およびLabianaは、ベータ−オキシ水酸化第二鉄およびデキストラングルコヘプトン酸のコロイド水溶液(Gleptosil(登録商標)、Ursoferran(登録商標)、およびGleptoferron 200 Labianaの商標の下で商品化されているGleptoferron)を含む注射用溶液を提供する。
したがって、本発明は、唯一の有効成分としての鉄錯体と水溶性ポリマーとを含む獣医用組成物を提供する。
−50〜300mg/mL、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの、本明細書に開示される唯一の有効成分としての鉄錯体として供給される鉄元素の濃度と、
−1〜100mg/mL、好ましくは5〜70mg/mL、好ましくは7〜60mg/mL、より好ましくは10〜50mg/mLの本明細書に開示される水溶性ポリマーの濃度と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される約133.4mg/mLの鉄元素の濃度と、
−約10または50mg/mLのポリビニルピロリドンの濃度と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される50〜300mg/mL、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの濃度の鉄元素と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、好ましくは7〜60mg/mL、より好ましくは10〜50mg/mLの濃度の水溶性ポリマーと、
−本明細書に開示される1〜20mg/mL、好ましくは5〜10mg/mL、より好ましくは5〜8mg/mLの濃度の有機溶媒と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される約133.4mg/mLの濃度の鉄元素と、
−約10または50mg/mLの濃度のポリビニルピロリドンと、
−約6.4mg/mLの濃度のフェノールと、を含む獣医用組成物である。
本発明の獣医学的組成物は、薬学的に許容される塩および/または界面活性剤、特に、8を超えるHLBを有する界面活性剤などの少なくとも1つの賦形剤をさらに含み得る。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される50〜300mg/mL、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの濃度の鉄元素と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、好ましくは7〜60mg/mL、より好ましくは10〜50mg/mLの濃度の水溶性ポリマーと、
−本明細書に開示される1〜20mg/mL、好ましくは5〜10mg/mL、より好ましくは5〜8mg/mLの濃度の有機溶媒と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、より好ましくは10〜50mg/mLの濃度の薬学的に許容される塩と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される約133.4mg/mLの濃度の鉄元素と、
−約10または50mg/mLの濃度のポリビニルピロリドンと、
−約6.4mg/mLの濃度のフェノールと、
−約10または50mg/mLの濃度の塩化ナトリウムと、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される50〜300mg/mL、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの濃度の鉄元素と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、好ましくは7〜60mg/mL、より好ましくは10〜50mg/mLの濃度の水溶性ポリマーと、
−本明細書に開示される1〜20mg/mL、好ましくは5〜10mg/mL、より好ましくは5〜8mg/mLの濃度の有機溶媒と、
−本明細書に開示される8を超えるHLBを有する0.01〜10mg/mL、好ましくは0.5〜8mg/mL、より好ましくは1〜5mg/mLの濃度の界面活性剤と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される約133.4mg/mLの濃度の鉄元素と、
−約10または50mg/mLの濃度のポリビニルピロリドンと、
−約6.4mg/mLの濃度のフェノールと、
−約1または5mg/mLの濃度のドクサートナトリウムと、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される50〜300mg/mL、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの濃度の鉄元素と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、好ましくは7〜60mg/mL、より好ましくは10〜50mg/mLの濃度の水溶性ポリマーと、
−本明細書に開示される1〜20mg/mL、好ましくは5〜10mg/mL、より好ましくは5〜8mg/mLの濃度の有機溶媒と、
−本明細書に開示される1〜100mg/mL、好ましくは5〜70mg/mL、より好ましくは10〜50mg/mLの濃度の薬学的に許容される塩と、
−本明細書に開示される8を超えるHLBを有する0.01〜10mg/mL、好ましくは0.5〜8mg/mL、より好ましくは1〜5mg/mLの濃度の界面活性剤と、を含む獣医用組成物である。
−本明細書に開示される唯一の有効成分としての鉄錯体として供給される約133.4mg/mLの濃度の鉄元素と、
−約10または50mg/mLの濃度のポリビニルピロリドンと、
−約6.4mg/mLの濃度のフェノールと、
−約10または50mg/mLの濃度の塩化ナトリウムと、
−約1または5mg/mLの濃度のドクサートナトリウムと、を含む獣医用組成物である。
本明細書に開示される本発明の組成物は、特に鉄欠乏症および貧血に罹患する任意の非ヒト哺乳動物の予防および/または治療に使用され得る。
Claims (16)
- 唯一の有効成分としての鉄錯体と水溶性ポリマーとを含む獣医用組成物。
- 前記水溶性ポリマーが、ポリビニルピロリドン、ポリビニルアルコール、ポリアクリル酸、ポリアクリルアミド、N−(2−ヒドロキシプロピル)メタクリルアミド、ジビニルエーテル−マレイン酸無水物、ポリオキサゾリン、ポリリン酸塩、ポリホスファゼン、およびそれらの混合物の中から選択され、好ましくは、ポリビニルピロリドンである、請求項1に記載の獣医用組成物。
- 前記水溶性ポリマーが、1〜100mg/mL、好ましくは5〜70mg/mL、より好ましくは7〜60mg/mL、さらにより好ましくは10〜50mg/mLの濃度である、請求項1または2に記載の獣医用組成物。
- 好ましくは、メタノール、エタノール、ブタノール、エチレングリコール、ポリエチレングリコール、プロピレングリコール、ポリプロピレングリコール、グリセロール、フェノール、ベンジルアルコール、フェニルエタノール、フェノキシエタノール、酢酸エチル、酢酸ブチル安息香酸ベンジル、オレイン酸エチル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノブチルエーテル、ジプロピレングリコールモノメチルエーテル、アセトン、メチルエチルケトン、グリセロールフォーマル、2,2−ジメチル−4−ヒドロキシメチル−1,3−ジオキソラン、N−メチル−ピロリドン、2−ピロリドン、N,N−ジメチルアセトアミド、グリコフルロール、ジメチル−イソソルビトール、ラウログリコール、炭酸プロピレン、オクチルドデカノール、ジメチルホルムアミド、およびそれらの混合物の中から選択される有機溶媒、より好ましくは、フェノールをさらに含む、請求項1〜3のいずれか一項に記載の獣医用組成物。
- 前記有機溶媒が、1〜20mg/mL、好ましくは5〜10mg/mL、より好ましくは5〜8mg/mLの濃度である、請求項4に記載の獣医用組成物。
- 薬学的に許容される塩および/または8を超えるHLBを有する界面活性剤をさらに含む、請求項1〜5のいずれか一項に記載の獣医用組成物。
- 前記薬学的に許容される塩が、グルコン酸カルシウム、リン酸カルシウム、塩化カルシウム、硫酸カルシウム、炭酸カルシウム、グルコン酸マグネシウム、リン酸マグネシウム、塩化マグネシウム、硫酸マグネシウム、炭酸マグネシウム、リン酸カリウム、グルコン酸カリウム、塩化カリウム、硫酸カリウム、炭酸カリウム、グルコン酸ナトリウム、塩化ナトリウム、炭酸ナトリウム、乳酸ナトリウム、プロピオン酸ナトリウム、リン酸ナトリウム、クエン酸ナトリウム、硫酸ナトリウム、塩化アンモニウム、および炭酸アンモニウム、ならびにそれらの混合物の中から選択され、好ましくは、塩化ナトリウムである、請求項6に記載の獣医用組成物。
- 前記薬学的に許容される塩が、1〜100mg/mL、好ましくは5〜70mg/mL、より好ましくは10〜50mg/mLの濃度である、請求項6または7に記載の獣医用組成物。
- 前記8を超えるHLBを有する界面活性剤が、ポリエチレンヒマシ油、ポリオキシエチレンアルキルエーテル、ポリオキシエチレンソルビタン脂肪酸エステル、ステアリン酸ポリオキシエチレン、ラウリル硫酸ナトリウム、ドクサートナトリウム、セトリミド、リン脂質、塩化セチルピリジニウム、およびそれらの混合物の中から選択され、好ましくは、ドクサートナトリウムである、請求項6に記載の獣医用組成物。
- 前記8を超えるHLBを有する界面活性剤が、0.01〜10mg/mL、好ましくは0.5〜8mg/mL、より好ましくは1〜5mg/mLの濃度である、請求項6または9に記載の獣医用組成物。
- 前記鉄錯体が、鉄(2+)カルボン酸錯体、鉄(3+)カルボン酸錯体、アミノ酸との鉄(2+)キレート錯体、アミノ酸との鉄(3+)キレート錯体、多核鉄(3+)多糖類錯体、およびそれらの混合物の中から選択される、請求項1〜10のいずれか一項に記載の獣医用組成物。
- 前記多核鉄(3+)多糖錯体が、ベータ−オキシ水酸化第二鉄およびデキストラングルコヘプトン酸、鉄(III)デキストラン、鉄(III)ヒドロキシポリマルトースの水性コロイド溶液の中から選択され、好ましくは、ベータ−オキシ水酸化第二鉄およびデキストラングルコヘプトン酸の水性コロイド溶液である、請求項11に記載の獣医用組成物。
- 鉄錯体として供給される鉄の濃度が、50〜300mg/mLの鉄元素、好ましくは100〜200mg/mL、より好ましくは120〜150mg/mLの濃度である、請求項1〜12のいずれか一項に記載の獣医用組成物。
- 非ヒト哺乳動物における鉄欠乏症および/または貧血状態を制御するための使用のための、請求項1〜13のいずれか一項に定義されるような獣医用組成物。
- 前記非ヒト哺乳動物が、ブタ、ヒツジ、ウシ、イヌ、またはネコ、好ましくは仔ブタである、請求項15に記載の使用のための獣医用組成物。
- 前記組成物が、注射によって、好ましくは筋肉内注射によって投与される、請求項13〜15のいずれか一項に記載の使用のための獣医用組成物。
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PCT/EP2019/062700 WO2019219855A1 (en) | 2018-05-16 | 2019-05-16 | Veterinary compositions and the uses thereof for controlling iron deficiencies in non-human mammals |
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CA3099827A1 (en) | 2019-11-21 |
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PH12020551926A1 (en) | 2021-06-14 |
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CL2020002956A1 (es) | 2021-04-30 |
AU2019270428A1 (en) | 2020-11-26 |
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WO2019219855A1 (en) | 2019-11-21 |
US20210220319A1 (en) | 2021-07-22 |
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