JP6083770B2 - 水溶液製剤及びその製造方法 - Google Patents
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Description
本発明は、化合物(I)を含有する水溶液製剤及びその製造方法を提供することを目的とする。
[1] 有機溶媒に下式(I)で表される化合物又は薬理学的に許容されるその塩、及び下記の一般式(II)〜(IV)のいずれかで表される化合物を溶解した溶解液を調製する第1の工程と、前記溶解液から前記有機溶媒を取り除く第2の工程と、第2の工程によって得られた残留物に溶液を加えて前記残留物を溶解する第3の工程を含み、一般式(II)中、nはポリエチレングリコールの平均ユニット数であり、14〜37の整数であり、一般式(III)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数であり、一般式(IV)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数であることを特徴とする水溶液製剤の製造方法;
[3] 一般式(III)で表される化合物のnが46である上記[1]に記載の水溶液製剤の製造方法;
[4] 一般式(IV)で表される化合物のnが46である上記[1]に記載の水溶液製剤の製造方法;
[5] 少なくとも1mg/mlの濃度で、前記の式(I)で表される化合物を含有し、前記の一般式(II)、一般式(III)又は一般式(IV)で表される化合物から選択されるいずれかを含有し、一般式(II)中、nはポリエチレングリコールの平均ユニット数であり、14〜37の整数であり、一般式(III)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数であり、一般式(IV)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数である、水溶液製剤などである。
なお、本発明の目的、特徴、利点、及びそのアイデアは、本明細書の記載により、当業者には明らかであり、当業者であれば本明細書の記載から容易に本発明を再現できる。以下に記載された発明の実施の形態及び具体的な実施例などは、本発明の好ましい実施態様を示すものであり、例示又は説明のために示されているものであって、本発明をそれらに限定するものではない。本明細書で開示されている本発明の意図並びに範囲内で、本明細書の記載に基づき、様々な改変並びに修飾ができることは、当業者にとって明らかである。
バイアルに、薬剤[化合物(I)]と下表に示される化合物とエタノールを加えて55〜60℃に加温し、薬剤及び化合物をエタノールに完全に(析出物及び沈殿物が生じることなく、無色透明に)溶解させ、各溶解溶液を調製した。各溶解溶液を60℃で1.5時間加温し、内容物を蒸発乾固させた。得られた残渣に生理食塩水又は水を所定量加えて55℃に加温し(実施例6では室温にて24時間インキュベーションした。実施例7では4℃で72時間インキュベーションした。)、溶解させた。バイアル内の水溶液をそれぞれ目視したところ、水溶液は析出物及び沈殿物がなく、無色澄明であったことから、薬剤が完全に溶解し、少なくとも1mg/mlの濃度で化合物(I)を含有する水溶液をそれぞれ調製できることが確認できた。なお、下表に示される化合物以外の化合物を用いて、1mg/mlの濃度で化合物(I)を含有する水溶液を調製することを試みたが、下表に示される化合物以外では、薬剤が完全に溶解した水溶液を調製できなかった。
実施例1で得られた水溶液をMillex(登録商標)-GV(0.22μm; 日本ミリポア株式会社/メルクミリポア)で濾過、滅菌し、雌雄Sprague-Daweley系IGSラット(6週齢)に静脈内投与し、化合物(I)の動態を調べた。
動物群は、雌雄Sprague-Daweley系IGSラット(チャールズリバージャパン)を用いた。前記ラットは6週齢であり、体重は、雄が166〜189g、雌が123〜145gであった。
前記ラットをSPF(Specific pathogen free)動物実験室で7日間検疫、馴化し、同時に健康状態を観察した。ラットは、滅菌済ステンレス製ゲージ内で、各ゲージに1匹ずつ飼育した。SPF動物実験室内は、室内温度を20.6〜22.5℃に、相対湿度を44〜60%に維持した。SPF動物実験室内の換気は、1時間あたり15回実施した。SPF動物実験室内の照明は、12時間ごとに明るい状態と暗い状態に切り替えた。
前記の検疫済ラットを体重によってランダムに、下記の3群(1群あたり雌雄各4匹)に群分けした。
(1) グループ1:実施例1で得られた水溶液を1mL/kg投与する群
(2) グループ2:実施例1で得られた水溶液を2mL/kg投与する群
(3) グループ3:実施例1で得られた水溶液を3mL/kg投与する群
前記検疫済ラットを一夜(約16時間)空腹にした後、実施例1で得られた水溶液を静脈内投与し、投与から0.083時間、0.25時間、0.5時間、1時間、4時間、及び24時間後に血液を採取し、化合物(I)の血中濃度を測定した。測定した各採取時間における化合物(I)の血中濃度から、注射用組成物を静脈内投与した直後の最大血中濃度C0(ng/mL)、及び投与後0〜24時間における化合物(I)の血中濃度曲線下面積AUC0-24(ng・h/mL)を算出した。
Claims (5)
- 有機溶媒に下式(I)で表される化合物又は薬理学的に許容されるその塩、及び下記の一般式(II)〜(IV)のいずれかで表される化合物を溶解した溶解液を調製する第1の工程と、前記溶解液から前記有機溶媒を取り除く第2の工程と、第2の工程によって得られた残留物に溶液を加えて前記残留物を溶解する第3の工程を含み、一般式(II)中、nはポリエチレングリコールの平均ユニット数であり、14〜37の整数であり、一般式(III)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数であり、一般式(IV)中、nはポリエチレングリコールの平均ユニット数であり、22〜46の整数であることを特徴とする水溶液製剤の製造方法。
- 一般式(II)で表される化合物のnが14又は37である請求項1に記載の水溶液製剤の製造方法。
- 一般式(III)で表される化合物のnが46である請求項1に記載の水溶液製剤の製造方法。
- 一般式(IV)で表される化合物のnが46である請求項1に記載の水溶液製剤の製造方法。
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