JP7091558B2 - 薬物がコーティングされたマイクロニードル及びその製造方法 - Google Patents
薬物がコーティングされたマイクロニードル及びその製造方法 Download PDFInfo
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Description
(b)薬物に、スルフヒドリル(Sulfhydryl、-SH)反応基を含むリンカーを結合させて、下記化学式2~8よりなる群から選択されるスルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物を製造するステップと、
(c)スルフヒドリル(Sulfhydryl、-SH)反応基を含むシリカ(SiO2)含有マイクロニードルと、スルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物とを酸化反応させるステップと、を含む、化学式1で表され、皮膚浸透後に酸化還元反応によって薬物が放出されることを特徴とする、薬物がコーティングされたマイクロニードルの製造方法である。
[化学式1]
MN-S-S-D
(式中、MNはシリカ(SiO2)含有マイクロニードルであり、S-Sはジスルフィド結合であり、Dは薬物である。)
[化学式2]:Lys-His-Gly-X
[化学式3]:Gly-His-Lys-X
[化学式4]:Ser-Lys-Thr-Thr-Lys-X
[化学式5]:Lys-Thr-Thr-Lys-Ser-X
[化学式6]:Arg-Arg-Gln-Met-Glu-Glu-X
[化学式7]:Glu-Glu-Met-Gln-Arg-Arg-X
[化学式8]:
(前記化学式2~8中、Xは、チオグリコール酸(Thioglycolic acid)及び11-メルカプトウンデカン酸(11-Mercaptoundecanoic acid)よりなる群から選択される1種以上である。)
化学式1で表され、皮膚浸透後に酸化還元反応によって薬物が放出されることを特徴とする、薬物がコーティングされたマイクロニードルである。
[化学式1]
MN-S-S-D
(式中、MNはシリカ(SiO2)含有マイクロニードルであり、S-Sはジスルフィド結合であり、Dは薬物である。)
[化学式2]:Lys-His-Gly-X
[化学式3]:Gly-His-Lys-X
[化学式4]:Ser-Lys-Thr-Thr-Lys-X
[化学式5]:Lys-Thr-Thr-Lys-Ser-X
[化学式6]:Arg-Arg-Gln-Met-Glu-Glu-X
[化学式7]:Glu-Glu-Met-Gln-Arg-Arg-X
[化学式8]:
(前記化学式2~8中、Xは、チオグリコール酸(Thioglycolic acid)及び11-メルカプトウンデカン酸(11-Mercaptoundecanoic acid)よりなる群から選択される1種以上である。)
Claims (9)
- (a)シリカ(SiO2)含有マイクロニードルの表面を改質して、スルフヒドリル(Sulfhydryl、-SH)反応基を含むシリカ(SiO2)含有マイクロニードルを製造するステップと、
(b)薬物に、スルフヒドリル(Sulfhydryl、-SH)反応基を含むリンカーを結合させて、下記化学式2~8よりなる群から選択されるスルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物を製造するステップと、
(c)スルフヒドリル(Sulfhydryl、-SH)反応基を含むシリカ(SiO2)含有マイクロニードルと、スルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物とを酸化反応させるステップと、を含む、化学式1で表され、皮膚浸透後に酸化還元反応によって薬物が放出されることを特徴とする、薬物がコーティングされたマイクロニードルの製造方法。
[化学式1]
MN-S-S-D
(式中、MNはシリカ(SiO2)含有マイクロニードルであり、S-Sはジスルフィド結合であり、Dは薬物である。)
[化学式2]:Lys-His-Gly-X
[化学式3]:Gly-His-Lys-X
[化学式4]:Ser-Lys-Thr-Thr-Lys-X
[化学式5]:Lys-Thr-Thr-Lys-Ser-X
[化学式6]:Arg-Arg-Gln-Met-Glu-Glu-X
[化学式7]:Glu-Glu-Met-Gln-Arg-Arg-X
[化学式8]:
(前記化学式2~8中、Xは、チオグリコール酸(Thioglycolic acid)及び11-メルカプトウンデカン酸(11-Mercaptoundecanoic acid)よりなる群から選択される1種以上である。) - 前記シリカ(SiO2)含有マイクロニードルが海綿動物由来の針状骨片であることを特徴とする、請求項1に記載の薬物がコーティングされたマイクロニードルの製造方法。
- 前記シリカ(SiO2)含有マイクロニードルの表面改質は、
シリカ(SiO2)含有マイクロニードルに、3-メルカプトプロピル-メチルジメトキシシラン((3-Mercaptopropyl)methyldimethoxysilane)、3-メルカプトプロピル-トリメトキシシラン)(3-Mercaptopropyl)trimethoxysilane)、N-[3-(トリメトキシシリル)プロピル]エチレンジアミン(N-[3-(Trimethoxysilyl)propyl]ethylenediamine)、チオグリコール酸(Thioglycolic acid、3-Mercaptopropionic acid)、11-メルカプトウンデカン酸(11-Mercaptoundecanoic acid)及び3,3’-ジチオジプロピオン酸(3,3’-Dithiodipropionic acid)よりなる群から選択される1種を攪拌させることを特徴とする、請求項1に記載の薬物がコーティングされたマイクロニードルの製造方法。 - 前記スルフヒドリル(Sulfhydryl、-SH)反応基を含むシリカ(SiO2)含有マイクロニードルと、スルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物との酸化反応は、ヨウ素(Iodine)、リン酸カリウム(Potassium Phosphate)、2,3-ジクロロ-5,6-ジシアノ-p-ベンゾキノン(2,3-Dichloro-5,6-dicyano-p-benzoquinone、DDQ)、デヒドロアスコルビン酸(Dehydroascorbic acid)、過酸化水素(H2O2)、及び酸素(O2)よりなる群から選択される1種以上の酸化剤によって行われることを特徴とする、請求項1に記載の薬物がコーティングされたマイクロニードルの製造方法。
- スルフヒドリル(Sulfhydryl、-SH)反応基を含むシリカ(SiO 2 )含有マイクロニードルと、化学式2~8よりなる群から選択される1以上であるスルフヒドリル(Sulfhydryl、-SH)反応基を含む薬物との結合で製造され、
化学式1で表され、皮膚浸透後に酸化還元反応によって薬物が放出されることを特徴とする、薬物がコーティングされたマイクロニードル。
[化学式1]
MN-S-S-D
(式中、MNはシリカ(SiO2)含有マイクロニードルであり、S-Sはジスルフィド結合であり、Dは薬物である。)
[化学式2]:Lys-His-Gly-X
[化学式3]:Gly-His-Lys-X
[化学式4]:Ser-Lys-Thr-Thr-Lys-X
[化学式5]:Lys-Thr-Thr-Lys-Ser-X
[化学式6]:Arg-Arg-Gln-Met-Glu-Glu-X
[化学式7]:Glu-Glu-Met-Gln-Arg-Arg-X
[化学式8]:
(前記化学式2~8中、Xは、チオグリコール酸(Thioglycolic acid)及び11-メルカプトウンデカン酸(11-Mercaptoundecanoic acid)よりなる群から選択される1種以上である。) - 前記シリカ(SiO2)含有マイクロニードルは海綿動物由来の針状骨片であることを特徴とする、請求項5に記載のマイクロニードル。
- 前記シリカ(SiO2)含有マイクロニードルは、スルフヒドリル(Sulfhydryl、-SH)反応基を0.8×10-6mol/g~10×10-6mol/g含むことを特徴とする、請求項6に記載のマイクロニードル。
- 請求項5~7のいずれか一項に記載のマイクロニードルを含む化粧品組成物。
- 前記化粧品は、柔軟化粧水、栄養化粧水、栄養クリーム、マッサージクリーム、エッセンス、アンプル、ジェル、アイクリーム、クレンジングクリーム、クレンジングフォーム、クレンジングウォーター、パック、スプレー及びパウダーよりなる群から選択されることを特徴とする、請求項8に記載の化粧品組成物。
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