JP2007511508A - 経皮送達のための組成物及び装置 - Google Patents
経皮送達のための組成物及び装置 Download PDFInfo
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- JP2007511508A JP2007511508A JP2006539538A JP2006539538A JP2007511508A JP 2007511508 A JP2007511508 A JP 2007511508A JP 2006539538 A JP2006539538 A JP 2006539538A JP 2006539538 A JP2006539538 A JP 2006539538A JP 2007511508 A JP2007511508 A JP 2007511508A
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Abstract
Description
許文献12〜24及び25に開示されており、それらすべてが全体を引用により本明細書に取り込まれている(特許文献5〜25参照)。これらの装置は角質層を貫通するための種々の形状及びサイズの貫通要素を使用する。これらの参考文献中に開示された貫通要素は概括的にパッド又はシートのような薄い平坦な部材から垂直に延伸する。貫通要素は、約25〜400ミクロンのみの長さ及び幅並びに約5〜50ミクロンのみの厚さを有するマイクロプロジェクションのように極めて小さくすることができる。これらのマイクロプロジェクションはそれに対応して、そこを通過する促進された経皮物質送達のために角質層中に小さい微小スリットを形成する。
粘度向上対イオンは少なくとも2種の塩基性のpKaを有する塩基を含んでなる。適当な塩基にはリシン、ヒスチジン、アルギニン、水酸化カルシウム及び水酸化マグネシウムが包含される。
本発明を詳細に説明する前に、物質、方法又は構造物はもちろん変動する可能性があるので、本発明は特に例示された物質、方法又は構造物に限定されないことを理解しなければならない。従って、本明細書に記載されたものと類似した又は等しい多数の物質及び方法を本発明の実施に使用することができるが、本明細書には好ましい物質及び方法が記載される。
本明細書で使用される用語「経皮的」は局所又は全身治療のための皮膚中へのそして/又は皮膚を通る物質の送達を意味する。
包含する成分の懸濁物をも包含することとする。
サミン、アンモニア及びモルホリンが包含される。
マイクロプロジェクション部材を固定するか又はその全体を引用により取り込まれている国際公開第97/48440号パンフレットに記載されたような固定されたマイクロプロジェクションを使用することにより実施することができる。
れらは本発明の範囲を限定するものと考えるべきではなく、単にそれらの代表として説明されるものと考えるべきである。
Claims (28)
- 生物学的活性物質及び粘度向上対イオンの調製物を含んでなり、かつ、該調製物が治療的有効濃度の該生物学的活性物質を有する、角質層貫通マイクロプロジェクションを有する経皮送達装置をコートするための組成物。
- 調製物が約20cp〜約200cpの範囲内の粘度を有する請求項1の組成物。
- 調製物が第1のpH値を有し、生物学的活性物質が該調製物のpHにおいて正の電荷を有し、そして粘度向上対イオンが第1の酸を含んでなる請求項1の組成物。
- 第1の酸が少なくとも2種の酸性のpKa値を有する請求項3の組成物。
- 第1の酸がマレイン酸、リンゴ酸、マロン酸、酒石酸、アジピン酸、シトラコン酸、フマル酸、グルタル酸、イタコン酸、メグルトール、メサコン酸、コハク酸、シトラマル酸、タルトロン酸、クエン酸、トリカルバリル酸、エチレンジアミン四酢酸、炭酸、硫酸及びリン酸からなる群から選択される請求項4の組成物。
- 粘度向上対イオンが更に第2の酸を包含する請求項3の組成物。
- 第2の酸が少なくとも1種の酸性のpKa値を有する請求項6の組成物。
- 第2の酸が塩酸、臭化水素酸、硝酸、スルホン酸、硫酸、マレイン酸、リン酸、ベンゼンスルホン酸、メタンスルホン酸、クエン酸、コハク酸、グリコール酸、グルコン酸、グルクロン酸、乳酸、リンゴ酸、ピルビン酸、酒石酸、タルトロン酸、フマル酸、酢酸、プロピオン酸、ペンタン酸、炭酸、マロン酸、アジピン酸、シトラコン酸、レブリン酸、グルタル酸、イタコン酸、メグルトール、メサコン酸、シトラマル酸、クエン酸、トリカルバリル酸及びエチレンジアミン四酢酸からなる群から選択される請求項7の組成物。
- 調製物が第2のpH値を有し、生物学的活性物質が該調製物の第2のpH値において負の電荷を有し、そして粘度向上対イオンが第1の塩基を含んでなる請求項1の組成物。
- 第1の塩基が少なくとも2種の塩基性のpKa値を有する請求項9の組成物。
- 第1の塩基がリシン、ヒスチジン、アルギニン、水酸化カルシウム及び水酸化マグネシウムからなる群から選択される請求項10の組成物。
- 粘度向上対イオンが更に第2の塩基を包含する請求項9の組成物。
- 第2の塩基が少なくとも1種の塩基性のpKa値を有する請求項12の組成物。
- 第2の塩基が水酸化ナトリウム、水酸化カリウム、水酸化カルシウム、水酸化マグネシウム、モノエタノールアミン、ジエタノールアミン、トリエタノールアミン、トロメタミン、リシン、ヒスチジン、アルギニン、メチルグルカミン、グルコサミン、アンモニア及びモルホリンからなる群から選択される請求項13の組成物。
- 生物学的活性物質の電荷を中和するのに十分な量の粘度向上対イオンを含んでなる請求項1の組成物。
- 生物学的活性物質がACTH(1〜24)、カルシトニン、デスモプレッシン、LHR
H、ゴセレリン、ロイプロリド、ブセレリン、トリプトレリン、他のLHRH類似体、PTH、PTH(1〜34)、バソプレッシン、デアミノ[val4,D−Arg8]アルギニンバソプレッシン、インターフェロンアルファ、インターフェロンベータ、インターフェロンガンマ、FSH、EPO、GM−CSF、G−CSF、IL−10、グルカゴン、GRF、それらの類似体及び製薬学的に許容できるそれらの塩からなる群から選択される請求項の組成物。 - 粘度向上対イオンがクエン酸、酒石酸、リンゴ酸、塩酸、グリコール酸及び酢酸からなる群から選択される1種又は複数の酸を含んでなる請求項16の組成物。
- 生物学的活性物質がPTH(1〜34)を含んでなる請求項17の組成物。
- 被験体の角質層を貫通するようになっている複数のマイクロプロジェクションを有するマイクロプロジェクション部材を含んでなり、かつ、該マイクロプロジェクション部材が少なくとも1種の生物学的活性物質を有する生物学的適合性のコーティングを包含し、該コーティングが少なくとも1種の粘度向上対イオンを有する調製物から形成される、被験体に生物学的活性物質を経皮送達するための装置。
- 調製物が約20〜200cpの範囲内の粘度を有する請求項19の装置。
- 生物学的適合性コーティングが約10ミクロン未満のコーティングの厚さを有する請求項19の装置。
- 調製物が第1のpH値を有し、そして生物学的活性物質が該調製物の第1の値において正の電荷を有する請求項19の装置。
- 調製物が少なくとも2種の酸性のpKa値を有する第1の粘度向上対イオンを包含する請求項22の装置。
- 調製物が第2の粘度向上対イオンを包含し、かつ、該第2の粘度向上対イオンが少なくとも1種の酸性のpKa値を有する請求項23の装置。
- 調製物が第2のpH値を有し、そして生物学的活性物質が該調製物の第2のpH値において負の電荷を有する請求項19の装置。
- 調製物が少なくとも2種の塩基性のpKa値を有する第1の粘度向上対イオンを包含する請求項25の装置。
- 調製物が第2の粘度向上対イオンを包含し、かつ、該第2の粘度向上対イオンが少なくとも1種の塩基性のpKa値を有する請求項26の装置。
- 第1の粘度向上対イオンが生物学的活性物質の電荷を中和するのに十分な活性を有する請求項23の装置。
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Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2013177376A (ja) * | 2012-02-09 | 2013-09-09 | Hisamitsu Pharmaceut Co Inc | マイクロニードル用ゾルミトリプタン含有コーティング組成物及びマイクロニードルデバイス |
JP2014517825A (ja) * | 2011-04-22 | 2014-07-24 | ラジウス ヘルス,インコーポレイテッド | PTH、PTHrP、および関連ペプチドの薬剤送達方法 |
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US11058630B2 (en) | 2016-02-19 | 2021-07-13 | Zosano Pharma Corporation | Method of rapidly achieving therapeutic concentrations of triptans for treatment of migraines |
US11839683B2 (en) | 2016-02-19 | 2023-12-12 | Emergex USA Corporation | Method of rapidly achieving therapeutic concentrations of triptans for treatment of migraines |
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Also Published As
Publication number | Publication date |
---|---|
EP1682012A2 (en) | 2006-07-26 |
WO2005051456A2 (en) | 2005-06-09 |
BRPI0416042A (pt) | 2007-01-02 |
MXPA06005510A (es) | 2006-12-14 |
EP1682012A4 (en) | 2008-09-24 |
CA2546280A1 (en) | 2005-06-09 |
US20050106209A1 (en) | 2005-05-19 |
TW200528154A (en) | 2005-09-01 |
AU2004292954A1 (en) | 2005-06-09 |
KR20070010115A (ko) | 2007-01-22 |
WO2005051456A3 (en) | 2005-11-10 |
AR046824A1 (es) | 2005-12-28 |
CN100548228C (zh) | 2009-10-14 |
JP5388415B2 (ja) | 2014-01-15 |
CN1901841A (zh) | 2007-01-24 |
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