JP5766121B2 - 口腔内への物質の送達のためのデリバリーシステム - Google Patents
口腔内への物質の送達のためのデリバリーシステム Download PDFInfo
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- JP5766121B2 JP5766121B2 JP2011542073A JP2011542073A JP5766121B2 JP 5766121 B2 JP5766121 B2 JP 5766121B2 JP 2011542073 A JP2011542073 A JP 2011542073A JP 2011542073 A JP2011542073 A JP 2011542073A JP 5766121 B2 JP5766121 B2 JP 5766121B2
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- carrier
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- galactose
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Images
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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- 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
- A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/61—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
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- Inorganic Chemistry (AREA)
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
a)α−アミラーゼ。アミラーゼは食物を嚥下する前にデンプンの消化を開始し、リパーゼは脂肪の消化を開始する。
b)リゾチーム。リゾチームは細菌の溶解を生ずるように機能する。
c)舌のリパーゼ。舌のリパーゼは約4.0の至適pHを有し、それは酸性環境に入るまで活性化されないことを意味する。
d)マイナーな酵素は唾液酸性ホスファターゼA+B、N-アセチルムラミル-L−アラニンアミダーゼ、NAD(P)Hデヒドロゲナーゼ−キノン、唾液ラクトペルオキシダーゼ、スーパーオキシドジスムターゼ、グルタチオントランスフェラーゼ、クラス3アルデヒドデヒドロゲナーゼ、グルコース−6−ホスファターゼイソメラーゼ、アルデヒドデヒドロゲナーゼ、及び組織カリクレインを含む。
糖結合部を有さない担体と比較した、本発明に係る結合した糖結合部を有する単体を含むデリバリーシステムの効果を示すために、以下の試験を実施した。
実施例2は、本発明に係るデリバリーシステムを使用した際の、スコポラミンのin vivo放出の効果を示すために実施された。
更なる試験をボランティアのヒトで実施した。
Claims (11)
- 生体活性物質のための担体(1)を含む、口腔内での使用のためのデリバリーシステムであって、
前記担体(1)は、酸素結合部位(X)を含む表面を有するセルロースベースの材料またはデンプンベースの材料を含み、
ならびに、前記システムは、前記担体(1)に結合する少なくとも一つの結合部(2)を含み、
前記結合部(2)は、式:キシロース−ガラクトース−ガラクトース−グルコースアミンまたはそれらのエピマーを有する一つ以上の糖基を含み、前記結合部(2)は、前記担体(1)上の酸素結合基にキシロース末端で結合しており、
一つ以上の生体活性分子(R)が少なくとも一つの結合部(2)における一つ以上の糖基に、または、少なくとも一つの結合部(2)における一つ以上の糖基上の一つ以上の置換基に、直接結合していることを特徴とするデリバリーシステム。 - 前記担体(1)上の酸素結合部位(X)がP、C、SまたはNから選択される、請求項1に記載のデリバリーシステム。
- 前記担体(1)がニトロセルロースを含む、請求項1に記載のデリバリーシステム。
- 前記少なくとも一つの結合部(2)が、グルコースアミンで末端化された第二の末端を有する、請求項1から3のいずれか一項に記載のデリバリーシステム。
- 前記結合部(2)が、キシロース−ガラクトース−ガラクトース−グルコースアミンの式を有する糖鎖である、請求項4に記載のデリバリーシステム。
- 前記少なくとも一つの結合部(2)が、生体活性物質(R)のための結合部位(B)を構成する、OH、NH、SO4及びPO4から選択される少なくとも一つの置換基を含む、請求項1から5のいずれか一項に記載のデリバリーシステム。
- 口腔内に生体活性物質(R)を放出するためのデリバリーシステムの製造方法であって、
a)セルロースベースの材料またはデンプンベースの材料を含み、かつ、酸素結合部位(X)を示す表面を有する担体(1)を準備する工程;
b)式:キシロース−ガラクトース−ガラクトース−グルコースアミンまたはそれらのエピマーを含む一つまたは複数の糖基を含む少なくとも一つの結合部(2)を前記担体(1)に結合する工程であって、前記キシロース基は、前記酸素結合部位(X)の一つに結合しており;
c)少なくとも1つの結合部(2)における一つ以上の糖基に、または少なくとも一つの結合部(2)における一つ以上の糖基上の一つ以上の置換基に、一つ以上の生体活性分子(R)を直接結合する工程;
を含むことを特徴とする方法。 - 前記担体(1)に対する少なくとも一つの結合部(2)の結合が、5.6以下のpHを有する水溶液中で実施される、請求項7に記載の方法。
- 前記担体(1)上の酸素結合部位(X)がP、C、S及びNから選択される、請求項7または8に記載の方法。
- 前記担体(1)がニトロセルロースを含む、請求項7から9のいずれか一項に記載の方法。
- 前記結合部(2)が、生体活性物質(R)のための結合部位(B)を構成する、OH、NH、SO4またはPO4から選択される少なくとも一つの置換基を含む、請求項7から10のいずれか一項に記載の方法。
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SE0802632A SE533540C2 (sv) | 2008-12-19 | 2008-12-19 | Administrerinssystem för administrering av en substans i munhålan |
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PCT/SE2009/051478 WO2010071593A1 (en) | 2008-12-19 | 2009-12-21 | Delivery system for delivery of a substance into the oral cavity |
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EP0308181A1 (en) | 1987-09-14 | 1989-03-22 | Novo Nordisk A/S | Trans-mucosal delivery formulations and a method for preparation thereof |
JPH08104651A (ja) * | 1993-03-10 | 1996-04-23 | Yoshiyuki Koyama | 経粘膜薬物運搬体及び高分子医薬複合体 |
DE19524515A1 (de) | 1995-07-05 | 1997-01-09 | Deutsches Krebsforsch | Saccharid-Konjugate |
TW580397B (en) | 1997-05-27 | 2004-03-21 | Takeda Chemical Industries Ltd | Solid preparation |
SE9803240D0 (sv) * | 1998-09-24 | 1998-09-24 | Diabact Ab | A pharmaceutical composition having a rapid action |
US20030119761A1 (en) | 2000-04-12 | 2003-06-26 | Christian Samuel T. | Novel pharmaceutical agents containing carbohydrate moieties and methods of their preparation and use |
JP3415835B2 (ja) | 2000-06-30 | 2003-06-09 | 山之内製薬株式会社 | 口腔内速崩壊錠およびその製造法 |
GB2381194A (en) | 2001-09-07 | 2003-04-30 | Gw Pharmaceuticals Ltd | Pharmaceutical formulations |
DE10209822A1 (de) | 2002-03-06 | 2003-09-25 | Biotechnologie Ges Mittelhesse | Kopplung niedermolekularer Substanzen an ein modifiziertes Polysaccharid |
US20040116348A1 (en) * | 2002-09-23 | 2004-06-17 | Ying Chau | Polymer-linker-drug conjugates for targeted drug delivery |
DE602004024960D1 (de) * | 2003-01-21 | 2010-02-25 | Nippon Shinyaku Co Ltd | Rasch in der mundhöhle schmelzende tablette |
ITMI20061117A1 (it) | 2006-06-09 | 2007-12-10 | Michele Bonanomi | Una composizione farmaceutica per la somministrazione sublinguale di vaccini metodo per la sua preparazione e sui usi |
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JP2008231013A (ja) | 2007-03-20 | 2008-10-02 | Kaneka Corp | 固定化糖鎖体 |
SE533540C2 (sv) | 2008-12-19 | 2010-10-19 | Neoinvent Medical Engineering Ab | Administrerinssystem för administrering av en substans i munhålan |
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BRPI0922342A2 (pt) | 2016-01-12 |
EP2373348A4 (en) | 2015-05-27 |
CN102256626B (zh) | 2015-04-29 |
US20120065160A1 (en) | 2012-03-15 |
IL213654A (en) | 2017-02-28 |
RU2011129759A (ru) | 2013-01-27 |
US9987376B2 (en) | 2018-06-05 |
EP2373348A1 (en) | 2011-10-12 |
EP2373348B1 (en) | 2018-08-01 |
JP2015098478A (ja) | 2015-05-28 |
JP2012512869A (ja) | 2012-06-07 |
CA2746052A1 (en) | 2010-06-24 |
SE533540C2 (sv) | 2010-10-19 |
IL213654A0 (en) | 2011-07-31 |
WO2010071593A1 (en) | 2010-06-24 |
CN102256626A (zh) | 2011-11-23 |
CA2746052C (en) | 2017-02-28 |
KR20110104068A (ko) | 2011-09-21 |
SE0802632A1 (sv) | 2010-06-20 |
RU2553351C2 (ru) | 2015-06-10 |
KR101735717B1 (ko) | 2017-05-15 |
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