JP5411398B2 - 長時間放出性の口腔生物接着性錠剤 - Google Patents
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Description
本発明は、活性成分の長時間制御放出用の生物接着性の生物侵食性錠剤に関する。より詳しくは、本発明は、代謝により、または水分、酵素、pH作用により惹起される活性成分の時期尚早な分解を伴わずに、活性成分を徐放させるための体腔壁接着性の漸進性水和錠剤に関する。
薬物およびその他の医薬品は伝統的に経口摂取、鼻腔スプレーまたは注射による形態で投与されている。これらの送達方法は、血流中に送達される活性成分が長期間定常的に供給されることの必要な患者にとって、無効であることが証明されている。特に難しいのは、睡眠時間中に投与を必要とする患者である。これらの患者に対しては、静脈内静脈糸、遅延溶解ピル、坐剤や経皮パッチなどが処方されている。しかし、IV(静脈内)の不便さと不快感、胃腸での分解または最初に通過する肝臓代謝による多くの摂取活性成分の寿命が短いこと、および多くの製品が適当な投与法でまたは調整した濃度で経皮的に好適に送達し得ないことなどが、これらの方法の不満足なことを証明している。
本発明は上記の技術上の必要性に合致する。従って、本発明の目的は生物接着性錠剤であって、体腔の標的組織領域に直ちにまたは殆ど直ちに接着し、一般に治療の全期間実質的に付着したままである錠剤を提供することである。本発明のこの態様によると、事実上18時間以上にわたり口腔に留まって活性成分を送達し得る生物接着性錠剤が提供される。本発明の関連する態様によると、事実上72時間以上にわたり膣内に留まって活性成分を送達し得る生物接着性錠剤が提供される。
図1は、本発明の生物接着性錠剤の漸進性水和を示す一連の写真である。
図2は、本発明の生物接着性錠剤をつくる現状で好ましい方法を示すフォローチャートである。
ヒドロキシプロピルメチルセルロース15000(=HPMC15000)をトウモロコシデンプンおよびラクトースと混合し、次いで水分に非感受性の活性成分の場合、活性物質を加える。混合物をヒドロキシプロピルメチルセルロース5(=HPMC5)の水溶液で湿らせ、次いで練る/顆粒とする。
タルク、二酸化ケイ素、ステアリン酸マグネシウム、および水分感受性の活性物質の場合、活性成分を加える。このすべてを、口径サイズ500μmのふるい器でふるい、次いでフリーフォール混合器に移す。
錠剤用混合物を回転式打錠器で錠剤とする。この打錠器は上側に9mm平面、下側に曲面(r=9mm)、両斜面縁のパンチを有しているものである。錠剤を取り出し、包装する。
下記は、ヒトにおける完全な生理的置換のための製剤(製剤8、バッチ#00029906)の例である。
テストステロン 30.000mg 24.0%
HPMC 26.250mg 21.0%
トウモロコシデンプン 22.500mg 18.0%
ラクトース一水和物 30.125mg 24.1%
シリカ 1.250mg 1.0%
ポリカルボフィル(Noveon) 3.125mg 2.5%
カルボマー974P 9.375mg 7.5%
タルク 1.500mg 1.2%
ステアリン酸マグネシウム 0.875mg 0.7%
表1:
バッチ:0069904
溶解器:ROTATING PADDLE 60 RPM/PLATINUM WIRE SPIRAL
バッチ:0049904
溶解器:ROTATING PADDLE 60 RPM/PLATINUM WIRE SPIRAL
バッチ:0029904
溶解器:ROTATING PADDLE 60 RPM/PLATINUM WIRE SPIRAL
バッチ:0019904
溶解器:ROTATING PADDLE 60 RPM/PLATINUM WIRE SPIRAL
Claims (19)
- 徐放性の漸進性水和生物接着錠剤であって、
有効量の活性成分、
0.5ないし10重量%の水不溶性架橋ポリカルボン酸ポリマー、
1ないし75重量%のカルボマー934Pおよびカルボマー974Pからなる群から選択される水溶性ポリマー、
5ないし50重量%のヒドロキシプロピルメチルセルロース、
0.5ないし25重量%のデンプン、および
1ないし50重量%のラクトース
を含む、錠剤。
- 該錠剤が50重量%までの活性成分を含む、請求項1の錠剤。
- 1重量%のシリカをさらに含む、請求項1または2の錠剤。
- 0.5ないし2重量%のタルクをさらに含む、請求項1〜3のいずれかの錠剤。
- 0.5ないし1重量%のステアリン酸マグネシウムをさらに含む、請求項1〜4のいずれかの錠剤。
- 該活性成分が、糖タンパク質、タンパク質、性ホルモン、抗ホルモン、硝酸エステル、ベータ−アゴニスト、ベータ−アンタゴニスト、オピオイド、オピオイド−アンタゴニスト、抗うつ剤、HMG−CoAレダクターゼ阻害剤、抗ヒスタミン剤、ACE阻害剤、プロスタグランジン、および水分、酵素またはpHにより代謝または分解される他の活性成分よりなる群から選ばれる、請求項1〜5のいずれかの錠剤。
- 徐放性の漸進性水和生物接着錠剤であって、
有効量の活性成分、
2ないし30重量%の結合剤、
5ないし40重量%のラクトース、
1ないし3重量%の水不溶性架橋ポリカルボン酸ポリマー、および
5ないし50重量%のカルボマー934Pおよびカルボマー974Pからなる群から選択される水溶性ポリマー、
を含む、錠剤。
- 0.2ないし2重量%のシリカをさらに含む、請求項7の錠剤。
- 該活性成分がテストステロンであり、該テストステロンが1ないし30重量%の量で存在している、請求項7または8の錠剤。
- 活性成分を患者の血流に送達して臨床状態を処置するための徐放性の漸進性水和生物接着錠剤であって、医療的に有効量の活性成分、0.5ないし10重量%の水不溶性架橋ポリカルボン酸ポリマー、1ないし75重量%のカルボマー934Pおよびカルボマー974Pからなる群から選択される水溶性ポリマー、1ないし50重量%のラクトースおよび0.5ないし25重量%のデンプンを含む錠剤。
- 水不溶性架橋ポリカルボン酸ポリマーがポリカルボフィルである、請求項10の錠剤。
- 活性成分がテストステロンである、請求項10または11の錠剤。
- 錠剤が口腔錠である、請求項10〜12のいずれかの錠剤。
- 錠剤が膣用錠である、請求項10〜12のいずれかの錠剤。
- 活性成分の徐放性投与を必要とする臨床状態を処置するための漸進性水和生物接着錠剤の製造における、活性成分、0.5ないし10重量%の水不溶性架橋ポリカルボン酸ポリマー、1ないし75重量%のカルボマー934Pおよびカルボマー974Pからなる群から選択される水溶性ポリマー、1ないし50重量%のラクトースおよび0.5ないし25重量%のデンプンの使用であって、活性成分の放出が、
i)ラクトースおよびデンプンの量を増加させ、そして水溶性ポリマーの量を減少させること;または
ii)ラクトースおよびデンプンの量を減少させ、そして水溶性ポリマーの量を増加させること、により制御される、使用。
- 水不溶性架橋ポリカルボン酸ポリマーがポリカルボフィルである、請求項15の使用。
- 活性成分がテストステロンである、請求項15または16の使用。
- 錠剤が口腔錠である、請求項15〜17のいずれかの使用。
- 錠剤が膣用錠である、請求項15〜17のいずれかの使用。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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US9784398P | 1998-08-25 | 1998-08-25 | |
US60/097,843 | 1998-08-25 | ||
US09/379,310 | 1999-08-23 | ||
US09/379,310 US6248358B1 (en) | 1998-08-25 | 1999-08-23 | Bioadhesive progressive hydration tablets and methods of making and using the same |
PCT/US1999/019260 WO2000010536A1 (en) | 1998-08-25 | 1999-08-24 | Extended release buccal bioadhesive tablet |
Related Child Applications (1)
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JP2010151682A Division JP2010248231A (ja) | 1998-08-25 | 2010-07-02 | 長時間放出性の口腔生物接着性錠剤 |
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Publication Number | Publication Date |
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JP2004500317A JP2004500317A (ja) | 2004-01-08 |
JP2004500317A5 JP2004500317A5 (ja) | 2013-03-28 |
JP5411398B2 true JP5411398B2 (ja) | 2014-02-12 |
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JP2000565858A Expired - Fee Related JP5411398B2 (ja) | 1998-08-25 | 1999-08-24 | 長時間放出性の口腔生物接着性錠剤 |
JP2010151682A Pending JP2010248231A (ja) | 1998-08-25 | 2010-07-02 | 長時間放出性の口腔生物接着性錠剤 |
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JP2010151682A Pending JP2010248231A (ja) | 1998-08-25 | 2010-07-02 | 長時間放出性の口腔生物接着性錠剤 |
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US (1) | US6248358B1 (ja) |
EP (1) | EP1105104B1 (ja) |
JP (2) | JP5411398B2 (ja) |
KR (1) | KR100716702B1 (ja) |
CN (2) | CN1879608A (ja) |
AR (1) | AR036972A1 (ja) |
AT (1) | ATE306253T1 (ja) |
AU (1) | AU754880B2 (ja) |
BR (1) | BR9913239B1 (ja) |
CA (1) | CA2341375C (ja) |
DE (1) | DE69927694T2 (ja) |
DK (1) | DK1105104T3 (ja) |
ES (1) | ES2251220T3 (ja) |
HK (1) | HK1034895A1 (ja) |
HU (1) | HU226591B1 (ja) |
IL (1) | IL141445A (ja) |
MA (1) | MA24964A1 (ja) |
MX (1) | MXPA01002007A (ja) |
MY (2) | MY125919A (ja) |
NO (1) | NO331255B1 (ja) |
NZ (1) | NZ509963A (ja) |
PE (1) | PE20001036A1 (ja) |
RU (1) | RU2227022C2 (ja) |
UA (1) | UA78967C2 (ja) |
WO (1) | WO2000010536A1 (ja) |
ZA (1) | ZA995445B (ja) |
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US6624200B2 (en) * | 1998-08-25 | 2003-09-23 | Columbia Laboratories, Inc. | Bioadhesive progressive hydration tablets |
AU2005203703B2 (en) * | 1998-08-25 | 2007-05-24 | Columbia Laboratories (Bermuda) Limited | Bioadhesive progressive hydration tablets |
US7803392B2 (en) | 2000-12-27 | 2010-09-28 | University Of Kentucky Research Foundation | pH-Sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules |
WO2002087552A2 (en) * | 2001-05-01 | 2002-11-07 | Mcgill University | Androgen-mediated neuroprotection and uses thereof |
US7709026B2 (en) * | 2001-10-29 | 2010-05-04 | Columbia Laboratories, Inc. | Low concentration of peroxide for treating or preventing vaginal infections |
CN101327326A (zh) * | 2001-10-29 | 2008-12-24 | 哥伦比亚实验室(百慕大群岛)有限公司 | 阴道给药治疗骨盆痛和不孕症的抗节律障碍剂 |
US8425892B2 (en) * | 2001-10-29 | 2013-04-23 | Columbia Laboratories, Inc. | Extended, controlled-release pharmaceutical compositions using charged polymers |
US20030114394A1 (en) * | 2001-10-29 | 2003-06-19 | Levine Howard L. | Vaginally administered anti-dysrhythmic agents for treating pelvic pain |
US7005138B2 (en) * | 2001-12-21 | 2006-02-28 | Duramed Pharmaceuticals, Inc. | Method of systematically delivering SSRIs |
GB0210397D0 (en) * | 2002-05-07 | 2002-06-12 | Ferring Bv | Pharmaceutical formulations |
US20050226926A1 (en) | 2002-07-25 | 2005-10-13 | Pfizer Inc | Sustained-release tablet composition of pramipexole |
AR040682A1 (es) * | 2002-07-25 | 2005-04-13 | Pharmacia Corp | Forma de dosificacion una vez al dia de pramipexol |
US20050202083A1 (en) * | 2002-08-02 | 2005-09-15 | Kumar Pananchukunnath M | Storage stable tablets of fosinopril sodium |
WO2004043434A1 (en) * | 2002-11-14 | 2004-05-27 | Shear/Kershman Laboratories, Inc. | Oral testosterone delivery system with improved sustained release |
SE0302947D0 (sv) | 2003-01-24 | 2003-11-07 | Magle Ab | A composition material for transmucosal delivery |
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