JP2019510729A - 含プレガバリン高膨潤性徐放性三重錠剤 - Google Patents
含プレガバリン高膨潤性徐放性三重錠剤 Download PDFInfo
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- JP2019510729A JP2019510729A JP2017541667A JP2017541667A JP2019510729A JP 2019510729 A JP2019510729 A JP 2019510729A JP 2017541667 A JP2017541667 A JP 2017541667A JP 2017541667 A JP2017541667 A JP 2017541667A JP 2019510729 A JP2019510729 A JP 2019510729A
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- pregabalin
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Abstract
【解決手段】本発明に係る多層錠剤は、主成分としてプレガバリンまたはその薬剤学的に許容可能な塩を含む多層錠剤であって、膨潤性高分子を含む上層及び下層と、媒質伝達剤を含み、上層と下層との間に配設される中間層と、を備えるが、前記多層錠剤は、水溶性媒質に接触してから2時間が経過したときに最初の体積の250%以上に膨潤する。また、本発明に係る多層錠剤の製造方法は、(i)プレガバリンまたはその薬剤学的に許容可能な塩及び膨潤性高分子を混合した混合物またはこれを顆粒化した顆粒物からなる上層及び下層用打錠物を製造するステップと、(ii)プレガバリンまたはその薬剤学的に許容可能な塩及び媒質伝達剤を混合した混合物またはこれを顆粒化した顆粒物からなる中間層用打錠物を製造するステップと、(iii)前記ステップ(i)における打錠物及びステップ(ii)における打錠物を打錠して三重錠剤を製造するステップと、を含む。
【選択図】図3
Description
実施例8の錠剤及び対照薬として市販中のリリカカプセル75mgに対して、ビーグル犬における薬物動態学的な評価を行った。約11kgのビーグル犬を1群当たり8匹ずつ群分けした。対照薬は1回につき1カプセルを投与するが、1日2回、10時間おきに投与し、実施例8の錠剤(試験薬)は1錠を1日1回投与した。最初の投与後に24時間採血し、これを分析してそれぞれの薬物動態学的なパラメーターを算出した。その結果を下記表4に示す。
Claims (8)
- 主成分としてプレガバリンまたはその薬剤学的に許容可能な塩を含む多層錠剤であって、膨潤性高分子を含む上層及び下層と、
媒質伝達剤を含み、上層と下層との間に配設される中間層と、を備えるが、
前記多層錠剤は、水溶性媒質に接触してから2時間が経過したときに最初の体積の250%以上に膨潤する多層錠剤。 - 前記上層及び下層は、プレガバリンまたはその薬剤学的に許容可能な塩をさらに含み、前記中間層もまた、プレガバリンまたはその薬剤学的に許容可能な塩をさらに含むことを特徴とする請求項1に記載の多層錠剤。
- 前記多層錠剤は、水溶性媒質に接触してから2時間から6時間の間に、最初の体積の250%以上に膨潤していることを特徴とする請求項1または請求項2に記載の多層錠剤。
- 前記多層錠剤は、水溶性媒質に接触してから2時間が経過したときに錠剤の短軸の長さが12mm以上であることを特徴とする請求項1または請求項2に記載の多層錠剤。
- 水溶性媒質に接触してから2時間から6時間の間に、錠剤の短軸の長さが12mm以上であることを特徴とする請求項4に記載の多層錠剤。
- 前記多層錠剤は、水溶性媒質に接触してから2時間が経過したときに最初の体積の300%以上に膨潤することを特徴とする請求項1または請求項2に記載の多層錠剤。
- 前記多層錠剤は、水溶性媒質に接触してから2時間から6時間の間に、最初の体積の300%以上に膨潤していることを特徴とする請求項6に記載の多層錠剤。
- 1日1回経口投与されることを特徴とする請求項1または請求項2に記載の多層錠剤。
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KR10-2017-0014591 | 2017-02-01 | ||
PCT/KR2017/003378 WO2018143512A1 (ko) | 2017-02-01 | 2017-03-29 | 프레가발린 함유 고팽윤성 서방성 삼중정제 |
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JP2010518073A (ja) * | 2007-02-07 | 2010-05-27 | ジーエル・ファームテック・コーポレイション | 経口徐放性三層錠剤 |
WO2011151708A1 (en) * | 2010-06-01 | 2011-12-08 | Rubicon Research Private Limited | Gastroretentive dosage forms of gaba analogs |
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JP2014521639A (ja) * | 2011-07-26 | 2014-08-28 | ユーハン・コーポレイション | 二相の放出制御システムによるプレガバリンを含む徐放錠 |
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WO1998003167A1 (en) | 1996-07-24 | 1998-01-29 | Warner-Lambert Company | Isobutylgaba and its derivatives for the treatment of pain |
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WO2011151708A1 (en) * | 2010-06-01 | 2011-12-08 | Rubicon Research Private Limited | Gastroretentive dosage forms of gaba analogs |
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