JP5199084B2 - 胃保持型製剤およびそれらの製造方法 - Google Patents
胃保持型製剤およびそれらの製造方法 Download PDFInfo
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- JP5199084B2 JP5199084B2 JP2008522096A JP2008522096A JP5199084B2 JP 5199084 B2 JP5199084 B2 JP 5199084B2 JP 2008522096 A JP2008522096 A JP 2008522096A JP 2008522096 A JP2008522096 A JP 2008522096A JP 5199084 B2 JP5199084 B2 JP 5199084B2
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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Description
(A)微結晶性セルロースおよびカルボキシメチルセルロースナトリウムの共処理材料を含む群から選択される弱ゲル化剤、および
(B)メチルセルロース、ヒドロキシプロピルメチルセルロース、低置換ヒドロキシプロピルセルロースを除くヒドロキシプロピルセルロース、ヒドロキシエチルセルロース、エチルセルロース、カルボキシメチルセルロースナトリウム、キサンタンガム、グアーガム、カラギーナンガム、ローカストビーンガム、アルギン酸ナトリウム、寒天、ゼラチン、加工デンプン、カルボキシビニルポリマーのコポリマー、アクリレートのコポリマー、オキシエチレンおよびオキシプロピレンのコポリマーならびにこれらの混合物からなる群から選択され、好ましくはキサンタンガムである、少なくとも1種の強ゲル化剤、
(C)場合によって、低粘性HPMC、PVP、ポリメタクリル酸コポリマー(Eudragit E100)およびこれらの混合物からなる群から選択される結合剤、
の混合物とともに粒状化された活性物質を含み、該製剤はまたガス発生剤を含む。
(1)活性物質が、(A)弱ゲル化剤と(B)強ゲル化剤との混合物、および場合によって、希釈剤もしくは帯電防止剤またはこれらの混合物を含む群から選択される少なくとも1種の添加剤(D)と乾式混合されるステップと、
(2)場合によって、得られた乾式混合物が、アルコールまたはアルコールと水との混合物に溶かした少なくとも1種の結合剤(C)とともに粒状化されるステップと、
(3)ガス発生剤が、ステップ(2)から得られる顆粒と、場合によって、希釈剤、潤滑剤、湿潤剤、甘味剤、着香剤、着色剤およびこれらの混合物を含む群から選択される賦形剤と乾式混合されるステップと、
(4)次いで、混合物が圧縮され錠剤にされるステップと、
(5)場合によって、錠剤がフィルムコートされるステップである。
(1)活性物質が、(A)弱ゲル化剤と(B)強ゲル化剤との混合物、および場合によって、希釈剤もしくは帯電防止剤またはこれらの混合物を含む群から選択される少なくとも1種の添加剤(D)、およびガス発生剤の少なくとも一部と乾式混合されるステップと、
(2)場合によって、得られた乾式混合物が、アルコールまたはアルコールと水との混合物に溶かした少なくとも1種の結合剤(C)とともに粒状化されるステップと、
(3)ガス発生剤の残りの部分があれば、ステップ(2)から得られる顆粒と、場合によって、希釈剤、潤滑剤、湿潤剤、甘味剤、着香剤、着色剤およびこれらの混合物を含む群から選択される賦形剤と乾式混合されるステップと、
(4)次いで、混合物が圧縮され錠剤にされるステップと、
(5)場合によって、錠剤がフィルムコートされるステップである。
実施例1
機械速度:25〜27rpm
錠剤形状−両凸カプレット
サイズ−長さ19mmおよび幅9mm
硬さ−120〜160N。
(重量で表される)
1 31.10
2 45.20
4 65.40
6 78.00
8 88.10
12 97.70。
錠剤形状−両凸カプレット
サイズ−長さ16mmおよび幅8mm
硬さ−100〜160N。
乳糖一水和物: 19.17%
タルク: 2.87%
二酸化チタン: 1.43%
ポリソルベート80: 0.1%
水: 76.39%。
(重量で表される)
1 37.18
2 56.09
4 77.14
6 92.59
8 98.26
Claims (13)
- 微結晶性セルロースおよびカルボキシメチルセルロースナトリウムの共処理材料である弱ゲル化剤、メチルセルロース、ヒドロキシプロピルメチルセルロース、低置換ヒドロキシプロピルセルロースを除くヒドロキシプロピルセルロース、ヒドロキシエチルセルロース、エチルセルロース、カルボキシメチルセルロースナトリウム、キサンタンガム、グアーガム、カラギーナンガム、ローカストビーンガム、アルギン酸ナトリウム、寒天、ゼラチン、加工デンプン、カルボキシビニルポリマーのコポリマー、アクリレートのコポリマー、オキシエチレンおよびオキシプロピレンのコポリマーならびにこれらの混合物からなる群から選択される強ゲル化剤ならびにガス発生剤の混合物とともに粒状化された活性物質を含む胃保持型製剤。
- 前記活性物質もまた、(C)結合剤とともに、および場合によって、(D)希釈剤、帯電防止剤またはこれらの混合物を含む群から選択される添加剤とともに粒状化される、請求項1に記載の胃保持型製剤。
- 希釈剤、潤滑剤、湿潤剤、甘味剤、着香剤、着色剤およびこれらの混合物からなる群から選択される賦形剤をさらに含む、請求項1または2に記載の胃保持型製剤。
- 前記ガス発生剤が、水溶性の炭酸塩、亜硫酸塩および重炭酸塩、例えば炭酸ナトリウム、重炭酸ナトリウム、メタ重亜硫酸ナトリウム、炭酸カルシウム、ならびにこれらの混合物からなる群から選択される、請求項1から3のいずれか一項に記載の胃保持型製剤。
- 前記結合剤が、低粘性ヒドロキシプロピルメチルセルロース(HPMC)、ポリビニルピロリドン(PVP)、ポリメタクリル酸コポリマーおよびこれらの混合物からなる群から選択される、請求項2から4のいずれか一項に記載の胃保持型製剤。
- 前記ポリメタクリル酸コポリマーがオイドラギットE100(Eudragit E100)(登録商標)である、請求項5に記載の胃保持型製剤。
- 前記活性物質の量が、製剤の総重量に対して、10から90重量%までの範囲である、請求項1から6のいずれか一項に記載の胃保持型製剤。
- 前記弱ゲル化剤および前記強ゲル化剤の両方の総重量が、製剤の総重量に対して2から40重量%までの範囲である、請求項1から7のいずれか一項に記載の胃保持型製剤。
- 前記弱ゲル化剤と前記強ゲル化剤との比率が1:1から1:10の間の範囲である、請求項1から8のいずれか一項に記載の胃保持型製剤。
- 前記活性物質と弱および強ゲル化剤の両方との比率が、1:99から99:1までの範囲である、請求項1から9のいずれか一項に記載の胃保持型製剤。
- 前記活性物質が、シプロフロキサシン、オフロキサシン、ペフロキサシン、グレパフロキサシン、エノキサシン、アミフロキサシン、フレロキサシン、テマフロキサシン、ロメフロキサシン、ノルフロキサシン、スパルフロキサシン、レボフロキサシン、ガチフロキサシンおよびモキシフロキサシンなどのフルオロキノロン系の抗菌性物質、アモキシシリン、セファレキシンの塩または塩基の形態での誘導体、ならびに塩酸メトホルミン、グリクラジドなどの抗糖尿病物質、塩酸ジルチアゼム、酒石酸メトプロロールまたはコハク酸メトプロロールなどの抗高血圧薬から選択される、請求項1から10のいずれか一項に記載の胃保持型製剤。
- (1)活性物質を、(A)微結晶性セルロースおよびカルボキシメチルセルロースナトリウムの共処理材料である弱ゲル化剤と(B)強ゲル化剤との混合物、ならびに場合によって、希釈剤もしくは帯電防止剤またはこれらの混合物を含む群から選択される少なくとも1種の添加剤(D)と乾式混合するステップと、
(2)得られた乾式混合物を、場合によってアルコールまたはアルコールと水との混合物に溶かした少なくとも1種の結合剤(C)とともに粒状化するステップと、
(3)ガス発生剤を、ステップ(2)から得られる顆粒と、場合によって、希釈剤、潤滑剤、湿潤剤、甘味剤、着香剤、着色剤およびこれらの混合物を含む群から選択される賦形剤と乾式混合するステップと、
(4)混合物を圧縮して錠剤にするステップと、
(5)場合によって、(4)において得られる錠剤をフィルムコーティングするステップと
を含む、請求項1から11のいずれか一項に記載の製剤を製造するための方法。 - (1)活性物質を、(A)微結晶性セルロースおよびカルボキシメチルセルロースナトリウムの共処理材料である弱ゲル化剤と(B)強ゲル化剤との混合物、ならびに場合によって、希釈剤もしくは帯電防止剤またはこれらの混合物を含む群から選択される少なくとも1種の添加剤(D)、ならびにガス発生剤の少なくとも一部と乾式混合するステップと、
(2)得られた乾式混合物を、場合によってアルコールまたはアルコールと水との混合物に溶かした少なくとも1種の結合剤(C)とともに粒状化するステップと、
(3)ガス発生剤の残りの部分があれば、ステップ(2)から得られる顆粒と、場合によって、希釈剤、潤滑剤、湿潤剤、甘味剤、着香剤、着色剤およびこれらの混合物を含む群から選択される賦形剤と乾式混合するステップと、
(4)混合物を圧縮して錠剤にするステップと、
(5)場合によって、錠剤をフィルムコーティングするステップと
を含む、請求項1から11のいずれか一項に記載の製剤を製造するための方法。
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WO2010038237A2 (en) | 2008-09-22 | 2010-04-08 | Rubicon Research Private Limited | Compositions exhibiting delayed transit through the gastrointestinal tract |
FR2945947B1 (fr) | 2009-05-29 | 2011-07-29 | Flamel Tech Sa | Compositions pharmaceutiques flottantes a liberation controlee |
WO2011004799A1 (ja) | 2009-07-06 | 2011-01-13 | 杏林製薬株式会社 | 中空構造を有する錠剤 |
EP2361615A1 (en) | 2010-02-19 | 2011-08-31 | Alfred E. Tiefenbacher GmbH & Co. KG | Dipyridamole prolonged-release tablet |
WO2011111068A2 (en) | 2010-03-09 | 2011-09-15 | Council Of Scientific And Industrial Research | Gastroretentive, extended release composition of therapeutic agent |
ES2543108T3 (es) * | 2010-03-31 | 2015-08-14 | Mochida Pharmaceutical Co., Ltd. | Preparación sólida fácilmente administrable |
CN101919817B (zh) * | 2010-07-23 | 2012-05-30 | 山东齐都药业有限公司 | 一种拉呋替丁胃内滞留控制释放组合物 |
KR101870004B1 (ko) | 2011-09-30 | 2018-06-22 | 모찌다 세이야쿠 가부시끼가이샤 | 복용 용이성 고형 제제 |
DE102012102414A1 (de) | 2012-03-21 | 2013-10-10 | Michael Dittgen | Pharmazeutische Zusammensetzung für die einmal tägliche Anwendung antidiabetischer Arzneimittel wie Metformin mit Zwei-Puls-Freisetzung |
WO2013168179A2 (en) * | 2012-04-03 | 2013-11-14 | Rubicon Research Private Limited | Controlled release pharmaceutical formulations of antiviral agents |
CN103110601B (zh) * | 2013-02-04 | 2014-10-29 | 成都恒瑞制药有限公司 | 一种格列齐特胃漂浮片及其制备方法 |
FR3014692B1 (fr) * | 2013-12-18 | 2016-01-29 | Ethypharm Sa | Compositions pharmaceutiques orales a retention gastrique. |
TWI705814B (zh) * | 2014-06-20 | 2020-10-01 | 美商梅琳塔有限責任公司 | 醫藥組成物及其用途 |
CA3017797A1 (en) | 2016-03-17 | 2017-09-21 | Thiogenesis Therapeutics, Inc. | Compositions for controlled release of cysteamine and systemic treatment of cysteamine sensitive disorders |
CN107184560B (zh) * | 2017-06-03 | 2021-02-02 | 寿光富康制药有限公司 | 二甲双胍胃滞留片及制备方法 |
US11612576B2 (en) | 2017-09-20 | 2023-03-28 | Thiogenesis Therapeutics, Inc. | Methods for the treatment of cysteamine sensitive disorders |
JP2021506984A (ja) * | 2017-12-18 | 2021-02-22 | トリス・フアルマ・インコーポレーテツド | トリガーパルス薬物放出を有する胃内滞留型raft形成システムを含む放出調節薬物粉末組成物 |
EP3737353A1 (en) | 2017-12-18 | 2020-11-18 | Tris Pharma, Inc. | Ghb pharmaceutical compositions comprising a floating interpenetrating polymer network forming system |
CN109602714B (zh) * | 2018-12-29 | 2020-06-12 | 广东中润药物研发有限公司 | 一种利伐沙班胃滞留片及其制备方法 |
GB2599950A (en) * | 2020-10-16 | 2022-04-20 | Zentiva Ks | Pharmaceutical compositions with low amounts of nitrosamine impurities and methods for producing the same |
WO2022152741A1 (en) * | 2021-01-13 | 2022-07-21 | DuPont Nutrition USA, Inc. | A gastroretentive drug delivery system |
Family Cites Families (17)
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---|---|---|---|---|
JPS61148115A (ja) * | 1984-12-21 | 1986-07-05 | Tooa Eiyoo Kk | 難溶性薬物の徐放性製剤及びその製造法 |
GB8618847D0 (en) * | 1986-08-01 | 1986-09-10 | Smith Kline French Lab | Pharmaceutical formulations |
FR2653337B1 (fr) * | 1989-10-23 | 1992-02-07 | Dow Corning Sa | Element a liberation prolongee et procede pour le fabriquer. |
US6635280B2 (en) | 1997-06-06 | 2003-10-21 | Depomed, Inc. | Extending the duration of drug release within the stomach during the fed mode |
PT1003476E (pt) * | 1997-08-11 | 2005-05-31 | Alza Corp | Forma de dosagem de agente activo de libertacao prolongada adaptada para retencao gastrica |
IN186245B (ja) | 1997-09-19 | 2001-07-14 | Ranbaxy Lab Ltd | |
JP4523153B2 (ja) * | 1998-03-19 | 2010-08-11 | ブリストル−マイヤーズ スクイブ カンパニー | 易溶性薬物の二層性放出制御送達システムおよび方法 |
NZ523747A (en) * | 1998-09-14 | 2004-04-30 | Ranbaxy Lab Ltd | Pharmaceutical composition comprising a drug, a gas generating component, a swelling agent, a viscolyzing agent and a gel forning polymer |
KR100618234B1 (ko) * | 1998-12-23 | 2006-09-01 | 알자 코포레이션 | 다공성 입자를 포함하는 제형 |
US6797283B1 (en) | 1998-12-23 | 2004-09-28 | Alza Corporation | Gastric retention dosage form having multiple layers |
US6635281B2 (en) * | 1998-12-23 | 2003-10-21 | Alza Corporation | Gastric retaining oral liquid dosage form |
HUP0204417A3 (en) * | 2000-03-03 | 2005-03-29 | Ranbaxy Lab Ltd | Oral ciprofloxacin-composition of controlled release |
BR0211317A (pt) * | 2001-07-04 | 2004-12-14 | Sun Pharmaceutical Ind Ltd | Sistema para a liberação controlada de uma droga por meio de retenção gástrica |
AU2002302890A1 (en) * | 2002-02-04 | 2003-12-02 | Ranbaxy Laboratories Limited | Hydrodynamically balancing oral drug delivery system with biphasic release |
GB0205253D0 (en) * | 2002-03-06 | 2002-04-17 | Univ Gent | Immediate release pharmaceutical granule compositions and a continuous process for making them |
WO2003101431A1 (en) | 2002-06-04 | 2003-12-11 | J.B. Chemicals & Pharmaceuticals Ltd. | Pharmaceutical composition for controlled drug delivery system |
WO2005060942A1 (en) * | 2003-12-19 | 2005-07-07 | Aurobindo Pharma Ltd | Extended release pharmaceutical composition of metformin |
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2005
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- 2006-07-19 EP EP06795542A patent/EP1904034A2/en not_active Withdrawn
- 2006-07-19 KR KR1020087003902A patent/KR101367814B1/ko active IP Right Grant
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BRPI0612901B1 (pt) | 2020-08-04 |
JP2009501777A (ja) | 2009-01-22 |
EP1904034A2 (en) | 2008-04-02 |
HK1122729A1 (en) | 2009-05-29 |
AU2006271314B2 (en) | 2011-07-07 |
US20080220060A1 (en) | 2008-09-11 |
KR20080048461A (ko) | 2008-06-02 |
RU2008106220A (ru) | 2009-08-27 |
KR101367814B1 (ko) | 2014-02-27 |
DE602005007205D1 (de) | 2008-07-10 |
BRPI0612901B8 (pt) | 2021-05-25 |
EP1745775A1 (en) | 2007-01-24 |
AU2006271314A1 (en) | 2007-01-25 |
CN101237858B (zh) | 2012-07-04 |
RU2376983C2 (ru) | 2009-12-27 |
US9629800B2 (en) | 2017-04-25 |
CA2616081C (en) | 2013-09-10 |
WO2007010400A3 (en) | 2007-04-05 |
BRPI0612901A2 (pt) | 2010-12-07 |
CN101237858A (zh) | 2008-08-06 |
CA2616081A1 (en) | 2007-01-25 |
ATE396710T1 (de) | 2008-06-15 |
WO2007010400A2 (en) | 2007-01-25 |
EP1745775B1 (en) | 2008-05-28 |
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