JP2009507048A - 1日1回投与用トラゾドン組成物 - Google Patents
1日1回投与用トラゾドン組成物 Download PDFInfo
- Publication number
- JP2009507048A JP2009507048A JP2008529431A JP2008529431A JP2009507048A JP 2009507048 A JP2009507048 A JP 2009507048A JP 2008529431 A JP2008529431 A JP 2008529431A JP 2008529431 A JP2008529431 A JP 2008529431A JP 2009507048 A JP2009507048 A JP 2009507048A
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- Prior art keywords
- pharmaceutical composition
- trazodone
- release pharmaceutical
- sustained
- composition according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Abstract
Description
トラゾドンは、通常使用されるその塩酸塩形態で示される式のトリアゾロピリジン誘導体である。この化合物の製剤は、1968年に公表されたG. Palazzoらの米国特許No. 3,381,009 に初めて開示された。
本発明は、1日1回経口投与用又はトラゾドン若しくはその誘導体用の徐放性医薬組成物を提供する。当該組成物は、約15質量%〜約60質量%のトラゾドン又はその誘導体、及び約15質量%〜約60質量%の放出制御性(controlled release)賦形剤を含む。当該放出制御性賦形剤は、哺乳動物、例えば、ヒトへ経口的に投与される場合に、トラゾドン又はその誘導体が投与開始の少なくとも約1時間後〜少なくとも約24時間後、有効血漿中濃度に達することを可能にする。いくつかの状況下では、当該放出制御性賦形剤は、トラゾドン又はトラゾドン誘導体が消化管上部及び消化管下部の両方を通過する間に吸収され得るように、トラゾドン又はその誘導体の実質的にpH非依存的な放出制御を提供する。
当該徐放性製剤は、鬱病の症状の1つ以上を治療する、すなわち改善するのに有効なトラゾドン又はトラゾドン誘導体の血漿中濃度を少なくとも24時間提供する。他の実施態様において、当該徐放性製剤は、睡眠障害を治療するために、例えば睡眠構築(sleep architecture)を改善するために有効な量のトラゾドン又はトラゾドン誘導体を提供する。
当該徐放性医薬組成物は、経口投与に適した錠剤及びカプレットのような種々の形状(shape)並びに形態(form)中に処方することができる。ある実施態様において、本発明は、300mgのトラゾドンを含むカプレットを提供する。そのようなカプレットは、就寝前投与用に適合させることができる。そのような製剤は、経口投与後速やかに傾眠を引き起こすが、それにもかかわらず、即放性トラゾドン組成物の反復投与と比較して、患者において経口投与の約8時間後に実質的に全く眠気を提供しない。
さらに、本発明は、その治療を必要とするヒトの睡眠構築(sleep architecture)を改善する方法であって、前記ヒトへ上記の徐放性医薬組成物の1つを1日1回投与することを含む、前記方法を提供する。当該組成物は、好ましくは就寝前に投与される。
本発明を、添付の図面により例証するが、限定するものではない。
本発明は一つには、トラゾドン又はトラゾドン誘導体の1日1回製剤であって、1つ以上の鬱病の系の治療、すなわちこれらを改善するのに有効な、1時間〜24時間の間、本質的に安定な当該活性成分の血漿中濃度を提供する、前記トラゾドン又はトラゾドン誘導体の1日1回製剤を処方することが可能であるという発見に基づく。この発見は驚くべきものであるが、その理由は、トラゾドンの溶解性がpH依存的でありかつ消化管下部で見出される高いpHで速やかに減少するにもかかわらず、腸管上部及び腸管下部を通したpH変化に無関係に少なくとも24時間血流中のトラゾドンの治療的濃度、安定的濃度及び/又は有効濃度を提供することが可能なことが見出されたためである。
さらに、同一製剤又は同様の製剤を、睡眠障害を治療するため、例えば、睡眠構築を改善するために使用することが可能である。当該放出制御性賦形剤は、哺乳動物、例えばヒトへ経口的に投与される場合に、トラゾドン又はその誘導体が、睡眠障害を治療するための有効血漿中濃度を達成することを可能にする。そのような製剤は、投与後速やかに(例えば、1時間以内に)傾眠を引き起こすが、それにもかかわらず、即放性トラゾドン組成物の反復投与と比較して、患者において経口投与の約8時間後に実質的に全く眠気を提供しない。
本明細書で熟慮される当該徐放性トラゾドン製剤は、例えば、投与される(例えば、1日2回又は3回)即放性製剤のAUC(曲線下面積)に関して生物学的に同等である有効血漿中濃度を有していてもよい。当該AUCは、与えられる薬物の長期にわたる身体への総曝露量を評価するための数学上の計算であり、薬剤の濃度 対 時間のプロットの曲線下面積を意味する。AUCは、投薬スケジュールの指針として使用され、また、身体における種々の薬物製剤の生物学的利用能を比較するのに使用される。
別の実施態様において、当該放出制御性賦形剤は、好ましくは架橋ハイアミロースデンプン、例えば当該架橋ハイアミロースデンプンがオキシ塩化リンによって架橋されており及び/又はヒドロキシプロピル側鎖を含む、前記架橋ハイアミロースデンプンを含む。いくつかの実施態様において、当該架橋ハイアミロースデンプンは、約65質量%〜約75質量%のアミロースを含み、オキシ塩化リンによって架橋される。適した賦形剤は、登録商標CONTRAMID(登録商標)として Labopharm, Inc., Laval, Canada により開発されたものであり、かつここから入手可能である。当該CONTRAMID(登録商標)賦形剤の合成は、参照によってその全てがあらゆる目的のために本明細書に取り込まれる、例えば、米国特許No. 6,607,748 に記載されている。本明細書で熟慮される組成物は、1つ以上の追加的な制御放出賦形剤と共に、架橋ハイアミロースデンプンを含んでいてもよい。
本発明の組成物は通常、錠剤の形態で調製される。当業者によく知られるとおり、当該錠剤は、広範な形状を採用することができるが、好ましい形状はカプレットである。当該カプレットは、当業界で知られるとおり、例えば、上部及び下部パンチ(upper and lower punches)を使用して形成してもよい。いくつかの実施態様において、錠剤は被覆を含んでいてもよく、例えば着色料を含むコーティング(coating)を含んでいてもよい。適したコーティングの例としては、ポリビニルアルコール、タルク、マクロゴールなど、及びそれらの混合物のような水性フィルムコーティングポリマーが挙げられる。適した着色料の例としては、酸化鉄、レーキ(lake)、天然着色料及び当業者に知られる別の着色料が挙げられる。
本明細書に記載される当該組成物はまた、睡眠困難を有する及び/又は崩壊した(disrupted)睡眠構築、すなわち、崩壊した(disrupted)ノンレム/レム段階及び崩壊した(disrupted)睡眠の周期基礎構造を有する患者を治療するのにも有用である。いくつかの実施態様において、本明細書に開示される製剤は経口投与後1時間以内に治療的有効量のトラゾドンの一部を放出し、従って速やかに傾眠を誘導するが、それにもかかわらず、即放性トラゾドン組成物の反復投与と比較して、患者において経口投与の約8時間後に実質的に全く眠気を提供しない。結果的に、当該製剤は、就業時間又は日中の好ましくない眠気を低減する。
本発明をここに、以下の実施例を手段として説明するが、これは例証の目的のためにのみ提示されるものであり、本発明の範囲を限定することをいっさい意図しない。
当該インビボ実験は、製剤1の経口投与の後、容認できる(acceptable)血漿中濃度に到達するための短期間の後に、トラゾドンの血漿中濃度が投与後約1時間〜投与後少なくとも24時間、比較的一定レベルに維持されたことを実証する。
本発明をその好ましい実施態様を手段として説明してきたが、添付の特許請求の範囲において定義されるとおり、本発明が、本発明の精神及び範囲から逸脱することなくその広範な態様を包含することが理解される。
Claims (42)
- 約15質量%〜約60質量%のトラゾドン又はその誘導体、及び約15質量%〜約85質量%の放出制御性賦形剤を含む1日1回経口投与用の徐放性医薬組成物であって、哺乳動物へ投与される際に、前記放出制御性賦形剤が、前記トラゾドン又はその誘導体が投与開始の少なくとも約1時間後〜少なくとも約24時間後、有効血漿中濃度を維持することを可能にする、前記徐放性医薬組成物。
- 前記血漿中濃度が哺乳動物の鬱病の治療に有効である、請求項1記載の徐放性医薬組成物。
- 前記血漿濃度が哺乳動物の睡眠障害の治療に有効である、請求項1又は2記載の徐放性医薬組成物。
- 塩酸トラゾドンを含む、請求項1〜3のいずれか1項記載の徐放性医薬組成物。
- 前記放出制御性賦形剤が、投与後約1時間〜約24時間にわたる間、実質的に一定のままである約50ng/mL〜約3000ng/mLの血漿中トラゾドン濃度を提供する、請求項1〜4のいずれか1項記載の徐放性医薬組成物。
- 150mgの塩酸トラゾドンを含む、請求項1記載の徐放性医薬組成物。
- 経口摂取の1時間後に達成される前記血漿中トラゾドン濃度が約150ng/mL〜約500ng/mLである、請求項6記載の徐放性医薬組成物。
- 300mgの塩酸トラゾドンを含む、請求項1記載の徐放性医薬組成物。
- 投与開始の1時間後の前記血漿中トラゾドン濃度が約300ng/mL〜約1000ng/mLである、請求項8記載の徐放性医薬組成物。
- 約20質量%〜約50質量%のトラゾドン又はトラゾドン誘導体、及び約20質量%〜約50質量%の放出制御性賦形剤を含む、請求項1〜9のいずれか1項記載の徐放性医薬組成物。
- 約35質量%〜約50質量%のトラゾドン又はトラゾドン誘導体、及び約15質量%〜約50質量%の放出制御性賦形剤を含む、請求項10記載の徐放性医薬組成物。
- 前記放出制御性賦形剤が架橋ハイアミロースデンプンを含む、請求項1〜11のいずれか1項記載の徐放性医薬組成物。
- 前記架橋ハイアミロースデンプンが、約65質量%〜約75質量%のアミロースを含み、オキシ塩化リンによって架橋される、請求項12記載の徐放性医薬組成物。
- 前記架橋ハイアミロースデンプンがヒドロキシプロピル側鎖を含む、請求項13記載の徐放性医薬組成物。
- 前記架橋ハイアミロースデンプンがゼラチン化される、請求項14記載の徐放性医薬組成物。
- 医薬添加剤をさらに含む、請求項1〜14のいずれか1項記載の徐放性医薬組成物。
- 前記医薬添加剤が結合剤、可溶化剤、酸性化剤、造孔剤、潤滑剤又は流動促進剤から選択される、請求項16記載の徐放性医薬組成物。
- 前記結合剤がヒドロキシプロピルメチルセルロースを含む、請求項17記載の徐放性医薬組成物。
- 前記可溶化剤がポビドン又は塩化セチルピリジニウムから選択される、請求項17記載の徐放性医薬組成物。
- 前記酸性化剤がアルギン酸を含む、請求項17記載の徐放性医薬組成物。
- 前記造孔剤がスクロースを含む、請求項17記載の徐放性医薬組成物。
- 前記潤滑剤がナトリウムステアリルフマラートを含む、請求項17記載の徐放性医薬組成物。
- 前記流動促進剤がコロイド状二酸化ケイ素を含む、請求項17記載の徐放性医薬組成物。
- 前記哺乳動物がヒトである、請求項1〜3のいずれか1項記載の徐放性医薬組成物。
- 約20質量%〜約50質量%の塩酸トラゾドン、約20質量%〜約50質量%の架橋ハイアミロースデンプン、約10質量%〜約25質量%のヒドロキシプロピルメチルセルロース、約0質量%〜約5質量%の塩化セチルピリジニウム、約0質量%〜約20質量%のアルギン酸、約1質量%〜約5質量%のナトリウムステアリルフマラート、及び約1質量%までのコロイド状二酸化ケイ素を含む、徐放性医薬組成物。
- 錠剤の形態である、請求項1〜25のいずれか1項記載の徐放性医薬組成物。
- 前記錠剤がカプレット形態に成形される、請求項26記載の徐放性医薬組成物。
- 前記カプレットが約300mgのトラゾドンを含む、請求項27記載の徐放性医薬組成物。
- 就寝前投与用に適合される、請求項1〜28のいずれか1項記載の徐放性医薬組成物。
- 即放性トラゾドン組成物の反復投与と比較して、ヒトにおいて経口投与の約8時間後に実質的に全く眠気を提供しない、請求項29記載の徐放性医薬組成物。
- 約20質量%〜約40質量%の放出制御性賦形剤を含む、300mgの塩酸トラゾドンの1日1回経口投与用の単位用量の徐放性医薬組成物であって、経口的に摂取される際に、3錠が24時間の間投与される市販の100mg力価×3錠の塩酸トラゾドン錠剤の1日用量と実質的に等価な濃度−時間曲線下面積を提供する、前記単位用量の徐放性医薬組成物。
- 約30質量%〜約50質量%の放出制御性賦形剤を含む、150mgの塩酸トラゾドンの1日1回経口投与用の単位用量の徐放性医薬組成物であって、経口的に摂取される際に、3錠が24時間の間投与される市販の50mg力価×3錠の塩酸トラゾドン錠剤の1日用量と実質的に等価な濃度−時間曲線下面積を提供する、前記単位用量の徐放性医薬組成物。
- 放出制御性賦形剤中にトラゾドン又はトラゾドン誘導体を含む徐放性医薬組成物を、睡眠障害のヒトへ投与することを含む、睡眠障害の治療方法。
- 請求項1〜32のいずれか1項記載の徐放性医薬組成物を、睡眠障害のヒトへ投与することを含む、睡眠障害の治療方法。
- 前記障害が治療されて睡眠構築が改善される、請求項33又は34記載の方法。
- 前記組成物が就寝前に投与される、請求項35記載の方法。
- 請求項1〜32のいずれか1項記載の徐放性医薬組成物を、鬱病のヒトへ1日1回投与することを含む、鬱病の治療方法。
- 前記組成物が就寝前に投与される、請求項37記載の方法。
- 鬱病の治療のための、請求項1〜32のいずれか1項記載の徐放性医薬組成物の使用。
- 鬱病の治療に有用な組成物の製造のための、請求項1〜32のいずれか1項記載の徐放性医薬組成物の使用。
- 睡眠障害の治療のための、請求項1〜32のいずれか1項記載の徐放性医薬組成物の使用。
- 睡眠障害の治療に有用な組成物の製造のための、請求項1〜32のいずれか1項記載の徐放性医薬組成物の使用。
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2015
- 2015-02-23 US US14/628,971 patent/US20150306041A1/en not_active Abandoned
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2016
- 2016-04-07 US US15/093,468 patent/US20160361262A1/en not_active Abandoned
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2017
- 2017-09-04 AR ARP170102452A patent/AR109571A2/es not_active Application Discontinuation
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JP2004501957A (ja) * | 2000-06-29 | 2004-01-22 | レナーツ,ビンセンツ | 徐放性医薬製剤に利用する架橋高アミローススターチとその製造方法 |
WO2004037222A2 (en) * | 2002-10-25 | 2004-05-06 | Labopharm Inc. | Sustained-release tramadol formulations with 24-hour efficacy |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2014221788A (ja) * | 2007-08-03 | 2014-11-27 | アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニAziende Chimiche Riunite Angelini Francesco A.C.R.A.F.Societa Per Azioni | 精製された形態のトラゾドンおよびトラゾドン塩酸塩 |
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