JP5180092B2 - インスリン感受性を増すための組成物および方法 - Google Patents
インスリン感受性を増すための組成物および方法 Download PDFInfo
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- JP5180092B2 JP5180092B2 JP2008542399A JP2008542399A JP5180092B2 JP 5180092 B2 JP5180092 B2 JP 5180092B2 JP 2008542399 A JP2008542399 A JP 2008542399A JP 2008542399 A JP2008542399 A JP 2008542399A JP 5180092 B2 JP5180092 B2 JP 5180092B2
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- insulin
- compound
- composition
- blood glucose
- zonisamide
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Description
治療を必要とする血中グルコース状態を有する対象を同定する工程、および、
前記対象に、血中グルコース濃度を調節するのに有効な量の組成物を投与する工程であって、前記組成物が、非スルファメート抗けいれん剤;精神治療薬;オピオイドアンタゴニスト;精神治療薬とオピオイドアンタゴニストとの組み合わせ;精神治療薬と抗けいれん剤との組み合わせ;オピオイドアンタゴニストと抗けいれん剤との組み合わせ;および、オピオイドアンタゴニストと抗けいれん剤と精神治療薬との組み合わせから選択される少なくとも1つを含む工程
を含む方法が提供される。
用語「血中グルコース状態」とは、患者のグルコース濃度を調節するのが望ましい状態を指す。幾つかの実施態様においては、血中グルコース状態は、血中グルコース濃度を低下するのが望ましい状態を含む。例えば、高い血中グルコース濃度は、血中グルコース状態であり得る。他の実施態様においては、血中グルコース状態は、血中グルコース濃度を、特定の値に、または値の範囲に維持するのが望ましい状態を含む。更に他の実施態様においては、血中グルコース状態は、血中グルコース濃度を増やすのが望ましい状態を含む。幾つかの実施態様においては、本明細書で開示した方法および組成物は、最初に血中グルコース濃度を低下させ、その後、血中グルコース濃度を、特定の値に、または値の範囲に維持するのに使用することができる。血中グルコース状態は、患者が、血中グルコース状態を発症する危険を有する状態を含む。1つの実施態様においては、インスリン耐性は、血中グルコース状態である。他の実施態様においては、糖尿病は、血中グルコース状態である。
前記で論じたように、1つの態様においては、血中グルコース状態を治療または阻害するためのBGM組成物を、提供する。一般的に、これらのBGM組成物は、オピオイドアンタゴニスト(例えばナルトレキソン)、MC3-R/MC3-Rアゴニストまたはα-MSH活性増加剤(例えば精神治療薬)、および抗けいれん剤(例えばゾニサミド)からなる群から選択される1つまたは複数の化合物を含む。非-スルファメート抗けいれん剤は、好ましくは、BGM量のオピオイドアンタゴニスト、MC3-R/MC3-Rアゴニストまたはα-MSH活性増加剤を含まないBGM組成物中に含まれる。同様に、抗けいれん剤を、BGM量のオピオイドアンタゴニスト、MC3-R/MC3-Rアゴニストまたはα-MSH活性増加剤と組み合わせて投与しない場合、抗けいれん剤は、好ましくは、非-スルファメート抗けいれん剤である。これらのBGM組成物は、インスリン耐性の阻害に有効な量で使用することができる。付加的に、これらは、1型もしくは2型糖尿病、または前記した疾患を含むグルコースの異常調節の任意の疾患を、阻害または治療するのに使用することができる。幾つかの実施態様においては、BGM組成物は、インスリンを更に含み、インスリン耐性が生じる危険性を低下させながら、1型糖尿病などの血中グルコース状態を治療するのに使用することができる。付加的に、BGM組成物とインスリンとの組み合わせは、追加の外因性インスリンを、対象に投与することを可能とすることによって、疾患のインスリン耐性の側面を、1つまたは複数の前記化合物によって解決しながら、2型糖尿病などの血中グルコース状態を治療するのに使用することができる。BGM組成物は、有効量の、任意の1つの化合物、または、化合物とインスリンとの任意の組み合わせを含みうる。幾つかの実施態様においては、使用する各化合物およびインスリンの量は、少なくとも有効量であり、好ましくは、顕著な望ましくない副作用をもたらす量よりも少ない。幾つかの実施態様においては、この量は、少なくとも有効量である、おおよその必要最低限量である。
Wは、窒素、CH、酸素または硫黄であり;
R1は、水素、置換されていてもよいC1-6アルキル、置換されていてもよいC3-8シクロアルキル、置換されていてもよいC2-6アルケニル、置換されていてもよいC2-6アルキニル、置換されていてもよいC1-6アルコキシアルキル、ならびに置換されていてもよいアリールおよびアリールアルキルからなる群から選択され;
R2、R3、R4およびR5は、それぞれ、独立に、水素、ハロゲン、置換されていてもよいC1-6アルキル、置換されていてもよいC1-8アルキルオキシ、置換されていてもよいC2-6アルケニル、置換されていてもよいC2-6アルキニル、置換されていてもよいC1-6アルコキシアルキル、置換されていてもよいC1-6アルキルチオ、パーハロアルキル、CN、COR10、CONHR10、ヘテロアルキル、およびNO2からなる群から選択され;
R6、R7、R8およびR9は、それぞれ、独立に、水素、ハロゲン、置換されていてもよいC1-6アルキル、置換されていてもよいC1-6アルキルオキシ、置換されていてもよいC2-6アルケニル、置換されていてもよいC2-6アルキニル、置換されていてもよいC1-6アルコキシアルキル、置換されていてもよいC1-6アルキルチオ、パーハロアルキル、CN、COR10、CONHR10、ヘテロアルキル、およびNO2からなる群から選択され;
R10は、C1-6アルキルである)
他の態様においては、本発明は、血中グルコース状態を阻害する方法であって、それを必要とする個体を同定する工程、その個体を、血中グルコース濃度を調節するのに有効な量の本明細書に開示するBGM組成物を用いて処理する工程を含む方法に関する。実施態様においては、BGM組成物は、精神治療薬(例えば、α-MSH活性増加剤)および抗けいれん剤を含む。精神治療薬および抗けいれん剤は、前記に開示したものである。幾つかの実施態様においては、前記BGM組成物および以下の方法を、2型糖尿病を阻害するために使用する。他の態様においては、これらを、1型糖尿病を阻害するために使用する。幾つかの実施態様においては、これらを、インスリンとともに投与して、対象に投与するインスリンの量を少なくすることを可能にする。幾つかの実施態様においては、方法は、治療または予防措置を必要とする対象を同定する工程、および、その後に前記化合物またはBGM組成物を対象に投与する工程を含む。場合によっては、外因性インスリンも、対象に投与することができる。好ましくは、化合物またはインスリンの量は、副作用を最小化するのに十分なほど低いが、血中グルコース状態を阻害するのに十分有効なほど高い。1つの実施態様においては、血中グルコース状態は、精神治療薬および/または抗けいれん剤の投与によって引き起こされる。
他の態様においては、本発明は、前記した、精神治療薬、抗けいれん剤および/もしくはインスリンの組み合わせを含む、または、前記した、結合した分子、および生理学的に許容可能な担体、希釈剤もしくは賦形剤、もしくはそれらの組み合わせを含む医薬組成物に関する。
本発明の医薬組成物の厳密な調合、投与経路および投与量は、個々の医師が患者の状態に照らし合わせて選択することができる。(例えば、Finglら、1975、「The Pharmacological Basis of Therapeutics」、第1章、1頁を参照されたい。)典型的には、患者に投与される組成物の投与量範囲は、患者の体重の約0.5から1000mg/kgであり得る。投与量は、患者の必要に応じて、単一投与量であってもよいし、1日間以上の過程に与えられる一連の2つ以上の投与量であってもよい。本開示に記載されている具体的な化合物およびインスリンのほぼすべてについて、少なくとも幾つかの状態を治療するためのヒト投与量が確立されたことに留意されたい。したがって、たいていの場合、本発明は、それらの同じ投与量、または確立されたヒト投与量の約0.1%から500%、約1%から約500%、約10%から約500%、約25%から約500%、約50%から約500%、約100%から約500%、約250%から約500%、約0.1%から約250%、約1%から約250%、約10%から約250%、約25%から約250%、約50%から約250%、約100%から約250%、約0.1%から約100%、約1%から約100%、約10%から約100%、約25%から約100%、約50%から約100%、約0.1%から約50%、約1%から約50%、約10%から約50%、約25%から約50%、約0.1%から約25%から約1%から約25%、約10%から約25%、約0.1%から約10%、約1%から約10%または約0.1%から1%の投与量を用いることになる。新たに発見された医薬化合物の場合のように、ヒト投与量が確立されていない場合は、好適なヒト投与量をED50またはID50値、あるいは動物における毒性試験および効能試験によって裏づけられた、インビトロまたはインビボ試験から導かれた他の適切な値から推断することができる。インスリンの投与量については、幾つかの実施態様においては、他の化合物の効果が原因で、単位投与量として、より少ない量が必要となる。しかしながら、このより少ない投与量は、本明細書に開示する手法および方法を使用することによって、ならびに、当業者の知識によって、容易に求めることができる。
本発明の実施態様の幾つかを、以下に記す。
インスリンを摂取する個体を同定する。各個体を、インスリン治療に加えて、1つの25mgの錠剤のゾニサミドを、一日当りに摂取するように指導する。
インスリンを摂取する個体を同定する。各個体を、インスリン治療に加えて、1つの25mgの錠剤のトピラメートを、一日当りに摂取するように指導する。
インスリンを摂取する個体を同定する。各個体のインスリンの投与スキームだけでなく、インスリンの特定の投与量から得られる個体の血糖値にも着目する。
インスリン耐性に罹患した個体を同定する。個体に投与したインスリンの量(インスリンの最初の濃度)および個体の血糖値に対するそのインスリンの影響を求める。
インスリン耐性を発症する危険を有する個体を同定する。各個体を、一日当り1つの50mgの錠剤のゾニサミドを摂取するように指導する。加えて、各個体を、一日当り1つの250mgの錠剤のブプロピオンを摂取するように指導する。
2型糖尿病の個体を同定する。個体の血糖値およびインスリンの一日の投与量をモニターする。個体に、一日当り50mgのゾニサミドおよび250mgのブプロピオンを投与する。個体の血糖値を再度測定する。個体に投与したインスリンの量を、適宜減少させて、望む血糖値を維持する。インスリンの量の低下が必要でないならば(例えば、個体が以前に投与したインスリンが、あまり多くない場合)、ゾニサミドおよびブプロピオンの量を、投与したインスリンの量を減らすことができるまで、増やすことができる。必要であるならば、追加の量のインスリンを個体に投与することができる。それ故、個体は、2型糖尿病を治療することができる。
マウス(n=3)に一晩餌を与え、その後、以下の1つを腹腔内(I.P.)注入した:ベヒクル、フルオキセチン(8.5mg/kg)、ナルトレキソン(2.5mg/kg)またはフルオキセチン+ナルトレキソン(8.5mgフルオキセチン、2.5mg/kgナルトレキソン)。ベースライン血糖値の測定を、注入2時間後に実施した。その後、マウスに、インスリンの標準的なI.P.注入を行った。血糖値を、その後、2時間にわたって追跡した(15分、30分、1時間および2時間)。結果を、ベヒクル、フルオキセチン、ナルトレキソンおよびナルトレキソン+ブプロピオンのそれぞれについて、表1-4に要約する。グルコース濃度は、mg/dlである。
マウス(n=12)を、ベヒクル、ナルトレキソン(3mg/kg)、ブプロピオン(50mg/kg)またはナルトレキソン(3mg/kg)+ブプロピオン(50mg/kg)を用いて処理した以外は、実施例7で開示したのと同じ試験を行った。曲線下の領域(AUC)を、各マウスの各時点でのグルコース濃度に基づいて計算した。AUCは、各時点で観察されたグルコース濃度の合計である。マウスについてのAUC値は以下のようであった(ND=測定せず):
ベヒクル:13575、10485、ND、12038、9353、9990、8160、ND、14258、10883、12555および10065 (平均値 = 11136.2)
ブプロピオン:13613、9083、11438、ND、14003、9668、8003、10725、8715、8715、12038、11280 (平均値 = 10661.91、この値は、ベヒクルのAUCの95.7%であり、AUCの4.3%の低下を表す)
ナルトレキソン:11445、ND、7208、14783、7215、13058、10493、9045、8003、10193、10763、15990 (平均値 = 10745.09、この値は、ベヒクルのAUCの96.5%であり、AUCの3.5%の低下を表す)
ナルトレキソン+ブプロピオン:7740、7680、12300、8685、ND、8775、ND、8550、12300、8625、ND、ND (平均値 = 9331.875、この値は、ベヒクルのAUCの83.8%であり、AUCの16.2%の低下を表す)
実験開始時に約235グラムの雌のSprague-Dawleyラットを使用した。試験を始める前の2週間にわたって、ゾニサミドベヒクルを使用して、注入を見せかけるように訓練した。イイソフルランの麻酔の元で、Alzet浸透圧ミニポンプ(2ml2)を、肩甲骨の間に、皮下移植した。そして、ラットを、回復後、すみかのケージへと戻した。ミニポンプは、14日間にわたり、一時間当り5μl伝達した。オランザピンを、dH2Oを用いて1.5%の乳酸中に溶かした。ゾニサミドを、10%のDMSO、13.4%のEtOH、20.1%のPPG、および66.5%の生理食塩水に溶かした。オランザピンの投与量は、1.75mg/dayであった。動物を個々に飼育し、標準的な実験用の餌を与えた。消費した食物および動物の体重を、毎日記録した。コントロール(ベヒクル)群として5匹の動物を用い、ゾニサミドのみの群として5匹の動物を用い、オランザピンのみの群として5匹の動物を用い、オランザピン+ゾニサミドの群として6匹の動物を用いた。
Claims (8)
- 対象とするヒト受領者における、インスリン耐性によって特徴付けられる血中グルコース状態の治療用組成物であって、ブプロピオンもしくはその医薬的に許容可能な塩、及びナルトレキソンもしくはその医薬的に許容可能である塩であるオピオイドアンタゴニストである、第1の化合物と第2の化合物との組み合わせを含む、組成物。
- 前記状態が、2型糖尿病である、請求項1に記載の組成物。
- 第1の化合物と第2の化合物の少なくとも1つが徐放性調合物中にある、請求項1または2に記載の組成物。
- 第1の化合物と第2の化合物のそれぞれが徐放性調合物中にある、請求項1から3のいずれか
一項に記載の組成物。 - 前記第1の化合物を前記第2の化合物とは別個に対象に投与する、請求項1から4のいずれ
か一項に記載の組成物。 - 前記第1の化合物と前記第2の化合物が単一の経口剤形中にある、請求項1から4のいずれ
か一項に記載の組成物。 - 前記単一経口剤形が錠剤、ピルまたはカプセルの形態にある、請求項6に記載の組成物。
- さらにインスリンを含む、請求項1から7のいずれか一項に記載の組成物。
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