JP2007332163A - プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 - Google Patents
プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 Download PDFInfo
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- JP2007332163A JP2007332163A JP2007242364A JP2007242364A JP2007332163A JP 2007332163 A JP2007332163 A JP 2007332163A JP 2007242364 A JP2007242364 A JP 2007242364A JP 2007242364 A JP2007242364 A JP 2007242364A JP 2007332163 A JP2007332163 A JP 2007332163A
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Abstract
【解決手段】カロリー摂取量の制限と組合せて患者の体重を減少させるための医薬の製造や、体脂肪を減少させるのに充分であり、且つ食事によるカロリー制限に通常伴う体の非脂肪性部分の削減を抑える若しくは伴わない、プロラクチン阻害剤の使用を特徴とする。該プロラクチン阻害剤の使用を、カロリー摂取量の制限と組合せて患者のII型糖尿病、インスリン抵抗性、高血糖症、高インスリン症、又はグルコース不耐症を治療することができる。
【選択図】なし
Description
しかしながら、カロリー摂取量を削減するとすぐに代謝率が低下し、体重の低下が遅くなり、さらには停止することにもなることが文献に示されている。さらに、カロリー削減を中止し、無制限な食生活が再開されると、代謝率が低いために、体重が急激に増加する。結果的に、カロリー制限によって体重制御を行なおうとする試みの大半は、失敗するか若しくは極僅かに成功するのみであり、どのような利点も長続きしない。実際、多くの場合、被検者はダイエットを開始する前よりも結局体重が増加している。さらに、体重を減少させるためには、通常大幅なカロリー制限(例えばダイエット前のカロリー摂取量の50%)が必要である。
図1を参照のこと。プロラクチンプロフィールを変更すると同時に被検者に適度にカロリーを削減したダイエットを行なわせると、所定時刻にプロラクチン阻害剤を投与して被検者の異常プロラクチンプロフィールを変更することにより、プロラクチン阻害剤処置のみの場合にみられる差異と比較して、上記の代謝指標の一つ以上が相乗的に改善される。
本発明の方法によれば、治療される被検者の食事のカロリー量は、好ましくは適度に削減される(例えば体重維持のために必要なカロリー摂取量の90〜70%まで)が、断食レベルまで削減するものではない。被検者は、開始時の体重を維持するために必要なカロリーの70%を消費することが好ましいが、被検者がヒトである場合の総カロリー摂取量は1日当たり1200カロリー未満まで削減してはならない。この30%の削減のために食事のどの要素を削減しても省略してもよいが、削減するカロリーの相当部分が脂肪分の削減であることが望ましい。さらに、ある特定の一回の食事を抜くのではなく、各食事について比較的一定にカロリーを削減することが好ましい。好ましいダイエットは、ヴァージニア州アレクサンドリアのAmerican Diabetes Association(1986年のガイドラインに公布されたもの)が推奨する、ここから入手可能なダイエットである。
前述のカロリー摂取量の制限と組み合わせたプロラクチンレベルの変更は、基本的に本願と同一の発明者の先行する同時係属中の出願である米国特許願第07/995,292号に記載されているように行なう。便宜上、このプロラクチン変更方法を以下のように要約する。
(a)24時間に渡って比較的平坦な(ピークがない)高いレベルである(この場合、「高い」とは「日中」つまり活動時間のプロラクチンレベルよりも高いことをいう)
(b)24時間に渡って比較的平坦な(ピークがない)低いレベルである(この場合、「低い」とは「日中」つまり活動時間のプロラクチンレベル又はそれ未満をいう)
(c)「日中」にピークがあり、「夜間」が低レベルである(この場合、「低い」とは1:00〜4:00の正常な平均就寝時プロラクチン値よりも低いことを意味する)
(d)「日中」にピークがあり、「夜間」に第二のピークがある。
プロラクチンのピークが7:00〜10:00に現れる場合、ブロモクリプチンは7:00に投与する、
プロラクチンのピークが10:01〜16:00に現れる場合、ブロモクリプチンは8:00に投与する、
プロラクチンのピークが16:01〜19:00に現れる場合、ブロモクリプチンは9:00に投与する、
プロラクチンのピークが19:01〜22:00に現れる場合、ブロモクリプチンは10:00に投与する、
プロラクチンのピークが22:01〜1:00に現れる場合、ブロモクリプチンは10:00に投与する、
プロラクチンのピークが1:01〜7:00に現れる場合、ブロモクリプチンは投与しない、
プロラクチンのピークが現れず且つ活動時間中において高過ぎる場合には、ブロモクリプチンは7:00に投与する。
ダイエットとブロモクリプチンの所定時刻における投与との組合せの効果を、肥満、若しくは肥満であり且つ肥満及び/又はタイプII糖尿病に関する症状(グルコース耐性障害、正常なグリコシル化ヘモグロビン値以上、正常なトリグリセリドレベル以上、正常なコレステロール値以上等)を患っている多くの個体について試験した。個体を二つのグループに分割した。一つのグループには偽薬を与え(被検者がコントロール被検者でなければブロモクリプチンが投与されたであろう時刻に同時に)、30%カロリー制限ダイエットを行なった(体重維持に必要なカロリー数に基づいたが、患者の食習慣を考慮した)。推奨されたダイエットはADAダイエットであった。食事は、6:30〜7:30に朝食、12:00〜13:00に昼食、そして17:30〜18:30に夕食を定期的に取ることが勧められた。20:30〜21:30に軽食を取ることが許容された。別のグループは同じダイエットを行ない、且つブロモクリプチンを投与された(5:00〜13:00に経口で0.8mgから3.2mg/日)。
Claims (11)
- カロリー摂取量の制限と組合せて患者の体重を減少させるための医薬の製造におけるプロラクチン阻害剤の使用。
- カロリー摂取量の制限と組合せて患者の体脂肪を選択的に減少させるための医薬の製造におけるプロラクチン阻害剤の使用であって、カロリー摂取量の制限と組合せた該医薬の投与が、体脂肪を減少させるのに充分であり、且つ食事によるカロリー制限に通常伴う体の非脂肪性部分の削減を抑える若しくは伴わない、プロラクチン阻害剤の使用。
- カロリー摂取量の制限と組合せて患者のII型糖尿病、インスリン抵抗性、高血糖症、高インスリン症、又はグルコース不耐症を治療するための医薬の製造におけるプロラクチン阻害剤の使用。
- 前記プロラクチン阻害剤がドーパミン作動薬である、請求項1〜3のいずれか1項に記載の使用。
- 前記プロラクチン阻害剤がブロモクリプチンである、請求項1〜3のいずれか1項に記載の使用。
- ブロモクリプチンの日毎の投与量が0.8〜3.2mgの範囲内である、請求項5に記載の使用。
- 前記プロラクチン阻害剤の投与期間が約10〜約180日間である、請求項1〜5のいずれか1項に記載の使用。
- 前記プロラクチン阻害剤の一回目の投与を5:00〜13:00の間に行う、請求項1〜5のいずれか1項に記載の使用。
- 前記プロラクチン阻害剤の一回目の投与を5:00〜10:00の間に行い、二回目の投与を9:00〜13:00の間に行う、請求項1〜5のいずれか1項に記載の使用。
- 前記カロリー摂取量の制限が、患者の体重維持に必要とされるカロリー数の70〜90%である、請求項1〜5のいずれか1項に記載の使用。
- 前記カロリー摂取量の制限が、患者の体重維持に必要とされるカロリー数の70%であり、且つ1日あたり1200カロリーを下回らない、請求項1〜5のいずれか1項に記載の使用。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US08/178,569 US5744477A (en) | 1988-05-10 | 1994-01-07 | Method for treatment of obesity using prolactin modulators and diet |
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JP7518718A Division JPH09510960A (ja) | 1994-01-07 | 1995-01-06 | プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 |
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JP2007332163A true JP2007332163A (ja) | 2007-12-27 |
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JP7518718A Withdrawn JPH09510960A (ja) | 1994-01-07 | 1995-01-06 | プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 |
JP2007242364A Pending JP2007332163A (ja) | 1994-01-07 | 2007-09-19 | プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 |
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JP7518718A Withdrawn JPH09510960A (ja) | 1994-01-07 | 1995-01-06 | プロラクチンモジュレータ及びダイエットを利用して肥満を治療する方法 |
Country Status (12)
Country | Link |
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US (2) | US5744477A (ja) |
EP (1) | EP0808164B1 (ja) |
JP (2) | JPH09510960A (ja) |
AT (1) | ATE290863T1 (ja) |
AU (1) | AU1569395A (ja) |
CA (1) | CA2180479C (ja) |
DE (1) | DE69534084T2 (ja) |
DK (1) | DK0808164T3 (ja) |
ES (1) | ES2239316T3 (ja) |
MX (1) | MX9602701A (ja) |
PT (1) | PT808164E (ja) |
WO (1) | WO1995018614A1 (ja) |
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US5668155A (en) * | 1988-05-10 | 1997-09-16 | The General Hospital Corporation | Administration of pirenzepine, methyl scopolamine and other muscarinic receptor antagonists for treatment of lipid metabolism disorders |
RU2233654C2 (ru) | 1998-11-20 | 2004-08-10 | Ртп Фарма Инк. | Диспергируемые стабилизированные фосфолипидом микрочастицы |
US20030082647A1 (en) * | 2000-12-12 | 2003-05-01 | Reenan Robert A. | Transporter protein |
WO2002059310A2 (en) | 2000-12-12 | 2002-08-01 | University Of Connecticut | Polynucleotides encoding cellular transporters and methods of use thereof |
WO2002067901A1 (en) * | 2001-02-22 | 2002-09-06 | Skyepharma Canada Inc. | Fibrate-statin combinations with reduced fed-fasted effects |
US20040018959A1 (en) * | 2002-05-02 | 2004-01-29 | Randall S. Hickle | System and methods of lipid removal from the body |
US9655865B2 (en) | 2002-07-29 | 2017-05-23 | Veroscience, Llc | Therapeutic treatment for metabolic syndrome, type 2 diabetes, obesity, or prediabetes |
US20040081678A1 (en) * | 2002-08-09 | 2004-04-29 | Anthony Cincotta | Therapeutic process for the treatment of obesity and associated metabolic disorders |
US8821915B2 (en) | 2002-08-09 | 2014-09-02 | Veroscience, Llc | Therapeutic process for the treatment of the metabolic syndrome and associated metabolic disorders |
US20100035886A1 (en) | 2007-06-21 | 2010-02-11 | Veroscience, Llc | Parenteral formulations of dopamine agonists |
US8741918B2 (en) | 2007-06-21 | 2014-06-03 | Veroscience Llc | Parenteral formulations of dopamine agonists |
WO2008157845A1 (en) | 2007-06-21 | 2008-12-24 | Veroscience, Llc | Method of treating metabolic disorders and depression with dopamine receptor agonists |
PL386294A1 (pl) | 2008-10-16 | 2010-04-26 | Ryszka Florian Biochefa Farmaceutyczny Zakład Naukowo-Produkcyjny | Sposób przyśpieszenia rozwoju prosiąt ssących |
US9352025B2 (en) | 2009-06-05 | 2016-05-31 | Veroscience Llc | Combination of dopamine agonists plus first phase insulin secretagogues for the treatment of metabolic disorders |
PL389116A1 (pl) * | 2009-09-24 | 2011-03-28 | Ryszka Florian Biochefa Farmaceutyczny Zakład Naukowo-Produkcyjny | Sposób przyśpieszenia rozwoju ssaków użytkowych |
US8431155B1 (en) | 2012-04-30 | 2013-04-30 | Veroscience Llc | Bromocriptine formulations |
CN109689057A (zh) | 2016-04-20 | 2019-04-26 | 维罗技术有限责任公司 | 用于治疗代谢失调的组合物和方法 |
EP3697418B1 (en) | 2017-10-18 | 2024-07-24 | VeroScience LLC | Improved bromocriptine formulations |
US11607455B2 (en) | 2019-09-23 | 2023-03-21 | Veroscience Llc | Method for inducing tumor regression |
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YU216177A (en) * | 1977-09-09 | 1984-02-29 | Rudolf Rucman | Process for preparing 2-bromo ergosine |
IT1157365B (it) * | 1977-10-24 | 1987-02-11 | Sandoz Ag | Medicamenti per trattare l'obesita' o ridurre il peso del corpo |
US4749709A (en) * | 1986-03-07 | 1988-06-07 | Louisiana State University And Agricultural And Mechanical College | Method of inhibiting body fat stores |
US4659715A (en) * | 1986-03-07 | 1987-04-21 | Louisiana State University And Agricultural And Mechanical College | Method of inhibiting body fat stores |
US4783469A (en) * | 1986-03-07 | 1988-11-08 | Meier Albert H | Method of inhibiting body fat stores |
DE3722383A1 (de) * | 1986-07-14 | 1988-01-28 | Sandoz Ag | Neue verwendung von bromocriptin |
US5344832A (en) * | 1990-01-10 | 1994-09-06 | The Board Of Supervisors Of Louisiana University And Agricultural And Mechanical College | Method for the long term reduction of body fat stores, insulin resistance, hyperinsulinemia and hyperglycemia in vertebrates |
US5585347A (en) * | 1988-05-10 | 1996-12-17 | Ergo Science Incorporated | Methods for the determination and adjustment of prolactin daily rhythms |
US5006526A (en) * | 1988-10-17 | 1991-04-09 | Louisiana State University | Method of treating a vertebrate animal to reduce plasma triglycerides and cholesterol levels and to alleviate and prevent atherosclerosis |
CA2030174C (en) * | 1990-01-10 | 1996-12-24 | Anthony H. Cincotta | Process for the long term reduction of body fat stores, insulin resistance, hyperinsulinemia and hypoglycemia in vertebrates |
FI904677A (fi) * | 1990-09-24 | 1992-03-25 | Ahlstroem Consumer Prod | Foerfarande foer inpackning av steriliseringsomslag. |
US5316367A (en) * | 1990-12-20 | 1994-05-31 | Audi Ag | Bearing structure for the bodywork of a vehicle |
HUT67688A (en) * | 1991-12-23 | 1995-04-28 | Univ Louisiana State | Preparations for treating pathologies of type ii |
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- 1994-01-07 US US08/178,569 patent/US5744477A/en not_active Expired - Lifetime
-
1995
- 1995-01-06 DK DK95907471T patent/DK0808164T3/da active
- 1995-01-06 AU AU15693/95A patent/AU1569395A/en not_active Abandoned
- 1995-01-06 PT PT95907471T patent/PT808164E/pt unknown
- 1995-01-06 EP EP95907471A patent/EP0808164B1/en not_active Expired - Lifetime
- 1995-01-06 DE DE69534084T patent/DE69534084T2/de not_active Expired - Lifetime
- 1995-01-06 ES ES95907471T patent/ES2239316T3/es not_active Expired - Lifetime
- 1995-01-06 JP JP7518718A patent/JPH09510960A/ja not_active Withdrawn
- 1995-01-06 CA CA002180479A patent/CA2180479C/en not_active Expired - Fee Related
- 1995-01-06 WO PCT/US1995/000663 patent/WO1995018614A1/en active IP Right Grant
- 1995-01-06 AT AT95907471T patent/ATE290863T1/de active
- 1995-01-06 MX MX9602701A patent/MX9602701A/es unknown
- 1995-05-10 US US08/438,650 patent/US5760047A/en not_active Expired - Lifetime
-
2007
- 2007-09-19 JP JP2007242364A patent/JP2007332163A/ja active Pending
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Also Published As
Publication number | Publication date |
---|---|
EP0808164B1 (en) | 2005-03-16 |
ES2239316T3 (es) | 2005-09-16 |
US5744477A (en) | 1998-04-28 |
AU1569395A (en) | 1995-08-01 |
US5760047A (en) | 1998-06-02 |
WO1995018614A1 (en) | 1995-07-13 |
MX9602701A (es) | 1997-04-30 |
DE69534084D1 (de) | 2005-04-21 |
EP0808164A4 (en) | 2001-02-07 |
ATE290863T1 (de) | 2005-04-15 |
PT808164E (pt) | 2005-05-31 |
DK0808164T3 (da) | 2005-06-27 |
CA2180479A1 (en) | 1995-07-13 |
JPH09510960A (ja) | 1997-11-04 |
CA2180479C (en) | 2009-10-06 |
DE69534084T2 (de) | 2006-02-09 |
EP0808164A1 (en) | 1997-11-26 |
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