JP2014193919A - シトルリンおよびアルギニンを含有する即効性血中アルギニン濃度上昇型経口剤 - Google Patents
シトルリンおよびアルギニンを含有する即効性血中アルギニン濃度上昇型経口剤 Download PDFInfo
- Publication number
- JP2014193919A JP2014193919A JP2014119457A JP2014119457A JP2014193919A JP 2014193919 A JP2014193919 A JP 2014193919A JP 2014119457 A JP2014119457 A JP 2014119457A JP 2014119457 A JP2014119457 A JP 2014119457A JP 2014193919 A JP2014193919 A JP 2014193919A
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- JP
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- Prior art keywords
- arginine
- salt
- citrulline
- blood
- oral preparation
- 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.)
- Granted
Links
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Abstract
【解決手段】血中アルギニン濃度を上昇させる必要のある被験体及び血流を促進させる必要のある被験体に対して、1回あたりの摂取量が、シトルリンまたはその塩およびアルギニンまたはその塩の総量として、遊離のシトルリンおよびアルギニンに換算して200mg〜3gであり、シトルリンまたはその塩およびアルギニンまたはその塩の組成比が、遊離のシトルリンおよびアルギニンに換算した重量比で1:2〜2:1となるように調整された経口剤を摂取させる工程を含む方法。血流を促進させることにより、肩凝り、冷え症、むくみ及び勃起不全から選ばれる症状に対して効果を有する。
【選択図】なし
Description
[1]シトルリンまたはその塩およびアルギニンまたはその塩を有効成分として含有する、即効性血中アルギニン濃度上昇型経口剤。
[2]シトルリンまたはその塩を有効成分として含有する経口剤と、アルギニンまたはその塩を有効成分として含有する経口剤を含む、キットまたはセット形態の即効性血中アルギニン濃度上昇型経口剤。
[3]血流促進用である、上記[1]または[2]に記載の経口剤。
[4]血流低下から生じる症状の予防または改善用である、上記[1]または[2]に記載の経口剤。
[5]血流低下から生じる症状が、肩凝り、冷え症、むくみおよび勃起不全より選ばれる少なくとも一つの症状である、上記[4]に記載の経口剤。
[6]血中アンモニア濃度の上昇抑制用である、上記[1]または[2]に記載の経口剤。
[7]血中アンモニア濃度の上昇から生じる症状の予防または改善用である、上記[1]または[2]に記載の経口剤。
[8]血中アンモニア濃度の上昇から生じる症状が、運動後の筋肉疲労または疲労感である、上記[7]に記載の経口剤。
[9]即効性血中アルギニン濃度上昇型経口剤を製造するための、シトルリンまたはその塩およびアルギニンまたはその塩の使用。
[10]即効性血流促進用経口剤を製造するための、シトルリンまたはその塩およびアルギニンまたはその塩の使用。
[11]血流低下から生じる症状の即効的な予防または改善用経口剤を製造するための、シトルリンまたはその塩およびアルギニンまたはその塩の使用。
[12]即効性血中アンモニア濃度上昇抑制用経口剤を製造するための、シトルリンまたはその塩およびアルギニンまたはその塩の使用。
[13]血中アンモニア濃度の上昇から生じる症状の即効的な予防または改善用経口剤を製造するための、シトルリンまたはその塩およびアルギニンまたはその塩の使用。
[14]即効的に血中アルギニン濃度を上昇させるための方法であって、即効的にアルギニンの血中濃度を上昇させる必要のある被験体に、該被験体の血中アルギニン濃度を即効的に上昇させるのに十分な量のシトルリンまたはその塩およびアルギニンまたはその塩を投与する工程を含む、方法。
[15]即効的に血流を促進させるための方法であって、即効的に血流を促進させる必要のある被験体に、該被験体の血流を促進させるのに十分な量のシトルリンまたはその塩およびアルギニンまたはその塩を投与する工程を含む、方法。
[16]血流低下から生じる症状を即効的に予防または改善するための方法であって、即効的に該症状の予防または改善の必要な被験体に、該被験体の該症状を予防または改善するのに十分な量のシトルリンまたはその塩およびアルギニンまたはその塩を投与する工程を含む、方法。
[17]即効的に血中アンモニア濃度の上昇を抑制するための方法であって、即効的に血中アンモニア濃度の上昇を抑制する必要のある被験体に、該被験体の血中アンモニア濃度上昇を抑制するのに十分な量のシトルリンまたはその塩およびアルギニンまたはその塩を投与する工程を含む、方法。
[18]血中アンモニア濃度の上昇から生じる症状を即効的に予防または改善するための方法であって、即効的に該症状の予防または改善の必要な被験体に、該被験体の該症状を予防または改善するのに十分な量のシトルリンまたはその塩およびアルギニンまたはその塩を投与する工程を含む、方法。
15匹の9週齢雄性SDラット(日本エスエルシー株式会社)の頸静脈にカテーテルを留置し、3日間予備飼育した後、3群に分けた。非絶食下にて、一匹あたりL−シトルリンまたはL−アルギニンが2.85mmol/kgとなるように(それぞれ499.3mg/kgおよび496.5mg/kg)、それぞれ第1群、第2群のラットにゾンデにて経口投与した。さらに、一匹あたりL−シトルリンおよびL−アルギニンを1.43mmol/kgずつとなるように(それぞれ250.5mg/kgおよび249.1mg/kg)、第3群のラットにゾンデにて経口投与した。
図1にて、投与後30分および1時間において、第1群(L−シトルリン投与群)および第2群(L−アルギニン投与群)と比較して、第3群(L−シトルリンおよびL−アルギニン投与群)では有意な最高血中濃度(Cmax)の上昇および最高血中濃度到達時間(Tmax)の短縮が認められた。
14週齢雄性ニュージーランドウサギ(北山ラベス株式会社)を購入し、28日間予備飼育した後、3群(n=3または4)に分けた。16時間絶食させた後、一羽あたりL−シトルリンまたはL−アルギニンが2.85mmol/kgとなるように(それぞれ499.3mg/kgおよび496.5mg/kg)、それぞれ第1群、第2群のウサギにゾンデにて経口投与した。さらに、一羽あたりL−シトルリンおよびL−アルギニン1.43mmol/kgずつとなるように(それぞれ250.5mg/kgおよび249.1mg/kg)、第3群のウサギにゾンデにて経口投与した。
L−シトルリン68.1kg、L−アルギニン68.1kg、微結晶セルロース36.0kg、ショ糖脂肪酸エステル6.6kg、リン酸カルシウム1.2kgおよびβ-シクロデキストリン20.0kgを、コニカルブレンダーで混合する。得られる混合物をロータリー圧縮成形機で圧縮成形して錠剤を製造する。
実施例1で製造する錠剤の表面をシェラック溶液でコーティングして、腸溶錠剤を製造する。
L−シトルリン68.1kg、L−アルギニン68.1kg、微結晶セルロース36.0kg、ショ糖脂肪酸エステル6.6kg、リン酸カルシウム1.2kgおよびβ-シクロデキストリン20.0kgを、コニカルブレンダーで混合する。得られる混合物20kgと0.2kgの二酸化ケイ素とを混合攪拌して得られた混合物をカプセル充填機に投入し、ハードカプセルに充填してハードカプセルを得る。得られるハードカプセルの表面をツェイン溶液でコーティングして腸溶カプセルを製造する。
L−シトルリン0.64kg、L−アルギニン0.64kg、エリスリトール3kg、クエン酸0.05kg、人工甘味料3g、香料0.06kgを液温70℃で水50Lに攪拌溶解し、クエン酸でpHを3.3に調整後、プレート殺菌を用いて滅菌して瓶に充填する。次いで、パストライザー殺菌し、飲料を製造する。
L−シトルリン1.00kg、L−アルギニン0.28kg、エリスリトール3kg、クエン酸0.05kg、人工甘味料3g、香料0.06kgを液温70℃で水50Lに攪拌溶解し、クエン酸でpHを3.3に調整した後、プレート殺菌を用いて滅菌して瓶に充填する。次いで、パストライザー殺菌し、飲料を製造する。
Claims (8)
- 血中アルギニン濃度を上昇させる必要のある被験体に、1回あたりの摂取量が、シトルリンまたはその塩およびアルギニンまたはその塩の総量として、遊離のシトルリンおよびアルギニンに換算して200mg〜3gであり、シトルリンまたはその塩およびアルギニンまたはその塩の組成比が、遊離のシトルリンおよびアルギニンに換算した重量比で1:2〜2:1となるように調整された経口剤を摂取させる工程を含む、血中アルギニン濃度を上昇させるための方法(但し、ヒトに対する医療行為を除く)。
- 経口剤を摂取させた後1時間以内に血中アルギニン濃度を上昇させる、請求項1記載の方法。
- 血流を促進させる必要のある被験体に、1回あたりの摂取量が、シトルリンまたはその塩およびアルギニンまたはその塩の総量として、遊離のシトルリンおよびアルギニンに換算して200mg〜3gであり、シトルリンまたはその塩およびアルギニンまたはその塩の組成比が、遊離のシトルリンおよびアルギニンに換算した重量比で1:2〜2:1となるように調整された経口剤を摂取させる工程を含む、血流を促進させるための方法(但し、ヒトに対する医療行為を除く)。
- 経口剤を摂取させた後40分以内に血流を促進させる、請求項3記載の方法。
- 該症状の予防または改善の必要な被験体に、1回あたりの摂取量が、シトルリンまたはその塩およびアルギニンまたはその塩の総量として、遊離のシトルリンおよびアルギニンに換算して200mg〜3gであり、シトルリンまたはその塩およびアルギニンまたはその塩の組成比が、遊離のシトルリンおよびアルギニンに換算した重量比で1:2〜2:1となるように調整された経口剤を摂取させる工程を含む、血流低下から生じる症状を予防または改善するための方法(但し、ヒトに対する医療行為を除く)。
- 経口剤を摂取させた後1時間以内に血流低下から生じる症状を改善させる、請求項5記載の方法。
- 経口剤を摂取させた後40分以内に血流低下から生じる症状を改善させる、請求項5記載の方法。
- 血流低下から生じる症状が、肩凝り、冷え症、むくみおよび勃起不全より選ばれる少なくとも一つの症状である、請求項5〜7のいずれか1項に記載の方法。
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