JP6789613B2 - 経口組成物 - Google Patents
経口組成物 Download PDFInfo
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- JP6789613B2 JP6789613B2 JP2015035882A JP2015035882A JP6789613B2 JP 6789613 B2 JP6789613 B2 JP 6789613B2 JP 2015035882 A JP2015035882 A JP 2015035882A JP 2015035882 A JP2015035882 A JP 2015035882A JP 6789613 B2 JP6789613 B2 JP 6789613B2
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- asperuloside
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- 239000000284 extract Substances 0.000 claims description 57
- ZJDOESGVOWAULF-OGJQONSISA-N Geniposidic acid Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1O[C@H]1[C@@H]2C(CO)=CC[C@@H]2C(C(O)=O)=CO1 ZJDOESGVOWAULF-OGJQONSISA-N 0.000 claims description 35
- VYAALAFRWREWLA-BVTMAQQCSA-N Geniposidic acid Natural products CCC1=CC[C@H]2[C@@H]1[C@H](O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)OC=C2C(=O)O VYAALAFRWREWLA-BVTMAQQCSA-N 0.000 claims description 35
- ZJDOESGVOWAULF-UHFFFAOYSA-N Geniposidinsaeure Natural products OC1C(O)C(O)C(CO)OC1OC1C2C(CO)=CCC2C(C(O)=O)=CO1 ZJDOESGVOWAULF-UHFFFAOYSA-N 0.000 claims description 35
- BZPMXJKRKXDRID-UOIKKKDVSA-N Scandoside Natural products OC[C@H]1O[C@@H](O[C@H]2CC=C([C@@H]3[C@@H](O)C=C(CO)[C@H]23)C(=O)O)[C@H](O)[C@@H](O)[C@@H]1O BZPMXJKRKXDRID-UOIKKKDVSA-N 0.000 claims description 35
- IBIPGYWNOBGEMH-DILZHRMZSA-N asperuloside Chemical compound O([C@@H]1OC=C2C(=O)O[C@H]3C=C([C@@H]1[C@H]32)COC(=O)C)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O IBIPGYWNOBGEMH-DILZHRMZSA-N 0.000 claims description 35
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- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Emergency Medicine (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Plant Substances (AREA)
Description
項1.(a)ゲニポシド酸、(b)アスペルロシド及び(c)クロロゲン酸を含有し、1日投与量中、成分(a)が50〜450mg、成分(b)が10〜300mgであり、成分(c)1重量部に対して、成分(a)が0.4〜2重量部、成分(b)が0.2〜2重量部である、経口組成物。
項2.血管内皮機能改善用組成物である、項1に記載の経口組成物。
項3.液状である、項1または2に記載の経口組成物。
試験例1:血管内皮機能改善確認試験
(1)経口組成物の調製
次の手順に従い経口組成物(実施例1)を調製した。
・杜仲葉の調製
杜仲の生葉5kgを、日本茶製造用の送帯蒸機により110℃で90秒間蒸熱した。具体的には、生葉を送帯蒸機の投入口から機内に投入し、ネットコンベヤ上を移動する間に上下スチーム供給装置からスチームを生葉に当て、110℃で90秒間蒸熱した。ネットコンベヤ上に杜仲生葉を広げ、ボイラーから供給される無圧蒸気を充満させた処理室を通過させることにより、杜仲生葉を蒸熱処理することができる。次いで、この蒸熱後の杜仲葉を揉捻機を用いて30分間揉捻した後、揉捻物を乾燥機を用いて80℃で5時間、水分量を5%になるまで乾燥させた。杜仲葉の色調が緑色を帯びた黒褐色に変化したことを確認し、炒葉機を用いて100℃で30分間焙煎し、杜仲葉乾燥物2kgを得た。
・杜仲葉抽出物の調製
前述のようにして得た杜仲葉乾燥物1kgを90℃の熱水15kgに投入し、90℃で30分間抽出し、14kgの抽出物を得た。これを150メッシュのフィルターを用いて濾過し、濾液を5℃に冷却し一晩放置した。次いで、上澄み液を取り出し、減圧下50℃で濾液を濃縮して濃縮液1kgを得た。この濃縮液を遠心分離機で処理して沈殿物を除去し、得られた上澄み液を85℃、2時間加熱殺菌し、杜仲葉抽出物を得た。
・経口組成物の調製
前述のようにして得た杜仲葉抽出物を、経口組成物350mL中にゲニポシド酸が85mg、アスペルロシドが22mgとなるように精製水で希釈して調整し、85℃で20分間加熱殺菌し、容器に充填して350mLの経口組成物(飲料)を得た。経口組成物350mLは350gに相当する。この際、杜仲葉抽出物1種を希釈等して飲料を調製することや2種以上の杜仲葉抽出物を混合、希釈等して所望の飲料を調製することもできるが、本試験例では1種の杜仲葉抽出物を用いて飲料を調製した。
[HPLC測定条件]
HPLC装置:LC−6(島津製作所社製)
カラム:YMC−Pack ODS A−312、φ6.0mm×150mm(YMC社製)
移動相:水/メタノール/リン酸=870/130/1(v/v)
カラム温度:40℃付近の一定温度
流速:1mL/分
検出器:UV検出器(測定波長:215nm)
ゲニポシド酸とアスペルロシドの含有量及び重量比は検量線法により算出した。
(2)血管内皮機能の評価試験
健常男女合計42名の被験者を2群に分け、一方の群に前述のようにして調製した経口組成物350mL/日を、もう一方の群にプラセボ組成物350mL/日を、12週間服用させた。該プラセボ組成物はゲニポシド酸及びアスペルロシドを含有しない組成物であり、水、着香剤、着色剤、pH調製剤を混合して目視において前記経口組成物と同様になるように調製し、対照として用いた。
%FMD=(最大拡張期血管径−安静時血管径)×100/安静時血管径
なお、本試験例では、前記組成物を服用させる前にも、各被験者の血管拡張率を同様にして測定、算出し、次の式に従って、服用前後の%FMDの変化量を更に算出した。
%FMDの変化量=服用後の%FMD−服用前の%FMD
(3)結果
結果を表1に示す。表1に示した値は、各被験者について求めた%FMD変化量の平均値である。
試験例2:風味確認試験
(1)経口組成物の調製
ゲニポシド酸、アスペルロシド及びクロロゲン酸が、後述の表4の含有量となるように経口組成物(実施例2〜5、比較例1)を調製した。具体的には、前記試験例1で得た杜仲葉抽出物にゲニポシド酸(商品名ゲニポシド酸標準品、和光純薬工業社製)、アスペルロシド、クロロゲン酸(商品名クロロゲン酸水和物、東京化成工業社製)、水を適宜添加して、後述する表4に示す各経口組成物を調製した。
[HPLC測定条件]
HPLC装置:LC−6(島津製作所社製)
カラム:YMC−Pack ODS A−312、φ6.0mm×150mm(YMC社製)
移動相:水/メタノール/リン酸=870/130/1(v/v)
カラム温度:40℃付近の一定温度
流速:1mL/分
検出器:UV検出器(測定波長:215nm)
アスペルロシドの含有量は検量線法により算出した。
(2)風味の評価試験
習熟したパネル合計5名に各経口組成物350mLを服用させ、苦味、渋味、酸味、甘み、すっきり感等を勘案して、総合的な飲みやすさを次の表2に示す5段階で評価させた。表2において値が大きいほど、飲みやすいことを示す。また、このように評価した値の合計値に基づいて、次の表3に示す基準に従って、風味について判定した。
判定結果を表4に示す。
処方例
以下に本発明の経口組成物の処方例を示すが、本発明はこれに限定されない。これらの経口組成物についても、前述の試験例と同様の効果が得られた。
飲料
前記試験例と同様にして杜仲葉抽出物、ゲニポシド酸(商品名ゲニポシド酸標準品、和光純薬工業社製)、アスペルロシド(試験例2に記載の調製物)、クロロゲン酸(商品名クロロゲン酸水和物、東京化成工業社製)、水を用いて、常法に従い次の表5に示す組成を有する飲料を製造した。
前述と同様にして杜仲葉抽出物、ゲニポシド酸、アスペルロシド、クロロゲン酸、その他の成分を用いて、常法に従い次の表6に示す組成を有するチュアブル剤を製造した。
前述と同様にして杜仲葉抽出物、ゲニポシド酸、アスペルロシド、クロロゲン酸、その他の成分を用いて、常法に従い次の表7に示す組成を有する飴剤を製造した。
Claims (3)
- (a)ゲニポシド酸、(b)アスペルロシド及び(c)クロロゲン酸を含有する杜仲葉抽出物配合経口組成物であって、
1日投与量中、成分(a)が50〜300mg、成分(b)が10〜150mgであり、
該経口組成物中、成分(c)1重量部に対して、成分(a)が0.6〜1.5重量部、成分(b)が0.2〜1.2重量部であり、
該経口組成物中、成分(c)が57/3500〜150/3500重量%であり、
該経口組成物が液状形態、または、散剤、顆粒剤、トローチ、チュアブル及び液状形態の凍結乾燥物からなる群より選択される少なくとも1種の固形形態である、
経口組成物。 - 血管内皮機能改善用組成物である、請求項1に記載の経口組成物。
- 液状形態である、請求項1または2に記載の経口組成物。
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