JP6572257B2 - アリピプラゾールの経口速溶性組成物 - Google Patents
アリピプラゾールの経口速溶性組成物 Download PDFInfo
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- JP6572257B2 JP6572257B2 JP2017097367A JP2017097367A JP6572257B2 JP 6572257 B2 JP6572257 B2 JP 6572257B2 JP 2017097367 A JP2017097367 A JP 2017097367A JP 2017097367 A JP2017097367 A JP 2017097367A JP 6572257 B2 JP6572257 B2 JP 6572257B2
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- aripiprazole
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- oral administration
- seconds
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- 238000000638 solvent extraction Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 239000000892 thaumatin Substances 0.000 description 1
- 235000010436 thaumatin Nutrition 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- FGMPLJWBKKVCDB-UHFFFAOYSA-N trans-L-hydroxy-proline Natural products ON1CCCC1C(O)=O FGMPLJWBKKVCDB-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
(2)前記担体がゼラチンである、上記(1)に記載の医薬組成物。
(3)マトリックス形成剤、糖、環状糖、アミノ酸、保存剤、界面活性剤、粘性増強剤、着色剤、調味料、pH調整剤、甘味剤及びそれらの組合せからなる群から選択した追加的成分をさらに含む、上記(1)又は(2)に記載の組成物。
該経口投与用医薬組成物が流体と接触した状態で10秒以内に崩壊し、急速に該活性成分を放出するように設計された急速分散投与剤型の形態をとる限り、上記担体は薬学的に許容できるいかなる担体であってもよい。好ましい担体はウシゼラチン、ブタゼラチン又は魚ゼラチンのようなゼラチンである。特にウシゼラチンが好ましい。
この発明に使用するのに適したその他の追加的成分としては、マンニトール、デキストロース、ラクトース、ガラクトース、トレハロースなどの糖類;シクロデキストリンなどの環状糖類;リン酸ナトリウム、塩化ナトリウム、ケイ酸アルミニウム類などの無機塩類;グリシン、L−アラニン、L−アスパラギン酸、L−グルタミン酸、L−ヒドロキシプロリン、L−イソロイシン、L−ロイシン、L−フェニルアラニンなどの炭素原子数が2から12までのアミノ酸などが含まれる。好ましい追加的成分は、マンニトール、デキストロース、ラクトース又はガラクトースなどの糖類である。
混合容器中でゼラチン及びマンニトールを純水に加え、これを次いで混合しながら約60℃に加熱した。混合をゼラチンが完全に溶解するまで真空中で続けた。この混合物を冷却した。
冷却後、アリピプラゾール、無水クエン酸及びアスパルテームを混合物に加えた。この混合を溶解性の成分が溶解し、完全に薬剤粒子が分散するまで続け、室温(約23℃)で均質化した。
各成分の割合を表1に示す。
崩壊試験は、現行の日本薬局方 一般試験方法 崩壊試験法(1)即放性製剤により行った。試験液として水を用い、補助盤は用いなかった。
試験6個につき、それぞれの崩壊時間を秒単位で記録した。
崩壊試験の結果:0〜4秒
Claims (1)
- 活性成分としてのアリピプラゾールとウシゼラチン、マンニトール、クエン酸及びアスパルテームからなる経口投与用凍結乾燥錠剤であって、流体と接触した状態で10秒以内に崩壊し、急速に該活性成分を放出するように設計された急速分散投与剤型の錠剤の形態である上記経口投与用凍結乾燥錠剤。
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AU691195B2 (en) * | 1993-07-09 | 1998-05-14 | R.P. Scherer Corporation | Method for making freeze dried drug dosage forms |
ATE185266T1 (de) * | 1994-01-27 | 1999-10-15 | Univ Oklahoma | Schnell auflösende orale darreichungsform |
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