JP7443663B2 - 改善された流動性を示す、リボフラビンを含有する薬剤 - Google Patents
改善された流動性を示す、リボフラビンを含有する薬剤 Download PDFInfo
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- JP7443663B2 JP7443663B2 JP2021521038A JP2021521038A JP7443663B2 JP 7443663 B2 JP7443663 B2 JP 7443663B2 JP 2021521038 A JP2021521038 A JP 2021521038A JP 2021521038 A JP2021521038 A JP 2021521038A JP 7443663 B2 JP7443663 B2 JP 7443663B2
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- JP
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- Prior art keywords
- active ingredient
- riboflavin
- composition
- spray
- amlodipine
- Prior art date
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Images
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Description
生物学的活性を有する成分は、その生物学的活性により、医薬品又は栄養補助食品として適するのであるが、その多くが結晶形で存在する。結晶は、物質の化学組成及び使用される精製又は結晶化の方法により、多くの形状をとり得る。結晶が板様の形状に、即ち略矩形で平らに構成されている場合、結晶はくっつき合う可能性があり、このため、加工する場合に困難が生じる。
1)アンジオテンシン変換酵素(ACE)阻害薬。これは血管を収縮させるホルモンであるアンジオテンシンの形成を妨げることで作用する。このクラスには、市販の薬物、例えば、エナラプリル、リシノプリル、ラミプリル、ペリンドプリル及びカプトプリルなどが含まれる。
2)アンジオテンシンII受容体遮断薬(ARB)。これはアンジオテンシンの作用を遮断することで機能するが、その形成は遮断しない。このクラスの市販の薬物の例としては、バルサルタン及びロサルタン他が挙げられる。
3)ベータ遮断薬、ベータアドレナリン遮断薬ともいう。これはホルモンであるエピネフリン(アドレナリン)の効果を遮断することで機能し、その結果、心臓の拍動をより遅く、その力をより弱くする。ベータ遮断薬の例としては、メトプロロール、ナドロール、アテノロール及びカルベジロールが挙げられる。
4)レニン阻害薬。これは、血圧の上昇に至る経路に関与する酵素であるレニンの産生を緩慢にする。これにはアリスキレンが含まれる。
5)カルシウムチャネル遮断薬は、心臓及び血管壁の細胞へのカルシウムの移動を緩慢にし、心臓がポンプ作用して血管を広げるのをより容易にする。例としては、アムロジピン、ジルチアゼム、フェロジピン、イスラジピン、ニカルジピン、ニフェジピン、ニソルジピン、アゼルニジピン及びベラパミルが挙げられる。
6)利尿薬-これは、腎臓が過剰な水を排泄するのを助けることで作用し、血管中に流体が少なくなり、このため、圧力を減少させ、心臓がポンプ作用するのをより容易にする。例としては、ヒドロクロロチアジド、クロロチアジド、インダパミド及びメトラゾンが挙げられる。
[発明の詳細な説明]
アスピリン(アセチルサリチル酸)、例えば、Jainら、2017、Eur J Pharma Sci 99:318-327を参照されたい。
アルテテル、抗マラリア薬物;例えば、Chadaら、2011、Acta Pharma Sinica B1(2):129-135を参照されたい。
エリスロマイシン、抗生物質;例えば、Mirzaら、2009、AAP PharmSCiTech 19(1)113-119を参照されたい。
シンバスタチン、抗コレステロール薬物;例えば、Bukovecら、Pharmazie71:263-268を参照されたい。
アムロジピン(図1を参照されたい)を含む種々の降圧剤。
a)活性成分を、噴霧乾燥したリボフラビンと混合して、活性成分及び噴霧乾燥したリボフラビンを含む組成物を得るステップ、
b)ステップa)の組成物の流速を決定するステップ、及び
c)ステップa)の組成物の流速を、リボフラビンが存在しない活性成分の流速と比較して、流動性が改善されているかどうかを判定するステップ
を含む、活性成分の流動性を改善する方法である。
a)降圧剤を、噴霧乾燥したリボフラビンと混合して、降圧剤及び噴霧乾燥したリボフラビンを含む組成物を得るステップ、
b)ステップa)の組成物の流速を決定するステップ、及び
c)ステップa)の組成物の流速を、リボフラビンが存在しない降圧剤の流速と比較して、流動性が改善されているかどうかを判定するステップ
を含む、降圧剤の流動性を改善する方法である。
活性成分は、その目的とする使用について当技術分野において公知の投与量で使用される。
[実施例1]
[方法]
[走査型電子顕微鏡法(SEM)]
試験した材料の形態を、走査型電子顕微鏡(TM3030、株式会社日立ハイテク、東京、日本)を倍率200で使用して解析した。
Pharmatest PTG-S4自動粉末特性評価機器(Pharma Test Apparatebau AG、ハンブルク(Hamburg)、ドイツ)を用いて、粉末流動性を決定した。このシステムは、現在の欧州薬局方(EP pharmacopoeia)<2.9.36/17>及び米国薬局方(USP pharmacopoeia)<1174>、並びに国際標準化機構(ISO)の国際規格4324に従って、顆粒及び粉末の流動挙動を測定する。
実施例1で概要を述べたものと同じ方法に従って、利尿薬であるヒドロクロロチアジドの流動性を、噴霧乾燥したリボフラビンを添加して、及び添加せずに測定した。結果を下の表2に示す。
実施例1で概要を述べたものと同じ方法に従って、ACE阻害薬であるエナラプリルの流動性を、噴霧乾燥したリボフラビンを添加して、及び添加せずに測定した。結果を下の表3に示す。
実施例1で概要を述べたものと同じ方法に従って、ベータ遮断薬であるアテノロールの流動性を、噴霧乾燥したリボフラビンを添加して、及び添加せずに測定した。結果を下の表4に示す。
[比較例]
上記の実施例1、2、3及び4に記載の方法を使用して、種々の降圧薬物の結晶をリボフラビンと混合した。結果を下に示す。
改善された流動性を示した実施例5の化合物を、粒径についてMalvern Morpho G3機器を使用してさらに検査した。「Vol.M.M」は、試料体積の大部分を占める粒子のサイズを反映している。粒径を測定した。結果を下に示す。
d(0.1)は全粒子の10%の直径を表し、d(0.5)は全粒子の50%の直径であり、d(0.9)は試料中の粒子の90%の直径を表す。
d(0.1)=25μm
d(0.5)=72μm
d(0.9)=163μm
Vol.M.M d(4,3):87μm
d(0.1)=147μm
d(0.5)=320μm
d(0.9)=478μm
Vol.M.M d(4,3):325μm
d(0.1)=123μm
d(0.5)=319μm
d(0.9)=551μm
Vol.M.M.d(4.3):337μm
d(0.1)=32μm
d(0.5)=129μm
d(0.9)=304μm
Vol.M.M.d(4,3):157μm
d(0.1)=36μm
d(0.5)=100μm
d(0.9)=218μm
Vol.M.M d(4,3):117μm
d(0.1)=44μm
d(0.5)=93μm
d(0.9)=172μm
Vol.M.M d(4,3):106μm
Claims (7)
- a)顕微鏡下で観察した場合の板状の結晶を少なくとも50体積%、又は、粒径及び粒子形状の解析機器によって測定した場合の球体及び不規則な球体を少なくとも50体積%含む活性成分;及び
b)噴霧乾燥したリボフラビン
を含む組成物であって、
前記活性成分がアムロジピン、フェロジピン、ヒドロクロロチアジド、エナラプリル及びアテノロール並びにこれらの薬学的に許容される塩からなる群から選択される、組成物。 - 前記活性成分と前記噴霧乾燥したリボフラビンとの間の重量比が10:1~1:10である、請求項1に記載の組成物。
- 前記活性成分が降圧剤である、請求項1又は2に記載の組成物。
- 前記降圧剤がカルシウムチャネル遮断薬である、請求項3に記載の組成物。
- アムロジピン又はアムロジピンベシル酸塩である、請求項1~4のいずれか一項に記載の組成物。
- 錠剤、カプセル剤、又は粉末剤の形態である、請求項1~5のいずれか一項に記載の組成物を含む経口製剤。
- a)活性成分を、噴霧乾燥したリボフラビンと混合して、活性成分及び噴霧乾燥したリボフラビンを含む組成物を得るステップ、
b)ステップa)の組成物の流速を決定するステップ、及び
c)ステップa)の組成物の流速を、リボフラビンが存在しない活性成分の流速と比較して、流動性が改善されているかどうかを判定するステップ
を含む、活性成分の流動性を改善する方法であって、
前記活性成分がアムロジピン、フェロジピン、ヒドロクロロチアジド、エナラプリル及びアテノロール並びにこれらの薬学的に許容される塩からなる群から選択される、方法。
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EP18204934 | 2018-11-07 | ||
EP18204935.3 | 2018-11-07 | ||
PCT/EP2019/077270 WO2020094319A1 (en) | 2018-11-07 | 2019-10-09 | Medicaments containing riboflavin exhibiting improved flowability |
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WO2005107759A1 (ja) | 2004-05-11 | 2005-11-17 | Daiichi Asubo Pharma Co., Ltd. | Bh4反応性高フェニルアラニン血症治療剤 |
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US1904699A (en) | 1929-05-24 | 1933-04-18 | James A Singmaster | Production of cement |
DE3682208D1 (de) | 1986-12-18 | 1991-11-28 | Kurt Heinz Bauer | Gegenueber lichteinfluss stabilisiertes nifedipin-konzentrat und verfahren zu seiner herstellung. |
US5034389A (en) * | 1989-07-28 | 1991-07-23 | Coors Biotech, Inc. | Riboflavin composition and method for production |
DE4014262A1 (de) | 1990-05-04 | 1991-11-07 | Basf Ag | Gut rieselfaehige, nichtstaubende bindemittelfreie riboflavinspruehgranulate oder -mikrogranulate aus reinem riboflavin und ein verfahren zu deren herstellung |
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US6093715A (en) | 1999-03-24 | 2000-07-25 | Basf Aktiengesellschaft | Process for producing riboflavin-containing granules |
US6723346B1 (en) | 1999-04-30 | 2004-04-20 | Roche Vitamins Inc. | Process for preparing spray granules containing riboflavin |
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