JP6130946B2 - 抗感染剤の徐放 - Google Patents
抗感染剤の徐放 Download PDFInfo
- Publication number
- JP6130946B2 JP6130946B2 JP2016029641A JP2016029641A JP6130946B2 JP 6130946 B2 JP6130946 B2 JP 6130946B2 JP 2016029641 A JP2016029641 A JP 2016029641A JP 2016029641 A JP2016029641 A JP 2016029641A JP 6130946 B2 JP6130946 B2 JP 6130946B2
- Authority
- JP
- Japan
- Prior art keywords
- amikacin
- liposomal
- phosphatidylcholine
- lipid
- complexed
- 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.)
- Expired - Lifetime
Links
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- NLVFBUXFDBBNBW-PBSUHMDJSA-N tobramycin Chemical compound N[C@@H]1C[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N NLVFBUXFDBBNBW-PBSUHMDJSA-N 0.000 claims description 32
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- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 description 1
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- A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
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Description
とりわけ、有効量のリポソーム性/複合体形成した抗感染剤を、患者に肺投与するステップを含む、嚢胞性線維症患者における肺感染症を治療又は改善する方法が提供され、この場合、(i)投与される量は、相対的遊離薬物量の50%以下であるか、又は(ii)投薬は1日一回以下であるか、又は(iii)両者、である。
回以下、である。
本出願は、脂質ベースの粒子に封入された抗感染剤(例えば抗生物質)の投与を含む、嚢胞性線維症患者などにおいて肺感染を治療又は改善する方法を開示するものである。
模で減少させるために有効な最小遊離薬物(それはもちろん、塩であってもよい)の50%以下、35%以下、20%以下、又は10%以下である。相対的遊離薬物とは、本発明の薬物投与に適用される投薬期間で用いられるであろう蓄積量である。本段落で定義された該相対的最小遊離薬物とは「相対的遊離薬物量」である。
ベシクルの開発に基礎となる。
たい。
メラベシクル(SPLV)と命名されており、Fountainらの米国特許第4,588,578号に解説された通りの単相ベシクルと、上に解説された通りの凍結解凍された多層ラメラベシクル(FATMLV)と含有する。
対称のフィルタを使用することもできる。
結果を以下の表1に示す。
isolates of Pseudomonas aeruginosaandentericgram-negative bacilli to Amikacinand other aminoglycosideantibiotics.JInfect Dis 134:S394-90 (1976).15.Pile,J.C.,Malone, J.D.,Eitzen,E.M.,Friedlander,A.M.,Anthrax as a potentialbiological warfare agent.Arch. Intern.Med. 158:429-434(1998).16. Gleiser,C.A.,Berdjis, C.C., Hartman, H.A.,& Glouchenour,W.S.,Pathologyofexperimental respiratory anthrax inMacacamulatta. Brit.J. Exp.Path.,44:416-426(1968).
Claims (9)
- 複数のリポソーム中に封入されたアミノグリコシドを含む組成物であって、該リポソームの脂質成分は、ホスファチジルコリン及びステロールを含み、該脂質成分とアミノグリコシドとの重量比が2.5:1未満であり、該組成物が、マイコバクテリア肺感染症の治療のために患者にネブライザ・スプレーとして肺投与するためのものである、組成物。
- 前記マイコバクテリア肺感染症が、マイコバクテリウム・アヴィウム複合体(M.avium complex)(マイコバクテリウム・アヴィウム(M.avium)及びマイコバクテリウム・イントラセルラ(M.intracellulare))肺感染症である、請求項1に記載の組成物。
- 前記ホスファチジルコリンがジパルミトイルホスファチジルコリン(DPPC)である、請求項1または請求項2に記載の組成物。
- 前記ホスファチジルコリンが、卵ホスファチジルコリン(EPC)、大豆ホスファチジルコリン(SPC)、水素化した卵ホスファチジルコリン(HEPC)、水素化した大豆ホスファチジルコリン(HSPC)、ジパルミトイルホスファチジルコリン(DPPC)、ジオレオイルホスファチジルコリン(DOPC)、ジミリストイルホスファチジルコリン(DMPC)、ジステアロイルホスファチジルコリン(DSPC)、パルミトイルステアロイルホスファチジルコリン(PSPC)、およびこれらの混合物からなる群より選択される、請求項1または請求項2に記載の組成物。
- 前記患者への肺投与は一日に1回以下である、請求項1〜4のいずれか一項に記載の組成物。
- 前記リポソームが、0.1乃至3.0μmの間の直径を有する、請求項1〜5のいずれか一項に記載の組成物。
- 前記アミノグリコシドが、ストレプトマイシン、ゲンタマイシン、トブラマイシン、ネチルミシン、またはカナマイシンである、請求項1〜6のいずれか一項に記載の組成物。
- 前記アミノグリコシドがアミカシンである、請求項1〜6のいずれか一項に記載の組成物。
- 前記アミカシンがアミカシンスルフェートである、請求項8に記載の組成物。
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