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クロスリンクされたコラーゲンの長作用注射用マイクロスフィアは,アリピプラゾールの生物利用性を高めるために固体分散をカプセル化します

Shanglun Li¹, Xiaoxuan Ji¹, Wei Huang¹

¹School of Pharmacy, Jiangsu University, Zhenjiang 212000, China.

Journal of pharmaceutical sciences

|February 13, 2026

まとめ

この研究では,統合失調症の治療順守を改善するために,アリピプラゾール (APZ) の新規注射用マイクロ球 (APZ@PVP@CC) が開発されました. この製剤は,APZの生物利用性を大幅に高め,30日間の持続的な放出を提供しました.

科学分野:

医薬品科学医薬品科学とは
バイオマテリアルエンジニアリング
薬物の配送システムです.

背景:

統合失調症のための口服アリピプラゾール (APZ) 製剤は,患者のコンプライアンス問題に直面しています.
APZの溶解性はpHの上昇とともに低下し,筋肉内注射の生物利用性を制限する.
これらの制約を克服するために,新しい注射用製剤が必要である.

研究の目的:

溶解性と生物利用性を向上させるアリピプラゾール注射用製剤 (APZ@PVP@CC) を開発する.
統合失調症の管理を改善するための長期間有効な配達システムを構築する.
クロスリンクされたコラーゲンマイクロスフィアの内部でのAPZ固体分散の準備を最適化するために.

主な方法:

ポリビニルピロリドン (PVP) ベースのAPZ固体分散 (APZ@PVP) を単軸電気スプレーで最適化しました.
合成されたクロスリンクコラーゲン (CC) とコーティングされたAPZ@PVPはコアシアル電気スプレーを使用しています.
SEM,XRD,in vitro放出研究,およびウサギの薬理学分析を用いてAPZ@PVP@CCを特徴づけました.

主要な成果:

APZ@PVP固体分散は,APZの溶解性を15倍に増加させ,in vitro放出を強化しました.
APZ@PVP@CCは,Hixson-Crowellモデル (表面浸食) に従って,30日間にわたって持続的な放出を示した.
製薬動態学的研究では,マイクロ結晶と比べて,生物利用度と30日間の長期放出が225%増加することが示されました.

結論:

APZ@PVP@CCの微球は,アリピプラゾールの有望な注射用製剤を提供している.
この製剤は,APZの生物利用性を高め,持続的な放出を提供し,統合失調症の治療における適合性と有効性の問題に対処します.
開発されたマイクロスフィアは,統合失調症の長期的な治療のための改良された効果的な選択肢を表しています.

キーワード:

アリピプラゾール (aripiprazole) とは生物学的利用可能性クロスリンクされたコラーゲン.長期作用の注射用マイクロスフィア固体分散固体の分散

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