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非诺贝特与布洛芬的自分散低共熔混合物:可加工性与活性药物成分粒径

Self-dispersible eutectic mixtures with fenofibrate and ibuprofen: Processability and API particle size.

作者信息

Schlosser Peter, Bunjes Heike

机构信息

Technische Universität Braunschweig, Institut für Pharmazeutische Technologie und Biopharmazie, Mendelssohnstraße 1, 38106 Braunschweig, Germany; Technische Universität Braunschweig, Zentrum für Pharmaverfahrenstechnik, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany.

Technische Universität Braunschweig, Institut für Pharmazeutische Technologie und Biopharmazie, Mendelssohnstraße 1, 38106 Braunschweig, Germany; Technische Universität Braunschweig, Zentrum für Pharmaverfahrenstechnik, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany.

出版信息

Eur J Pharm Biopharm. 2025 Jun;211:114701. doi: 10.1016/j.ejpb.2025.114701. Epub 2025 Mar 23.

Abstract

In order to increase the dissolution rate of poorly water-soluble drugs, the preparation of eutectics is a practical way to minimize the drug particle size without the need of grinding and handling of poorly flowing powders. The use of solid self-dispersible excipients as a component of the eutectic may further enhance the drug dissolution rate. In the current study, phase diagrams of eutectic mixtures of polyethylene glycol stearates and polyethylene glycol stearyl ethers differing in their polyethylene glycol chain lengths and two model drugs were established. Their processability and disintegration properties were investigated. Moreover, the resulting drug particle sizes in the eutectics were determined. The eutectic concentration and temperature of fusion of the eutectics increased with the melting temperature of the respective excipient. The eutectics with the self-dispersing excipients disintegrated faster than more conventional eutectics containing polyethylene glycols that were prepared for comparison. The drug particle sizes were smaller for mixtures with higher recrystallization tendency and with drug concentrations close to the eutectic concentration.

摘要

为了提高难溶性药物的溶出速率,制备低共熔物是一种切实可行的方法,无需研磨和处理流动性差的粉末即可使药物粒径最小化。使用固体自分散辅料作为低共熔物的一种成分可能会进一步提高药物溶出速率。在本研究中,建立了聚乙二醇硬脂酸酯和聚乙二醇硬脂基醚的低共熔混合物的相图,这些混合物的聚乙二醇链长不同,还建立了两种模型药物的相图。研究了它们的可加工性和崩解性能。此外,还测定了低共熔物中所得药物的粒径。低共熔物的低共熔浓度和熔融温度随各自辅料的熔点升高而升高。含有自分散辅料的低共熔物比为作比较而制备的含有聚乙二醇的传统低共熔物崩解更快。对于具有较高重结晶倾向且药物浓度接近低共熔浓度的混合物,药物粒径更小。

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