Amorphous drug nanosuspensions. 1. Inhibition of Ostwald ripening

被引:169
作者
Lindfors, L [1 ]
Skantze, P
Skantze, U
Rasmusson, M
Zackrisson, A
Olsson, U
机构
[1] AstraZeneca R&D, Pharmaceut & Analyt R&D, Ecpt Formulat, SE-43183 Molndal, Sweden
[2] Lund Univ, SE-22100 Lund, Sweden
关键词
D O I
10.1021/la0523661
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Amorphous drug nanosuspensions are prone to particle growth due to Ostwald ripening. By incorporating a second component of extremely low aqueous solubility, Ostwald ripening can be inhibited. These studies indicate that to inhibit ripening, the drug/inhibitor mixture (in the particles) must form a single phase. The drug/inhibitor mixture can be characterized by the interaction parameter chi using the Bragg-Williams theory, in which single phase mixtures are obtained for chi < 2. The chi parameter can be calculated from the (crystalline) solubility of the drug in the inhibitor, provided the inhibitor is a liquid, and the melting entropy and temperature of the drug.
引用
收藏
页码:906 / 910
页数:5
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