Ibuprofen agglomerates preparation by phase separation

被引:40
作者
Jbilou, M
Ettabia, A
Guyot-Hermann, AM
Guyot, JC
机构
[1] Pharm Galen Lab, F-59006 Lille, France
[2] Lab Pharmacotechnie Ind, F-59006 Lille, France
关键词
D O I
10.1081/DDC-100102174
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The compression ability and dissolution rare of ibuprofen are poor. There are many processes to optimize these properties through adapted formulations. However, it would be more satisfactory to obtain directly during the crystallization step crystalline particles that can be directly compressed and quickly dissolved. This was the aim of this work. Ibuprofen spherical agglomerates were obtained using a very simple method based on the difference of solubility of ibuprofen in ethanol and in water. By cooling down an ibuprofen-saturated solution in an ethanol/water 50/50 mixture from 60 degrees C to room temperature under stirring, a phase separation occurs. Ibuprofen crystallizes in separated water droplets. After separation by sieving and drying, spherical agglomerates were obtained. A study of the physical properties of ibuprofen agglomerates was carried out using electron scanning microscopy and X-ray powder diffraction. The compression ability was tested using an instrumented tablet machine, and the dissolution rate was measured using continuous flow cells. An improvement in compression and dissolution properties of the spherical agglomerates produced was observed The process of crystallization in a separated dispersed phase could be envisaged each time a drug exhibits opposite solubilities in two miscible solvents.
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页码:297 / 305
页数:9
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