Physicochemical Stability of Solid Dispersions of Enantiomeric or Racemic Ibuprofen in Stearic Acid

被引：22
作者：
Corvis, Yohann [1 ]
Negrier, Philippe [2 ]
Espeau, Philippe [1 ]
机构：
[1] Univ Paris 05, EA 4066, Lab Physicochim Ind Medicament, Fac Sci Pharmaceut & Biol, F-75006 Paris, France
[2] Univ Bordeaux, CNRS, UMR 5798, Lab Onde & Matiere Aquitaine, F-33405 Talence, France
来源：
JOURNAL OF PHARMACEUTICAL SCIENCES | 2011年 / 100卷 / 12期
关键词：
drug-excipient interactions; phase diagram; solid-state stability; miscibility; melt-recrystallization process; solubility; polymorphism; thermal analysis; X-ray powder diffraction; CRYSTAL-STRUCTURE; B-FORM; RHEUMATOID-ARTHRITIS; OCTADECANOIC ACID; PHASE-DIAGRAMS; S-IBUPROFEN; POLYMORPHISM; CALORIMETRY; SOLUBILITY; INVERSION;
D O I：
10.1002/jps.22727
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The aim of this study was to investigate the solid dispersion phase behavior of S-or RS-ibuprofen in stearic acid. By means of thermal analysis, we have demonstrated the total immiscibility, in solid state, of the corresponding binary mixtures. This indicates that no specific interactions exist between the chosen excipient and active pharmaceutical ingredient (API) that lead to eutectic systems. Furthermore, based on calorimetric and X-ray diffraction experiments, we have showed that upon cooling of the molten state, only stearic acid recrystallizes in the presence of S-ibuprofen, whereas a quaternary phase mixture is obtained for the racemic ibuprofen/stearic acid preparation. The solubility of stearic acid in S-ibuprofen liquid in all proportions was also determined. Overall, the results presented here offer an approach for the study of API/excipient interactions. (C) 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:5235-5243, 2011
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页码：5235 / 5243
页数：9
相关论文
共 33 条
[1]   PHARMACOLOGICAL DIFFERENCES BETWEEN OPTICAL ISOMERS OF IBUPROFEN - EVIDENCE FOR METABOLIC INVERSION OF (-)-ISOMER [J].
ADAMS, SS ;
BRESLOFF, P ;
MASON, CG .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1976, 28 (03) :256-257
[2]   A DIRECT METHOD FOR THE DERIVATION OF THERMODYNAMIC EXCESS FUNCTIONS FROM TX PHASE-DIAGRAMS .2. IMPROVED METHOD APPLIED TO EXPERIMENTAL REGIONS OF DEMIXING [J].
BROUWER, N ;
OONK, HAJ .
ZEITSCHRIFT FUR PHYSIKALISCHE CHEMIE-WIESBADEN, 1979, 117 :55-67
[3]  
Burger A, 1996, EUR J PHARM BIOPHARM, V42, P142
[4]   Evidence for a New Crystalline Phase of Racemic Ibuprofen [J].
Dudognon, Emeline ;
Danede, Florence ;
Descamps, Marc ;
Correia, Natalia T. .
PHARMACEUTICAL RESEARCH, 2008, 25 (12) :2853-2858
[5]   IBUPROFEN RACEMATE AND ENANTIOMERS - PHASE-DIAGRAM, SOLUBILITY AND THERMODYNAMIC STUDIES [J].
DWIVEDI, SK ;
SATTARI, S ;
JAMALI, F ;
MITCHELL, AG .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1992, 87 (1-3) :95-104
[6]  
ESPEAU P, 1995, THESIS U BORDEAUX 1
[7]   STRUCTURE OF (S)-(+)-IBUPROFEN [J].
FREER, AA ;
BUNYAN, JM ;
SHANKLAND, N ;
SHEEN, DB .
ACTA CRYSTALLOGRAPHICA SECTION C-CRYSTAL STRUCTURE COMMUNICATIONS, 1993, 49 :1378-1380
[8]   PHARMACOKINETICS OF S(+)-IBUPROFEN AND R(-)-IBUPROFEN IN VOLUNTEERS AND 1ST CLINICAL-EXPERIENCE OF S(+)-IBUPROFEN IN RHEUMATOID-ARTHRITIS [J].
GEISSLINGER, G ;
SCHUSTER, O ;
STOCK, KP ;
LOEW, D ;
BACH, GL ;
BRUNE, K .
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1990, 38 (05) :493-497
[9]   Arrangement of molecules in a single layer and in multiple layers [J].
Germer, LH ;
Storks, KH .
JOURNAL OF CHEMICAL PHYSICS, 1938, 6 (05) :280-293
[10]   UTILIZATION OF DIFFERENTIAL SCANNING CALORIMETRY IN THE COMPATIBILITY SCREENING OF IBUPROFEN WITH THE STEARATE LUBRICANTS AND CONSTRUCTION OF PHASE-DIAGRAMS [J].
GORDON, RE ;
VANKOEVERING, CL ;
REITS, DJ .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1984, 21 (01) :99-105
1234