Isothermal microcalorimetry to investigate the phase separation for amorphous solid dispersions of AMG 517 with HPMC-AS

Molecular Pharmaceutics

Volumn 10, Issue 5, 2013, Pages 1949-1957

  Calahan, Julie L ^a   Zanon, Roger L ^a   Alvarez Nunez, Fernando ^a   Munson, Eric J ^b  

^a AMGEN INC   (United States)

^b UNIVERSITY OF KANSAS   (United States)

Author keywords

amorphous solid dispersion; microcalorimetry; solid state stability; spray dry

Indexed keywords

HYDROXYPROPYLMETHYLCELLULOSE ACETATE SUCCINATE; N [4 [6 [4 (TRIFLUOROMETHYL)PHENYL] 4 PYRIMIDINYLOXY]BENZOTHIAZOL 2 YL]ACETAMIDE; BENZOTHIAZOLE DERIVATIVE; FLUORINE; METHYLCELLULOSE; N-(4-(6-(4-TRIFLUOROMETHYLPHENYL)PYRIMIDIN-4-YLOXY)BENZOTHIAZOL-2-YL)ACETAMIDE; PYRIMIDINE DERIVATIVE;

ARTICLE; CRYSTALLIZATION; DIFFERENTIAL SCANNING CALORIMETRY; DISPERSION; DRUG STABILITY; HUMIDITY; ISOTHERMAL MICROCALORIMETRY; MICROCALORIMETRY; NUCLEAR MAGNETIC RESONANCE; PRIORITY JOURNAL; SCANNING ELECTRON MICROSCOPY; SOLID STATE NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; TEMPERATURE; ANALOGS AND DERIVATIVES; CALORIMETRY; CHEMISTRY; MEDICINAL CHEMISTRY; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PHASE TRANSITION; PROCEDURES; TRANSITION TEMPERATURE;

BENZOTHIAZOLES; CALORIMETRY; CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; DRUG STABILITY; FLUORINE; MAGNETIC RESONANCE SPECTROSCOPY; METHYLCELLULOSE; MICROSCOPY, ELECTRON, SCANNING; PHASE TRANSITION; PYRIMIDINES; TRANSITION TEMPERATURE;

EID: 84877273099     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp300714g     Document Type: Article

References (24)

1. Chiou, W. L.; Riegelmann, S. Pharmaceutical Applications of Solid Dispersion Systems J. Pharm. Sci. 1971, 60 (9) 1281-1302
2. Doherty, C.; York, P. Evidence for solid- and liquid-state interactions in a furosemide-polyvinylpyrrolidone solid dispersion J. Pharm. Sci. 1987, 76 (9) 731-7
3. Janssens, S.; Van den Mooter, G. Review: physical chemistry of solid dispersions J. Pharm. Pharmacol. 2009, 61 (12) 1571-1586
4. Tiwari, R.; Tiwari, G.; Srivastava, B.; Rai, A. K. Solid dispersions: an overview to modify bioavailability of poorly water soluble drugs Int. J. PharmTech Res. 2009, 1 (4) 1338-1349
5. Craig, D. Q. M. The mechanisms of drug release from solid dispersions in water-soluble polymers Int. J. Pharm. 2002, 231 (2) 131-144
6. Ghaste, R. P.; Chougule, D. D.; Shah, R. R.; Ghodake, D. S. Solid dispersions: an overview. Pharm. Rev. 2009, 7 (5).
7. Rumondor, A. C. F.; Stanford, L. A.; Taylor, L. S. Effects of Polymer Type and Storage Relative Humidity on the Kinetics of Felodipine Crystallization from Amorphous Solid Dispersions Pharm. Res. 2009, 26 (12) 2599-2606
8. Greenhalgh, D. J.; Williams, A. C.; Timmins, P.; York, P. Solubility Parameters as Predictors of Miscibility in Solid Dispersions J. Pharm. Sci. 1999, 88 (11) 1182-1190
9. Marsac, P. J.; Li, T.; Taylor, L. S. Estimation of Drug-Polymer Miscibility and Solubility in Amorphous Solid Dispersions Using Experimentally Determined Interaction Parameters Pharm. Res. 2009, 26 (1) 139-151
10. Yu, L. Amorphous pharmaceutical solids: preparation, characterization and stabilization Adv. Drug Delivery Rev. 2001, 48 (1) 27-42
11. IUPAC. Compendium of Chemical Terminology, 2 nd ed.; the "Gold Book", compiled by McNaught, A. D.; Wilkinson, A.; Blackwell Scientific Publications: Oxford, U.K., 1997.
12. Newman, A.; Knipp, G.; Zografi, G. Assessing the Performance of Amorphous Solid Dispersions J. Pharm. Sci. 2012, 101 (4) 1355-1377
13. Qian, F.; Huang, J.; Hussain, M. A. Drug-polymer solubility and miscibility: Stability consideration and practical challenges in amorphous solid dispersion development J. Pharm. Sci. 2010, 99 (7) 2941-2947
14. Muela, S.; Escalera, B.; Pena, M. A.; Bustamante, P. Influence of temperature on the solubilization of thiabendazole by combined action of solid dispersions and co-solvents Int. J. Pharm. 2010, 384 (1-2) 93-99
15. Vasanthavada, M.; Tong, W.-Q.; Joshi, Y.; Kislalioglu, M. S. Phase Behavior of Amorphous Molecular Dispersions I: Determination of the Degree and Mechanism of Solid Solubility Pharm. Res. 2004, 21 (9) 1598-1606
16. Yoo, S.-u.; Krill, S. L.; Wang, Z.; Telang, C. Miscibility/stability considerations in binary solid dispersion systems composed of functional excipients towards the design of multi-component amorphous systems J. Pharm. Sci. 2009, 98 (12) 4711-4723
17. FDA. ICH Guidance for Industry: Q1A(R2) Stability Testing of New Drug Substances and Products; US Department of Health and Human Services: Rockville, MD, 2003.
18. Loftsson, T.; Fridriksdottir, H.; Gudmundsdottir, T. K. The effect of water-soluble polymers on aqueous solubility of drugs Int. J. Pharm. 1996, 127 (2) 293-296
19. Kennedy, M.; Hu, J.; Gao, P.; Li, L.; Ali-Reynolds, A.; Chal, B.; Gupta, V.; Ma, C.; Mahajan, N.; Akrami, A.; Surapaneni, S. Enhanced Bioavailability of a Poorly Soluble VR1 Antagonist Using an Amorphous Solid Dispersion Approach: A Case Study Mol. Pharmaceutics 2008, 5 (6) 981-993
20. Balan, C.; Chen, N.; Doherty, E. M.; Gore, V. K.; Norman, M. H.; Wang, H.-l. Preparation of 4-heteroaryloxy-6-piperazinopyrimidines and 2-heteroaryloxy-4-piperazinopyridines as vanilloid receptor ligands. 2005-56534 20050182067, 20050211, 2005.
21. Six, K.; Berghmans, H.; Leuner, C.; Dressman, J.; Van Werde, K.; Mullens, J.; Benoist, L.; Thimon, M.; Meublat, L.; Verreck, G.; Peeters, J.; Brewster, M.; Van den Mooter, G. Characterization of Solid Dispersions of Itraconazole and Hydroxypropyl methyl cellulose Prepared by Melt Extrusion, Part II Pharm. Res. 2003, 20 (7) 1047-1054
22. Kawakami, K.; Miyoshi, K.; Tamura, N.; Yamaguchi, T.; Ida, Y. Crystallization of sucrose glass under ambient conditions: evaluation of crystallization rate and unusual melting behavior of resultant crystals J. Pharm. Sci. 2006, 95 (6) 1354-1363
23. Schmitt, E. A.; Law, D.; Zhang, G. G. Z. Nucleation and Crystallization Kinetics of Hydrated Amorphous Lactose above the Glass Transition Temperature J. Pharm. Sci. 1999, 88 (3) 291-296
24. Malek, J. Crystallization kinetics by thermal analysis J. Therm. Anal. Calorim. 1999, 56 (2) 763-769