Rapid assessment of homogeneity and stability of amorphous solid dispersions by atomic force microscopy - From Bench to Batch

Pharmaceutical Research

Volumn 30, Issue 8, 2013, Pages 2010-2022

  Lauer, Matthias E ^a   Siam, Monira ^a   Tardio, Joseph ^a   Page, Susanne ^a   Kindt, Johannes H ^b   Grassmann, Olaf ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b BRUKER DALTONIK GMBH   (Germany)

Author keywords

amorphous solid dispersion; atomic force microscopy; hot melt extrusion; process optimization; stability prediction

Indexed keywords

CHOLESTEROL ESTER TRANSFER PROTEIN INHIBITOR; EXCIPIENT; NEUROKININ 1 RECEPTOR ANTAGONIST;

AMORPHOUS SOLID DISPERSION; ANALYTIC METHOD; ANALYTICAL EQUIPMENT; ARTICLE; ATOMIC FORCE MICROSCOPY; CONTROLLED STUDY; DATA ANALYSIS; DISPERSION; DRUG FORMULATION; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HOT MELT EXTRUDER; HUMIDITY; INCUBATION TEMPERATURE; MATHEMATICAL COMPUTING; MATHEMATICAL MODEL; MICROSCOPY; MOLECULAR IMAGING; MOLECULAR MODEL; MOLECULAR STABILITY; PHASE SEPARATION; PRIORITY JOURNAL; PROCESS OPTIMIZATION; QUALITY CONTROL; QUANTITATIVE STUDY; RAMAN MICROSCOPY; RAPID TEST; SURFACE PROPERTY; TEMPERATURE SENSITIVITY;

CRYSTALLIZATION; DRUG STABILITY; EXCIPIENTS; HOT TEMPERATURE; HUMIDITY; MICROSCOPY, ATOMIC FORCE; PHARMACEUTICAL PREPARATIONS; PHASE TRANSITION; SOLUBILITY;

EID: 84879797938     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-013-1045-0     Document Type: Article

References (37)

1. Williams III RO, Watts AB, Miller DA (Eds): Formulating poorly soluble drugs. New York USA: Springer; 2012.
2. Forster A, Hempenstall J, Tucker I, Rades T. Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis. Int J Pharm. 2001;226:147-61.
3. Forster A, Hempenstall J, Tucker I, Rades T. The potential of small-scale fusion experiments and the Gordon-Taylor equation to predict the suitability of drug/polymer blends for melt extrusion. Drug Dev Ind Pharm. 2001;27:549-60.
4. Van Eredenbrugh B, Taylor LS. Small scale screening to determine the ability of different polymers to inhibit drug crystallization upon rapid solvent evaporation. Mol Pharm. 2010;7:1328-37.
5. Weuts I, Van Dycke F, Voorspoels J, De Cort S, Stokbroekx S, Leemans R, et al. Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: etravirine. J Pharm Sci. 2011;100:260-74.
6. Barillaro V, Pescarmona PP, Van Speybroeck M, Do Thi T, Van Humbeeck J, Vermant J, et al. High-throughput study of phenytoin solid dispersions: formulation using an automated solvent casting method, dissolution testing, and scaling-up. J Comb Chem. 2008;10:637-43.
7. Ivanisevic I, Bates S, Chen P. Novel methods for the assessment of miscibility of amorphous drug-polymer dispersions. J Pharm Sci. 2009;98:3373-86.
8. Newman A, Engers D, Bates S, Ivanisevic I, Kelly RC, Zografi G. Characterization of amorphous api:polymer mixtures using x-ray powder diffraction. J Pharm Sci. 2008;97:4840-56.
9. Bairdand JA, Taylor LS. Evaluation of amorphous solid dispersion properties using thermal analysis techniques. Adv Drug Deliver Rev. 2012;64:396-421.
10. Qian F, Huang J, Zhu Q, Haddadin R, Gawel J, Garmise R, et al. Is a distinctive single T-g a reliable indicator for the homogeneity of amorphous solid dispersion? Int J Pharm. 2010;395:232-5.
11. Sawyer LC, Grubb DT, Meyers GF. Polymer Microscopy. 3rd ed. New York USA: Springer; 2008.
12. Palermo RN, Anderson CA, Drennen JK. Review: use of thermal, diffraction, and vibrational analytical methods to determine mechanisms of solid dispersion stability. J Pharm Innov. 2012;7:2-12.
13. Nollenberger K, Gryczke A, Meier C, Dressman J, Schmidt MU, Bruhne S. Pair distribution function X-Ray analysis explains dissolution characteristics of felodipine melt extrusion products. J Pharm Sci. 2009;98:1476-86.
14. Karavas E, Georgarakis M, Docoslis A, Bikiaris D. Combining SEM, TEM, and micro-Raman techniques to differentiate between the amorphous molecular level dispersions and nanodispersions of a poorly water-soluble drug within a polymer matrix. Int J Pharm. 2007;340:76-83.
15. Magonov SN, Reneker DH. Characterization of polymer surfaces with atomic force microscopy. Annu Rev Mater Sci. 1997;27:175-222.
16. Garcia R, Herruzo ET. The emergence of multifrequency force microscopy. Nat Nanotechnol. 2012;7:217-26.
17. Lamm MS, Simpson A, McVevin M, Frankenfeld C, Nay R, Variankaval N. Probing the Effect of Drug Loading and Humidity on the Mechanical Properties of Solid Dispersions with Nanoindentation: Antiplasticization of a Polymer by a Drug Molecule. Mol Pharmaceut. 2012;9:(11):3396-402.
18. Hu SQ, Mininni L, Hu Y, Erina N, Kindt J, Su CM. High-Speed Atomic Force Microscopy and Peak Force Tapping Control. Proc Spie. 2012;11:8324-30.
19. Zhang JX, Bunker M, Chen XY, Parker AP, Patel N, Roberts CJ. Nanoscale thermal analysis of pharmaceutical solid dispersions. Int J Pharm. 2009;380:170-3.
20. Van Eerdenbrugh B, Lo M, Kjoller K, Marcott C, Taylor LS. Nanoscale mid-infrared imaging of phase separation in a drug-polymer blend. J Pharm Sci. 2012;101:2066-73.
21. Mahlin D, Berggren J, Alderborn G, Engstrom S. Moisture-induced surface crystallization of spray-dried amorphous lactose particles studied by atomic force microscopy. J Pharm Sci. 2004;93:29-37.
22. Marsac PJ, Rumondor ACF, Nivens DE, Kestur US, Stanciu L, Taylor LS. Effect of temperature and moisture on the miscibility of amorphous dispersions of felodipine and poly(vinyl pyrrolidone). J Pharm Sci. 2010;99:169-85.
23. Priceand R, Young PM. Visualization of the crystallization of lactose from the amorphous state. J Pharm Sci. 2004;93:155-64.
24. Qi S, Belton P, Nollenberger K, Gryczke A, Craig DQM. Compositional analysis of low quantities of phase separation in hot-melt-extruded solid dispersions: a combined atomic force microscopy, photothermal fourier-transform infrared microspectroscopy, and localised thermal analysis approach. Pharmaceut Res. 2011;28:2311-26.
25. Meeus J, Chen XY, Scurr DJ, Ciarnelli V, Amssoms K, Roberts CJ, et al. Nanoscale surface characterization and miscibility study of a spray-dried injectable polymeric matrix consisting of poly(lactic-co-glycolic acid) and polyvinylpyrrolidone. J Pharm Sci. 2012;101:3473-85.
26. Lauer ME, Grassmann O, Siam M, Tardio J, Jacob L, Page S, et al. Atomic force microscopy-based screening of drug-excipient miscibility and stability of solid dispersions. Pharmaceut Res. 2011;28:572-84.
27. Conte-Mayweg A, Kuehne H, Luebbers T, Maugeais C, Mueller W, Pflieger Philippe, inventor; F. Hoffmann La Roche Ltd. Assignee. Indole, Indazole or Indoline Derivatives. United States patent 7259183. 2007.
28. Hoffmann-Emery F, Hilpert H, Scalone M, Waldmeier P. Efficient synthesis of novel NK1 receptor antagonists: selective 1,4-addition of grignard reagents to 6-chloronicotinic acid derivatives. J Org Chem. 2006;71:2000-8.
29. Van Eerdenbrugh B, Baird JA, Taylor LS. Crystallization tendency of active pharmaceutical ingredients following rapid solvent evaporation- classification and comparison with crystallization tendency from undercooled melts. J Pharm Sci. 2010;99:3826-38.
30. Chiou L, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60:1281-302.
31. Paudeland A, Van den Mooter G. Influence of solvent composition on the miscibility and physical stability of naproxen/PVP K 25 solid dispersions prepared by cosolvent spray-drying. Pharmaceut Res. 2012;29:251-70.
32. Budd PM, McKeown NB, Fritsch D. Free volume and intrinsic microporosity in polymers. J Mater Chem. 2005;15:1977-86.
33. Berggrenand J, Alderborn G. Effect of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone). Pharm Res. 2003;20:1039-46.
34. Yang H, Mittal V: Molecular Dynamic Simulation Studies of Binary Blend Miscibility in Functional Polymer Blends, Synthesis, Properties and Performance. 6000 Broken Sound Parkway NW,. Suite 300, Boca Raton, FL 33487: CRC Press, Francis & Taylor Group: 2012.
35. Mitra MK, Muthukumar M. Theory of spinodal decomposition assisted crystallization in binary mixtures. J Chem Phys. 132: (2010).
36. Sagui C, Grant M. Theory of nucleation and growth during phase separation. Phys Rev E. 1999;59:4175-87.
37. Jones RAL, Norton LJ, Kramer EJ, Bates FS, Wiltzius P. Surface-directed spinodal decomposition. Phys Rev Lett. 1991;66:1326-9.