Combination of (M)DSC and Surface Analysis to Study the Phase Behaviour and Drug Distribution of Ternary Solid Dispersions

详细信息    查看全文

• 作者：Joke Meeus (1)
  David J. Scurr (2)
  Xinyong Chen (2)
  Katie Amssoms (3)
  Martyn C. Davies (2)
  Clive J. Roberts (2)
  Guy Van den Mooter (1)
  
  1. Drug Delivery and Disposition ; KU Leuven ; Department of Pharmaceutical and Pharmacological Sciences ; Campus Gasthuisberg ON2 ; Herestraat 49 b921 ; 3000 ; Leuven ; Belgium
  2. Laboratory of Biophysics and Surface Analysis ; School of Pharmacy ; The University of Nottingham ; Nottingham ; UK
  3. Pharmaceutical Companies of Johnson & Johnson ; Janssen ; Discovery Sciences ; PD&S_PDM ; Beerse ; Belgium
  
• 关键词：AFM ; MDSC ; Miscibility ; Solid dispersions ; ToF ; SIMS
• 刊名：Pharmaceutical Research
• 出版年：2015
• 出版时间：April 2015
• 年：2015
• 卷：32
• 期：4
• 页码：1407-1416
• 全文大小：4,241 KB
• 参考文献：1. Janssens, S, Mooter, G (2009) Review: physical chemistry of solid dispersions. J Pharm Pharmacol 61: pp. 1571-86 CrossRef
  2. Mooter, G (2012) The use of amorphous solid dispersions: a formulation strategy to overcome poor solubility and dissolution rate. Drug Discov Today Technol 9: pp. e71-e174 CrossRef
  3. Leuner, C, Dressman, J (2000) Improving drug solubility for oral delivery using solid dispersions. Eur J Pharm Biopharm 50: pp. 47-60 CrossRef
  4. Vasconcelos, T, Sarmento, B, Costa, P (2007) Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today 12: pp. 1068-75 CrossRef
  5. Vo, CL-N, Park, C, Lee, B-J (2013) Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. Eur J Pharm Biopharm 85: pp. 799-813 CrossRef
  6. Kalogeras, IM (2011) A novel approach for analyzing glass-transition temperature vs. composition patterns: application to pharmaceutical compound + polymer systems. Eur J Pharm Sci 42: pp. 470-83 CrossRef
  7. Gordon, M, Taylor, S (1952) Ideal copolymers and the second-order transitions of synthetic rubbers. I. non-crystalline copolymers. J Appl Chem 2: pp. 493-500 CrossRef
  8. Meeus, J, Chen, X, Scurr, DJ, Ciarnelli, V, Amssoms, K, Roberts, CJ (2012) 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 101: pp. 3473-85 CrossRef
  9. Meeus, J, Scurr, DJ, Amssoms, K, Davies, MC, Roberts, CJ, Mooter, G (2013) Surface characteristics of spray-dried microspheres consisting of PLGA and PVP: relating the influence of heat and humidity to the thermal characteristics of these polymers. Mol Pharm 10: pp. 3213-24 CrossRef
  10. Rafati, A, Boussahel, A, Shakesheff, KM, Shard, AG, Roberts, CJ, Chen, X (2012) Chemical and spatial analysis of protein loaded PLGA microspheres for drug delivery applications. J Control Release 162: pp. 321-9 CrossRef
  11. Scoutaris, N, Hook, AL, Gellert, PR, Roberts, CJ, Alexander, MR, Scurr, DJ (2012) ToF-SIMS analysis of chemical heterogenities in inkjet micro-array printed drug/polymer formulations. J Mater Sci Mater Med 23: pp. 385-91 CrossRef
  12. Kreye, F, Hamm, G, Karrout, Y, Legouffe, R, Bonnel, D, Siepmann, F (2012) MALDI-TOF MS imaging of controlled release implants. J Control Release 161: pp. 98-108 CrossRef
  13. Weuts, I, Dycke, F, Voorspoels, J, Cort, S, Stokbroekx, S, Leemans, R (2011) 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 100: pp. 260-74 CrossRef
  14. Lauer, ME, Siam, M, Tardio, J, Page, S, Kindt, JH, Grassmann, O (2013) Rapid assessment of homogeneity and stability of amorphous solid dispersions by atomic force microscopy鈥攆rom bench to batch. Pharm Res 30: pp. 2010-22 CrossRef
  15. Lauer, ME, Grassmann, O, Siam, M, Tardio, J, Jacob, L, Page, S (2011) Atomic force microscopy-based screening of drug-excipient miscibility and stability of solid dispersions. Pharm Res 28: pp. 572-84 CrossRef
  16. Qi, S, Moffat, JG, Yang, Z (2013) Early stage phase separation in pharmaceutical solid dispersion thin films under high humidity: improved spatial understanding using probe-based thermal and spectroscopic nanocharacterization methods. Mol Pharm 10: pp. 918-30 CrossRef
  17. Alsteens, D, Dupres, V, Yunus, S, Latg茅, J-P, Heinisch, JJ, Dufr锚ne, YF (2012) High-resolution imaging of chemical and biological sites on living cells using peak force tapping atomic force microscopy. Langmuir 28: pp. 16738-44 CrossRef
  18. Adamcik, J, Berquand, A, Mezzenga, R (2011) Single-step direct measurement of amyloid fibrils stiffness by peak force quantitative nanomechanical atomic force microscopy. Appl Phys Lett AIP Publ 98: pp. 193701 CrossRef
  19. Paragkumar, NT, Edith, D, Six, J-L (2006) Surface characteristics of PLA and PLGA films. Appl Surf Sci 253: pp. 2758-64 CrossRef
  20. Mooter, G, Wuyts, M, Blaton, N, Busson, R, Grobet, P, Augustijns, P (2001) Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25. Eur J Pharm Sci 12: pp. 261-9 CrossRef
  21. Janssens, S, Zeure, A, Paudel, A, Humbeeck, J, Rombaut, P, Mooter, G (2010) Influence of preparation methods on solid state supersaturation of amorphous solid dispersions: a case study with itraconazole and eudragit e100. Pharm Res 27: pp. 775-85 CrossRef
  22. Tobyn, M, Brown, J, Dennis, AB, Fakes, M, Gao, Q, Gamble, J (2009) Amorphous drug-PVP dispersions: application of theoretical, thermal and spectroscopic analytical techniques to the study of a molecule with intermolecular bonds in both the crystalline and pure amorphous state. J Pharm Sci 98: pp. 3456-68 CrossRef
  23. Janssens, S, Nagels, S, Armas, HN, D鈥橝utry, W, Schepdael, A, Mooter, G (2008) Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study. Eur J Pharm Biopharm 69: pp. 158-66 CrossRef
  24. Wan, F, Bohr, A, Maltesen, MJ, Bjerregaard, S, Foged, C, Rantanen, J (2013) Critical solvent properties affecting the particle formation process and characteristics of celecoxib-loaded plga microparticles via spray-drying. Pharm Res 30: pp. 1065-76 CrossRef
  25. Paudel, A, Worku, ZA, Meeus, J, Guns, S, Mooter, G (2013) Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations. Int J Pharm 453: pp. 253-84 CrossRef
  
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Biomedicine
  Pharmacology and Toxicology
  Pharmacy
  Biochemistry
  Medical Law
  Biomedical Engineering
  
• 出版者：Springer Netherlands
• ISSN：1573-904X

文摘

Purpose Miscibility of the different compounds that make up a solid dispersion based formulation play a crucial role in the drug release profile and physical stability of the solid dispersion as it defines the phase behaviour of the dispersion. The standard technique to obtain information on phase behaviour of a sample is (modulated) differential scanning calorimetry ((M)DSC). However, for ternary mixtures (M)DSC alone is not sufficient to characterize their phase behaviour and to gain insight into the distribution of the active pharmaceutical ingredient (API) in a two-phased polymeric matrix. Methods MDSC was combined with complementary surface analysis techniques, specifically time-of-flight secondary ion mass spectrometry (ToF-SIMS) and atomic force microscopy (AFM). Three spray-dried model formulations with varying API/PLGA/PVP ratios were analyzed. Results MDSC, TOF-SIMS and AFM provided insights into differences in drug distribution via the observed surface coverage for 3 differently composed ternary solid dispersions. Conclusions Combining MDSC and surface analysis rendered additional insights in the composition of mixed phases in complex systems, like ternary solid dispersions.