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Volumn 10, Issue 1, 2013, Pages 236-248

Construction of drug-polymer thermodynamic phase diagrams using flory-huggins interaction theory: Identifying the relevance of temperature and drug weight fraction to phase separation within solid dispersions

Author keywords

drug polymer thermodynamic phase diagrams; Flory Huggins interaction theory; high speed differential scanning calorimetry; HPMCAS HF felodipine; Soluplus felodipine

Indexed keywords

FELODIPINE; HYDROXYPROPYLMETHYLCELLULOSE ACETATE SUCCINATE; MACROGOL; POLYMER; POLYVINYL CAPROLACTAM POLYVINYL ACETATE POLYETHYLENE GLYCOL; UNCLASSIFIED DRUG;

EID: 84872164745     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp300386v     Document Type: Article
Times cited : (188)

References (45)
  • 1
    • 0034601240 scopus 로고    scopus 로고
    • Improving drug solubility for oral delivery using solid dispersions
    • Leuner, C.; Dressman, J. Improving drug solubility for oral delivery using solid dispersions Eur. J. Pharm. Biopharm. 2000, 50, 47-60
    • (2000) Eur. J. Pharm. Biopharm. , vol.50 , pp. 47-60
    • Leuner, C.1    Dressman, J.2
  • 2
    • 0035897584 scopus 로고    scopus 로고
    • Amorphous pharmaceutical solids: Preparation, characterization and stabilization
    • Yu, L. Amorphous pharmaceutical solids: Preparation, characterization and stabilization Adv. Drug Delivery Rev. 2001, 48, 27-42
    • (2001) Adv. Drug Delivery Rev. , vol.48 , pp. 27-42
    • Yu, L.1
  • 3
    • 36549042006 scopus 로고    scopus 로고
    • Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs
    • Vasconcelos, T.; Sarmento, B.; Costa, P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs Drug Discovery Today 2007, 12, 1068-1075
    • (2007) Drug Discovery Today , vol.12 , pp. 1068-1075
    • Vasconcelos, T.1    Sarmento, B.2    Costa, P.3
  • 4
    • 1142303337 scopus 로고    scopus 로고
    • What is the true solubility advantage for amorphous pharmaceuticals?
    • Hancock, B.; Parks, M. What is the true solubility advantage for amorphous pharmaceuticals? Pharm. Res. 2000, 17, 397-404
    • (2000) Pharm. Res. , vol.17 , pp. 397-404
    • Hancock, B.1    Parks, M.2
  • 5
    • 68249128120 scopus 로고    scopus 로고
    • Supersaturating Drug Delivery Systems: The Answer to Solubility-Limited Oral Bioavailability?
    • Brouwers, J.; Brewster, M.; Augustijns, P. Supersaturating Drug Delivery Systems: The Answer to Solubility-Limited Oral Bioavailability? J. Pharm. Sci. 2009, 98, 2549-2572
    • (2009) J. Pharm. Sci. , vol.98 , pp. 2549-2572
    • Brouwers, J.1    Brewster, M.2    Augustijns, P.3
  • 6
    • 79961078425 scopus 로고    scopus 로고
    • An Investigation into the Dissolution Properties of Celecoxib Melt Extrudates: Understanding the Role of Polymer Type and Concentration in Stabilizing Supersaturated Drug Concentrations
    • Abu Diak, O.; Jones, D.; Andrews, G. An Investigation into the Dissolution Properties of Celecoxib Melt Extrudates: Understanding the Role of Polymer Type and Concentration in Stabilizing Supersaturated Drug Concentrations Mol. Pharm. 2011, 8, 1362-1371
    • (2011) Mol. Pharm. , vol.8 , pp. 1362-1371
    • Abu Diak, O.1    Jones, D.2    Andrews, G.3
  • 7
    • 0032885450 scopus 로고    scopus 로고
    • Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs
    • Serajuddin, A. Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs J. Pharm. Sci. 1999, 88, 1058-1066
    • (1999) J. Pharm. Sci. , vol.88 , pp. 1058-1066
    • Serajuddin, A.1
  • 8
    • 38749130125 scopus 로고    scopus 로고
    • Method for screening of solid dispersion formulations of low-solubility compounds-Miniaturization and automation of solvent casting and dissolution testing
    • Shanbhag, A.; Rabel, S.; Nauka, E.; Casadevall, G.; Shivanand, P.; Eichenbaum, G.; Mansky, P. Method for screening of solid dispersion formulations of low-solubility compounds-miniaturization and automation of solvent casting and dissolution testing Int. J. Pharm. 2008, 351, 209-218
    • (2008) Int. J. Pharm. , vol.351 , pp. 209-218
    • Shanbhag, A.1    Rabel, S.2    Nauka, E.3    Casadevall, G.4    Shivanand, P.5    Eichenbaum, G.6    Mansky, P.7
  • 10
    • 33749442356 scopus 로고    scopus 로고
    • Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility
    • Marsac, P.; Shamblin, S.; Taylor, L. Theoretical and practical approaches for prediction of drug-polymer miscibility and solubility Pharm. Res. 2006, 23, 2417-2426
    • (2006) Pharm. Res. , vol.23 , pp. 2417-2426
    • Marsac, P.1    Shamblin, S.2    Taylor, L.3
  • 11
    • 82255179484 scopus 로고    scopus 로고
    • Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: Characterisation of microstructural properties using thermal, spectroscopic and drug release methods
    • Abu Diak, O.; Jones, D.; Andrews, G. Understanding the performance of melt-extruded poly(ethylene oxide)-bicalutamide solid dispersions: Characterisation of microstructural properties using thermal, spectroscopic and drug release methods J. Pharm. Sci. 2011, 101, 200-213
    • (2011) J. Pharm. Sci. , vol.101 , pp. 200-213
    • Abu Diak, O.1    Jones, D.2    Andrews, G.3
  • 12
    • 79952259745 scopus 로고    scopus 로고
    • Prediction of Solubility Parameters and Miscibility of Pharmaceutical Compounds by Molecular Dynamics Simulations
    • Gupta, J.; Nunes, C.; Vyas, S.; Jonnalagadda, S. Prediction of Solubility Parameters and Miscibility of Pharmaceutical Compounds by Molecular Dynamics Simulations J. Phys. Chem. B 2011, 115, 2014-2023
    • (2011) J. Phys. Chem. B , vol.115 , pp. 2014-2023
    • Gupta, J.1    Nunes, C.2    Vyas, S.3    Jonnalagadda, S.4
  • 13
    • 57749206650 scopus 로고    scopus 로고
    • Estimation of Drug-Polymer Miscibility and Solubility in Amorphous Solid Dispersions Using Experimentally Determined Interaction Parameters
    • Marsac, P.; Li, T.; Taylor, L. Estimation of Drug-Polymer Miscibility and Solubility in Amorphous Solid Dispersions Using Experimentally Determined Interaction Parameters Pharm. Res. 2009, 26, 139-151
    • (2009) Pharm. Res. , vol.26 , pp. 139-151
    • Marsac, P.1    Li, T.2    Taylor, L.3
  • 14
    • 77955243354 scopus 로고    scopus 로고
    • Theoretical and Experimental Investigation on the Solid Solubility and Miscibility of Naproxen in Poly(vinylpyrrolidone)
    • Paudel, A.; Van Humbeeck, J. Theoretical and Experimental Investigation on the Solid Solubility and Miscibility of Naproxen in Poly(vinylpyrrolidone) Mol. Pharmaceutics 2010, 7, 1133-1148
    • (2010) Mol. Pharmaceutics , vol.7 , pp. 1133-1148
    • Paudel, A.1    Van Humbeeck, J.2
  • 15
    • 61449135800 scopus 로고    scopus 로고
    • Solubility of Small-Molecule Crystals in Polymers: D-Mannitol in PVP, Indomethacin in PVP/VA, and Nifedipine in PVP/VA
    • Tao, J.; Sun, Y.; Yu, L. Solubility of Small-Molecule Crystals in Polymers: d-Mannitol in PVP, Indomethacin in PVP/VA, and Nifedipine in PVP/VA Pharm. Res. 2009, 26, 855-864
    • (2009) Pharm. Res. , vol.26 , pp. 855-864
    • Tao, J.1    Sun, Y.2    Yu, L.3
  • 16
    • 77956381209 scopus 로고    scopus 로고
    • Solubilities of Crystalline Drugs in Polymers: An Improved Analytical Method and Comparison of Solubilities of Indomethacin and Nifedipine in PVP, PVP/VA, and PVAc
    • Sun, Y.; Tao, J.; Yu, L. Solubilities of Crystalline Drugs in Polymers: An Improved Analytical Method and Comparison of Solubilities of Indomethacin and Nifedipine in PVP, PVP/VA, and PVAc J. Pharm. Sci. 2010, 99, 4023-4031
    • (2010) J. Pharm. Sci. , vol.99 , pp. 4023-4031
    • Sun, Y.1    Tao, J.2    Yu, L.3
  • 17
    • 79953835955 scopus 로고    scopus 로고
    • A Comparison of Spray Drying and Milling in the Production of Amorphous Dispersions of Sulfathiazole/Polyvinylpyrrolidone and Sulfadimidine/ Polyvinylpyrrolidone
    • Caron, V.; Tajber, L.; Corrigan, O. I.; Healy, A. M. A Comparison of Spray Drying and Milling in the Production of Amorphous Dispersions of Sulfathiazole/Polyvinylpyrrolidone and Sulfadimidine/Polyvinylpyrrolidone Mol. Pharm. 2011, 8, 532-542
    • (2011) Mol. Pharm. , vol.8 , pp. 532-542
    • Caron, V.1    Tajber, L.2    Corrigan, O.I.3    Healy, A.M.4
  • 19
    • 77956885126 scopus 로고    scopus 로고
    • A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersions
    • Lin, D.; Huang, Y. A thermal analysis method to predict the complete phase diagram of drug-polymer solid dispersions Int. J. Pharm. 2010, 399, 109-115
    • (2010) Int. J. Pharm. , vol.399 , pp. 109-115
    • Lin, D.1    Huang, Y.2
  • 20
    • 0013352184 scopus 로고
    • A Lattice Treatment of Crystalline Solvent-Amorphous Polymer Mixtures on Melting-Point Depression
    • Hoei, Y.; Yamaura, K.; Matsuzawa, S. A Lattice Treatment of Crystalline Solvent-Amorphous Polymer Mixtures on Melting-Point Depression J. Phys. Chem. 1992, 96, 10584-10586
    • (1992) J. Phys. Chem. , vol.96 , pp. 10584-10586
    • Hoei, Y.1    Yamaura, K.2    Matsuzawa, S.3
  • 21
    • 0032101667 scopus 로고    scopus 로고
    • Flory-Huggins interaction parameter of poly(ethyleneoxide)/ poly(epichlorohydrin) and poly(ethyleneoxide)/poly(epichlorohydrin-co- ethyleneoxide) blends
    • Silva, M.; De Paoli, M.; Felisberti, M. Flory-Huggins interaction parameter of poly(ethyleneoxide)/poly(epichlorohydrin) and poly(ethyleneoxide)/ poly(epichlorohydrin-co-ethyleneoxide) blends Polymer 1998, 39, 2551-2556
    • (1998) Polymer , vol.39 , pp. 2551-2556
    • Silva, M.1    De Paoli, M.2    Felisberti, M.3
  • 22
    • 21344486195 scopus 로고
    • Liquid-Liquid Phase-Separation in Multicomponent Polymer Systems-Influence of Molar-Mass Distribution on Shadow Curve and Phase-Volume Ratio
    • Koningsveld, R.; Solc, K. Liquid-Liquid Phase-Separation in Multicomponent Polymer Systems-Influence of Molar-Mass Distribution on Shadow Curve and Phase-Volume Ratio Collect. Czech. Chem. Commun. 1993, 58, 2305-2320
    • (1993) Collect. Czech. Chem. Commun. , vol.58 , pp. 2305-2320
    • Koningsveld, R.1    Solc, K.2
  • 23
    • 21844519069 scopus 로고
    • Liquid-liquid phase separation in multicomponent polymer systems 0.26. Blends of two polydisperse polymers
    • Solc, K.; Koningsveld, R. Liquid-liquid phase separation in multicomponent polymer systems 0.26. Blends of two polydisperse polymers Collect. Czech. Chem. Commun. 1995, 60, 1689-1718
    • (1995) Collect. Czech. Chem. Commun. , vol.60 , pp. 1689-1718
    • Solc, K.1    Koningsveld, R.2
  • 24
    • 0031279765 scopus 로고    scopus 로고
    • Liquid-liquid phase separation in multicomponent polymer systems 0.27. Determination of the pair-interaction function for polymer blends
    • Koningsveld, R.; MacKnight, W. Liquid-liquid phase separation in multicomponent polymer systems 0.27. Determination of the pair-interaction function for polymer blends Polym. Int. 1997, 44, 356-364
    • (1997) Polym. Int. , vol.44 , pp. 356-364
    • Koningsveld, R.1    MacKnight, W.2
  • 26
    • 75749094421 scopus 로고    scopus 로고
    • Review: Physical chemistry of solid dispersions
    • Janssens, S. Review: Physical chemistry of solid dispersions J. Pharm. Pharmacol. 2009, 61, 1571-1586
    • (2009) J. Pharm. Pharmacol. , vol.61 , pp. 1571-1586
    • Janssens, S.1
  • 27
    • 77953296607 scopus 로고    scopus 로고
    • Drug-Polymer Solubility and Miscibility: Stability Consideration and Practical Challenges in Amorphous Solid Dispersion Development
    • Qian, F.; Huang, J.; Hussain, M. Drug-Polymer Solubility and Miscibility: Stability Consideration and Practical Challenges in Amorphous Solid Dispersion Development J. Pharm. Sci. 2010, 99, 2941-2947
    • (2010) J. Pharm. Sci. , vol.99 , pp. 2941-2947
    • Qian, F.1    Huang, J.2    Hussain, M.3
  • 28
    • 79958842268 scopus 로고    scopus 로고
    • Prediction of the Thermal Phase Diagram of Amorphous Solid Dispersions by Flory-Huggins Theory
    • Zhao, Y.; Inbar, P.; Chokshi, H.; Malick, A. W.; Choi, D. Prediction of the Thermal Phase Diagram of Amorphous Solid Dispersions by Flory-Huggins Theory J. Pharm. Sci. 2011, 100, 3196-3207
    • (2011) J. Pharm. Sci. , vol.100 , pp. 3196-3207
    • Zhao, Y.1    Inbar, P.2    Chokshi, H.3    Malick, A.W.4    Choi, D.5
  • 31
    • 0035845751 scopus 로고    scopus 로고
    • Selection of excipients for melt extrusion with two poorly water-soluble drugs by solubility parameter calculation and thermal analysis
    • 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, 147-161
    • (2001) Int. J. Pharm. , vol.226 , pp. 147-161
    • Forster, A.1    Hempenstall, J.2    Tucker, I.3    Rades, T.4
  • 32
    • 64649098724 scopus 로고    scopus 로고
    • Thermodynamics, Molecular Mobility and Crystallization Kinetics of Amorphous Griseofulvin
    • Zhou, D.; Law, D.; Schmitt, E. Thermodynamics, Molecular Mobility and Crystallization Kinetics of Amorphous Griseofulvin Mol. Pharmaceutics 2008, 5, 927-936
    • (2008) Mol. Pharmaceutics , vol.5 , pp. 927-936
    • Zhou, D.1    Law, D.2    Schmitt, E.3
  • 33
    • 43249092894 scopus 로고    scopus 로고
    • Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state
    • Bhugra, C.; Pikal, M. Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state J. Pharm. Sci. 2008, 97, 1329-1349
    • (2008) J. Pharm. Sci. , vol.97 , pp. 1329-1349
    • Bhugra, C.1    Pikal, M.2
  • 34
    • 3543008927 scopus 로고    scopus 로고
    • The use of high-speed differential scanning calorimetry (hyper-DSCTM) to study the thermal properties of carbamazepine polymorphs
    • McGregor, C.; Saunders, M.; Buckton, G.; Saklatvala, R. The use of high-speed differential scanning calorimetry (hyper-DSCTM) to study the thermal properties of carbamazepine polymorphs Thermochim. Acta 2004, 417, 231-237
    • (2004) Thermochim. Acta , vol.417 , pp. 231-237
    • McGregor, C.1    Saunders, M.2    Buckton, G.3    Saklatvala, R.4
  • 35
    • 1842557588 scopus 로고    scopus 로고
    • The potential of high speed DSC (hyper-DSC) for the detection and quantification of small amounts of amorphous content in predominantly crystalline samples
    • Saunders, M.; Podluii, K.; Shergill, S.; Buckton, G.; Royall, P.; Podluii, K.; Shergill, S.; Buckton, G.; Royall, P. The potential of high speed DSC (hyper-DSC) for the detection and quantification of small amounts of amorphous content in predominantly crystalline samples Int. J. Pharm. 2004, 274, 35-40
    • (2004) Int. J. Pharm. , vol.274 , pp. 35-40
    • Saunders, M.1    Podluii, K.2    Shergill, S.3    Buckton, G.4    Royall, P.5    Podluii, K.6    Shergill, S.7    Buckton, G.8    Royall, P.9
  • 36
    • 80054796578 scopus 로고    scopus 로고
    • Solid dispersions, Part I: Recent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs
    • Bikiaris, D. Solid dispersions, Part I: Recent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs Expert Opin. Drug Delivery 2011, 8, 1501-1519
    • (2011) Expert Opin. Drug Delivery , vol.8 , pp. 1501-1519
    • Bikiaris, D.1
  • 38
    • 83555168268 scopus 로고    scopus 로고
    • Understanding the Tendency of Amorphous Solid Dispersions to Undergo Amorphous-Amorphous Phase Separation in the Presence of Absorbed Moisture
    • Rumondor, A. C. F.; Wikstroem, H.; Van Eerdenbrugh, B.; Taylor, L. Understanding the Tendency of Amorphous Solid Dispersions to Undergo Amorphous-Amorphous Phase Separation in the Presence of Absorbed Moisture AAPS PharmSciTech 2011, 12, 1209-1219
    • (2011) AAPS PharmSciTech , vol.12 , pp. 1209-1219
    • Rumondor, A.C.F.1    Wikstroem, H.2    Van Eerdenbrugh, B.3    Taylor, L.4
  • 39
    • 80054726007 scopus 로고    scopus 로고
    • 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
    • Qi, S.; Belton, P.; Nollenberger, K.; Gryczke, A. 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 Pharm. Res. 2011, 28, 2311-2326
    • (2011) Pharm. Res. , vol.28 , pp. 2311-2326
    • Qi, S.1    Belton, P.2    Nollenberger, K.3    Gryczke, A.4
  • 40
    • 3643117787 scopus 로고
    • Melting-Point Depression and Kinetic Effects of Cooling on Crystallization in Poly (vinylidene fluoride) Poly(Methyl methacrylate) Mixtures
    • Nishi, T.; Wang, T. Melting-Point Depression and Kinetic Effects of Cooling on Crystallization in Poly (vinylidene fluoride) Poly(Methyl methacrylate) Mixtures Macromolecules 1975, 8, 909-915
    • (1975) Macromolecules , vol.8 , pp. 909-915
    • Nishi, T.1    Wang, T.2
  • 41
    • 0032166972 scopus 로고    scopus 로고
    • The role of metastability in polymer phase transitions
    • Keller, A.; Cheng, S. The role of metastability in polymer phase transitions Polymer 1998, 39, 4461-4487
    • (1998) Polymer , vol.39 , pp. 4461-4487
    • Keller, A.1    Cheng, S.2
  • 42
    • 0031645250 scopus 로고    scopus 로고
    • The role of metastable states in polymer phase transitions: Concepts, principles, and experimental observations
    • Cheng, S.; Keller, A. The role of metastable states in polymer phase transitions: Concepts, principles, and experimental observations Annu. Rev. Mater. Sci. 1998, 28, 533-562
    • (1998) Annu. Rev. Mater. Sci. , vol.28 , pp. 533-562
    • Cheng, S.1    Keller, A.2
  • 43
    • 64649100465 scopus 로고    scopus 로고
    • Hydroxypropyl Methylcellulose Acetate Succinate-Based Spray-Dried Dispersions: An Overview
    • Friesen, D.; Shanker, R.; Crew, M.; Smithey, D.; Curatolo, W. J. Hydroxypropyl Methylcellulose Acetate Succinate-Based Spray-Dried Dispersions: An Overview Mol. Pharmaceutics 2008, 5, 1003-1019
    • (2008) Mol. Pharmaceutics , vol.5 , pp. 1003-1019
    • Friesen, D.1    Shanker, R.2    Crew, M.3    Smithey, D.4    Curatolo, W.J.5
  • 44
    • 0032756138 scopus 로고    scopus 로고
    • Physical properties of solid molecular dispersions of indomethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinylacetate) in relation to indomethacin crystallization
    • Matsumoto, T.; Zografi, G. Physical properties of solid molecular dispersions of indomethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinylacetate) in relation to indomethacin crystallization Pharm. Res. 1999, 16, 1722-1728
    • (1999) Pharm. Res. , vol.16 , pp. 1722-1728
    • Matsumoto, T.1    Zografi, G.2
  • 45
    • 0001537245 scopus 로고    scopus 로고
    • Constraints, metastability, and inherent structures in liquids
    • Corti, D. S.; Debenedetti, P. G.; Sastry, S.; Stillinger, F. H. Constraints, metastability, and inherent structures in liquids Phys. Rev. E 1997, 55, 5522-5534
    • (1997) Phys. Rev. E , vol.55 , pp. 5522-5534
    • Corti, D.S.1    Debenedetti, P.G.2    Sastry, S.3    Stillinger, F.H.4


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