Homogeneity of amorphous solid dispersions – an example with KinetiSol^®

References

• Loftsson T, Brewster ME. Pharmaceutical applications of cyclodextrins: basic science and product development. J Pharm Pharmacol. 2010;62:1607–1621.
   PubMed Web of Science ®Google Scholar
• Ellenberger DJ, Miller DA, Williams RO. Expanding the application and formulation space of amorphous solid dispersions with KinetiSol®: a Review. AAPS PharmSciTech. 2018;19:1933–1956.
   PubMed Web of Science ®Google Scholar
• DiNunzio JC, Brough C, Miller DA, et al. Applications of KinetiSol® dispersing for the production of plasticizer free amorphous solid dispersions. Eur J Pharm Sci. 2010;40:179–187.
   PubMed Web of Science ®Google Scholar
• Miller DA, DiNunzio JC, Hughey JR, et al. KinetiSol: a new processing paradigm for amorphous solid dispersion systems. Drug Dev Deliv. 2012;11:22–31.
   Google Scholar
• Brouwers J, Brewster ME, Augustijns P. Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability? J Pharm Sci. 2009;98:2549–2572.
   PubMed Web of Science ®Google Scholar
• Guzmán HR, Tawa M, Zhang Z, et al. Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of celecoxib from solid oral formulations. J Pharm Sci. 2007;96:2686–2702.
   PubMed Web of Science ®Google Scholar
• Jermain SV, Brough C, Williams RO. Amorphous solid dispersions and nanocrystal technologies for poorly water-soluble drug delivery – an update. Int J Pharm. 2018;535:379–392.
   PubMed Web of Science ®Google Scholar
• LaFountaine JS, McGinity JW, Williams RO. Challenges and strategies in thermal processing of amorphous solid dispersions: a review. AAPS PharmSciTech. 2016;17:43–55.
   PubMed Web of Science ®Google Scholar
• Miller DA, Ellenberger D, Gil M. Spray-Drying Technology. In: Williams III, RO, Watts AB, Miller DA, editors. Formulating Poorly Water Soluble Drugs. Second ed. Cham, Switzerland: Springer International; 2016. p. 437–525.
   Google Scholar
• Jermain SV, Miller DA, Williams RO. III, The case for continued innovation - novel amorphous solid dispersion technologies for an increasing insoluble drug problem. AAPS News magazine. 2018;09:14–18.
   Google Scholar
• Hughey JR, Keen JM, Brough C, et al. Thermal processing of a poorly water-soluble drug substance exhibiting a high melting point: the utility of KinetiSol® dispersing. Int J Pharm. 2011;419:222–230.
   PubMed Web of Science ®Google Scholar
• Ellenberger DJ, Miller DA, Kucera SU, et al. Improved vemurafenib dissolution and pharmacokinetics as an amorphous solid dispersion produced by KinetiSol® processing. AAPS PharmSciTech. 2018;19:1957–1970.
   PubMed Web of Science ®Google Scholar
• Miller DA, Keen JM, Kucera SU, inventors; DisperSol Technologies, LLC, assignee. Formulations of deferasirox and methods of making the same. US patent US20170027911A1. 2016 June 17.
   Google Scholar
• Bennett RC, Brough C, Miller DA, et al. Preparation of amorphous solid dispersions by rotary evaporation and KinetiSol dispersing: approaches to enhance solubility of a poorly water-soluble gum extract. Drug Dev Ind Pharm. 2015;41:382–397.
   PubMed Web of Science ®Google Scholar
• Miller DA, Keen JM, Brough C, et al. Bioavailability enhancement of a BCS IV compound via an amorphous combination product containing ritonavir. J Pharm Pharmacol. 2016;68:678–691.
   PubMed Web of Science ®Google Scholar
• LaFountaine JS, Prasad LK, Brough C, et al. Thermal processing of PVP- and HPMC-based amorphous solid dispersions. AAPS PharmSciTech. 2016;17:120–132.
   PubMed Web of Science ®Google Scholar
• Miller DA, Keen JM, Brough C, inventors; Tetrabenazine modified release formulation. United States. WO patent WO2015175505A1. 2015 Nov 19.
   Google Scholar
• LaFountaine JS, Jermain SV, Prasad LK, et al. Enabling thermal processing of ritonavir–polyvinyl alcohol amorphous solid dispersions by KinetiSol® dispersing. Eur J Pharm Biopharm. 2016;101:72–81.
   PubMed Web of Science ®Google Scholar
• DiNunzio JC, Brough C, Hughey JR, et al. Fusion production of solid dispersions containing a heat-sensitive active ingredient by hot melt extrusion and Kinetisol® dispersing. Eur J Pharm Biopharm. 2010;74:340–351.
   PubMed Web of Science ®Google Scholar
• Brough C, McGinity JW, Miller DA, et al., inventors; DisperSol technologies, LLC, assignee. Thermo-kinetic mixing for pharmaceutical applications patent. US 8,486,423 B2. 2013.
   Google Scholar
• Hughey JR, DiNunzio JC, Bennett RC, et al. Dissolution enhancement of a drug exhibiting thermal and acidic decomposition characteristics by fusion processing: a comparative study of hot melt extrusion and Kinetisol® dispersing. AAPS PharmSciTech. 2010;11:760–774.
   PubMed Web of Science ®Google Scholar
• Hughey JR, Keen JM, Miller DA, et al. Preparation and characterization of fusion processed solid dispersions containing a viscous thermally labile polymeric carrier. Int J Pharm. 2012;438:11–19.
   PubMed Web of Science ®Google Scholar
• Keen JM, LaFountaine JS, Hughey JR, et al. Development of Itraconazole tablets containing viscous KinetiSol solid dispersions: in vitro and in vivo analysis in dogs. AAPS PharmSciTech. 2018;19:1998–2008.
   PubMed Web of Science ®Google Scholar
• Brough C, Miller DA, Keen JM, et al. Use of polyvinyl alcohol as a solubility-enhancing polymer for poorly water soluble drug delivery (part 1). AAPS PharmSciTech. 2016;17:167–179.
   PubMedGoogle Scholar
• Brough C, Miller DA, Ellenberger D, et al. Use of polyvinyl alcohol as a solubility enhancing polymer for poorly water-soluble drug delivery (part 2). AAPS PharmSciTech. 2016;17:180–190.
   PubMedGoogle Scholar
• DiNunzio JC, Brough C, Miller DA, et al. Fusion processing of itraconazole solid dispersions by kinetisol dispersing: a comparative study to hot melt extrusion. J Pharm Sci. 2010;99:1239–1253.
   PubMed Web of Science ®Google Scholar
• Qian F, Huang J, Hussain MA. Drug-polymer solubility and miscibility: stability consideration and practical challenges in amorphous solid dispersion development. J Pharm Sci. 2010;99:2941–2947.
   PubMed Web of Science ®Google Scholar
• Hanada M, Jermain SV, Lu X, et al. Predicting physical stability of ternary amorphous solid dispersions using specific mechanical energy in a hot melt extrusion process. Int J Pharm. 2018;548:571–585.
   PubMed Web of Science ®Google Scholar
• Baird JA, Taylor LS. Evaluation of amorphous solid dispersion properties using thermal analysis techniques. Adv Drug Deliv Rev. 2012;64:396–421.
   PubMed Web of Science ®Google Scholar
• Johnston A, Holt DW. Substandard drugs: a potential crisis for public health. Br J Clin Pharmacol. 2014;78:218–243.
   PubMed Web of Science ®Google Scholar
• Ma H, Choi DS, Zhang Y-E, et al. Evaluation on the drug–polymer mixing status in amorphous solid dispersions at the early stage formulation and process development. J Pharm Innov. 2013;8:163–174.
   Web of Science ®Google Scholar
• Huang Y, Dai W-G. Fundamental aspects of solid dispersion technology for poorly soluble drugs. Acta Pharmaceutica Sinica B. 2014;4:18–25.
   PubMed Web of Science ®Google Scholar
• Administration FaD. Guidance for Industry - Powder blends and finished dosage units - stratified in-process dosage unit sampling and assessment. 2003 [cited 2018 Aug 18]. Available from: https://app.gxp-services.net/guidemgr/files/5831dft.pdf
   Google Scholar
• Administration FaD. Questions and answers on current good manufacturing practices - production and process controls 2013 [updated 2013 Aug 6; cited 2018 Aug 15]. Available from: https://www.fda.gov/drugs/guidancecomplianceregulatoryinformation/guidances/ucm124782.htm
   Google Scholar
• Vogt FG. Solid-state characterization of amorphous dispersions. In: Pharmaceutical Amorphous Solid Dispersions. John Wiley & Sons, Inc.; 2015. p.117–178. Available from: https://doi.org/10.1002/9780470571224.pse525
   Google Scholar
• Beata S-H, Radoslaw B, Aneta O-C, et al. Scanning electron microscopy and X-ray energy dispersive spectroscopy – useful tools in the analysis of pharmaceutical products. J Phy: Confer Series. 2017;931:012008.
   Google Scholar
• Scoutaris N, Vithani K, Slipper I, et al. SEM/EDX and confocal Raman microscopy as complementary tools for the characterization of pharmaceutical tablets. Int J Pharm. 2014;470:88–98.
   PubMedGoogle Scholar
• Mah PT, Fraser SJ, Reish ME, et al. Use of low-frequency Raman spectroscopy nd chemometrics for the quantification of crystallinity in amorphous griseofulvin tablets. Vibr Spec. 2015;77:10–16.
   Web of Science ®Google Scholar
• Taylor LS, Zografi G. The quantitative analysis of crystallinity using FT-Raman spectroscopy. Pharm Res. 1998;15:755–761.
   PubMed Web of Science ®Google Scholar
• Strachan CJ, Rades T, Gordon KC, et al. Raman spectroscopy for quantitative analysis of pharmaceutical solids. J Pharm Pharmacol. 2007;59:179–192.
   PubMed Web of Science ®Google Scholar
• Aaltonen J, Gordon KC, Strachan CJ, et al. Perspectives in the use of spectroscopy to characterise pharmaceutical solids. Int J Pharm. 2008;364:159–169.
   PubMed Web of Science ®Google Scholar
• Wabuyele BW, Sotthivirat S, Zhou GX, et al. Dispersive Raman spectroscopy for quantifying amorphous drug content in intact tablets. J Pharm Sci. 2017;106:579–588.
   PubMed Web of Science ®Google Scholar
• Yuan X, Xiang T-X, Anderson BD, et al. Hydrogen bonding interactions in amorphous indomethacin and its amorphous solid dispersions with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinyl acetate) studied using 13C solid-state NMR. Mol Pharm. 2015;12:4518–4528.
   PubMed Web of Science ®Google Scholar
• Bashiri-Shahroodi A, Nassab PR, Szabó-Révész P, et al. Preparation of a solid dispersion by a dropping method to improve the rate of dissolution of Meloxicam. Drug Dev Ind Pharm. 2008;34:781–788.
   PubMed Web of Science ®Google Scholar
• Haser A, Huang S, Listro T, et al. An approach for chemical stability during melt extrusion of a drug substance with a high melting point. Int J Pharm. 2017;524:55–64.
   PubMed Web of Science ®Google Scholar
• Seedher N, Bhatia S. Solubility enhancement of cox-2 inhibitors using various solvent systems. AAPS PharmSciTech. 2003;4:36–44.
   Google Scholar
• Overhoff KA, Johnston K, Tam J, et al. Use of thin film freezing to enable drug delivery: a review. J Drug Deliv Sci Technol. 2009;19:89–98.
   Google Scholar
• van Drooge DJ, Hinrichs WLJ, Visser MR, et al. Characterization of the molecular distribution of drugs in glassy solid dispersions at the nano-meter scale, using differential scanning calorimetry and gravimetric water vapour sorption techniques. Int J Pharm. 2006;310:220–229.
   PubMed Web of Science ®Google Scholar
• Karavas E, Georgarakis M, Docoslis A, et al. 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.
   PubMed Web of Science ®Google Scholar