Manufacturing classification system in the real world: factors influencing manufacturing process choices for filed commercial oral solid dosage formulations, case studies from industry and considerations for continuous processing

References

• Aguilar-Díaz JE, García-Montoya E, Pérez-Lozano P, Suñé-Negre JM, Miñarro M, Ticó JR. 2014. SeDeM expert system a new innovator tool to develop pharmaceutical forms. Drug Dev Ind Pharm. 40:222–236.
   PubMed Web of Science ®Google Scholar
• Allesø M, Torstenson AS, Bryder M, Holm P. 2013. Presenting a rational approach to QbD-based pharmaceutical development: A roller compaction case study. Eur Pharma Rev. 18:17–24.
   Google Scholar
• Almaya A. 2008. Development of low-dose solid oral formulations using wet granulation. In: Zheng J, editor. Formulation and analytical development for low-dose oral drug products. Hoboken (NJ): Wiley; p. 89–115.
   Google Scholar
• Amidon GL, Lennernäs H, Shah VP, Crison JR. 1995. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res. 12:413–420.
   PubMed Web of Science ®Google Scholar
• Amin MCI, Fell JT. 2004. Comparison studies on the percolation thresholds of binary mixture tablets containing excipients of plastic/brittle and plastic/plastic deformation properties. Drug Dev Ind Pharm. 30:937–945.
   PubMed Web of Science ®Google Scholar
• Batra A, Desai D, Serajuddin ATM. 2017. Investigating the use of polymeric binders in twin screw melt granulation process for improving compactibility of drugs. J Pharm Sci. 106:140–150.
   PubMed Web of Science ®Google Scholar
• Benet LZ. 2010. Predicting drug disposition via application of a biopharmaceutics drug disposition classification system. Basic Clin Pharmacol Toxicol. 106:162–167.
   PubMed Web of Science ®Google Scholar
• Butler JM, Dressman JB. 2010. The developability classification system: application of biopharmaceutics concepts to formulation development. J Pharm Sci. 99:4940–4954.
   PubMed Web of Science ®Google Scholar
• Capece M, Ho R, Strong J, Gao P. 2015. Prediction of powder flow performance using a multi-component granular bond number. Powder Technol. 286:561–571.
   Web of Science ®Google Scholar
• Capece M, Huang Z, Davé R. 2017. Insight into a novel strategy for the design of tablet formulations intended for direct compression. J Pharm Sci. 106:1608–1617.
   PubMed Web of Science ®Google Scholar
• Caraballo I, Millan M, Rabasco AM. 1996. Relationship between drug percolation threshold and particle size in matrix tablets. Pharm Res. 13:387–390.
   PubMed Web of Science ®Google Scholar
• Chattoraj S, Daugherity P, McDermott T, Olsofsky A, Roth WJ, Tobyn M. 2018. Sticking and picking in pharmaceutical tablet compression: an IQ consortium review. J Pharm Sci. 107:2267–2282.
   PubMed Web of Science ®Google Scholar
• Chattoraj S, Sun CC. 2018. Crystal and particle engineering strategies for improving powder compression and flow properties to enable continuous tablet manufacturing by direct compression. J Pharm Sci. 107:968–974.
   PubMed Web of Science ®Google Scholar
• Crooks MJ, Ho R. 1976. Ordered mixing in direct compression of tablets. Powder Technol. 14:161–167.
   Web of Science ®Google Scholar
• Elder DP. 2016. Excipients: current perspectives. Chim Oggi/Chem Today. 34:16–20.
   Web of Science ®Google Scholar
• EMA. Annex II to note for guidance on process validation CHMP/QWP/848/99 and EMA/CVMP/589/99 non-standard processes 2004 [updated 10-Aug-2004; accessed 2018 Feb 3]. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002914.pdf.
   Google Scholar
• EMA. European Public Assessment Reports: European Medicines Agency; 2017 [accessed May 2017]. http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/landing/epar_search.jsp.
   Google Scholar
• Ferreira AP, Olusanmi D, Sprockel O, Abebe A, Nikfar F, Tobyn M. 2016. Use of similarity scoring in the development of oral solid dosage forms. Int J Pharm. 514:335–340.
   PubMedGoogle Scholar
• Fonteyne M, Vercruysse J, De Leersnyder F, Van Snick B, Vervaet C, Remon JP, De Beer T. 2015. Process analytical technology for continuous manufacturing of solid-dosage forms. Trac Trend Anal Chem. 67:159–166.
   Web of Science ®Google Scholar
• Fonteyne M, Wickström H, Peeters E, Vercruysse J, Ehlers H, Peters BH, Remon JP, Vervaet C, Ketolainen J, Sandler N, et al. 2014. Influence of raw material properties upon critical quality attributes of continuously produced granules and tablets. Eur J Pharm Biopharm. 87:252–263.
   PubMed Web of Science ®Google Scholar
• Fridgeirsdottir GA, Harris R, Fischer PM, Roberts CJ. 2016. Support tools in formulation development for poorly soluble drugs. J Pharm Sci. 105:2260–2269.
   PubMed Web of Science ®Google Scholar
• Gamble J, Jones J, Tobyn M. 2017. Understanding the effect of API changes in pharmaceutical processing. Eur Pharm Rev. 22:20–22.
   Google Scholar
• Gao JZH, Jain A, Motheram R, Gray DB, Hussain MA. 2002. Fluid bed granulation of a poorly water-soluble, low density, micronized drug: comparison with high shear granulation. Int J Pharm. 237:1–14.
   PubMed Web of Science ®Google Scholar
• Goh HP, Heng PWS, Liew CV. 2018. Comparative evaluation of powder flow parameters with reference to particle size and shape. Int J Pharm. 547:133–141.
   PubMed Web of Science ®Google Scholar
• Goodwin DJ, van den Ban S, Denham M, Barylski I. 2018. Real-time release testing of tablet content and content uniformity. Int J Pharm. 537:183–192.
   PubMedGoogle Scholar
• Grote S, Kleinebudde P. 2018a. A comparative study of the influence of alpha-lactose monohydrate particle morphology on granule and tablet properties after roll compaction/dry granulation. Pharm Dev Tech. Forthcoming. doi:10.1080/10837450.2018.1476977
   PubMedGoogle Scholar
• Grote S, Kleinebudde P. 2018b. Impact of functionalized particle structure on roll compaction/dry granulation and tableting of calcium carbonate. Int J Pharm. 544:235–241.
   PubMedGoogle Scholar
• Grote S, Kleinebudde P. 2018c. Roll compaction/dry granulation of dibasic calcium phosphate anhydrous-does the morphology of the raw material influence the tabletability of dry granules? J Pharm Sci. 107:1104–1111.
   PubMed Web of Science ®Google Scholar
• Hancock BC, Garcia-Munoz S. 2013. How do formulation and process parameters impact blend and unit dose uniformity? Further analysis of the product quality research institute blend uniformity working group industry survey. J Pharm Sci. 102:982–986.
   PubMed Web of Science ®Google Scholar
• Hayashi Y, Oishi T, Shirotori K, Marumo Y, Kosugi A, Kumada S, Hirai D, Takayama K, Onuki Y. 2018. Modeling of quantitative relationships between physicochemical properties of active pharmaceutical ingredients and tensile strength of tablets using a boosted tree. Drug Dev Ind Pharm. 44:1090–1098.
   PubMed Web of Science ®Google Scholar
• Hirschberg C, Sun CC, Rantanen J. 2016. Analytical method development for powder characterization: Visualization of the critical drug loading affecting the processability of a formulation for direct compression. J Pharmaceut Biomed. 128:462–468.
   PubMed Web of Science ®Google Scholar
• Kimura G, Betz G, Leuenberger H. 2008. Influence of loading volume of mefenamic acid on granules and tablet characteristics using a compaction simulator. Pharm Dev Technol. 13:57–64.
   PubMed Web of Science ®Google Scholar
• Kimura G, Puchkov M, Leuenberger H. 2013. An attempt to calculate in silico disintegration time of tablets containing mefenamic acid, a low water-soluble drug. J Pharm Sci. 102:2166–2178.
   PubMed Web of Science ®Google Scholar
• Košir D, Ojsteršek T, Vrečer F. 2018. Does the performance of wet granulation and tablet hardness affect the drug dissolution profile of carvedilol in matrix tablets? Drug Dev Ind Pharm. 44:1543–1550.
   PubMed Web of Science ®Google Scholar
• Kuentz M, Holm R, Elder DP. 2016. Methodology of oral formulation selection in the pharmaceutical industry. Eur J Pharm Sci. 87:136–163.
   PubMed Web of Science ®Google Scholar
• Kurrer C, Schulten K. 1993. Dependence of percolation thresholds on lattice connectivity. Phys Rev E. 48:614–617.
   Web of Science ®Google Scholar
• Kushner J. 2013. Utilizing quantitative certificate of analysis data to assess the amount of excipient lot-to-lot variability sampled during drug product development. Pharm Dev Tech. 18:333–342.
   PubMed Web of Science ®Google Scholar
• Leane M, Pitt K, Reynolds G, Anwar J, Charlton S, Crean A, Creekmore R, Davies C, DeBeer T, De MM, et al. 2015. A proposal for a drug product Manufacturing Classification System (MCS) for oral solid dosage forms. Pharm Dev Tech. 20:12–21.
   PubMed Web of Science ®Google Scholar
• Leane M. 2015. Classifying manufacture: a classification systemcould make the R&D manufacturing interface much easier to navigate. Medicine Maker. 17–18.
   Google Scholar
• Leuenberger H, Bonny JD, Kolb M. 1995. Percolation effects in matrix-type controlled drug release systems. Int J Pharm. 115:217–224.
   Web of Science ®Google Scholar
• Leuenberger H. 1999. The application of percolation theory in powder technology. Adv Powder Technol. 10:323–352.
   Web of Science ®Google Scholar
• Löbenberg R, Amidon GL. 2000. Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur J Pharm Biopharm. 50:3–12.
   PubMed Web of Science ®Google Scholar
• Mangal S, Meiser F, Morton D, Larson I. 2015. Particle engineering of excipients for direct compression: Understanding the role of material properties. CPD. 21:5877–5889.
   Google Scholar
• Markarian J. 2015. Choosing oral solid-dosage production processes: could a classification system help? Pharm Tech. 39:30.
   Google Scholar
• McCormick D. 2005. Evolutions in direct compression. Pharm Tech. 29:52–62.
   Google Scholar
• Meena AK, Desai D, Serajuddin ATM. 2017. Development and optimization of a wet granulation process at elevated temperature for a poorly compactible drug using twin screw extruder for continuous manufacturing. J Pharm Sci. 106:589–600.
   PubMed Web of Science ®Google Scholar
• Morin G, Briens L. 2014. A comparison of granules produced by high-shear and fluidized-bed granulation methods. AAPS PharmSciTech. 15:1039–1048.
   PubMed Web of Science ®Google Scholar
• Orubu ESF, Tuleu C. 2017. Medicines for children: flexible solid oral formulations. Bull World Health Organ. 95:238–240.
   PubMed Web of Science ®Google Scholar
• Pandey P, Bindra DS, Gour S, Trinh J, Buckley D, Badawy S. 2014. Excipient–process interactions and their impact on tablet compaction and film coating. J Pharm Sci. 103:3666–3674.
   PubMed Web of Science ®Google Scholar
• Patra CN, Pandit HK, Singh SP, Devi MV. 2008. Applicability and comparative evaluation of wet granulation and direct compression technology to Rauwolfia serpentina root powder: a technical note. AAPS PharmSciTech. 9:100–104.
   PubMed Web of Science ®Google Scholar
• Pudasaini N, Parker CR, Hagen SU, Bond AD, Rantanen J. 2018. Role of solvent selection on crystal habit of 5-aminosalicylic acid-combined experimental and computational approach. J Pharm Sci. 107:1112–1121.
   PubMed Web of Science ®Google Scholar
• Pudasaini N, Upadhyay PP, Parker CR, Hagen SU, Bond AD, Rantanen J. 2017. Downstream processability of crystal habit-modified active pharmaceutical ingredient. Org Process Res Dev. 21:571–577.
   Web of Science ®Google Scholar
• Rees JE, Shotton E. 1970. Some observations on the ageing of sodium chloride compacts. J Pharm Pharmacol. 22:17S–23S.
   Web of Science ®Google Scholar
• Roth WJ, Almaya A, Kramer TT, Hofer JD. 2017. A demonstration of mixing robustness in a direct compression continuous manufacturing process. J Pharm Sci. 106:1339–1346.
   PubMed Web of Science ®Google Scholar
• Scholtz JC, Steenekamp JH, Hamman JH, Tiedt LR. 2017. The sedem expert diagram system: its performance and predictability in direct compressible formulations containing novel excipients and different types of active ingredients. Powder Technol. 312:222–236.
   Web of Science ®Google Scholar
• Stauffer F, Vanhoorne V, Pilcer G, Chavez PF, Rome S, Schubert MA, Aerts L, De Beer T. 2018. Raw material variability of an active pharmaceutical ingredient and its relevance for processability in secondary continuous pharmaceutical manufacturing. Eur J Pharm Biopharm. 127:92–103.
   PubMed Web of Science ®Google Scholar
• Sun WJ, Aburub A, Sun CC. 2017. Particle engineering for enabling a formulation platform suitable for manufacturing low-dose tablets by direct compression. J Pharm Sci. 106:1772–1777.
   PubMed Web of Science ®Google Scholar
• SurveyMonkey. 2017. [accessed 2017 Aug 31]. http://tmm.txp.to/0215/MCS
   Google Scholar
• Suzuki M, Oshima T. 1985. Co-ordination number of a multi-component randomly packed bed of spheres with size distribution. Powder Technol. 44:213–218.
   Web of Science ®Google Scholar
• Swainson S, McGarry A, Reynolds GK, Roberts R. A big data approach to powder flowability understanding. Poster Presentation at the 2016 AAPS Annual Meeting and Exposition; November 13–17, 2016; Denver, CO. Poster 36T1000.
   Google Scholar
• Ticehurst MD, Marziano I. 2015. Integration of active pharmaceutical ingredient solid form selection and particle engineering into drug product design. J Pharm Pharmacol. 67:782–802.
   PubMed Web of Science ®Google Scholar
• Trementozzi AN, Leung CY, Osei-Yeboah F, Irdam E, Lin Y, MacPhee JM, Boulas P, Karki SB, Zawaneh PN. 2017. Engineered particles demonstrate improved flow properties at elevated drug loadings for direct compression manufacturing. Int J Pharm. 523:133–141.
   PubMedGoogle Scholar
• Upadhyay PP, Pudasaini N, Mishra MK, Ramamurty U, Rantanen J. 2018. Early assessment of bulk powder processability as a part of solid form screening. Chem Eng Res Des. 136:447–455.
   Web of Science ®Google Scholar
• van den Ban S, Pitt KG, Whiteman M. 2018. Application of a tablet film coating model to define a process-imposed transition boundary for robust film coating. Pharm Dev Tech. 23:176–182.
   PubMed Web of Science ®Google Scholar
• Van Snick B, Holman J, Vanhoorne V, Kumar A, De Beer T, Remon JP, Vervaet C. 2017. Development of a continuous direct compression platform for low-dose drug products. Int J Pharm. 529:329–346.
   PubMed Web of Science ®Google Scholar
• Vasconcelos T, Marques S, Sarmento B. 2017. The biopharmaceutical classification system of excipients. Ther Deliv. 8:65–78.
   PubMed Web of Science ®Google Scholar
• Vercruysse J, Delaet U, Van Assche I, Cappuyns P, Arata F, Caporicci G, De Beer T, Remon JP, Vervaet C. 2013. Stability and repeatability of a continuous twin screw granulation and drying system. Eur J Pharm Biopharm. 85:1031–1038.
   PubMed Web of Science ®Google Scholar
• Wenzel T, Stillhart C, Kleinebudde P, Szepes A. 2017. Influence of drug load on dissolution behavior of tablets containing a poorly water-soluble drug: estimation of the percolation threshold. Drug Dev Ind Pharm. 43:1265–1275.
   PubMed Web of Science ®Google Scholar
• Willecke N, Szepes A, Wunderlich M, Remon JP, Vervaet C, De Beer T. 2017. Identifying overarching excipient properties towards an in-depth understanding of process and product performance for continuous twin-screw wet granulation. Int J Pharm. 522:234–247.
   PubMedGoogle Scholar
• Willecke N, Szepes A, Wunderlich M, Remon JP, Vervaet C, De Beer T. 2018. A novel approach to support formulation design on twin screw wet granulation technology: understanding the impact of overarching excipient properties on drug product quality attributes. Int J Pharm. 545:128–143.
   PubMedGoogle Scholar
• Yu LX, Amidon G, Khan MA, Hoag SW, Polli J, Raju GK, Woodcock J. 2014. Understanding pharmaceutical quality by design. AAPS J. 16:771–783.
   PubMed Web of Science ®Google Scholar
• Yu LX. 2008. Pharmaceutical quality by design: product and process development, understanding, and control. Pharm Res. 25:781–791.
   PubMed Web of Science ®Google Scholar