Quality-by-design (QbD): An integrated process analytical technology (PAT) approach for real-time monitoring and mapping the state of a pharmaceutical coprecipitation process

Journal of Pharmaceutical Sciences

Volumn 99, Issue 3, 2010, Pages 1516-1534

  Wu, Huiquan ^a   Khan, Mansoor A ^a  

^a Office of Testing and Research   (United States)

Author keywords

Coprecipitation; Crystal growth; Crystal size distribution (CSD); Incubation; Nucleation; Principal component analysis; Process analytical technology (PAT); Process trajectory; Quality by design (QbD); Real time process monitoring

Indexed keywords

EUDRAGIT; NAPROXEN;

ACCURACY; ARTICLE; CRYSTALLIZATION; DRUG DESIGN; DRUG INDUSTRY; DRUG MANUFACTURE; DRUG MONITORING; INCUBATION TIME; NEAR INFRARED SPECTROSCOPY; PRINCIPAL COMPONENT ANALYSIS; PROCESS CONTROL; PROCESS DESIGN; PROCESS TECHNOLOGY; THERMODYNAMICS; TURBIDITY;

EID: 76649117080     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21923     Document Type: Article

References (56)

1. FDA, CDER. 1987. Guideline for Submitting Supporting Documentation in Drug Applications for the Manufacturing of Drug Substances. Available at: http://www.fda.gov/cder/guidance/drugsub.pdf.
2. FDA. 1998. Guidance for Industry, Manufacturing, Processing, or Holding Active Pharmaceutical Ingredients. Draft Guidance Available at: http://www.fda.gov/cder/guidance/1289dft.pdf.
3. FDA, CDER. 2007. Guidance for Industry. ANDAs: Pharmaceutical Solid Polymorphism. Chemistry, manufacturing, and Controls Information. Available at: http://www.fda.gov/cder/guidance/7590fnl.pdf.
4. FDA/ICH. 2006. Guidance for Industry. Q8 Pharmaceutical Development. Available at: http://www.fda.gov/cder/guidance/6746fnl.pdf.
5. Cairia M. 1998. Crystalline polymorphism of organic compounds. Top Curr Chem 198:163-208.
6. Morissette SL, Soukasene S, Levinson D, Cima MJ, Almarsson O ̈ . 2003. Elucidation of crystal from diversity of the HIV protease inhibitor ritonavir by high-throughput crystallization. Proc Natl Acad Soc USA 100:2180-2184.
7. Kempf DJ, Marsh KC, Denissen JF, McDonald E, Vasavanonda S, Flentge CA, Green BE, Fino L, Park CH, Kong X, Wieburg NE, Salvidar A, Ruiz L, Kati WM, Sham HL, Robins T, Stewart KD, Hsu A, Plattner JJ, Leonard JM, Norbeck DW. 1995. ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. Proc Natl Acad Soc USA 92:2484-2488.
8. Law D, Krill SL, Schmitt EA, Fort JJ, Qiu Y, Wang W, Porter WR. 2001. Physicochemical considerations in the preparation of amorphous ritonavir-polyethylene glycol 8000 solid dispersions. J Pharm Sci 90:1015-1025.
9. Chemburkar SR, Bauer J, Deming K, Spiwek H, Patel K, Moris J, Henry R, Spanton S, Dziki W, Porter W, Quick J, Bauer P, Donaubauer J, Narayanan BA, Soldani M, Riley D, McFarland K. 2000. Dealing with the impact of Ritonavir polymorphs on the late stages of bulk drug process development. Org Proc Res Dev 4:413-417.
10. Podr?́guez-Hornedo N, Murphy D. 1999. Significance of controlling crsyatllization mechanisms and kinetics in pharmaceutical systems. J Pharm Sci 88:651-660.
11. Bhugra C, Pikal MJ. 2008. Role of thermodynamic, molecular, and kinetic factors in crystallization from the amorphous state. J Pharm Sci 97:1329-1349.
12. Caira MR. 1998. Crystalline polymorphism of organic compounds. Top Curr Chem 198:163-208.
13. Farber L, Tardos GI, Michaels JN. 2003. Evolution and structure of drying material bridges of pharmaceutical excipients: Studies on a microscopic slide. Chem Eng Sci 58:4515-4525.
14. Févotte G. 2007. In situ Raman spectroscopy for inline control of pharmaceutical crystallization and solids elaboration processes: A review. Trans IChemE, part A. Chem Eng Des. 85:906-920.
15. Nagy ZK, Chew JW, Fujiwara M, Braatz RD. 2008. Comparative performance of concentration and temperature controlled batch crystallizations. J Process Control 18:399-407.
16. Yu L, Lionberger RA, Raw AS, D'Costa R, Wu H, Hussain AS. 2004. Applications of process analytical technology to crystallization processes. Adv Drug Deliv Rev 56:349-369.
17. Wu H, Hussain AS. 2005. Use of PAT for Active Pharmaceutical Ingredients Crystallization Process Control. Conference Proceedings of the 16th International Federation of Automatic Control (IFAC) World Congress (CD-ROM). Edited by P. Horacek, M. Simandl, and P. Zitek. Prague, Czech Republic, July 4-9, 2005.
18. FDA/ICH. 2008. Q8(R1) Pharmaceutical Development Revision 1. Draft available at: http://www.fda.gov/cder/guidance/8084dft.pdf.
19. Parker RL, Manning JR, Peterson NC. 1985. Application of pulse-echo ultrasonics to locate the solid/liquid interface during solidification and melting of steel and other metals. J Appl Phys 58:4150-4164.
20. Wu H, Hussain AS, Khan MA. 2007. Process control perspective for process analytical technology: Integration of chemical engineering practice into semiconductor and pharmaceutical industries. Chem Eng Commun 194:760-779.
21. FDA. 2004. Guidance for Industry. PAT-A Framework for Innovative Pharmaceutical Development, Manufacturing, and Quality Assurance. Available at: http://www.fda.gov/cder/guidance/6419fnl.pdf.
22. FDA. 2008. Guidance for Industry. Process Validation: General Principles and Practices. Draft Guidance. Available at: http://www.fda.gov/cder/ guidance/8019dft.pdf.
23. FDA/ICH. 2006. Guidance for Industry. Q9 Quality Risk Management. Available at: http://www.fda.gov/cder/guidance/7153fnl.pdf.
24. FDA/ICH. 2007. Q10. Pharmaceutical Quality System. Draft Consensus Guideline. Available at: http://www.fda.gov/cder/guidance/7891dft.pdf.
25. Woodcock J. 2004. The concept of pharmaceutical quality. Am Pharm Rev 7:10-15.
26. Nasr MM. 2005. Quality by Design in the New Pharmaceutical Quality Assessment System (PQAS). Quality-International 2005 Conference, London, Nov. 21, 2005. Available at: http://www. fda.gov/cder/Offices/ONDQA/presentations/ 051116-QbD-%20PQAS.pdf (accessed on January 07, 2009).
27. Wu H, Lyon RC, Hussain AS, Drennen JD III, DasGupta D, Voytilla RJ, Bejic L. 2003. Application of Principal Component Analysis in Assessing Pharmaceutical Formulation Design: Exploring the Casual Links between the Tablet Processing Conditions and Drug Dissolution Rate. In: Proceedings of Symposium on Innovations in Pharmaceutical and Biotechnology Development and Manufacturing, 2003 AIChE Annual Meeting [TE001], pp. 635-642. San Francisco, Nov. 17-21, 2003.
28. Wu H, Hussain AS. 2005. Integration of multivariate statistics and design of experiments to identify critical process variables for pharmaceutical process analytical technology (PAT) applications. In: American Statistical Association 2005 Proceedings of Joint Statistical Meetings, Minneapolis, Minnesota, August 7-11, 2005. CD-ROM, Mira Digital Publishing.
29. Wu H, Heilweil E, Hussain AS, Khan M. 2007. Process Analytical Technology (PAT): Quantification Approaches in Terahertz Spectroscopy for Pharmaceutical Application. J Pharm Sci 97: 970-984.
30. Wu H, Heilweil E, Hussain AS, Khan MA. 2007. Process Analytical Technology (PAT): Effects of instrumental and compositional variables on terahertz spectral data quality to characterize pharmaceutical materials and tablets. Int J Pharm 343:148-158.
31. Xie L, Wu H, Shen M, Augsburger L, Lyon RC, Khan MA, Hussain AS, Hoag SW. 2008. Quality-by-Design (QbD): Effects of testing parameters and formulation variables on the segregation tendency of pharmaceutical powder measured by the ASTM D 6940-04 Segregation Tester. J Pharm Sci 97:4485-4497.
32. Wu H, Khan MA. 2009. Quality-by-Design (QbD): An integrated approach for evaluation of powder blending process kinetics and determination of powder blending end-point. J Pharm Sci 98: 2784-2798.
33. Wu H, Tawakkul M, White M, Khan MA. 2009. Quality-by-Design (QbD): An integrated multivariate approach for the component quantification in powder blends. Int J Pharm 372:39-48.
34. Khan MA, et al. 1994. Optimization of process variables for the preparation of ibuprofen coprecipitates with Eudragit S100. Int J Pharm 102:185-192.
35. Zaghloul AA, Faltinek J, Vaithiyalingam SR, Reddy IK, Khan MA. 2001. Naproxen-Eudragit microspheres: Screening of process and formulation variables for the preparation of extended release tablets. Pharmazie 56:321-324.
36. Kislalioglu MS, Khan MA, Blount C, Goettsch RW, Bolton S. 1991. Physical characterization and dissolution properties of ibuprofen: Eudragit coprecipitates. J Pharm Sci 80:799-804.
37. Wu H, Khan MA. 2006. Mapping the State of a Pharmaceutical Co-precipitation Process: An Integrated Process Analytical Technology (PAT) Approach. Conference Proceedings of the 2006 AIChE Annual Meeting (CD-ROM). AIChE Proceeding P-235, ISBN:0-8169-1012-X.
38. Caillet A, Puel F, Fevotte G. 2008. Quantitative in situ monitoring of citric acid phase transition in water using Raman spectroscopy. Chem Eng Process 47:377-382.
39. Radhakrishnan R, Trout BL. 2003. Nucleation of crystalline phases of water in homogeneous and inhomogeneous environments. Phys Rev Lett 90:158301(4).
40. Radhakrishnan R, Trout BL. 2003. Nucleation of hexagonal Ice (Ih) in liquid water. J Am Chem Soc 125:7743-7747.
41. Beckham GT, Peters B, Starbuck C, Variankaval N, Trout BL. 2007. Surface-mediated nucleation in the solid-state polymorph transformation of terephthalic acid. J Am Chem Soc 129:4714-4723.
42. Beckham GT, Peters B, Trout BL. 2008. Evidence for a size dependent nucleation mechanism in solid state polymorph transformations. J Phys Chem B 112:7460-7466.
43. Seborg DE, Edgar TF, Mellichamp DA. 1989. Process dynamics and control. New York, NY: John Wiley & Sons. p 3.
44. Hotelling H. 1933. Analysis of a complex of statistical variables into principal components. J Educ Psychol 24:417-441, 498-520.
45. Pearson K. 1901. On lines and planes of closet fit to systems of points in space. Philos Mag 2:559-572.
46. Wise BM, Gallagher NB. 1996. The process chemometrics approach to process monitoring and fault detection. J Process Control 6:329-348.
47. Ralston P, Depuy G, Graham JH. 2001. Computerbased monitoring and fault diagnosis: A chemical process case study. ISA Trans 40:85-98.
48. Russel EL, Chiang LH, Brattz RD. 2000. Datadriven techniques for fault detection and diagnosis in chemical process. London: Springer-Verlag.
49. Srinivasan R, Qian MS. 2005. Off-line temporal signal comparison using singular points augmented time warping. Ind Eng Chem Res 44:4697-4716.
50. Doan X-T, Srinivasan R, Bapat PM, Wangikar PP. 2007. Detection of phase shifts in batch fermentation via statistical analysis of the online measurements: A case study with rifamycin B fermentation. J Biotechnol 132:156-166.
51. Sulub Y, Wabuyele B, Gargiulo P, Pazdan J, Cheney J, Berry J, Gupta A, Shah R, Wu H, Khan M. 2009. Real-time on-line blend uniformity monitoring using near-infrared reflectance spectroscopy: A noninvasive off-line calibration approach. J Pharm Biomed Anal 49:48-54.
52. Sekulic SS, Ward HW, Brannegan DR, Stanley ED, Evans CL, Sciavolino ST, Hailey PA, Aldridge PK. 1996. On-line monitoring of powder blend homogeneity by near-infrared spectroscopy. Anal Chem 68:509-513.
53. Hailey PA, Doherty P, Tapsell P, Oliver T, Aldridge PK. 1996. Automated system for the on-line monitoring of powder blending process using near-infrared spectroscopy. Part I. System development and control. J Pharm Biomed Anal 14:551-559.
54. Sekulic SS,WakemanJ,Doherty P,HaileyPA. 1998. Automated systemfor the on-line monitoring of powder blending process using near-infrared spectroscopy. Part II. Qualitative approaches to blend evaluation. J Pharm Biomed Anal 17:1285-1309.
55. Lai C-K, Holt D, Leung JC, Cooney CL, Raju GK, Hansen P. 2001. Real time and noninvasive monitoring of dry powder blend homogeneity. AIChE J 47:2618-2622.
56. Ciurczak EW, Drennen JD III. 2001. Near-infrared spectroscopy in pharmaceutical applications. In: Burns DA, Ciurczak EW, editors. Handbook of Near-Infrared Analysis, 2nd edition New York: Marcel Dekker.