Particle engineering: A strategy for establishing drug substance physical property specifications during small molecule development

Journal of Pharmaceutical Sciences

Volumn 99, Issue 1, 2010, Pages 51-75

  Iacocca, Ronald G ^a   Burcham, Christopher L ^a   Hilden, Lori R ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

Bioavailability; Content uniformity; Dissolution; Drug product manufacturability; Drug substance physical property characterization methods; GastroPlus; Particle engineering; Strategy

Indexed keywords

BULK DENSITY; DRUG BIOAVAILABILITY; DRUG DOSAGE FORM; DRUG INDUSTRY; DRUG MANUFACTURE; DRUG STABILITY; IMAGE ANALYSIS; LASER DIFFRACTION; MATHEMATICAL MODEL; MOISTURE; PARTICLE SIZE; PHYSICAL CHEMISTRY; REVIEW;

EID: 73949104446     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21801     Document Type: Article

References (46)

1. Byrn SR, Pfeiffer RR, Stowell JG. 1999. Solid-state chemistry of drugs, West Lafayette, IN: SSCI. NOTE - WHY Start at 2?
2. Hilfiker R, Blatter F, von Raumer M. 2006. Polymorphism. Basel, Switzerland: Wiley-VCH verlag GmbH & Co.
3. Gu C-H, Li H, Gandhi RB, Raghavan K. 2004. Grouping solvents by statistical analysis of solvent property parameters: Implication to polymorph screening. Int J Pharm 283:117-125.
4. Mullins JW. 2001. Crystallization. 4th edition. Amsterdam: Butterworth Heineman.
5. Brunauer S, Emmett PH, Teller E. 1938. Adsorption of gases in multimolecular layers. JACS 60: 109-319.
6. Newman A, et al. 2008. Characterization of the "Hyrgroscopic" properties of active pharmaceutical ingredients. J Pharm Sci 97:1047-1059.
7. Heffels C, et al. 1996. Correction of the effect of particle shape on the size distribution measured with a laser diffraction instrument. Part Part Syst Char 13:271-279.
8. Munlenweg H, Hirleman ED. 1998. Laser diffraction spectroscopy: Influence of particle shape and a shape adaptation technique. Part Part Syst Char 15:163-169.
9. Ma Z, et al. 2000. New developments in particle characterization by laser diffraction: Size and shape. Powder Technol 111:66-78.
10. Ma Z, Merkus HG, Scarlett B. 2001. Extending laser diffraction for particle shape considerations: Technical aspects and application. Powder Technol 118:180-187.
11. Yamamoto H, Matsuyama T, Wada M. 2002. Shape distinction of particulate materials by laser diffraction powder analysis. Powder Technol 122:205-211.
12. Heywood AE. 1993. The shape of powder-particle outlines. In: GW, Greenwood editor. Materials science and technology, Vol. 1. Taunton: Research Studies Press Ltd. p. 150.
13. Kaye B. 1993. Fractal dimensions in dataspace; new descriptor for fineparticle systems. Part Part Syst Char 10:191-200.
14. Kaye B, Hollinger M, Tobyn M. 2001. The effect of shape and particle size distribution on the flow of powders. Powder/Bulk Solids.
15. Snorek S, et al. 2007. PQRI recommendations on particle-size analysis of drug substances used in oral dosage forms. J Pharm Sci 96:1451-1467.
16. Allen TA. 1997. Particle size measurement. 5th edition. New York: Chapman and Hall.
17. Nelson RD, Jr. 1988. Dispersing powders in liquids. New York: Elsevier Science.
18. ISO 13320-1: 1999 Particle Size Analysis - Laser Diffraction Methods; Part I: General Principles. 1999, International Standards Organization.
19. Mie G. 1908. Beitrage zur Optik trüber Medien speziell kolloidaler Metallösungen. Ann Phys 25: 377-445.
20. Alderliesten M. 1990. Mean particle diameters. Part I: Evaluation of definition systems. Part Part Syst Char 7:233-241.
21. Alderliesten M. 1991. Mean particle diameters. Part II: Standardization of nomenclature. Part Part Syst Char 8:237-241.
22. Alderliesten M. 2002. Mean particle diameters. Part III: An empirical evaluaton of integration and summation methods for estimating mean particle diameters from histogram data. Part Part Syst Char 19:373-386.
23. Alderliesten M. 2004. Mean particle diameters. Part IV: Empirical selection of the proper type of mean particle diameter describing of a product or material property. Part Part Syst Char 21:179-196.
24. Witt W, Rothele S. 1996. Laser diffraction, unlimited? Part Part Syst Char 13:280-286.
25. Picard E, Michel F, et al. 2007. Size distributions of powders in the range 1 μm-200 μm: Comparison of digital imaging and laser diffraction. Partec 2007: International Congress on Particle Technology. Nürnberg: University of Erlangen.
26. ISO 13322-1:2004. Image Analysis Methods - Part I: Static Image Analysis Methods. 1-39.
27. Drescher S, Heidenreich E. 1990. Technologically relevant particle shape analysis. Part Part Syst Char 7:30-35.
28. Leurkens DW. 1991. Theory and application of morphological analysis: Fine particles and surfaces. In: Beddow JK, editor. CRC series on fine particle science and technology. Boca Raton: CRC Press. p. 282.
29. Kohlus R, Bottlinger M. 1993. Particle shape analysis as an example of knowledge extraction by neural nets. Part Part Syst Char 10:275-278.
30. Podczek F. 1997. Shape factor to assess the shape of particles using image analysis. Powder Technol 93: 47-53.
31. Laitinen N, Rantanen J, et al. 2002. Visualization of particle size and shape distributions using self-organizing maps. Chemometr Intell Lab Syst 62: 47-60.
32. Food and Drug Administration. 2000. Guidance for Industry Waiver of In Vivo Bioavailability Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System.
33. Amidon GL, Lennernäs H, Shah VP, Crison JR. 1995. A theoretical basis for a biopharmaceutics drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12:413-420.
34. Oh D-M, Curl RL, Amidon GL. 1993. Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: A mathematical model. Pharm Res 10:264-270.
35. Oh D-M, Curl RL, Amidon GL. 1993. Estimating the fraction dose absorbed from suspensions of poorly soluble compounds in humans: A mathematical model. Pharm Res 10:264-270.
36. Johnson MCR. 1972. Particle size distribution of the active ingredient for solid dosage forms of low dosage. Pharm Act Helv 47A:546-559.
37. Yalkowski SH, Bolton S. 1990. Particle size and content uniformity. Pharm Res 7:962-966.
38. Zhang Y, Johnson KC. 1997. Effect of drug particle size on content uniformity of low-dose solid dosage forms. Int J Pharm 154:179-183.
39. Rohr BR, Amidon GE, Meury RH, Secreast PJ, King HM, Skoug CJ. 2006. Particle size limits to meet USP content uniformity criteria for tablets and capsules. J Pharm Sci 95:1049-1059.
40. Popov KI, Krstic SB, Obradovic MC, Pavlovic MG, Irvanovic ER. 2003. The effect of the particle shape and structure on the flowability of electrolytic copper powder. I. Modeling of a representative powder particle. J Seb Chem Soc 68:771-777.
41. Tan SB, Newton JM. 1990. Powder flowability as an indication of capsule filling performance. Int J Pharm 61:145-155.
42. Danjo K, Kinoshita K, Kitagawa K, Iida K, Sunada H, Otsuka A. 1989. Effect of particle shape on the compaction and flow properties of powders. Chem Pharm Bull 37:3070-3073.
43. Podczeck F, Miah Y. 1996. The influence of particle size and shape on the angle of internal friction and the flow factor on unlubricated and lubricated powders. Int J Pharm 144:187-194.
44. Burgess DJ, Duffy E, Etzler F, Hickey AJ. 2004. Particle size analysis: AAPS workshop report, cosponsored by the Food and Drug Administration and the United States Pharmacopeia. AAPS J 6:20.
45. Burcham CL, Collins PC, Jarmer DJ, Seibert KD. 2008. Chapter 8: Reduction of particle size of drug substance for low-dose drug products. In: Zheng J, editor. Book chapter in formulation and analytical development for low-dose oral drug products. John-Wiley and Sons, Inc.
46. Aburub A, Risley D, Mishra D. 2008. A critical evaluation of fasted state simulating gastric fluid (FaSSGF) that contains sodium lauryl sulfate and proposal of a modified recipe. Int J Pharm 347: 16-22.