Towards the understanding and prediction of material changes during micronisation using atomic force microscopy

European Journal of Pharmaceutical Sciences

Volumn 38, Issue 1, 2009, Pages 1-8

  Perkins, M C ^a   Bunker, M ^a   James, J ^a   Rigby Singleton, S ^a   Ledru, J ^a   Madden Smith, C ^a   Luk, S ^a   Patel, N ^a   Roberts, C J ^a,b  

^a Molecular Profiles Ltd   (United Kingdom)

^b UNIVERSITY OF NOTTINGHAM   (United Kingdom)

Author keywords

Atomic force microscopy; Hardness; Micronisation; Surface energy; Young's modulus

Indexed keywords

CARBAMAZEPINE;

ARTICLE; ATOMIC FORCE MICROSCOPY; DRUG FORMULATION; DRUG SYNTHESIS; HARDNESS; MATERIAL STATE; NANOANALYSIS; PARTICLE SIZE; PHYSICAL CHEMISTRY; PREDICTION; PRIORITY JOURNAL; X RAY POWDER DIFFRACTION; YOUNG MODULUS;

CARBAMAZEPINE; CHEMISTRY, PHARMACEUTICAL; CRYSTALLIZATION; ELASTIC MODULUS; HARDNESS; MICROSCOPY, ATOMIC FORCE; MICROSCOPY, ELECTRON, SCANNING; PARTICLE SIZE; PHYSICOCHEMICAL PHENOMENA; SURFACE PROPERTIES; X-RAY DIFFRACTION;

EID: 67650239161     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2009.05.004     Document Type: Article

References (51)

1. Begat P., Morton D.A.V., Staniforth J.A., and Price R. The cohesive-adhesive balances in dry powder inhaler formulations I: direct quantification by atomic force microscopy. Pharm. Res. 21 (2004) 1591-1597
2. Buckton G., and Darcy P. Water mobility in amorphous lactose below and close to the glass transition temperature. Int. J. Pharm. 136 1-2 (1996) 141-146
3. Buckton G., and Darcy P. Assessment of disorder in crystalline powders-a review of analytical techniques and their application. Int. J. Pharm. 179 2 (1999) 141-158
4. Bunker M., Davies M., and Roberts C. Towards screening of inhalation formulations: measuring interactions with atomic force microscopy. Expert Opin. Drug Deliv. 2 4 (2005) 613-624
5. Burnham N.A., Chen X., Hodges C.S., Matei G.A., Thoreson E.J., Roberts C.J., Davies M.C., and Tendler S.J.B. Comparison of calibration methods for atomic-force microscopy cantilevers. Nanotechnology 14 1 (2003) 1-6
6. Chaumeil J.C. Micronization: a method of improving the bioavailability of poorly soluble drugs. Methods Finding Exp. Clin. Pharmacol. 20 3 (1998) 211-215
7. Chikhalia V., Forbes R.T., Storey R.A., and Ticehurst M. The effect of crystal morphology and mill type on milling induced crystal disorder. Eur. J. Pharm. Sci. 27 1 (2006) 19-26
8. Davies M., Brindley A., Chen X., Marlow M., Doughty S.W., Shrubb I., and Roberts C.J. Characterization of drug particle surface energetics and young's modulus by atomic force microscopy and inverse gas chromatography. Pharm. Res. 22 7 (2005) 1158-1166
9. Duncan-Hewitt W.C., and Weatherly G.C. Evaluating the hardness, young modulus and fracture-toughness of some pharmaceutical crystals using microindentation techniques. J. Mater. Sci. Lett. 8 11 (1989) 1350-1352
10. Feeley J.C., York P., Sumby B.S., and Dicks H. Determination of surface thermodynamic properties of unmilled and milled salbutamol sulphate by inverse gas chromatography (IGC). J. Pharm. Pharmacol. 49 suppl. 4 (1997) 37
11. Feeley J.C., York P., Sumby B.S., and Dicks H. Comparison of the surface properties of salbutamol sulphate prepared by micronization and a supercritical fluid technique. J. Pharm. Pharmacol. 50 suppl. (1998) 54
12. Feeley J.C., York P., Sumby B.S., and Dicks H. Determination of surface properties and flow characteristics of salbutamol sulphate, before and after micronisation. Int. J. Pharm. 172 1-2 (1998) 89-96
13. Grzesiak A.L., Lang M.D., Kim K., and Matzger A.J. Comparison of the four anhydrous polymorphs of carbamazepine and the crystal structure of form I. J. Pharm. Sci. 92 11 (2003) 2260-2271
14. Hancock B.C., and Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J. Pharm. Sci. 86 1 (1997) 1-12
15. Heng J.Y.Y., Thielmann F., and Williams D.R. The effects of milling on the surface properties of form I paracetamol crystals. Pharm. Res. 23 8 (2006) 1918-1927
16. Hiestand E.N. Mechanical properties of compacts and particles that control tableting success. J. Pharm. Sci. 86 9 (1997) 985-990
17. Hlinak A., Kuriyan K., Morris K., Reklaitis G., and Basu P. Undertsaniding critical material properties for solid dosage form design. J. Pharm. Innovation 1 1 (2006) 12-17
18. Huang L.F., and Tong W.Q. Impact of solid state properties on developability assessment of drug candidates. Adv. Drug. Deliv. Rev. 56 3 (2004) 321-334
19. Jain S. Mechanical properties of powders for compaction and tableting: an overview. Pharm. Sci. Technol. Today 2 1 (1999) 20-31
20. James J., Crean B., Davies M., Toon R., Jinks P., and Roberts C.J. The surface characterisation and comparison of two potential sub-micron, sugar bulking excipients for use in low-dose, suspension formulations in metered dose inhalers. Int. J. Pharm. 361 1-2 (2008) 209-221
21. Johnson L.A., and McCauley R.A. The monitoring of crysallite size by an X-ray method applicable to the processing and synthesis of micron-sized powders. J. ASTM. Int. 3 8 (2006) 1-10
22. Kim J., Jung D.H., Rhee H., Choi S.H., Sung M.J., and Choi W.S. Improvement of bioavailability of water insoluble drugs: estimation of intrinsic bioavailability, Korean. J. Chem. Eng. 25 1 (2008) 171-175
23. Kwan C.C., Chena Y.Q., Ding Y.L., Papadopoulos D.G., Bentham A.C., and Ghadiri M. Development of a novel approach towards predicting the milling behaviour of pharmaceutical powders. Eur. J. Pharm. Sci. 23 4-5 (2004) 327-336
24. Leyland A., and Matthews A. On the significance of the H/E ratio in wear control: a nanocomposite coating approach to optimised tribological behaviour. Wear 246 1-2 (2000) 1-11
25. Mahlin D., Berggren J., Alderborn G., and Engström S. Moisture-induced surface crystallization of spray-dried amorphous lactose particles studied by atomic force microscopy. J. Pharm. Sci. 93 1 (2003) 29-37
26. Meier M., John E., Wieckhusen D., Wirth W., and Peukert W. Influence of mechanical properties on impact fracture: Prediction of the milling behaviour of pharmaceutical powders by nanoindentation. Powder. Technol. 188 3 (2009) 301-313
27. Midoux N., Hosek P., Pailleres L., and Authelin J.R. Micronization of pharmaceutical substances in a spiral jet mill. Powder. Technol. 104 2 (1999) 113-120
28. Newell H.E., Buckton G., Butler D.A., Thielmann F., and Williams D.R. The use of inverse phase gas chromatography to measure the surface energy of crystalline, amorphous, and recently milled lactose. Pharm. Res. 18 5 (2001) 662-666
29. Newell H.E., Buckton G., Butler D.A., Thielmann F., and Williams D.R. The use of inverse phase gas chromatography to study the change of surface energy of amorphous lactose as a function of relative humidity and the process of collapse and crystallisation. Int. J. Pharm. 217 1-2 (2001) 45-56
30. O'Brien L.E., Timmins P., Williams A.C., and York P. Use of in situ FT-Raman spectroscopy to study the kinetics of the transformation of carbamazepine polymorphs. J. Pharm. Biomed. Anal. 36 2 (2004) 335-340
31. Oh D.M., Curl R.L., Yong C.S., and Amidon G.L. Effect of micronization on the extent of drug absorption from suspensions in humans. Arch. Pharm. Res. 18 6 (1995) 427-433
32. Oliver W.C., and Pharr G.M. An improved technique for determining hardness and elastic modulus using load and displacement sensisng indentation experiments. J. Mater. Res. 7 6 (1992) 1564-1583
33. Perkins M., Ebbens S.J., Hayes S., Roberts C.J., Madden C.E., Luk S.Y., and Patel N. Elastic modulus measurements from individual lactose particles using atomic force microscopy. Int. J. Pharm. 332 1-2 (2007) 168-175
34. Ramos K.J., and Bahr D.F. Mechanical behavior assessment of sucrose using nanoindentation. J. Mater. Res. 22 7 (2007) 2037-2045
35. Rasenack N., and Muller B.W. Micron-size drug particles: common and novel micronization techniques. Pharm. Dev. Technol. 9 1 (2004) 1-13
36. Rasenack N., Steckel H., and Muller B.W. Micronization of anti-inflammatory drugs for pulmonary delivery by a controlled crystallization process. J. Pharm. Sci. 92 1 (2003) 35-44
37. Rasenack N., Steckel H., and Muller B.W. Preparation of microcrystals by in situ micronization. Powder. Technol. 143-4 (2004) 291-296
38. Roberts C.J. What can we learn from atomic force microscopy adhesion measurements with single drug particles?. Eur. J Pharm. Sci. 24 2-3 (2005) 153-157
39. Roberts R.J., Payne R.S., and Rowe R.C. Mechanical property predictions for polymorphs of sulphathiazole and carbamazepine. Eur. J. Pharm. Sci. 9 3 (2000) 277-283
40. Roberts R.J., and Rowe R.C. Influence of polymorphism on the Young's modulus and yield stress of carbmazepine, sulfathiazole and sulfanilamide. Int. J. Pharm. 129 1-2 (1996) 79-94
41. Sader J.E., Larson I., Mulvaney P., and White L.R. Method for the calibration of atomic-force microscope cantilevers. Rev. Sci. Instrum. 66 7 (1995) 3789-3798
42. Saxena V., Panicucci R., Joshi Y., and Garad S. Developability assessment in pharmaceutical industry: An integrated group approach for selecting developable candidates. J. Pharm. Sci. 98 6 (2009) 1962-1979
43. Staniforth J.A. Particle size reduction. In: Aulton M.E. (Ed). Pharmaceutics: The Science of Dossge Form Design (2000), Churchill Livingstone, London
44. Sunkersett M.R., Grimsey I.M., Doughty S.W., Osborn J.C., York P., and Rowe R.C. The changes in surface energetics with relative humidity of carbamazepine and paracetamol as measured by inverse gas chromatography. Eur. J. Pharm. Sci. 13 2 (2001) 219-225
45. Timsina M.P., Martin G.P., Marriott C., Ganderton D., and Yianneskis M. Drug-delivery to the respiratory-tract using dry powder inhalers. Int. J. Pharm. 101 1-2 (1994) 1-13
46. Turner Y.T.A., Roberts C.J., and Davies M.C. Scanning probe microscopy in the field of drug delivery. Adv. Drug. Deliv. Rev. 59 14 (2007) 1453-1473
47. Ward S., Perkins M., Zhang J.X., Roberts C.J., Madden C.E., Luk S.Y., Patel N., and Ebbens S.J. Identifying and mapping surface amorphous domains. Pharm. Res. 22 7 (2005) 1195-1202
48. Wildfong P.L.D., Hancock B.C., Moore M.D., and Morri K.R. Towards an understanding of the structurally based potential for mechanically activated disordering of small molecule organic crystals. J. Pharm. Sci. 95 12 (2006) 2645-2656
49. Young P.M., Tobyn M.J., Price R., Buttrum M., and Dey F. The use of colloid probe microscopy to predict aerosolization performance in dry powder inhalers: AFM and in vitro correlation. J. Pharm.Sci. 95 8 (2006) 1800-1809
50. Zhang J.X., Ebbens S., Chen X.Y., Jin Z., Luk S., Madden C., Patel N., and Roberts C.J. Determination of the surface free energy of crystalline and amorphous lactose by atomic force microscopy adhesion measurement. Pharm. Res. 23 2 (2006) 401-407
51. Zugner S., Marquardt K., and Zimmermann I. Influence of nanomechanical crystal properties on the comminution process of particulate solids in spiral jet mills. Eur. J. Pharm. Biopharm. 62 2 (2006) 194-201