A biorelevant dissolution stress test device background and experiences

Expert Opinion on Drug Delivery

Volumn 7, Issue 11, 2010, Pages 1251-1261

  Garbacz, Grzegorz ^a,b   Klein, Sandra ^a   Weitschies, Werner ^a  

^a UNIVERSITY OF GREIFSWALD   (Germany)

^b Physiolution GmbH   (Germany)

Author keywords

Biorelevant dissolution testing; Dissolution stress test device; Dose dumping; Predictive dissolution testing

Indexed keywords

DICLOFENAC; NIFEDIPINE;

DEVICE; DRUG BLOOD LEVEL; DRUG DOSAGE FORM; DRUG RELEASE; DRUG SOLUBILITY; GASTROINTESTINAL MOTILITY; INTESTINE FLUID; REVIEW; SHEAR STRESS; TABLET;

ADMINISTRATION, ORAL; CHEMISTRY, PHARMACEUTICAL; DELAYED-ACTION PREPARATIONS; DICLOFENAC; GASTROINTESTINAL MOTILITY; GASTROINTESTINAL TRACT; HUMANS; NIFEDIPINE; PHARMACEUTICAL PREPARATIONS; SOLUBILITY; STRESS, MECHANICAL; TABLETS;

EID: 77958603039     PISSN: 17425247     EISSN: None     Source Type: Journal    
DOI: 10.1517/17425247.2010.527943     Document Type: Review

References (74)

1. Noyes AA, Whitney WR. The rate of solution of solid substances in their own solutions. J Am Chem Soc 1897;19:930-34
2. Bruner L, Tolloczko S. On the dissolution speed of firm bodies. Z Physik Ch 1900;35:283-90
3. Nernst W, Brunner E. Theorie der reaktionsgeschwindigkeit in heterogenen systemen. Z Phys Chem 1904;47:52-5
4. Banakar UV. (1992) Pharmaceutical dissolution testing. New York; Marcel Dekker Inc.
5. Siewert M. FIP guidelines for dissolution testing of solid oral products. Drug Info J 1996;30:1071-84
6. European Pharmacopoeia Edition 6.3. Legally valid from 1.1. 2009 until 31.3.2009. Available from: www.pheur.org [Last accessed October 2010]
7. USP Pharmacopoeia and National Formulary, United States Pharmacopoeial Convention, Inc., 29th edition and 24th edition, 2006
8. Commission Regulation (EC) No 1084/2003, 2003, EMEA, London
9. Committee for Proprietary Medicinal Products, (2001). Note for guidance on the investigation of bioavailability and bioequivalence CMP/EWP/QWP1401/98 EMEA, London
10. Gupta E, Barends DM, Yamashita E, et al. Review of global regulations concerning biowaivers for immediate release solid oral dosage forms. Eur J Pharm Sci 2006;29:315-24
11. Gaynor C, Dunne A, Davis J. A comparison of the prediction accuracy of two IVIVC modelling techniques. J Pharm Sci 2008;8:3422-32
12. Polli JE. Dependence of in vitro-in vivo correlation analysis acceptability on model selections. Pharm Dev Technol 1999;4:89-96
13. McAllister M. Dynamic dissolution: a step closer to predictive dissolution testing. Mol Pharm 2010;7:1374-87
14. Russell TL, Berardi RR, Barnett JL, et al. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. Pharm Res 1993;10:187-96
15. Kalantzi L, Goumas K, Kalioras V, et al. Characterization of the human upper gastrointestinal contents under conditions simulating bioavailability/ bioequivalence studies. Pharm Res 2006;23:165-76
16. Galia E, Nicolaides E, Horter D, et al. Evaluation of various dissolution media for predicting in vivo performance of Classes I and II drugs. Pharm Res 1998;15:698-705
17. Jantratid E, Janssen N, Reppas C, et al. Dissolution media simulating conditions in the proximal human gastrointestinal tract: an update. Pharm Res 2008;25:1663-76
18. Ghazal HS, Dyas AM, Ford JL, et al. In vitro evaluation of the dissolution behaviour of itraconazole in bio-relevant media. Int J Pharm 2009;366:117-23
19. Klein S, Butler J, Hempenstall JM, et al. Media to simulate the postprandial stomach I. Matching the physicochemical characteristics of standard breakfasts. J Pharm Pharmacol 2004;56:605-10
20. Kavanagh N, Corrigan OI. Swelling and erosion properties of hydroxypropylmethylcellulose (Hypromellose) matrices-influence of agitation rate and dissolution medium composition. Int J Pharm 2004;279:141-52
21. Horter D, Dressman JB. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv Drug Deliv Rev 2001;46:75-87 (Pubitemid 33653415)
22. Anwar S, Fell JT, Dickinson PA. An investigation of the disintegration of tablets in biorelevant media. Int J Pharm 2005;290:121-27
23. Abrahamsson B, Albery T, Eriksson A, et al. Food effects on tablet disintegration. Eur J Pharm Sci 2004;22:165-72
24. Abrahamsson B, Johansson D, Torstensson A, et al. Evaluation of solubilizers in the drug release testing of hydrophilic matrix extended-release tablets of felodipine. Pharm Res 1994;11:1093-97
25. Zoeller T, Klein S. Simplified biorelevant media for screening dissolution performance of poorly soluble drugs. Dissol Technol 2007;14:8-13
26. Taupitz T, Klein S. Can biorelevant media be simplified by using SLS and tween 80 to replace bile compounds? Open Drug Deliv J 2010;4:30-7
27. Soni T, Nagda C, Gandhi T, Chotai NP. Development of discriminating method for dissolution of aceclofenac marketed formulations. Dissol Technol 2008;15:31-5
28. Bertocchia P, Antoniella E, Valvo L, et al. Diclofenac sodium multisource prolonged release tablets - a comparative study on the dissolution profiles. J Pharm Biomed Anal 2005;37:679-85
29. Kamba M, Seta Y, Kusai A, et al. A unique dosage form to evaluate the mechanical destructive force in the gastrointestinal tract. Int J Pharm 2000;208:61-70
30. Katori N, Ma WS, Aoyagi N, et al. Effect of destructive force on drug release from multiple unit conlrolled release dosage forms in humans. Pharm Res 1996;13:1541-46
31. Weitschies W, Kosch O, Monnikes H, et al. Magnetic marker monitoring: an application of biomagnetic measurement instrumentation and principles for the determination of the gastrointestinal behavior of magnetically marked solid dosage forms. Adv Drug Deliv Rev 2005;57:1210-22
32. Weitschies W, Blume H, Monnikes H. Magnetic marker monitoring: high resolution real-time tracking of oral solid dosage forms in the gastrointestinal tract. Eur J Pharm Biopharm 2010;74:93-101
33. Laulicht B, Tripathi A, Schlageter V, et al. Understanding gastric forces calculated from high-resolution pill tracking. PNAS 2010;107:8201-6
34. Abrahamsson B, Anupam P, Sjoberg M, et al. A novel in vitro and numerical analysis of shear-induced drug release from extended-release tablets in the fed stomach. Pharm Res 2005;22:1215-26
35. Schulze K. Imaging and modelling of digestion in the stomach and the duodenum. Neurogastroenterol Motil 2006;18:172-83
36. Pal A, Brasseur J, Abrahamsson B. A stomach road or 'Magenstrasse' for gastric emptying. J Biomech 2007;40:1202-10
37. Cassilly D, Kantor S, Knight LC, et al. Gastric emptying of a non-digestible solid: assessment with simultaneous SmartPill pH and pressure capsule, antroduodenal manometry, gastric emptying scintigraphy. Neurogastroenterol Motil 2008;20:311-19
38. Dinning PG, Bampton PA, Kennedy ML, et al. Basal pressure patterns and reflexive motor responses in the human ileocolonic junction. Am J Physiol 1999;276:G331-40
39. Schiller C, Frohlich CP, Giessmann T, et al. Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging. Aliment Pharmacol Ther 2005;22:971-79
40. Meredith PA. The unique adalat story - nifedipine gastrointestinal therapeutic system. European Cardiovascular Disease 2007;1:97-102
41. Wikstrand J. Achieving optimal beta1-blockade with metoprolol CR/Zok. Basic Res Cardiol 2000;95:I46-51
42. Breekveldt-Postma NS, Herings RM. Persistence with antihypertensives related to formulation: the case of nifedipine. Ann Pharmacother 2005;39:237-42
43. Abrahamsson B, Allpsten M, Bake B. Drug absorption from nifedipine hydrophilic matrix extended-release (ER) tablet-comparison with an osmotic pump tablet and effect of food. J Control Release 1998;52:301-10
44. Wonnemann M, Schug B, Schmucker K. Significant food interactions observed with a nifedipine modified-release formulation marketed in the European Union. Int J Clin Pharmacol Ther 2006;44:38-48.
45. Weitschies W, Wedemeyer RS, Kosch O, et al. Impact of the intragastric location of extended release tablets on food interactions. J Control Release 2005;108:375-85
46. Schug B, Brendel E, Wolf D, et al. Formulation dependent food effects demonstrated for nifedipine modified-release preparations marketed in the European Union. Eur J Pharm Sci 2002;15:279-85
47. Klein S. Predicting food effects on drug release from extended-release oral dosage forms containing a narrow therapeutic index drug. Dissol Technol 2009;16:28-40
48. Jantratid E, De Maio V, Ronda E, et al. Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form. Eur J Pharm Sci 2009;37:434-41
49. Garbacz G, Wedemeyer RS, Nagel S, et al. Irregular absorption profiles observed from diclofenac extended release tablets can be predicted using a dissolution test apparatus that mimics in vivo physical stresses. Eur J Pharm Biopharm 2008;70:421-8
50. Aoki S, Ando H, Tatsuishi K, et al. Determination of the mechanical impact force in the in vitro dissolution test and evaluation of the correlation between in vivo and in vitro release. Int J Pharm 1993;95:67-75
51. Qureshi SA. Improved drug dissolution and product characterization using a crescent-shaped spindle. J Pharm Pharmacol 2004;56:1135-41
52. Qureshi SA. A new crescent-shaped spindle for drug dissolution testing - but why a new spindle? Dissol Technol 2004;11:13-8
53. Baxter JL, Kukura J, Muzzio FJ. Shear-induced variability in the United States pharmacopeia apparatus 2: modifications to the existing system. AAPS J 2006;7(4):E857-64
54. Parojcic J, Vasiljevic D, Ibric S, et al. Tablet disintegration and drug dissolution in viscous media: paracetamol IR tablets. Int J Pharm 2008;355:93-9
55. Rohrs BR, Burch-Clark DL, Witt MJ, et al. USP dissolution apparatus 3 (reciprocating cylinder): instrument parameter effects on drug release from sustained release formulations. J Pharm Sci 2006;84:922-26
56. Kong F, Singh FP. A model stomach system to investigate disintegration kinetics of solid foods during gastric digestion. J Food Sci 2008;73:E202-10
57. Yoo M, Yeon J, Xiao Dong C. GIT physicochemical modeling - a critical review. Int J Food Eng 2006;2:Article 4. Available at: http://www.bepress.com/ ijfe/vol2/iss4/art4 DOI: 10.2202/1556-3758
58. Blanquet S, Zeijdner E, Beyssac E, et al. A dynamic artificial gastrointestinal system for studying the behavior of orally administered drug dosage forms under various physiological conditions. Pharm Res 2004;21:585-91
59. Souliman S, Beyssac E, Cardot J-M, et al. Investigation of the biopharmaceutical behavior of theophylline hydrophilic matrix tablets using USP methods and an artificial digestive system. Drug Dev Ind Pharm 2007;33:475-83
60. Souliman S, Blanquet S, Beyssac E, Cardot J-M. A level A in vitro/in vivo correlation in fasted and fed states using different methods: applied to solid immediate release oral dosage form. Eur J Pharm Sci 2006;27:72-9
61. Garbacz G, Golke B, Wedemeyer R-S, et al. Comparison of dissolution profiles obtained for nifedipine extended release once daily tablets using different 56. dissolution test apparatuses. Eur J Pharm Sci 2009;38:147-55
62. Garbacz G, Weitschies W. Investigation of dissolution characteristics of four diclofenac sodium extended release tablets using USP apparatus 2 and novel biorelevant dissolution stress test device. Drug Dev Ind Pharm 2010;36:518-30
63. Garbacz G, Blume H, Weitschies W. Investigation of the dissolution characteristics of six different nifedipine 20 mg extended release tablets using USP apparatus 2 and a novel dissolution test apparatus that mimics in vivo physical stress. Dissol Technologies 2009;16:7-11
64. Meredith PA, Elliott HL. Dihydropyridine calcium channel blockers: basic pharmacological similarities but fundamental therapeutic differences. J Hypertens 2004;22:1641-48
65. Colombo P, Bettini R, Santi P, et al. Swellable matrixes for controlled drug delivery: gel-layer behaviour, mechanisms and optimal performance. Pharm Sci Tech 2000;6:198-204
66. Varma MVS, Kaushal AM, Garg A, et al. Factors affecting mechanism and kinetics of drug release from matrix-based oral controlled drug delivery systems. Am J Drug Deliv 2004;2:43-57
67. Colombo P, Bettini R, Peppas NA. Observation of swelling process and diffusion front position during swelling in hydroxypropyl methyl cellulose (HPMC) matrices containing a soluble drug. J Control Release 1999;61:83-91
68. Jamzad S, Tutunji L, Fassihi R. Analysis of macromolecular changes and drug release from hydrophilic matrix systems. Int J Pharm 2005;292:75-85
69. Nazzal S, Nazzal M, El-Malah Y. A novel texture-probe for the simultaneous and real-time measurement of swelling and erosion rates of matrix tablets. Int J Pharm 2007;330:195-98
70. Yang L, Johnson B, Fassihi R. Determination of continuous changes in the gel layer thickness of poly(ethylene oxide) and HPMC tablets undergoing hydration: a texture analysis study. Pharm Res 1998;12:1902-6
71. Lia H, Gu X. Correlation between drug dissolution and polymer hydration: a study using texture analysis. Int J Pharm 2007;342:18-25
72. Pavli M, Kristl J, Dolenc A, et al. The reflection of the texture of swollen polymer matrix on the release of incorporated substance. e-Polymers 2009;17:1-15
73. Persson E. Drug dissolution under physiologically relevant conditions in vitro and in vivo. Digital comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy 39 Acta Universitatis Upsalinesis, Uppsala 2006
74. Diakidou A, Vertzoni M, Abrahamsson B. Simulation of gastric lipolysis and prediction of felodipine release from a matrix tablet in the fed stomach. Eur J Pharm Sci 2009;37:133-40