Relevance of equivalence assessment of topical products based on the dermatopharmacokinetics approach

European Journal of Pharmaceutical Sciences

Volumn 42, Issue 3, 2011, Pages 173-179

  Boix Montanes, Antonio ^a  

^a UNIVERSITY OF BARCELONA   (Spain)

Author keywords

Dermatological generic; Skin stripping; Statistical moment; Topical bioequivalence

Indexed keywords

BETAMETHASONE VALERATE; DERMATOLOGICAL AGENT; GLUCOCORTICOID; PREDNISOLONE 17 ETHYLCARBONATE; PREDNISOLONE 21 PROPIONATE; RETINOIC ACID; TOPICAL AGENT; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; BIOEQUIVALENCE; DOSE CALCULATION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG FORMULATION; DRUG METABOLISM; DRUG PENETRATION; DRUG RELEASE; EPIDERMIS; HUMAN; PRIORITY JOURNAL; REVIEW; SKIN ABSORPTION; SKIN PENETRATION; STRATUM CORNEUM;

ADMINISTRATION, TOPICAL; AREA UNDER CURVE; DERMATOLOGIC AGENTS; HUMANS; THERAPEUTIC EQUIVALENCY;

EID: 79251599381     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2010.11.003     Document Type: Review

References (69)

1. Agencia española del and medicamento, 2010. Agencia española del medicamento. Registered products database. http://www.agemed.es (access on 15 August 2010).
2. E. Baker, and J. Hadgraft In vitro percutaneous absorption of Arildone, a highly lipophilic drug, and the apparent no-effect of the penetration enhancer Azone in excised human skin Pharm. Res. 12 7 1995 993 997
3. S.J. Bashir, F. Dreher, A.L. Chew, H. Zhai, C. Levin, R. Stern, and H.I. Maibach Cutaneous bioassay of salicylic acid as a keratolytic Int. J. Pharm. 292 2005 187 194
4. F. Beisson, M. Aoubala, S. Marull, A.M. Moustacas-Gardies, R. Voultoury, R. Verger, and V. Arondel Use of the tape stripping technique for directly quantifying esterase activities in human stratum corneum Anal. Biochem. 290 2001 179 185
5. M. Bhosle, R. Balkrishnan, T. Dewan, C.B. Yelverton, and S.R. Feldman The rise of the generic drug market and its implications for dermatology J. Dermatol. Treat. 16 5-6 2005 295 298
6. M. Breternitz, M. Flach, J. Präßler, P. Elsner, and J.W. Fluhr Acute barrier disruption by adhesive tapes is influences by pressure, time and anatomical location: integrity and cohesion assessed by sequential tape stripping Br. J. Dermatol. 156 2007 231 240
7. D. Brockmeier In vitro in vivo correlation of dissolution using moments of dissolution and transit times Acta Pharm. Technol. 32 1986 164 174
8. CDER, 1997. Guidance for Industry. Nonsterile Semisolid Dosage Forms Scale-Up and Postapproval Changes: Chemistry, Manufacturing, and Controls. In Vitro Release Testing and In Vivo Bioequivalence Documentation.
9. CDER, 1998. Guidance for Industry. Topical Dermatological Drug Product NDAs and ANDAs. In Vivo Bioavailability, Bioequivalence, In Vitro Release, and Associated Studies.
10. CDER, 2009. Guidance for Industry. Submission of Summary Bioequivalence Data for ANDAs.
11. Y.W. Cheung, A. Li Wan Po, and W.J. Irwin Cutaneous biotransformation as a parameter in the modulation of the activity of topical corticosteroids Int. J. Pharm. 26 1985 175 189
12. F. Dreher, A. Arens, J.J. Hostynek, S. Mudumba, J. Ademola, and H.I. Maibach Colorimetric method for quantifying human stratum corneum removed by adhesive-tape stripping Acta Derm. Venereol. 78 1998 186 189
13. EMA, 2010. Guideline on the investigation of bioequivalence. CPMP/EWP/QWP/1401/98 Rev.1. 20 January 2010.
14. EMEA, 2000. Points to consider on switching between superiority and non-inferiority. CPMP/EWP/482/99 July 2000
15. EMEA, 2006. Questions and answer on guideline title: clinical investigation of corticosteroids intended for use on the skin. CHMP/EWP/21441/2006.
16. Federal Register, 2002. Notice of the Department of Health and Human Services. Draft Guidance for Industry on Topical Dermatological Drug Product NDAs and ANDAs; Withdrawal. Fed. Reg. 67, 35122-3.
17. R.H. Guy, and J. Hadgraft Physicochemical interpretation of the pharmacokinetics of percutaneous absorption J. Pharmacokinet. Biopharm. 11 1983 189 203
18. A. Gysler, B. Kleuser, W. Sippl, K. Lange, H.C. Korting, H.D. Holtje, and M. Schafer-Korting Skin penetration and metabolism of topical glucocorticoids in reconstructed epidermis and in excised human skin Pharm. Res. 16 1999 1386 1391
19. M. Hashida, H. Okamoto, and H. Sezaki Analysis of drug penetration through skin considering donor concentration decrease J. Pharmacobio-dyn. 11 1988 636 644
20. C. Herkenne, I. Alberti, A. Naik, Y.N. Kalia, F.X. Mathy, V. Préat, and R.H. Guy In vivo methods for the assessment of topical drug bioavailability Pharm. Res. 25 1 2008 87 103
21. C. Herkenne, A. Naik, Y.N. Kalia, J. Hadgraft, and R.H. Guy Dermatopharmacokinetic prediction of topical drug bioavailability in vivo J. Invest. Dermatol. 127 2007 887 894
22. C. Herkenne, A. Naik, Y.N. Kalia, J. Hadgraft, and R.H. Guy Ibuprofen transport into and through skin from topical formulations: in vitro-in vivo comparison J. Invest. Dermatol. 127 2007 135 142
23. Hoffmann, S., Edler, L., Gardner, I., Gribaldo, L., Hartung, T., Klein, C., Liebsch, M., Sauerland, S., Schechtman, L., Stammati, A., Nikolaidis, E., 2008. Points of Reference in the Validation Process. The Report and Recommendations of ECVAM Workshop 66. ATLA 36, 343-352
24. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use, 2009. ICH Harmonised Tripartite Guideline: Pharmaceutical Development Q8.
25. U. Jacobi, M. Kaiser, H. Richter, H. Audring, W. Sterry, and J. Lademann The number of SC cell layers correlates with the pseudo-absorption of the corneocytes Skin Pharmacol. Physiol. 18 2005 175 179
26. R. Johnson, B.P. Nusbaum, S.N. Horwitz, and P. Frost Transfer of topically applied tetracycline in various vehicles Arch. Dermatol. 119 1983 660 663
27. G.B. Kastings, and P.J. Robinson Can we assign an upper limit to skin permeability? Pharm. Res. 10 6 1993 930 931
28. J. Lademann, A. Ilgevicius, O. Zurbau, H.D. Liess, S. Schanzer, H.J. Weigmann, C. Antoniou, R.V. Pelchrzim, and W. Sterry Penetration studies of topically applied substances: optical determination of the amount of stratum corneum removed by tape stripping J. Biomed. Opt. 11 2006 5 13
29. J. Lademann, U. Jacobi, C. Surber, H.J. Weigmann, and J.W. Fluhr The tape stripping procedure - evaluation of some critical parameters Eur. J. Pharm. Biopharm. 72 2009 317 323
30. J. Lademann, H. Richter, M. Meinke, W. Sterry, and A. Patzelt Which skin model is the most appropriate for the investigation of topically applied substances into the hair follicles? Skin Pharmacol. Physiol. 23 1 2010 47 52
31. C.S. Leopold Pharmacokinetic analysis of the FDA guidance for industry 'Topical dermatologic corticosteroids: in vivo bioequivalence' Eur. J. Pharm. Biopharm. 56 2003 53 58
32. R.H. Levy, and M. Rowland Absorption kinetics of a series of local anaesthetics from rat subcutaneous tissue J. Pharmacokinet. Biopharm. 2 1974 313 335
33. U. Lindemann, K. Wilken, H.J. Weigmann, H. Schaefer, W. Sterry, and J. Lademann Quantification of the horny layer using tape stripping and microscopic techniques J. Biomed. Opt. 8 2003 601 607
34. M. Lodén, U. Akerström, K. Lindahl, and B. Berne Bioequivalence determination of topical ketoprofen using a dermatopharmacokinetic approach and excised skin penetration Int. J. Pharm. 284 2004 23 30
35. H. Loffler, F. Dreher, and H.I. Maibach Stratum corneum adhesive tape stripping: influence of anatomical site, application pressure, duration and removal Br. J. Dermatol. 151 2004 746 752
36. S. Lombardi Borgia, P. Schlupp, W. Mehnert, and M. Schäfer-Korting In vitro skin absorption and drug release - a comparison of six commercial prednicarbate preparations for topical use Eur. J. Pharm. Biopharm. 68 2008 380 389
37. A. Mahmoud, A. Haberland, M. Dürrfeld, D. Heydeck, S. Wagner, and M. Schafer-Korting Cutaneous estradiol permeation, penetration and metabolism in pig and man Skin Pharmacol. Physiol. 18 2005 27 35
38. E. Malzfeldt, P. Lehmann, G. Goerz, and B.C. Lippold Influence of drug solubility in the vehicle on clinical efficacy of ointments Arch. Dermatol. Res. 281 1989 193 197
39. W. Montagna Histology and cytochemistry of human skin. IX. The distribution of non-specific esterases J. Biophys. Biochem. Cytol. 1 1955 13 16
40. A.P. Morris, K.R. Brain, and C.M. Heard Skin permeation and ex vivo skin metabolism of O-acyl haloperidol ester prodrugs Int. J. Pharm. 367 2009 44 50
41. B. N'Dri-Stempfer, W.C. Navidi, R.H. Guy, and A.L. Bunge Optimizing metrics for the assessment of bioequivalence between topical drug products Pharm. Res. 25 2008 1621 1629
42. B. N'Dri-Stempfer, W.C. Navidi, R.H. Guy, and A.L. Bunge Improved bioequivalence assessment of topical dermatological drug products using dermatopharmacokinetics Pharm. Res. 26 2009 316 328
43. L.K. Pershing, L.D. Lambert, V.P. Shah, and S.Y. Lam Variability and correlation of chromameter and skin stripping method with the visual skin blanching assay in the quantitative assessments of topical 0.05% betamethasone dipropionate bioavailability in humans Int. J. Pharm. 86 1992 210
44. L.K. Pershing, J.L. Nelson, J.L. Coreltt, S.P. Shrivastave, D.B. Hare, and V.P. Shah Assessment of dermatopharmacokinetic approach in the bioequivalence determination of topical tretinoin gel products J. Am. Acad. Dermatol. 48 2003 740 751
45. F. Podczeck Comparison of in vitro dissolution profiles by calculating mean dissolution time (MDT) or mean residence time (MRT) Int. J. Pharm. 97 1993 93 100
46. R. Potts, and R.H. Guy Drug transport across the skin and the attainment of steady-state flux Proc. Int. Symp. Control. Release Bioact. Mater. 21 1994 162 163
47. Z. Qian, J.E. Grice, L. Peng, O.G. Jepps, W. Guang-Ji, and M.S. Roberts Skin solubility determines maximum transepidermal flux for similar size molecules Pharm. Res. 26 2009 1974 1985
48. M.L. Rebelo, and E. Pina Release kinetics of tretinoin from dermatological formulations Drug Dev. Ind. Pharm. 23 1997 727 730
49. L.M. Russell, and R.H. Guy Measurement and prediction of the rate and extent of drug delivery into and through the skin Expert Opin. Drug Deliv. 6 2009 355 369
50. E. Sachdeva, S. Siddoju, Y.Y. Yu, H.D. Kim, P.M. Friden, and A.K. Banga Transdermal iontophoretic delivery of terbinafine hydrochloride: quantitation of drug levels in stratum corneum and underlying skin Int. J. Pharm. 388 2010 24 31
51. F.P. Schmook, J.G. Meingassner, and A. Billich Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption Int. J. Pharm. 215 2001 51 56
52. O. Shirakura, A. Ohshima, S. Tsunemi, S. Ishimaru, T. Sakaguchi, K. Takayama, and T. Nagai Synergistic effect of the limonene and ethanol on the transdermal permeation of NB 818 Drug Dev. Ind. Pharm. 21 4 1995 411 425
53. O. Siddiqui, M.S. Roberts, and A.E. Polack Topical absorption of methotrexate: role of dermal transport Int. J. Pharm. 27 1985 193 203
54. J.P. Skelly, V.P. Shah, H.I. Maibach, R.H. Guy, R.C. Wester, and G. Flynn FDA and AAPS report of the workshop on principles and practices of in vitro percutaneous penetration studies: relevance to bioavailability and bioequivalence Pharm. Res. 4 1987 265 267
55. G. Stagni, D. O'Donnell, Y.J. Liu, D.L. Kellogg, T. Morgan, and A.M.M. Shepherd Intradermal microdialysis: kinetics of iontophoretically delivered propranolol in forearm dermis J. Control. Release 63 2000 331 339
56. A.L. Stinchcomb Xenobiotic bioconversion in human epidermis models Pharm. Res. 20 2003 1113 1119
57. M. Tanaka, Y. Iwata, Y. Kouzuki, K. Taniguchi, H. Matsuda, H. Arima, and S. Tsuchiya Effect of 2-hydroxypropyl-beta-cyclodextrin on percutaneous absorption of methyl paraben J. Pharm. Pharmacol. 47 1995 897 900
58. E. Touitou, B. Fabin, S. Dany, and S. Almog Transdermal delivery of tetrahydrocannabinol Int. J. Pharm. 43 1988 9 15
59. L. Trottet, C. Merly, M. Mirza, J. Hadgraft, and A.F. Davis Effect of finite doses of propyleneglycol on enhancement of in vitro percutaneous permeation of loperamide hydrochloride Int. J. Pharm. 274 2004 213 219
60. L. Trottet, H. Owen, P. Holme, J. Heylings, I.P. Collin, A.P. Breen, M.N. Siyad, R.S. Nandra, and A.F. Davis Are all aciclovir cream formulations bioequivalent? Int. J. Pharm. 304 2005 63 71
61. J.C. Tsai, S.A. Chuang, M.Y. Hsu, and H.M. Sheu Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations Int. J. Pharm. 188 1999 145 153
62. S. Valiveti, K.S. Paudel, D.C. Hammell, M.O. Hamad, J. Chen, P.A. Crooks, and A.L. Stinchomb In vitro/in vivo correlation of transdermal maltrexone prodrugs in hairless guinea pigs Pharm. Res. 22 2005 981 989 (Pubitemid 40898108)
63. R.G. van der Molen, F. Spies, J.M. van't Noordende, E. Boelsma, A.M. Mommaas, and H.K. Koerten Tape stripping of human stratum corneum yields cell layers that originate from various depths because of furrows in the skin Arch. Dermatol. Res. 289 1997 514 518
64. D. Voegele, H.M. von Hattingberg, and D. Brockmeier Ein einfaches verfahren zur ermittlung von in vitro/in vivo Zusammenhängen in der Galenik Acta Pharm. Technol. 27 1981 115 120
65. H. Wagner, K.H. Kostka, C.M. Lehr, and U.F. Schaefer Interrelation of permeation and penetration parameters obtained from in vitro experiments with human skin and skin equivalents J. Control. Release 75 2001 283 295
66. H.J. Weigmann, U. Lindemann, C. Antoniou, G.N. Tsikrikas, A.I. Stratigos, A. Katsambas, W. Sterry, and J. Lademann UV/vis absorbance allows rapid, accurate, and reproducible mass determination of corneocytes removed by tape stripping Skin Pharmacol. Appl. Skin Physiol. 16 2003 217 227
67. S. Wiedersberg, C.S. Leopold, and R.H. Guy Dermatopharmacokinetics of betamethasone 17-valerate: influence of formulation viscosity and skin surface cleaning procedure Eur. J. Pharm. Biopharm. 71 2009 362 366
68. K. Yamaoka, T. Nakagawa, and T. Uno Statistical moments in pharmacokinetics J. Pharmacokinet. Biopharm. 11 1978 189 203
69. D. Yoshida, H. Todo, T. Hasegawa, and K. Sugibayashi Effect of molecular weight on the dermatopharmacokinetics and systemic disposition of drugs after intracutaneous injection Eur. J. Pharm. Sci. 35 2008 5 11