Pharmacodynamics and dermatopharmacokinetics of betamethasone 17-valerate: Assessment of topical bioavailability

British Journal of Dermatology

Volumn 160, Issue 3, 2009, Pages 676-686

  Wiedersberg, S ^a   Naik, A ^b   Leopold, C S ^c   Guy, R H ^a  

^a University of Bath   (United Kingdom)

^b Triskel Integrated Services   (Switzerland)

^c UNIVERSITY OF HAMBURG   (Germany)

Author keywords

Corticosteroids; Dermatopharmacokinetics; Topical bioavailability; Topical bioequivalence; Vasoconstrictor assay

Indexed keywords

BETAMETHASONE; CORTICOSTEROID; STEROID;

ADULT; ARTICLE; BIOEQUIVALENCE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG UPTAKE; FEMALE; HUMAN; HUMAN EXPERIMENT; IN VIVO STUDY; INTERMETHOD COMPARISON; MALE; METHODOLOGY; NORMAL HUMAN; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RELIABILITY; SKIN; STRATUM CORNEUM; THERMODYNAMICS; VASOCONSTRICTION;

ADMINISTRATION, CUTANEOUS; ADULT; BETAMETHASONE 17-VALERATE; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GLUCOCORTICOIDS; HUMANS; MALE; MIDDLE AGED; REPRODUCIBILITY OF RESULTS; SKIN; SKIN ABSORPTION; SPECIMEN HANDLING; SURGICAL TAPE; THERMODYNAMICS; VASOCONSTRICTION; VEHICLES; YOUNG ADULT;

EID: 60449119318     PISSN: 00070963     EISSN: 13652133     Source Type: Journal    
DOI: 10.1111/j.1365-2133.2008.08757.x     Document Type: Article

References (41)

1. FDA. Guidance for Industry: Topical dermatologic corticosteroids: In vivo bioequivalence. U.S. Department of Health and Human Services. Food and Drug Administration. Rockville, MD, U.S.A.: Center for Drug Evaluation and Research (CDER), 1995.
2. Rougier A, Dupuis D, Lotte C et al. In vivo correlation between stratum corneum reservoir function and percutaneous absorption. J Invest Dermatol 1983 81 : 275 8.
3. Dupuis D, Rougier A, Roguet R et al. In vivo relationship between horny layer reservoir effect and percutaneous absorption in human and rat. J Invest Dermatol 1984 82 : 353 6.
4. Dupuis D, Rougier A, Roguet R et al. The measurement of the stratum corneum reservoir: a simple method to predict the influence of vehicles on in vivo percutaneous absorption. Br J Dermatol 1986 115: 233 8.
5. Rougier A, Lotte C, Maibach HI. In vivo percutaneous penetration of some organic compounds related to anatomic site in humans: Predictive assessment by the stripping method. J Pharm Sci 1987 76 : 451 4.
6. FDA. Guidance for Industry: Topical dermatologic drug product NDAs and ANDAs-in vivo bioavailability, bioequivalence, in vitro release, and associated studies. U.S. Department of Health and Human Services. Food and Drug Administration. Rockville, MD, U.S.A.: Center for Drug Evaluation and Research (CDER), 1998.
7. Shah VP, Flynn GL, Yacobi A et al. Bioequivalence of topical dermatological dosage forms-methods of evaluation of bioequivalence. Pharm Res 1998 15 : 167 71.
8. Caron D, Queille-Roussel C, Shah VP et al. Correlation between the drug penetration and the blanching effect of topically applied hydrocortisone creams in human beings. J Am Acad Dermatol 1990 23 : 458 62.
9. Pershing LK, Lambert LD, Shah VP et al. Variability and correlation of chromameter and tape-stripping methods with the visual skin blanching assay in the quantitative assessment of topical 0.05% betamethasone dipropionate bioavailability in humans. Int J Pharm 1992 86 : 201 10.
10. Pershing LK, Lambert LD, Wright ED et al. Topical 0.050% betamethasone dipropionate pharmacokinetic and pharmacodynamic dose-response studies in humans. Arch Dermatol 1994 130 : 740 7.
11. Pershing LK, Bakhtian S, Poncelet CE et al. Comparison of skin stripping, in vitro release, and skin blanching response methods to measure dose response and similarity of triamcinolone acetonide cream strengths from two manufactured sources. J Pharm Sci 2002 91 : 1312 23.
12. FDA. Guidance for Industry on special protocol assessment; Availability. Fed. Reg. 67: 35122 U.S. Department of Health and Human Services. Food and Drug Administration. Rockville, MD, U.S.A. : Center for Drug Evaluation and Research (CDER), 2002.
13. Löffler H, Dreher F, Maibach HI. Stratum corneum adhesive tape stripping: influence of anatomical site, application pressure, duration and removal. Br J Dermatol 2004 151 : 746 52.
14. Breternitz M, Flach M, Prassler J et al. Acute barrier disruption by adhesive tapes is influenced by pressure, time and anatomical location: integrity and cohesion assessed by sequential tape stripping; a randomized, controlled study. Br J Dermatol 2007 156 : 231 40.
15. Kalia YN, Alberti I, Sekkat N et al. Normalization of stratum corneum barrier function and transepidermal water loss in vivo. Pharm Res 2000 17 : 1148 50.
16. Alberti I, Kalia YN, Naik A et al. In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum. J Control Release 2001 71 : 319 27.
17. Alberti I, Kalia YN, Naik A et al. Effect of ethanol and isopropyl myristate on the availability of topical terbinafine in human stratum corneum, in vivo. Int J Pharm 2001 219 : 11 9.
18. Alberti I, Kalia YN, Naik A et al. Assessment and prediction of the cutaneous bioavailability of topical terbinafine, in vivo, in man. Pharm Res 2001 18 : 1472 5.
19. Herkenne C, Naik A, Kalia YN et al. Pig ear skin ex vivo as a model for in vivo dermatopharmacokinetic studies in man. Pharm Res 2006 23 : 1850 6.
20. Herkenne C, Naik A, Kalia YN et al. Ibuprofen transport into and through skin from topical formulations: In vitro-in vivo comparison. J Invest Dermatol 2007 127 : 135 42.
21. Herkenne C, Naik A, Kalia YN et al. Dermatopharmacokinetic prediction of topical drug bioavailability in vivo. J Invest Dermatol 2007 127 : 887 94.
22. Herkenne C, Naik A, Kalia YN et al. Effect of propylene glycol on ibuprofen absorption into human skin in vivo. J Pharm Sci 2008 97 : 185 97.
23. Leopold CS, Lippold BC. Enhancing effects of lipophilic vehicles on skin penetration of methyl nicotinate in vivo. J Pharm Sci 1995 84 : 195 8.
24. Joint Formulary Committee 2003-04. British National Formulary. Vol. No. 47 (March). London : British Medical Association and the Royal Pharmaceutical Society of Great Britain, 2004.
25. Anderson RL, Cassidy JM. Variations in physical dimensions and chemical composition of human stratum corneum. J Invest Dermatol 1973 61 : 30 2.
26. Kalia YN, Pirot F, Guy RH. Homogeneous transport in a heterogeneous membrane: water diffusion across human stratum corneum in vivo. Biophys J 1996 71 : 2692 700.
27. Dreher F, Arens A, Hostynek JJ et al. Colorimetric method for quantifying human stratum corneum removed by adhesive-tape-stripping. Acta Derm Venereol 1998 78 : 186 9.
28. Bashir SJ, Chew A-L, Anigbogu A et al. Physical and physiological effects of stratum corneum tape stripping. Skin Res Technol 2001 7 : 40 8.
29. Kalia YN, Alberti I, Naik A et al. Assessment of topical bioavailability in vivo: The importance of stratum corneum thickness. Skin Pharmacol Appl Skin Physiol 2001 14 : 82 6.
30. Crank J. Diffusion in a plane sheet. In : The Mathematics of Diffusion (Crank J, ed 2nd edn. London : Oxford University Press, 1975 44 68.
31. Pirot F, Kalia YN, Stinchcomb AL et al. Characterization of the permeability barrier of human skin in vivo. Proc Natl Acad Sci USA 1997 94 : 1562 7.
32. Vickers CFH. Existence of reservoir in the stratum corneum. Arch Dermatol 1963 88 : 72 5.
33. Carr RD, Wieland RG. Corticosteroid reservoir in the stratum corneum. Arch Dermatol 1966 94 : 81 4.
34. Teichmann A, Jacobi U, Weigmann HJ et al. Reservoir function of the stratum corneum: development of an in vivo method to quantitatively determine the stratum corneum reservoir for topically applied substances. Skin Pharmacol Physiol 2005 18 : 75 80.
35. Roberts MS, Cross SE, Anissimov YG. Factors affecting the formation of a skin reservoir for topically applied solutes. Skin Pharmacol Physiol 2004 17 : 3 16.
36. Bach M, Lippold BC. Influence of penetration enhancers on the blanching intensity of betamethasone 17-benzoate. Int J Pharm 1998 168 : 97 108.
37. Godwin DA, Kim N-H, Felton LA. Influence of Transcutol® CG on the skin accumulation and transdermal permeation of ultraviolet absorbers. Eur J Pharm Biopharm 2002 53 : 23 7.
38. Mura P, Faucci MT, Bramanti G et al. Evaluation of transcutol as a clonazepam transdermal permeation enhancer from hydrophilic gel formulations. Eur J Pharm Sci 2000 9 : 365 72.
39. Harrison JE, Watkinson AC, Green DM et al. The relative effect of Azone and Transcutol on permeant diffusivity and solubility in human stratum corneum. Pharm Res 1996 13 : 542 6.
40. Bendas B, Schmalfuss U, Neubert R. Influence of propylene glycol as cosolvent on mechanism of drug transport from hydrogels. Int J Pharm 1995 116 : 19 30.
41. Lippold BC, Schneemann H. The influence of vehicles on the local bioavailability of betamethasone-17-benzoate from solution- and suspension-type ointments. Int J Pharm 1984 22 : 31 43.