FEASIBILITY OF MEASURING THE BIOAVAILABILITY OF TOPICAL BETAMETHASONE DIPROPIONATE IN COMMERCIAL FORMULATIONS USING DRUG CONTENT IN SKIN AND A SKIN BLANCHING BIOASSAY

被引:75
作者
PERSHING, LK [1 ]
SILVER, BS [1 ]
KRUEGER, GG [1 ]
SHAH, VP [1 ]
SKELLEY, JP [1 ]
机构
[1] US FDA,CTR DRUG EVALUAT & RES,ROCKVILLE,MD 20857
关键词
BIOAVAILABILITY; SKIN BLANCHING; VASOCONSTRICTION; TOPICAL CORTICOSTEROIDS; BETAMETHASONE DIPROPIONATE; TAPE-STRIPPING;
D O I
10.1023/A:1018975626210
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An in vivo technique has been developed which simultaneously compares a skin blanching bioassay with drug content in human stratum corneum following topical application of four 0.05% beta-methasone dipropionate formulations. Bioavailability of drug from commercial cream and ointment formulations was assessed by quantification of drug content in tape-stripped stratum corneum and skin blanching in the treated skin site under occluded conditions. Tape-stripping removed stratum corneum to a varying degree between individuals but was consistent (35%) within an individual with all formulations, day to day. A correlation (r = 0.9935) between the amount of drug in the treated stratum corneum normalized for surface area and the corresponding skin blanching score was observed with four 0.05% betamethasone dipropionate formulations. Increasing the amount of drug in the tape-stripped stratum corneum correlated with an increased skin blanching score. Ointment formulations delivered more drug to the skin and produced greater blanching scores than the cream formulations. Topical corticosteroid content in the treated skin site can therefore be quantified and correlates well with the resulting pharmacodynamic activity.
引用
收藏
页码:45 / 51
页数:7
相关论文
共 20 条
[1]   COMPARATIVE BIO-AVAILABILITY OF PROPRIETARY TOPICAL CORTICOSTEROID PREPARATIONS - VASOCONSTRICTOR ASSAYS ON 30 CREAMS AND GELS [J].
BARRY, BW ;
WOODFORD, R .
BRITISH JOURNAL OF DERMATOLOGY, 1974, 91 (03) :323-338
[2]   COMPARATIVE BIO-AVAILABILITY AND ACTIVITY OF PROPRIETARY TOPICAL CORTICOSTEROID PREPARATIONS - VASOCONSTRICTOR ASSAYS ON 31 OINTMENTS [J].
BARRY, BW ;
WOODFORD, R .
BRITISH JOURNAL OF DERMATOLOGY, 1975, 93 (05) :563-571
[3]   VARIOUS VAGARIES OF VASOCONSTRICTION [J].
BURDICK, KH .
ARCHIVES OF DERMATOLOGY, 1974, 110 (02) :238-242
[4]   CORRELATION BETWEEN THE DRUG PENETRATION AND THE BLANCHING EFFECT OF TOPICALLY APPLIED HYDROCORTISONE CREAMS IN HUMAN-BEINGS [J].
CARON, D ;
QUEILLEROUSSEL, C ;
SHAH, VP ;
SCHAEFER, H .
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, 1990, 23 (03) :458-462
[5]  
COLDMAN MF, 1971, BRIT J DERMATOL, V85, P381
[6]   CORRELATION OF THE VASOCONSTRICTION ASSAY AND CLINICAL ACTIVITY IN PSORIASIS [J].
CORNELL, RC ;
STOUGHTON, RB .
ARCHIVES OF DERMATOLOGY, 1985, 121 (01) :63-67
[7]   THE USE OF TOPICAL STEROIDS IN PSORIASIS [J].
CORNELL, RC ;
STOUGHTON, RB .
DERMATOLOGIC CLINICS, 1984, 2 (03) :397-409
[8]   INVIVO RELATIONSHIP BETWEEN HORNY LAYER RESERVOIR EFFECT AND PERCUTANEOUS-ABSORPTION IN HUMAN AND RAT [J].
DUPUIS, D ;
ROUGIER, A ;
ROGUET, R ;
LOTTE, C ;
KALOPISSIS, G .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1984, 82 (04) :353-356
[9]  
GIBSON JR, 1984, BR J DERMATOL S27, V3, P204
[10]   COMPARISON OF EFFECT OF VARIOUS TOPICALLY ACTIVE STEROIDS ON CLINICAL AND HISTOLOGICAL FEATURES OF PSORIASIS [J].
GOODWIN, PG ;
HAMILTON, S ;
FRY, L .
BRITISH JOURNAL OF DERMATOLOGY, 1973, 89 (01) :61-66