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IN VIVO STUDIES FURTHER DETAILS

In Vivo Study No: 197

METHODS

Chemical	Membrane	Concentration mg/ml	Concentration mg/ml	loading (mg/cm2)	Species	Site	Area (cm2)	Occluded?	Exposure Time (h)	Analytical Method
Beta-Estradiol	6	10	75	75% Ethanol	Human skin grafted rat	Abdomen	0.8	1	5	Radiolabelled (3H)

RESULTS

Length of Study (h)	% Recovery	+/-	Dose remaining on surface (mg)	% remaining on Surface	Dose remaining in stratum corneum (mg)	% remaining in stratum corneum	Dose remaining in the viable skin	% remaining in the viable skin	Amount Absorbed (mg)	% Absorbed	+/-	% Absorbed

Length of Study (h)

% Recovery

+/-

Dose remaining on surface (mg)

% remaining on Surface

Dose remaining in stratum corneum (mg)

% remaining in stratum corneum

Dose remaining in the viable skin

% remaining in the viable skin

Amount Absorbed (mg)

% Absorbed

+/-

% Absorbed

Maximal Flux (mcrg/cm2/h)	Average Flux (mcrg/cm2/h)	+/-	Time Plasma/Blood Levels Peaked (h)	Peak Blood Concentration (mg/l)	n	kp (cm/h)	Lag Time (h)
	8.4	1.8			4	0.0008

NOTES

An infinite dose was used so it is as though the study was occluded as evaporation was not an influence. Athymic nude mice were used. The human skin was grafted in a three step proceedure to produce a human skin sandwich flap. The beta-estradiol solutions were applied via STeCC cells. Details of the internal area and volume of the STeCC cell were obtained from Ref number 35. Absorption was measured by collecting samples from the local flap and systemic circulations. Beta-Estradiol Solutions were prepared by adding an excess of the drug to the vehicle. These solutions were allowed to equilibriate over 3 days and then spiked with radiolabelled drug at 0.1microCi/mg. The specific radioactivity of the drug was 60Ci/mmol

REFERENCE

Disparity Of In Vitro And In Vivo Oleic Acid-Enhanced Beta-Estradiol Percutaneous Absorption Across Human Skin (1993) Pharmaceut. Res., 10 :1745-1750