Transdermal absorption and topical bioavailability of coumarin.
Coumarin was administered I.V., P.O. and topically to male Sprague-Dawley rats. The concentration-time profile after I.V. administration could be best described by an open-two compartment model. After P.O. administration the fraction of drug absorbed was 0.21 +/- 0.08 (S.D.). 1 g of hydrophilic ointment (U.S.P. XIX) containing 5% w/w of coumarin was applied on the shaven back skin. When the area of application was 4.91 cm2 the drug was absorbed in a zero-order fashion. The fraction of administered drug absorbed in 6 h was 0.086 +/- 0.02 (S.D.). Increasing the area of application to 30.0 cm2 resulted in deviation from the zero-order absorption characteristic. This is attributed to decrease in the concentration gradient as more drug is absorbed and to the change in formulation characteristics as a function of time. The fraction of drug absorbed in 24 h was 0.66 +/- 0.21 (S.D.).
Ritschel
W A
WA
Division of Pharmaceutics and Drug Delivery Systems, University of Cincinnati Medical Center, OH.
Hussain
S A
SA
D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D003374:Coumarins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
D003374:Coumarins; C030123:coumarin