Enhanced Bioavailability by Transdermal Administration of Pranoprofen Gels Containing Octanoic Acid to Rats

Abstract

− The pharmacokinetic parameters and bioavailability of pranoprofen from the gel were measured to determine the enhancing effect of octanoic acid on the transdermal absorption of pranoprofen in rats. 8 mg/kg of pranoprofen was administered from gel with octanoic acid (the enhancer group) or that without octanoic acid (the control group) via the transdermal route, and the results were compared with those obtained from the intravenously (0.5 mg/kg, IV group) or orally administered group (4 mg/kg, oral group). The AUC of the control, the enhancer, the IV, and the oral groups were 20.2±5.1, 50.7±12.7, 19.9±2.5, and 70.5±17.6 ug/ml·h respectively. The average C max of the control and the enhancer group were 0.93±0.23 and 2.82±0.71 ug/ml, respectively, and the mean T max of the control and the enhancer group was 7.00 h. The relative bioavailability of the transdermally administered pranoprofen gel containing octanoic acid was approximately 2.50 times higher than the control group, showing a relatively constant, sustained blood concentration with minimal fluctuation. This suggests that it might be feasible to develop a pranoprofen gel preparation containing an enhancer for the transdermal administration, which is more convenient dosage form than the oral dosage forms.

Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels

“…Among the unsaturated fatty acids like oleic acid and linoleic acid, oleic acid showed signifi cantly increased permeation of ropivacaine from CMC gel. In the case of fatty acids, a saturated fatty acid group increased the permeation rate more than an unsaturated fatty acid group (Choi and Shin, 2008).…”

Enhanced bioavailability and antihistamine effects by transdermal administration of loratadine gels containing an enhancer in rats

“…In a previous report, in order to increase the skin permeation of loratadine from the gels using various enhancers, a loratadine gel system containing polyoxyethylene 2-stearyl ether was formulated as a best enhancer for the enhanced transdermal delivery of loratadine [Song and Shin, 2009]. Here, the bioavailability and pharmacokinetics of the transdermal administration of loratadine gel containing an enhancer were examined by comparing with those of orally or intravenously administered loratadine to rats [Choi and Shin, 2008;Shin et al, 2007]. We also evaluated the antihistamine effect of loratadine by transdermal application of the gels containing polyoxyethylene 2-stearyl ether by the Evans blue dye method [Shin and Choi, 2005].…”