Reference

Pharmacokinetics and tolerance of sertaconazole in man after repeated percutaneous administration

Pharmacokinetics and tolerance of sertaconazole in man after repeated percutaneous administration. Farre, M.; Ugena, B.; Badenas, J. M.; Marquez, M.; Roset, P.; Ortiz, J. A. (Dep. Pharmacol. Toxicol., Inst. Munic. Invest. Med., Barcelona, Spain). Arzneim.-Forsch., 42(5A), 752-4 (English) 1992. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 63 The local and systemic tolerance of sertaconazole (FI-7045, CAS 99592-32-2) 2% cream was studied in healthy volunteers after cutaneous application in an increasing-dose schedule during 13 days. Blood and urine samples were collected after the application of 16 g of cream. Percentage of absorption was detd. in eight 3 ′ 3 cm areas of the volar arm skin after 2 mg cream topical application. No changes on vital signs (blood pressure, heart rate and body temp.) or in the ECG were found during the trial. Sertaconazole did not produce skin irritation nor systemic side effects. Sertaconazole was not detected in either the serum and urine samples obtained. The percentage of cutaneous absorption at 24 h after administration reached 72% of the applied dose.

Pharmacokinetic evaluation of labeled sertaconazole after dermal application

Pharmacokinetic evaluation of labeled sertaconazole after dermal application. Agut, J.; Moren, M.; Rego, M.; Sacristan, A.; Ortiz, J. A. (Res. Cent., Ferrer Group, Barcelona, Spain). Arzneim.-Forsch., 42(5A), 748-51 (English) 1992. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 63 14C-labeled sertaconazole (FI-7045, CAS 99592-32-2) was administered systemically (i.v. route) and topically (dermal route) in different formulations at doses of 10 mg/kg to hairless Sprague-Dawley rats. Detn. of plasma and liver levels of radioactivity demonstrated that the dermal application of sertaconazole induced very low systemic absorption with all the formulations used: 1.47% for sertaconazole cream, 1.97% for sertaconazole soln., 0.665% for sertaconazole powder and 0.885% for sertaconazole gel. Calcns. were made from the areas under plasma levels curves of each topical administration in comparison with i.v. administration. Significant radioactivity levels were found in the liver, which was consistent with a high hepatic metabolization and fecal excretion of the substance. However, the liver levels after topical application were virtually insignificant in comparison with the levels in the same organ obtained after i.v. administration.