CICLOPIROX TOPICAL SUSPENSION, USP
0.77% (w/w) (LOTION)
Rx only
FOR DERMATOLOGIC USE ONLY
NOT FOR OPHTHALMIC USE
DESCRIPTION:
Ciclopirox Topical Suspension, USP 0.77% (Lotion) is for topical use.
Each gram of Ciclopirox Topical Suspension, USP 0.77% (Lotion) contains 7.7 mg of ciclopirox (as ciclopirox olamine) in a water miscible lotion base consisting of purified water USP, cocamide DEA, octyldodecanol NF, mineral oil USP, stearyl alcohol NF, cetyl alcohol NF, polysorbate 60 NF, myristyl alcohol NF, sorbitan monostearate NF, lactic acid USP, and benzyl alcohol NF (1%) as a preservative.
Ciclopirox Topical Suspension, USP 0.77% (Lotion) contains a synthetic, broad-spectrum, antifungal agent ciclopirox (as ciclopirox olamine). The chemical name is 6-cyclohexyl-1-hydroxy-4-methyl-2(1 H)-pyridone, 2-aminoethanol salt.
The CAS Registry Number is 41621-49-2. The chemical structure is:
Ciclopirox Topical Suspension, USP 0.77% (Lotion) has a pH of 7.
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CLINICAL PHARMACOLOGY:
Ciclopirox is a broad-spectrum, antifungal agent that inhibits the growth of pathogenic dermatophytes, yeasts, and Malassezia furfur. Ciclopirox exhibits fungicidal activity in vitro against isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida albicans.
Pharmacokinetic studies in men with radiolabeled ciclopirox solution in polyethylene glycol 400, showed an average of 1.3% absorption of the dose when it was applied topically to 750 cm2 on the back followed by occlusion for 6 hours. The biological half-life was 1.7 hours and excretion occurred via the kidney. Two days after application only 0.01% of the dose applied could be found in the urine. Fecal excretion was negligible. Autoradiographic studies with human cadaver skin showed that ciclopirox penetrates into the hair and through the epidermis and hair follicles into the sebaceous glands and dermis, while a portion of the drug remains in the stratum corneum.
In vitro penetration studies in frozen or fresh excised human cadaver and pig skin indicated that the penetration of Ciclopirox Topical Suspension, USP 0.77% (Lotion) is equivalent to that of Ciclopirox Cream 0.77%. Therapeutic equivalence of cream and lotion formulations also was indicated by studies of experimentally induced guinea pig and human trichophytosis.
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