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Micro-liquid chromatography method for the determination of ciclopiroxolamine after pre-column derivatization in topical formulations.

Belliardo F, Bertolino A, Brandolo G, Lucarelli C.

Dipartimento di Scienza e Tecnologia del Farmaco, Facolta di Farmacia, Universita di Torino, Italy.

Ciclopiroxolamine is a broad-spectrum antimycotic drug. Neither the free acid (ciclopirox) nor its salt with ethanolamine (ciclopiroxolamine) can directly be quantified by liquid chromatography (LC) on both normal and reversed phases. This is due to the chelating function of the N-hydroxypyridone group that interacts strongly with stationary phases. Derivatization by alkylation forms a 1-alkyloxypirydone with regular chromatographic behaviour. A micro-LC method based on an isocratic elution reversed-phase system for quantification of ciclopiroxolamine in topical formulations is described. Chromatography was carried out using an LC Packings fused-silica capillary column (15 cm x 330 microns I.D.; Delta Pak, RP-18, 5 microns, 300 A) coupled to a Kontron 433 UV capillary detector. Data with respect to the derivatization reaction, recovery, reproducibility and limits of detection of the proposed method are reported and discussed.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1787166&dopt=Abstract ciclopirox Penlac



Penlac
Ciclopirox nail lacquer 8%: in vivo penetration into and through nails and in vitro effect on pig skin.

Ceschin-Roques CG, Hanel H, Pruja-Bougaret SM, Luc J, Vandermander J, Michel G.

Laboratoire de Microbiologie Industrielle et Virologie, Faculte des Sciences Pharmaceutiques, Toulouse, France.

This report presents original methods to assess the bioavailability of an antifungal drug from a varnish preparation in finger nails. For the studies with human volunteers a ciclopirox 8% nail lacquer was used to determine its efficacy in the treatment of onychomycoses. In vivo studies were performed on the fingernails of healthy volunteers by determining the total amount of ciclopirox penetrated per milligram of nail and the partition of the drug in the plate of the nails (technically divided into four layers). Ciclopirox concentrations were evaluated by measuring the inhibition of Candida pseudotropicalis growth in vitro. The ciclopirox concentration after 30 days treatment was determined as 3.35 +/- 0.82 micrograms/mg nail material. This is a sufficient amount to kill the fungal pathogens. In addition, in vitro penetration experiments were carried out with excised pig skin. Lacquer formulations from 0.5 to 8% were used to inhibit the growth of Trichophyton mentagrophytes. Formulations from 2 to 8% led to a strong to total inhibition of the dermatophyte after 30 min treatment time.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1831626&dopt=Abstract ciclopirox Penlac



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A clinical and laboratory study of ciclopirox olamine (8% Batrafen) in the treatment of onychomycosis.

Yu B, Zhou G, Wang B, Ben Y, Yan H, Shao Y, Wang B.

PUMC Hospital, CAMS, Beijing.

Ciclopirox olamine, a new synthetic substituted pyridone derivative, is an antimycotic agent with activity against a broad spectrum of pathogenic and nonpathogenic fungi. The clinical efficacy and safety of 8% ciclopirox olamine nail liquor were evaluated in 100 cases with finger (or great toe) onychomycosis. After 16 weeks and 24 weeks of treatment for finger and great toe onychomycosis, respectively, the overall therapeutic results were excellent in 36 cases, good in 17, fair in 24, and poor in 23. The period of treatment was extended in 31 cases; among them, 10 cases showed further improvement. As for in vitro inhibitory activity, the MIC of ciclopirox olamine against T. rubrum and C. albicans was 1 to 4 mg/L and 1 to 16 mg/L, respectively. This study indicates that 8% ciclopirox olamine nail liquor, with its satisfactory efficacy and lack of side effects, is a good remedy for onychomycosis.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1838936&dopt=Abstract ciclopirox Penlac



Penlac
Ciclopiroxolamine cream 1%: in vitro and in vivo penetration into the stratum corneum.

Ceschin-Roques CG, Hanel H, Pruja-Bougaret SM, Lagarde I, Vandermander J, Michel G.

Laboratoire de Microbiologie Industrielle et Virologie, Faculte des Sciences Pharmaceutiques, Toulouse, France.

Studies were conducted to assess the penetration of 1% ciclopiroxolamine cream, establishing the concentrations of the antimycotic compound in different layers of the stratum corneum with two skin models. Results of in vitro studies using skin from domestic pigs indicate that ciclopiroxolamine has the ability to penetrate fast into the epidermis, by inhibiting and killing inoculated Trichophyton mentagrophytes. In vivo investigation of the stratum corneum has been performed in healthy human volunteers by 20 strippings collected in four layers. Fungicidal concentrations of ciclopiroxolamine were determined after extraction from the strippings. These studies demonstrate that the concentrations reached levels which are sufficient to inhibit and kill pathogenic fungi.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1878248&dopt=Abstract ciclopirox Penlac



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[Experience in the treatment of skin mycoses with ciclopirox olamine]

[Article in Spanish]

Lecha Carralero V, Martinez Tomas C.

Servicio de Dermatologia, Hospital Clinico y Provincial, Barcelona.

Ciclopirox olamine cream 1%, a new antifungal agent has been studied in 30 patients with dermatophytosis and pityriasis versicolor. Diagnosis of dermatophytosis was confirmed by microscopic examination of KOH preparations and culture in Sabouraud medium. Pityriasis versicolor was diagnosed by direct exam preparation. Cultures and direct exam preparations were performed before starting treatment and weekly thereafter. Cultures and KOH preparations were positive in all patients. Treatment with ciclopirox olamine cream 1% was applied topically twice daily. Direct examination and cultures were negative in 26 cases (86.6%) after one week treatment and in 4 cases (13.4%) after two weeks. A parallel improvement in clinical signs and symptoms was evident with disappearance of erythema, pruritus and scaling. Clinical cure was achieved in most all cases (96.7%), between the third and fourth week of treatment.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2666788&dopt=Abstract ciclopirox Penlac