ABSTRACT
Abstract Candidiasis is one of the most common fungal infections of oral cavity in humans, causing great oral discomfort, pain and aversion to food. To develop more effective antifungal systems for the treatment of oral candidiasis, an oral mucoadhesive wafer containing sertaconazole solid dispersion (STZ-SD) was developed in this study. Dispersion of STZ in Soluplus® as a solubility enhancement excipient was done by melting, solvent evaporation and freeze drying method at various STZ to Soluplus® ratios. The optimized STZ-SD was then incorporated in the sodium carboxymethyl cellulose (SCMC) gel, xanthan gum gel, or their combination to prepare the lyophilized wafers. The swelling capacity, porosity, and mechanical, release and mucoadhesive properties of the wafers, together with their antifungal activity, were then evaluated. The melting method sample with the ratio of 8:1 showed the best results in terms of saturation solubility and dissolution rate. The STZ-SD-composite wafer exhibited higher hardness and mucoadhesion, as compared to those made of the SCMC polymer. The STZ-SD-wafer also exhibited a greater antifungal effect when compared to the STZ-wafer. The present study, thus, suggested that the STZ-SD-wafer could serve as a novel effective delivery system for oral candidiasis treatment.
Subject(s)
Mouth/pathology , Candidiasis, Oral/drug therapy , Food/classification , Freeze Drying/classification , Gingiva/abnormalitiesABSTRACT
Objective:To investigate clinical efficacy of mucopolysaccharide polysulfate cream combined with sertaconazole nitrate cream in the treatment of scaly hyperkeratotic tinea pedis.Methods:From March 2019 to January 2020, 100 patients with scaly hyperkeratotic tinea pedis were enrolled into this study, and randomly and equally divided into 2 groups by using a random number table: control group treated with topical sertaconazole nitrate cream alone at a dose of 0.5-1 g twice a day; combined group treated with topical mucopolysaccharide polysulfate cream at a dose of 0.5-1 g followed by topical sertaconazole nitrate cream at a dose of 0.5-1 g 30 minutes later, which were performed twice a day. The treatment lasted 4 weeks. The time to clinical symptom relief, efficacy and incidence of adverse reactions were compared between the two groups. Dermatology life quality index (DLQI) was assessed at 0, 2 and 4 weeks after the start of treatment. Two-independent-sample t test, repeated measures analysis of variance and chi-square test were used for statistical analysis. Results:After treatment, the time to pruritus relief and that to desquamation improvement were 6.05 ± 1.98 and 12.03 ± 3.92 days respectively in the combined group, which were significantly shorter than those in the control group (8.39 ± 2.11, 15.11 ± 4.05 days, t = 5.72, 3.86, respectively, both P < 0.001) . During the 4 weeks of treatment, DLQI scores gradually decreased in both the 2 groups (all P < 0.001) , which were significantly lower in the combined group than in the control group at weeks 2 and 4 (both P < 0.001) . After 4-week treatment, the total response rate was 98% (49/50) in the combined group, significantly higher than that in the control group (82%, 41/50; χ2= 7.11, P= 0.007) . There was no significant difference in the incidence of adverse reactions between the two groups ( P > 0.05) . Conclusion:Mucopolysaccharide polysulfate cream can improve the efficacy of sertaconazole nitrate cream in the treatment of scaly hyperkeratotic tinea pedis.
ABSTRACT
Background: Dermatophytosis is becoming increasingly unresponsive to conventional antifungals. Newer topical antifungals may be more effective in these patients. Aims: To evaluate and compare the efficacy and safety of amorolfine 0.25% cream and sertaconazole 2% cream in limited tinea cruris/corporis. Methods: A single-center, randomized (1:1), double-blind, parallel group, active-controlled trial (CTRI/2014/12/005246) was performed. Sixty-six untreated adults with acutely symptomatic tinea cruris/corporis were included in the study. All patients had limited cutaneous involvement and were KOH mount positive. Group A received amorolfine 0.25% cream, and group B received sertaconazole 2% cream twice daily application to the lesions for 4 weeks. After the baseline visit, four follow-up visits were carried out. The outcome measures for effectiveness were clinical and mycological cure. Safety parameters studied were treatment-emergent adverse events and changes in routine laboratory parameters. Results: Both sertaconazole and amorolfine significantly reduced symptoms (P < 0.001) in both groups. However, improvement in symptoms (pruritus, burning sensation, erythema, scaling and crusting) was significantly greater in the sertaconazole group at every follow-up visit. Sertaconazole cream was also more effective than amorolfine cream in reducing the number of lesions (P = 0.002 at 12 weeks) and improving the Dermatology Life Quality Index (P < 0.001) at all the follow-up visits. Adverse events were similar in the two groups (P = 0.117). Fungal cultures became negative in 92.3% of the sertaconazole group as compared to 80% in the amorolfine group (P = 0.010). Limitations: Antifungal susceptibility testing could not be done. Conclusion: Sertaconazole 2% is superior to amorolfine 0.25%, both in terms of effectiveness and tolerability. Improvement can be appreciated from second week onwards.
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OBJECTIVE:To establish a method for determination of the related substances in Sertaconazole nitrate vaginal tab-let. METHODS: HPLC was performed on the column of Hypersil BDS C18(150 mm×4.6 mm,5 μm)with mobile phase of 0.5%Ammomium acetate solution-acetonitrile-methanol(15∶42.5∶42.5,V/V/V) at a flow rate of 1.0 ml/min,detection wavelength was 220 nm,column temperature was 25℃,and the injection volume was 20μl. RESULTS:The related substances in Sertaconazole ni-trate vaginal tablet can be well separated;the liner range of sertaconazole nitrate was 12.24-28.56 μg/ml (r=0.999 9);RSDs of precision,stability and reproducibility tests were lower than 1%;recovery was 99.38%-99.80%(RSD=0.14%,n=9). CONCLU-SIONS:The method is accurate and reliable with high sensitivity and strong specificity,and can be used for the related substances in Sertaconazole nitrate vaginal tablet.
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Background: Tinea corporis is a common dermatophytic infection of the body involving keratin layer of skin. This lesion presents as an annular plaque with an advancing border along with central clearing. Clotrimazole is topical, conventional imidazole antifungal drug and has given good efficacy in tinea corporis. Sertaconazole is new topical imidazole antifungal claimed to be superior to old topical imidazoles in tinea corporis. The aim of this study was to compare efficacy, safety and cost effectiveness of topical antifungals, clotrimazole 1% cream and sertaconazole 2% cream in patients suffering from mild to moderate tinea corporis attending out-patient department of tertiary care hospital in Vidarbha region of Maharashtra. Methods: This was a prospective, comparative, randomized trial with 2 parallel treatment arms of 4 weeks duration. Patients were diagnosed on the basis of clinical evaluation and microscopic findings of KOH mount. Hundred patients were randomly assigned into two groups of clotrimazole 1% cream, and sertaconazole 2% cream with 50 patients in each group. Evaluation was carried out at baseline, 1st week, 2nd week and 4th week for efficacy parameters viz. itching, erythema and scaling, physician’s global assessment (PGA), safety and cost effectiveness. Results: Topical sertaconazole 2% cream was highly efficacious and superior to clotrimazole 1% cream in improvement of clinical parameters, PGA and mycological cure at the end of the treatment phase. At end of the follow-up phase both the trial drugs were effective with no recurrence or relapse of tinea corporis. However, clotrimazole 1% cream was safe and cheaper. Conclusions: Topical clotrimazole 1% cream and sertaconazole 2% were effective and well tolerated in patients of tinea corporis. Effectiveness of sertaconazole was early and superior with tolerable side-effects. However, clotrimazole was costeffective.
ABSTRACT
Background: Sertaconazole is a new imidazole fungicide introduced for vulvo-vaginal candidiasis. It has an azole group with benzothiophene that inhibits biosynthesis of ergosterol and brings about a massive leak of cytoplasm with consequent fungal cell death. Objective: Assess the safety and efficacy of Sertaconazole in the treatment of fungal vulvo-vaginitis for comparison with Fluconazole and Clotrimazole. Subjects and methods: One-hundred eighty-eight outpatients with fungal vulvo-vaginitis were recruited at Siriraj Hospital, Thailand between August 31, 2004 and January 30, 2006. The patients were given Sertaconazole, Fluconazole, or Clotrimazole, and received vaginal swab and culture for fungus at seventh and 28th days after treatment. Results: Out of 188 cases, 177 cases were followed-up completely. Sertaconazole group included 66 cases where 35 cure, 20 fail, and 7 recurrent cases. Fluconazole group included 60 cases and had 37 cure, six fail, and 20 recurrence cases. Clotrimazole group included 55 cases and had 32 cure, nine fail and 11 recurrent cases. There were risk factors of fungal vulvo-vaginitis, including frequent micturition and small toilet shower flushing. Conclusion: Sertaconazole had similar effectiveness and less side-effect as compared with Fluconazole and Clotrimazole. It appeared to work well with lowest recurrence.