ABSTRACT
OBJECTIVE: To prepare butenafine hydrochloride thermosensitive microemulsion-based hydrogel and evaluate the quality. METHODS: A series of temperature sensitive microemulsion gels with different gelation temperatures were prepared, using ethyl oleate as oil phase, Tween 80 as surfactant, ethanol as co-surfactant, and poloxamer as temperature-sensitive material. The morphology, particle size, Zeta potential, percutaneous absorption speed and skin retention were evaluated. RESULTS: The best formulation was composed of ethyl oleate-Tween 80-ethanol-poloxamer 407-poloxamer 188-distilled water at ratios of 4∶15∶10∶16.33∶5.68∶71. The oil/water microemulsion exhibited a spherical shape without adhesion or aggregation observed by TEM. The average diameter was 91.03 nm and the PDI was 0.246. The transdermal speed of microemulsion gel was faster than the marketed cream, and the drug retention in the skin was 5 times of the marketed cream. CONCLUSION: The hydrogel exhibits good temperature sensitivity and skin retention effect, and can penetrate skin cutin and act as a depot thus increase the local drug concentration and enhance the antibacterial effect.
ABSTRACT
Objective To prepare butenafine hydrochloride plastics,investigate the prescription composition and make a quality control standard for the preparation.Methods Film-forming time and appearance quality as the evaluation index,the quality control standard of butenafine hydrochloride according to the Chinese pharmacopoeia two section ( 2010 edition ) was made.ResuIts The prescription of butenafine hydrochloride plastics was identified as:1%butenafine hydrochloride(w/w),10%glycerol(w/w),3%carbomer 971PNF(w/w),0.1% ethyl p-hydroxybenzoate(w/w),moderate anhydrous sodium sulfite(pH adjusting agent) and 95% ethanol (solution).The preparation was colorless,transparent and viscous semi-solid with pH4.5.A content determination method of butenafine hydrochloride with HPLC was established and the result was stable and reliable .ConcIusion The butenafine hydrochloride has several advantages such as preparation simply , stable property,application convenience and quality control.It is a potential preparation to develop.
ABSTRACT
BACKGROUND: Topical 1% butenafine hydrochloride cream, a new benzylamine derivative, has been reported to have antimycotic effect. OBJECTIVE: An open trial as conducted to assess the efficacy and safety of 1% butenafine hydrochloride cream used once daily in the treatment of tinea pecis. METHODS: Of 45 patients with clinically and mycologically proertinea pedis from the department of dermatology at Kosin medical college hospital, 42 patient, who could be monitored to the end of this study were evaluated. They applied 1% butenafine hydrochloride cream once daily until clinical improvement became evident or for 4 weeks and the effects were evaluated clinically and mycologically. RESULTS: 1. From the mycological studies at the initial visit, causative organisms were isolated from 36 patients out of the 42 subjects and Trichophyton rubrum was most comnmon organism. 2. The negative conversion rate of the mycological study( negative microscopy and negative culture) was 90.5%(38/42) after 4 weeks of treatment. 3. The effective treatment vate at 4 weeks was 90.5%(38/42) 4. A adverse effects of using 1% butenafine hydrochloride cream was noted in 1 patient, who had a moderate degree of puritus, out of the 42 subjects. The presritus disappeared soon after the cessation of application of the cream. CONCLUSION: 1% butenafine lydrochloride cream is effective andafe in the treatment of tinea pedis.