• 환경위생공학
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• 제12권3호
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• pp.87-94
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• 1997

Influences of clotrimazole on the blood cholesterol and HDL-cholesterol level were studied in rats. Rats were provided food and water ad libitum and clotrimazole and methylcellulose were gavaged for 6 days. Clotrimazole was suspended in 1% methylcellulose solution as and administered at concentration 20mg/Kg, 40mg/Kg, 60mg/Kg. Body weight gain and liver weight/body weight ratio, serum cholesterol level, serum HDL-cholesterol level, serum triglyceride level, the activity of cytochrome p450 and erythromycin demethylase were determined at 6th day. Clotrimazole decreased the body weight gain a little as compared with control group and did not show any influence on liver weight/body weight ratio. Clotrimazole increased the serum HDL-cholesterol and serum triglyceride level significantly. Clotrimazole increased the microsomal cytochrome P450 significantly and increased the erythromycin demethylase (cytochrome P450 IIIA) significantly too. It might be conclued that clotrimazole showed a little influence on body weight and increased the serum lipid, especially HDL-cholesterol level. It also increased microsomal cytochrome P450 IIIA significantly. It might be concluded that clotrimazole showed a corelative influence between HDL-cholesterol and cytochrome P450 IIIA. In these results clotrimazole can be used as an anti-atherosclerotic agent by increasing the HDL-cholesterol but it is necessary that cloreimazole will show any adverse or side action on body or not.

• Natural Product Sciences
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• 제13권3호
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• pp.258-262
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• 2007

The antifungal activity of the essential oil fraction from Thymus magus, and its major component thymol, against Candida albicans was investigated in vitro and in vivo. The combined effects of the oils and clotrimazole, a commonly used antifungal drug for treatment of external candidiasis, were evaluated in this study. In experimental vaginal candidiasis the essential oil fraction of T. magnus resulted in relatively milder inhibition of fungal growth following the inoculation of test mice compared to clotrimazole. However, new fungal growth was not detected up to 12 days after cessation of treatment. In contrast, in a similar experiment using clotrimazole, C. albicans was detected in the $12^{th}$ day post-treatment with the sample. This result indicates that T. magnus oil could be a promising drug to control vaginal candidiasis. In checkerboard titer tests, the combination of clotrimazole with the essential oil fraction of T. magus or T. quinquecostatus resulted in significant synergism, with FIC indices between 0.14 and 0.27 against C. albicans, while clotrimazole combined with thymol, the major component of these oils, produced only an additive effect, with FIC indices ranging between 0.50 and 1.00. Thus, the prominent synergistic effects of clotrimazole combined with T. magus essential oil indicate that these compounds may be an effective treatment for C. albicans infections.

• 대한수의학회지
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• 제29권1호
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• pp.69-73
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• 1989

준임상형 유방염 이환 젖소의 유즙과 유두컵으로부터 분리된 Candida속 균의 8종 항진균성약제에 대한 감수성을 조사하였던 결과는 다음과 같다. 총 53주의 Candida속균 중 98.2%, 94.4%, 84.8%의 균주가 각각 clotrimazole, econazole, miconazole의 농도 $25{\mu}g/ml$이하에서 발육이 억제됨으로서, 이들 약제의 항균력이 타 약제에 비하여 우수하였다. 균종별로 보면 C albicans는 clotrimazole에 대한 감수성이 가장 높았으며, 기타 비교적 감수성이 높았던 약제는 5-fluorocytosine, econazole, miconazole의 순이었다. C pseudotropicalis와 C guilliermondii는 haloprogin, clotrimazole, miconazole, econazole, 5-fluorocytosine등에 높은 감수성을 나타내었으며, haloprogin의 평균 MIC가 $0.17{\sim}0.19{\mu}g/ml$로 가장 우수하였다. C krusei는 cycloheximide에 대한 감수성이 가장 높았으며, 그의 비교적 감수성이 높았던 약제는 clotrimazole, haloprogin, miconazole, econazole의 순이었다. 한편 C parapsilosis는 econazole, cycloheximide, clotrimazole등에 다소 감수성을 나타내었으나, 이들 약제의 MIC는 econazole(기하평균 MIC $7.26{\mu}g/ml$)을 제외하고는 타균종에서 보다 현저히 낮았다. 또한 C tropicalis는 전 공시약제에 대하여 감수성이 낮은 경향이었다.

• 방사선산업학회지
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• 제4권1호
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• pp.7-11
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• 2010

Clotrimazole [1-{(2-chlorophenyl)-diphenylmethyl}-1H-imidazole, CLT] has been reported to inhibit the proliferation of vascular endothelial and act as an in vitro anti-VEGF drug. It is also shown to inhibit angiogenesis in an animal model. The radioisotope labeled clotrimazole derivative can be utilized to monitor the physiologic processes of cancer. In this study, we synthesized [$^{18}F$]fluoride labeled clotrimazole derivatives as a new tumor imaging agent for PET. The references were prepared by a refluxing with clotrimazole and an excess of fluoroalkyltosylate in acetonitrile for 36 h and clotrimazole reacted with ditosylalkane to give precursors. [$^{18}F$]Fluoride labeled reaction was performed with precursor in Kryptofix[2.2.2]/$K_2CO_3$ for 10 min at $80^{\circ}C$. The radiolabeling mixture was passed through a silica Sep-Pak cartridge to remove $^{18}F^-$. The [$^{18}F$]F-clotrimazole derivatives were synthesized with a 20~25% yield. In the radiofluorination step, we used acetonitrile and DMSO as a solvent and observed a higher yield at the acetonitrile (25%) reaction compared with the DMSO reaction (5%).

• 대한미생물학회지
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• 제19권1호
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• pp.35-40
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• 1984

The effectiveness of three antifungal antibiotics amphotericin B, clotrimazole and 5-fluorocytosine was tested against 120 clinical isolated Candida species. The minimum inhibitory concentrations of amphotericin B was considerably lower than those of clotrimazole and 5-fluorocytosine. High-level resistance to 5-fluorocytosine was present in 50% of the isolates. The combination of clotrimazole and 5-fluorocytosine produced synergistic inhibition against all 20 strains of Candida albicans tested that were relatively resistant to both antifungal agents.

• 대한청각학회지
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• 제23권1호
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• pp.15-19
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• 2019

Background and Objectives: To determine the efficacy of filling the external auditory meatus with 1% clotrimazole at a single visit for the treatment of otomycosis. Subjects and Methods: This prospective study included 40 patients who were referred to our clinic with complaints of ear itching, pain, and fullness, and were diagnosed with unilateral otomycosis. After cleaning the mycotic hyphae from the external auditory meatus, the ear canal was filled with 1% clotrimazole, using an intravenous catheter and syringe. The patients received follow-up examinations on post-treatment days 7, 15, and 45. Results: The follow-up otomicroscopic examinations revealed that 95% of the ear canals were entirely clean and that all symptoms had resolved. The post-treatment scores of pain, aural fullness and itching were significantly lower than the pre-treatment scores (p<0.01). Conclusions: Filling the external auditory meatus with 1% clotrimazole at a single visit is an easy, efficient, and cost-effective treatment for otomycosis. Additionally, high patient compliance makes this treatment superior to long-term topical therapy.

• Journal of Audiology & Otology
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• 제23권1호
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• pp.15-19
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• 2019

Background and Objectives: To determine the efficacy of filling the external auditory meatus with 1% clotrimazole at a single visit for the treatment of otomycosis. Subjects and Methods: This prospective study included 40 patients who were referred to our clinic with complaints of ear itching, pain, and fullness, and were diagnosed with unilateral otomycosis. After cleaning the mycotic hyphae from the external auditory meatus, the ear canal was filled with 1% clotrimazole, using an intravenous catheter and syringe. The patients received follow-up examinations on post-treatment days 7, 15, and 45. Results: The follow-up otomicroscopic examinations revealed that 95% of the ear canals were entirely clean and that all symptoms had resolved. The post-treatment scores of pain, aural fullness and itching were significantly lower than the pre-treatment scores (p<0.01). Conclusions: Filling the external auditory meatus with 1% clotrimazole at a single visit is an easy, efficient, and cost-effective treatment for otomycosis. Additionally, high patient compliance makes this treatment superior to long-term topical therapy.

• Journal of Pharmaceutical Investigation
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• 제35권2호
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• pp.107-110
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• 2005

To develop a clotrimazole-loaded solid suppository with poloxamer and propylene glycol, the melting points of various formulations composed of poloxamer 188 (P 188) and propylene glycol were investigated. The dissolution study of clotrimazole delivered by the suppository composed of P 188 and propylene glycol was performed. The mixtures composed of P 188 and propylene glycol were homogeneous. Propylene glycol affected the melting points of poloxamer mixtures. In particular, the mixture [P 188/propylene glycol (70/30%)] with the melting point of about $32^{\circ}C$ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, propylene glycol affected greatly the dissolution rates of clotrimazole from the suppository. Dissolution mechanism analysis showed the dissolution of clotrimazole was proportional to the time. Our results indicated that the solid suppository with P 188 and propylene glycol would be a candidate of rectal dosage form for clotrimazole.

• Journal of Pharmaceutical Investigation
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• 제38권5호
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• pp.289-293
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• 2008

To develop a poloxamer-based solid suppository with poloxamer and polyethylene glycol mixtures, the melting point of various formulations composed of P 188 and propylene glycol were investigated. The dissolution and antitumor activity of clotrimazole delivered by the poloxamer-based suppository were performed. The poloxamer mixtures composed of P 188 and propylene glycol were homogeneous phases. P 188 greatly affected the melting point of poloxamer mixtures. In particular, the poloxamer mixture [P 188/propylene glycol(70/30%)] with the melting point of about $32^{\circ}C$ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, the ratio of P 188/propylene glycol greatly affected the dissolution rates of clotrimazole from poloxamer-based suppository. It gave the more effective anti-tumor activity than conventional PEG-based suppository due to fast dissolution. Thus, the clotrimazole-Ioaded poloxamer-based solid suppository was an effective rectal dosage form with anti-tumor activity.

• Journal of Pharmaceutical Investigation
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• 제39권6호
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• pp.437-443
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• 2009

To develop a topical bioadhesive formulation of clotrimazole for enhanced transdermal delivery, hydroxypropyl methylcellulose gel containing permeation enhancer was formulated and permeation studies were carried out. The release characteristics of the drug from the gel formulation were examined according to the receptor medium, drug concentration, and temperature. The rate of drug release from the gel increased with increasing drug concentration and temperature. The activation energy (Ea) of drug permeation, which was calculated from the slope of log P versus 1/T plots, was 14.41kcal/mol for a 1%(w/w) loading dose. The enhancer, such as saturated, unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants, were incorporated onto the gels to increase the amount of drug permeation into the skin. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest level of enhancement. These results show that clotrimazole gels containing polyoxyethylene 2-oleyl ether could be used for the enhanced transdermal delivery of clotrimazole.