• Title/Summary/Keyword: Itraconazole

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Minimal Inhibitory Concentration of Antifungal Drugs on Pityrosporum Species (Pityrosporum 균속의 항진균제에 대한 연구)

  • 정병천;노병의;방용준
    • Biomedical Science Letters
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    • v.3 no.1
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    • pp.49-54
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    • 1997
  • Meanwhile Pityrosporum species as well as Candida species in yeast phase are not pathogenic, Pityrosporum in mycelial phase is pathogenic. Pityrosporum species can be isolated not only from tinea versicolor patients but also from ninety (90) percent of healthy persons. Minimal inhibitory concentration (MIC) of ketoconazole against Pityrosporum spp. was 0.05~0.8$\mu\textrm{g}$ ml$^{-1}$and the MIC of ketoconazole was the lowest. Of itraconazole, selenium sulfide, sodium thiosulfate and ketoconazole had the lowest MIC against P. orbiculare. The P. orbiculare strains isolated from healthy persons were inhibited by lower MIC than those isolated from tinea versicolor patients. P. ovale strains were inhibited by lower MIC at MIC$_{50}$ and MIC$_{90}$ of oral and topical antifungal agents than p. orbiculare.

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Imidazole Antifungal Drugs Inhibit the Cell Proliferation and Invasion of Human Breast Cancer Cells

  • Bae, Sung Hun;Park, Ju Ho;Choi, Hyeon Gyeom;Kim, Hyesook;Kim, So Hee
    • Biomolecules & Therapeutics
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    • v.26 no.5
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    • pp.494-502
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    • 2018
  • Breast cancer is currently the most prevalent cancer in women, and its incidence increases every year. Azole antifungal drugs were recently found to have antitumor efficacy in several cancer types. They contain an imidazole (clotrimazole and ketoconazole) or a triazole (fluconazole and itraconazole) ring. Using human breast adenocarcinoma cells (MCF-7 and MDA-MB-231), we evaluated the effects of azole drugs on cell proliferation, apoptosis, cell cycle, migration, and invasion, and investigated the underlying mechanisms. Clotrimazole and ketoconazole inhibited the proliferation of both cell lines while fluconazole and itraconazole did not. In addition, clotrimazole and ketoconazole inhibited the motility of MDA-MB-231 cells and induced $G_1$-phase arrest in MCF-7 and MDA-MB-231 cells, as determined by cell cycle analysis and immunoblot data. Moreover, Transwell invasion and gelatin zymography assays revealed that clotrimazole and ketoconazole suppressed invasiveness through the inhibition of matrix metalloproteinase 9 in MDA-MB-231 cells, although no significant changes in invasiveness were observed in MCF-7 cells. There were no significant changes in any of the observed parameters with fluconazole or itraconazole treatment in either breast cancer cell line. Taken together, imidazole antifungal drugs showed strong antitumor activity in breast cancer cells through induction of apoptosis and $G_1$ arrest in both MCF-7 and MDA-MB-231 cells and suppression of invasiveness via matrix metalloproteinase 9 inhibition in MDA-MB-231 cells. Imidazole drugs have well-established pharmacokinetic profiles and known toxicity, which can make these generic drugs strong candidates for repositioning as antitumor therapies.

Preparation of Micro- and Submicron-Particles of a Poorly Water-Soluble Antifungal Drug Using Supercritical Fluid Process (초임계유체공정을 이용한 난용성 항진균제의 미세입자 제조)

  • Kim, Seok-Yun;Lee, Jung-Min;Won, Byoung- Hyun;Jung, In-Il;Ryu, Jong-Hoon;Lim, Gio-Bin
    • Clean Technology
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    • v.16 no.2
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    • pp.80-87
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    • 2010
  • In this study, micro- and submicron particles of itraconazole, a poorly water-soluble antifungal drug, were prepared for improving its aqueous solubility using an ultrasound-assisted supercritical fluid technique, called SAS-EM. The SAS-EM process used in our experiments was different from the conventional SAS-EM in that the ultrasound was applied directly to the spray nozzle. The effect of the ultrasonic power, temperature, and solvent on the formation of itraconazole particles were investigated. Smaller particles were obtained through our SAS-EM process compared with the ASES process, and the mean particle size decreased as the ultrasonic power increased. Our experimental results confirmed that the ultrasound-assisted supercritical fluid process is an efficient method for producing ultrafine particles.

Determination of itraconazole in human plasma by high performance liquid chromatography (HPLC/UV를 이용한 혈장 중 이트라코나졸의 분석)

  • Jang, Hae Jong;Lee, Ye Rie;Lee, Kyung Ryul;Han, Sang-Beom;Kang, Seung Woo;Lee, Hee Joo
    • Analytical Science and Technology
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    • v.19 no.3
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    • pp.239-243
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    • 2006
  • This method is used for the determination of itraconazole in human plasma by liquid-liquid extraction and high performance liquid chromatography. Felodipine was used as an internal standard. After extraction of the plasma with diethyl ether, the centrifuged upper layer was then transferred. The supernantant was evaporated and then reconsituted with mobile phase. The mobile phase was composed of 10 mM ammonium acetate adjusted to pH 7 by phosphoric acid with a flow rate of 0.2 mL/min. A C18 reversed-phase column with a pre-column was used as the analytial column. Linear detection responses were obtained for itraconzole concentration range for 2~1,000 ng/mL. The correlation coefficient of linear regression($R^2$) was 0.9991, limit of quantification (LOQ) was 2 ng/mL, reproducibility was less than 10.8 %, and accuracy was 97.2~108.2%. This method has been successfully applied to the pharmacokinetic study of itraconazole in human plasma.

Pulmonary Candidiasis in a Dog Receiving Long-term Management for Atopic Dermatitis (아토피성 피부염의 장기 치료중인 개에서 발생한 폐 칸디다증)

  • Han, Jae-Ik;Lee, Chang-Min;Kim, Taewoo;Lee, In;Choi, Soo-Young;Park, Hee-Myung
    • Journal of Veterinary Clinics
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    • v.32 no.3
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    • pp.259-262
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    • 2015
  • A canine patient exhibited partial anorexia and sudden respiratory distress. Diagnostic imaging and cytology of tracheal-lavage fluids revealed fungal pneumonia. Molecular identification and phylogenetic analysis detected Candida catenulata. Treatment with oral itraconazole for 3 weeks was effective. This is the first report of C. catenulata infection in a dog.

CASE REPORT : MAXILLARY SINUS ASPERGILLOSIS (상악동 국균증의 치험 2례)

  • Jang, Yong-Wook;Song, Kyung-Ho;Jung, Jin-Won;Lee, Seul-Ki;Kim, Jwa-Young;Song, Sang-Hoon;Yang, Byoung-Eun;Kim, Seong-Gon
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.34 no.4
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    • pp.480-484
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    • 2008
  • The incidence of aspergillosis infections in the maxillary sinus has increased recently, because of overuse of antibiotics, steroids, anticancer agents, immunosuppressant, antimetabollites, and uncontrolled diabetes mellitus. The clinical features of maxillary sinus aspergillosis include pain, swelling and foul odor nasal excretion. This needs to be differentiated from bacterial maxillary sinusitis, and surgical treatment with antifungal agents are suggested. Recently, we treated two patients with maxillary sinus aspergillosis surgically (Caldwell Luc operation) and with antifungal agents(itraconazole). The results were satisfactory so we report these cases with literature review.

Allergic Bronchopulmonary Aspergillosis Associated with Aspergilloma (폐국균종과 동반된 알레르기성 기관지폐 아스페르길루스증 1예)

  • Ryu, Jeon-Su;Baik, Jae-Joong;Kim, Do-Kyun;Kim, Young-Jin;Eom, Woo-Seob;Cho, Jea-Hyun
    • Tuberculosis and Respiratory Diseases
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    • v.56 no.3
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    • pp.302-307
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    • 2004
  • Aspergilloma and Allergic Bronchopulmonary Aspergillosis(ABPA) are different types of the pulmonary aspergillosis spectrum of diseases. ABPA is an inflammatory disease that causes hypersensitivity to Aspergillus spores growing in the bronchi, which is characterized by asthma, recurrent pulmonary infiltrations or mucoid impaction, eosinophilia and central bronchiectasis. Aspergilloma is a simple colonization of fungus within a cavitary lung lesion, but these diseases rarely coexist. A case of ABPA, coexistent with Aspergilloma, was experienced in a 31 year-old female. The diagnosis was confirmed by the immediate cutaneous reactivity to Aspergillus fumigatus, elevated total IgE antibodies, peripheral eosinophilia, bronchiectasis, growth of Aspergillus species in a sputum culture and radiographic infiltration. Treatment, with prednisone and itraconazole, led to improvement of the respiratory symptoms, reduction of the cavitary lesion and in the total serum IgE level.