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, South Korea), ketoconazole (5 mg/kg; Ketoconazole Tablets, Eaglevet, Seoul, South Korea) and amoxicillin–potassium clavulanate (25 mg/kg; Clavet-50, Cipla, Mumbai, India), while discontinuing trimethoprim–sulphamethoxazole. Ketoconazole was used to both

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Abstract  

The objective of this work was to develop and validate a fast and reproducible method which is able to determine the concentration of ketoconazole in raw materials and tablets. The samples were analyzed by dynamic thermogravimetry at heating rates of 10, 20, 40, 60 and 80°C min−1 in nitrogen and nitrogen-synthetic air mixture. The concentrations of ketoconazole in the raw material and in the tablets were obtained from the vapor pressure curves. The data showed that there is no significant difference between the vapor pressure profiles of ketoconazole itself and in its tablet in both studied environmental conditions confirming that the process is really vaporization. The concentration of ketoconazole was determined in the raw material and tablets of the drug.

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Abstract  

Inclusion complexation between cyclodextrin derivatives (hydroxypropyl-β-cyclodextrin and methyl-β-cyclodextrin) and a very poorly water-soluble antifungal agent, ketoconazole, was studied. Solid products were prepared by physical mixing, kneading and spray-drying methods in four molecular ratios: 2:1, 1:1, 1:2 and 1:3. The possibility of complex formation between the drug and the cyclodextrins was studied by thermal analysis. Supplementary techniques, such as X-ray diffractometry and Fourier transformation-infrared spectroscopy, were also applied to interpret the results of the thermal study of the products.

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Malassezia pachydermatis is a commonly isolated yeast in veterinary dermatology that can produce biofilms in vitro and in vivo, lowering its susceptibility to antimicrobial drugs. The aim of this study was to determine and compare the in vitro susceptibility of planktonic cells and biofilms of M. pachydermatis isolates to ketoconazole and itraconazole. The presence of biofilm formation was confirmed by crystal violet staining and absorbance measurement at 595 nm wavelength, and by a scanning electron microscopy method. Cell viability was determined by the Celltiter 96 Aqueous One solution assay containing a water-soluble tetrazolium compound (MTS) with absorbance measurement at 490 nm. Planktonic cell minimum inhibitory concentrations (MICs) and minimum fungicidal concentrations (MFCs) of ketoconazole and itraconazole were very low: MIC90 and MFC90 were 0.032 and 0.125 μg/ml for ketoconazole, while 0.063 and 0.25 μg/ml for itraconazole, respectively. Also, the half maximal effective concentrations (EC50) of itraconazole were higher for planktonic cells and biofilms compared to ketoconazole. The EC50 values of ketoconazole were 18–169 times higher and those of itraconazole 13–124 times higher for biofilms than for planktonic cells. Biofilm EC50 levels exceeded MICs 103–2060 times for ketoconazole and 84–1400 times for itraconazole. No significant difference was found between these values of the two substances. In conclusion, biofilms of all examined M. pachydermatis strains were much less susceptible to ketoconazole and itraconazole than their planktonic forms.

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Abstract  

Four azole derivatives showing antimycotic activity (Miconazole, Ketoconazole, Clotrimazole, Fluconazole) in solid phase were exposed to beta irradiation at the dose of 20-200 kGy and then alterations in the physicochemical properties of the above derivatives were studied using the methods: scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. It was found that the compounds irradiated with sterilising doses (20-50 kGy) showed no significant alterations in their physicochemical properties, while application of doses >50 kGy resulted in small changes in the X-ray diffraction patterns and in the course of DSC curves, including a decrease in the melting points and enthalpy of the process. For Miconazole and Fluconazole, a linear and relatively strong correlation was found (from r =0.9782 to r =0.9003) between the size of the dose of irradiation and the decrease in the melting point and enthalpy value.

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, Jenkis , JK , Murphy , FY , et al.J Persistent adrenal insufficiency secondary to low-dose ketoconazole therapy . 82 : 676 – 680 , 1987 . 7 Chakrapee-Sirisuk , S , Amornpichetkul , K

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Interventional Medicine and Applied Science
Authors: Mohammed Rifaat Ahmed, Ashraf Saad Abou-Halawa, Waheed F. Hessam, and Diaa’ Salaheldin Aly Abdelkader

agar [ 8 ]. Inhibition zone around each disc was measured in millimeters and the fungal isolates were classified as sensitive, intermediate, or resistant. The used antifungals were fluconazole, ketoconazole, itraconazole, miconazole, and nystatin

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with acetylsalicylic acid, acetaminophen, diflunisal, dimenhydrinate, ketoconazole, and mefenamic acid. Experimental Chemicals Acetyl salicylic acid, acetaminophen, diflunisal, dimenhydrinate, ketoconazole

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In vitro susceptibilities of Scedosporium apiospermum isolates recovered from clinical and environmental samples in Nigeria were tested against ten conventional antifungal agents, namely: amphotericin B, nystatin, flucytosine, itraconazole, posaconazole, fluconazole, voriconazole, micafungin, ketoconazole, and terbinafine using the CLSI M38-A broth dilution reference method. The isolates showed varied response/sensitivities to the antifungal agents tested. This is probably the first documented testing of Scedosporium apiospermum isolates from Africa in general and Nigeria in particular against a broad range of conventional antifungal agents.

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JPC - Journal of Planar Chromatography - Modern TLC
Authors: Mirjana Aleksic, Slavica Eric, Danica Agbaba, Jadranka Odovic, Dušica Milojkovic-Opsenica, and Živoslav Tesic

The retention behavior of bifonazole, clotrimazole, fenticonazole, fluconazole, ketoconazole, miconazole, metronidazole, and itraconazole, widely used antimycotic drugs have been determined by TLC by use of the binary mobile phases acetone- n -hexane, methanol-toluene, and methyl ethyl ketone-toluene containing different amounts of organic modifier. Hydrophobicity was established from the linear relationships between the solute R M values and the concentration of organic modifier. Calculated values of R M 0 and C 0 were considered for application in QSAR studies of the antimycotics.

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