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  • Author or Editor: P. Hermann x
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Authors: T. Hermann and P. Vértesi
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Authors: T. Hermann, O. Kis and P. Vértesi
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Abstract  

When the DSC analysis of different samples of terpin hydrate is carried out, a non identified small endotherm is observed at about 100°C, just before the melting endotherm. This phenomenon is detected whatever the experimental conditions are.After some trials, this endotherm was identified as an eutectic formed with terpin hydrate and desolvated terpin (17/83).The importance of the experimental conditions is preponderant. In an open pan, the desolvation occurs and the melting endotherm of the anhydrous form can be observed at 105°C. In a closed pan, no desolvation is detected and the melting endotherm at 120°C is that of the terpin hydrate.The eutectic exhibits a good compression ability and a fast dissolution. Its stability is correct. Its use in therapeutic tablets can be envisaged.The eutectic structure could be, more generally, favourable to compression owing to the isotropic texture of this particular solid state.

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The clinical significance of the oral candidiasis (either as independent disorder, or as a part of another disease) is increasing with time. The diagnosis and local treatment of the oral candidiasis may not be satisfactory, this disorder cannot be eliminated without the correct diagnosis and management of the underlying disease. At the same time, some disorders, such as Candida induced leukoplakia, may significantly enhance tumor development. Fungal infection of the mouth is often the initial sign of several immunodeficiency diseases. It is, therefore, very important to clarify the background of a fungal infection, since this may be critical regarding the prognosis.

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Authors: P. Hermann, Zsuzsanna Berek, G. Kriván, Krisztina Márton and Anna Lengyel

Eighty persons with haematological malignancies receiving stem cell transplantation (SCT) were examined over a 24 months period. Hyposalivation, a common complaint in patients treated by intensive chemotherapy and radiotherapy can predispose to oral candidal colonisation as well. This study was focused on correlation between the fungal colonisation of the oral cavity and the total unstimulated saliva flow rate of 80 patients with haematological malignancies before and after stem cell transplantation and in addition, on their oral health state. Despite the fact that prior to being involved in the transplantation programme, the patients were subjected to dental examination and decayed teeth were found in 20 out of 80 patients (25%). From the 2233 different oropharyngeal specimens fungi were isolated before conditioning from 16 patients (20%), and during aplasia from 19 patients (23.7%). Objective xerostomia (unstimulated total saliva flow rate = 0.1 ml/min) was detected in 28 patients (35%). Stem cell transplant patients with pretransplant mouth dryness had higher incidence of Candida albicans and other fungal colonisation than those with normal saliva secretion.

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Candida inconspicua is an emerging pathogen in immunocompromised patients possessing inherently decreased susceptibility to fluconazole. We determined the MICs and killing activity of fluconazole and amphotericin B against C. inconspicua clinical isolates as well as reference strain C. inconspicua ATCC 16783 for comparison. MICs were determined using the standard broth microdilution method. Killing rates were determined using time-kill methodology at 0.5–16 × MIC fluconazole and amphotericin B concentrations. Fluconazole and amphotericin B MIC values varied between 16–128 mg/l and 0.5–1 mg/l, respectively. In time kill-assays fluconazole showed fungistatic effect at 1–16 × MIC concentrations against all tested strains after 24 h-incubation, but became fungicidal after 48 h at 4–16 × MIC concentrations. The time necessary to achieve fungicidal endpoint at 1 mg/l amphotericin B concentration ranged from 2 to 24 h. Our in vitro results confirm the data that fluconazole is ineffective against C. inconspicua at the fluconazole serum concentration attainable in humans. Amphotericin B due to its rapid killing activity seems to be a good alternative for the treatment of infections caused by C. inconspicua .

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Abstract  

The complex formation of the bifunctional monophosphinic acid DOTA analogue DO3APABn (1,4,7,10-tetraazacyclododecane-4,7,10-triacetic-1-{methyl[(4-aminophenyl)methyl] phosphinic acid}) with 111In at a tracer level was analyzed. Formation of a complex between 111In and DO3APABn was very rapid even at room temperature and high radiolabeling yields were achieved. As introducing the methylphosphinic acid arm to the DOTA structure generated a chiral centre, more than one peak (probably corresponding to various diastereoisomers) of 111In-DO3APABn were separated on HPLC. Four peaks were separated by HPLC, they probably correspond to four diastereoisomers of 111In-DO3APABn originating from combination of chirality of complexes of DOTA-like ligands with chirality of coordinated phosphorus atom. Studies in rats showed rapid elimination of radioactivity from the blood and other organs and tissues. The results indicate that DO3APABn represents a promising ligand for radiolabeling of target-specific biomolecules with radiometals.

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Authors: P. Di Martino, P. Conflant, M. Drache, J. -P. Huvenne and A. -M. Guyot-Hermann

The polymorphic forms II and III of paracetamol were obtained by melting the marketed form I. Under the melting and cooling conditions used, it was possible to obtain forms I, II and III. The recrystallization conditions and the physical properties of forms II and III were investigated by means of various techniques: thermomicroscopy, DSC analysis, infrared microspectrometry and X-ray powder diffraction at room temperature and as a function of temperature. Form III was found to be very unstable. However, its formation seems to be an important intermediate step in the preparation of form II.

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