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911.
912.
913.
H Han RL de Vrueh JK Rhie KM Covitz PL Smith CP Lee DM Oh W Sadée GL Amidon 《Canadian Metallurgical Quarterly》1998,15(8):1154-1159
PURPOSE: General use of nucleoside analogues in the treatment of viral infections and cancer is often limited by poor oral absorption. Valacyclovir, a water soluble amino acid ester prodrug of acyclovir has been reported to increase the oral bioavailability of acyclovir but its absorption mechanism is unknown. This study characterized the intestinal absorption mechanism of 5' -amino acid ester prodrugs of the antiviral drugs and examined the potential of amino acid esters as an effective strategy for improving oral drug absorption. METHODS: Acyclovir (ACV) and Zidovudine (AZT) were selected as the different sugar-modified nucleoside antiviral agents and synthesized to L-valyl esters of ACV and AZT (L-Val-ACV and L-Val-AZT), D-valyl ester of ACV (D-Val-ACV) and glycly ester of ACV (Gly-ACV). The intestinal absorption mechanism of these 5' -amino acid ester prodrugs was characterized in three different experimental systems; in situ rat perfusion model, CHO/hPEPT1 cells and Caco-2 cells. RESULTS: Testing 5' -amino acid ester prodrugs of acyclovir and AZT, we found that the prodrugs increased the intestinal permeability of the parent nucleoside analogue 3- to 10-fold. The dose- dependent permeation enhancement was selective for L-amino acid esters. Competitive inhibition studies in rats and in CHO cells transfected with the human peptide transporter, hPEPT1, demonstrated that membrane transport of the prodrugs was mediated predominantly by the PEPT1 H+/dipeptide cotransporter even though these prodrugs did not possess a peptide bond. Finally, transport studies in Caco-2 cells confirmed that the 5' - amino acid ester prodrugs enhanced the transcellular transport of the parent drug. CONCLUSIONS: This study demonstrates that L-amino acid-nucleoside chimeras can serve as prodrugs to enhance intestinal absorption via the PEPT1 transporter, providing a novel strategy for improving oral therapy of nucleoside drugs. 相似文献
914.
Congenital subluxation of the peroneal tendons is an uncommon, but not rare condition. In almost all cases, it will spontaneously resolve without requiring any treatment. Presented is a case report of the condition affecting the patient bilaterally. The subluxation did not resolve and the patient was subsequently treated with a modification of the Kelly procedure. 相似文献
915.
通过扫描电子显微镜对氧化锆增韧的羟基磷灰石和纯羟基磷灰石的裂纹扩展和断口形貌特征的观察,发现增韧的羟基磷灰石是以沿晶方式断裂,而纯羟基磷灰石是以解理方式断裂。本文分析了造成增韧前后两种材料不同断裂方式的机制,并讨论了颗粒增韧生物陶瓷的机理。 相似文献
916.
H.-W. Chung H. Delincée S.-B. Han J.-H. Hong H.-Y. Kim J.-H. Kwon 《Journal of food science》2002,67(7):2517-2522
ABSTRACT: Detection characteristics of perilla seeds exposed to electron beam doses of 0 to 2 kGy were investigated. DNA comet assay, photostimulated luminescence (PSL) and thermoluminescence (TL) measurements, and hydrocarbon determinations by GC-MS were carried out. The irradiated samples showed comets with longer tails (152 ± 6 mm) than did nonirradiated samples (35 ± 11 mm). PSL values (photon counts) for the irradiated samples were more than 7865; whereas those of nonirradiated samples were less than 294. TL ratios (Glow 1/Glow 2) obtained from nonirradiated samples were less than 0.01 and above 0.48 from irradiated ones. The prominent radiation-induced hydrocarbons were 16:2, 16:3, 17:1, and 17:2, of which 16:2 was the most abundant. 相似文献
917.
RN Younes KC Yin CJ Amino M Itinoshe M Rocha e Silva D Birolini 《Canadian Metallurgical Quarterly》1998,22(1):2-5
The weeping fig, Ficus benjamina (Fb), is a relatively common indoor allergen. Many cases of perennial allergic rhinoconjunctivitis and allergic asthma caused by Fb hypersensitivity are not detected. These patients typically have proven sensitization to housedust mites and do not improve after avoidance of exposure (encasing) and specific immunotherapy. The number of Fb sensitizations is increasing in Germany, which can partly be explained by the cross-reactivity between Hevea brasiliensis (Hb) latex and Fb and the rapidly increasing number of mostly occupational latex allergies. But Fb itself is a potential sensitizer which is widely spread as ornamental plant in homes and offices. As relevant indoor allergen Fb ranks third after housedust mites and pets but before molds among our allergy patients. For diagnosis, prick-tests with Fb-latex seem to be more sensitive than in vitro-methods (RAST, CAPRAST). Fb plants should not be kept in the homes of atopic individuals or persons with latex (Hb) allergy. 相似文献
918.
MM Ferreira H Mansinho A Fernandes FS Pereira JA Assis e Santos 《Canadian Metallurgical Quarterly》1994,7(5):307-309
Benign mesothelioma of the pleura is a very rare tumor. The cells responsible originate from either the mesothelium or the submesothelium. This is why such tumors are described in the literature as fibroma of the pleura, mesothelial fibroma, localized fibrous mesothelioma and monophasic spindle cell tumor. Their growth, is very slow taking several years or even decades. In contrast to the more common malignant mesothelioma of the pleura, it is not related to asbestos exposure. This report deals with a 47-year-old woman patient with a giant benign mesothelioma of the pleura in the region of the right thorax, which was completely removed by thoracotomy. 相似文献
919.
Surface temperatures were measured on dry Douglas fir sapwood specimens during Cone Calorimeter tests using thermocouples and an infra-red pyrometer. Good agreement between the thermocouples and the pyrometer was obtained when (1) the emissivity was assumed to be 1.0 and (2) the thermocouples were in good contact with the surface and were not located in the proximity of a fissure. The major fissures were normal to the grain of the wood and the volatiles vented through the fissures. Char oxidation in the region between the vertical fissures resulted in higher surface temperatures. 相似文献
920.