共查询到20条相似文献,搜索用时 15 毫秒
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《Journal of labelled compounds & radiopharmaceuticals》2002,45(3):199-211
γ‐Vinyl‐γ‐aminobutyric acid (GVG, Vigabatrin®), a suicide inhibitor of GABA‐transaminase (GABA‐T), has been suggested as a new drug for the treatment of substance abuse. In order to better understand its pharmacokinetics and potential side effects, we have developed a radiosynthesis of carbon‐11 (t1/2=20 min) labeled GVG for positron emission tomographic (PET) studies. We report here a novel synthetic strategy to prepare the precursor and to efficiently label GVG with C‐11. 5‐Bromo‐3‐(carbobenzyloxy)amino‐1‐pentene was synthesized in five steps from homoserine lactone, including reduction and methylenation. This was used in a one‐pot, two‐step radiosynthesis. Displacement of bromide with no‐carrier‐added [11C]cyanide followed by acid hydrolysis afforded [1‐11C]GVG with decay corrected radiochemical yields of 27±9% (n=6, not optimized) with respect to [11C]cyanide in a synthesis time of 45 min. Copyright © 2002 John Wiley & Sons, Ltd. 相似文献
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《Journal of labelled compounds & radiopharmaceuticals》2003,46(4):333-342
A new approach for 11C–C bond formation via a Sonogashira‐like cross‐coupling reaction of terminal alkynes with [11C]methyl iodide was exemplified by the synthesis of 17α‐(3′‐[11C]prop‐1‐yn‐1‐yl)‐3‐methoxy‐3,17β‐estradiol. The LC‐purified title compound was obtained in decay‐corrected radiochemical yields of 27–47% (n=8) based on [11C]methyl iodide within 21–27 min after EOB. In a typical synthesis starting from 9.6 GBq [11C]methyl iodide, 1.87 GBq of 17α‐(3′‐[11C]prop‐1‐yn‐1‐yl)‐3‐methoxy‐3,17β‐estradiol was synthesized in radiochemical purity >99%. The specific radioactivity ranged between 10 and 19 GBq/µmol, and the labeling position was verified by 13C‐NMR analysis of the corresponding 13C‐labeled compound. Copyright © 2003 John Wiley & Sons, Ltd. 相似文献
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Randomised clinical trial: deep remission in biologic and immunomodulator naïve patients with Crohn's disease – a SONIC post hoc analysis
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J.‐F. Colombel W. Reinisch G. J. Mantzaris A. Kornbluth P. Rutgeerts K. L. Tang A. Oortwijn G. S. Bevelander F. J. Cornillie W. J. Sandborn 《Alimentary pharmacology & therapeutics》2015,41(8):734-746
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Somashekar Shyale K.P.R. Chowdary Y.S.R. Krishnaiah Narasimha K. Bhat 《Drug development research》2006,67(2):154-165
The present investigation assessed the in vivo properties of the guar gum–based colon‐targeted matrix tablets of albendazole‐β‐cyclodextrin (KA), albendazole matrix tablet (GA), and an immediate‐release albendazole tablet (CA) in humans. A single oral dose was administered in healthy human volunteers and a completely randomized, two‐way, three‐period crossover design was adopted. The data were statistically analyzed and a value of P<0.05 was considered statistically significant. In healthy human volunteers, guar gum colon‐targeted tablets showed delayed tmax and absorption time, decreased absorption rate constant, and unaltered t1/2indicating that albendazole is not released in stomach and small intestine, but is delivered to the colon, resulting in a slow absorption of the drug and making the drug available for local action in the colon. The increase in Cmax and AUC0‐∞ of KA shows that the bioavailability of albendazole in humans could be definitely improved by complexing the drug with β‐cyclodextrin. Furthermore, an open, parallel, single‐blind clinical study was conducted in patient volunteers who had helminthiasis. Clinical studies showed that the guar gum colon‐targeted tablets could reduce eggs per gram faster than conventional tablets could, resulting in improved clinical symptoms, Hb content, and decreased total count as compared to conventional tablets of albendazole. The investigation shows that albendazole, when complexed with β‐cyclodextrin, improves in vivo bioavailability of the drug and colon targeting using guar gum ensures drug delivery in the colonic fluids, and therefore improves clinical efficacy in human beings with helminthiasis. Drug Dev. Res. 67:154–165, 2006. © 2006 Wiley‐Liss, Inc. 相似文献
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Randomised clinical trial: mucosal protection combined with acid suppression in the treatment of non‐erosive reflux disease – efficacy of Esoxx,a hyaluronic acid–chondroitin sulphate based bioadhesive formulation
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V. Savarino F. Pace C. Scarpignato the Esoxx Study Group 《Alimentary pharmacology & therapeutics》2017,45(5):631-642
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《Biopharmaceutics & drug disposition》2017,38(4):290-300
Liver volume is a critical scaling factor for predicting drug clearance in physiologically based pharmacokinetic modelling and for both donor/recipient graft size estimation in liver transplantation. The accurate and precise estimation of liver volume is therefore essential. The objective here was to extend an existing meta‐analysis using a non‐linear mixed effects modelling approach for the estimation of liver volume to other race groups and paediatric and geriatric populations. Interrogation of the PubMed® database was undertaken using a text string query to ensure as objective a retrieval of liver volume data for the modelling exercise as possible. Missing body size parameters were estimated using simulations from the Simcyp Simulator V13R1 for an age and ethnically appropriate population. Non‐linear mixed effect modelling was undertaken in Phoenix 1.3 (Certara) utilizing backward deletion and forward inclusion of covariates from fully parameterized models. Existing liver volume models based on body surface area (BSA) and body weight and height were implemented for comparison. The extension of a structural model using a BSA equation and incorporating the Japanese race and age as covariates and exponents on LV0 (θ Baseline) and body surface area (θ BSA), respectively, delivered a comparatively low objective function value. Bootstrapping of the original dataset revealed that the confidence intervals (2.5–97.5%) for the fitted (theta) parameter estimates were bounded by the bootstrapped estimates of the same. In conclusion, extension and re‐parameterization of the existing Johnson model adequately describes changes in liver volume using the body surface area in all investigated populations. Copyright © 2017 John Wiley & Sons, Ltd. 相似文献
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《Journal of labelled compounds & radiopharmaceuticals》2017,60(2):130-134
Metallo‐beta‐lactamase enzymes make bacteria resistant to a broad range of commonly used beta‐lactam antibiotics. Several thiol derivatives of L‐amino acids have been shown their inhibitory effects against the metallo‐β‐lactamase IMP‐1. In this study, (2‐mercaptoacetyl)‐L‐tryptophan as a new inhibitor of metallo‐β‐lactamases labeled with carbon‐14 in the 2‐position of the indole ring was prepared from [2‐14C]indole as a key synthetic intermediate based on chiral pool strategy. The overall synthesis was performed in 10 steps with the overall radiochemical yield 3.6% on the basis of the barium [14C]carbonate as a starting material. 相似文献
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Jeppe Ragnar Andersen Inger Byrjalsen Asger Bihlet Faidra Kalakou Hans Christian Hoeck Gitte Hansen Henrik Bo Hansen Morten Asser Karsdal Bente Juel Riis 《British journal of clinical pharmacology》2015,79(4):660-668