非离子型X—CT造影剂磺海醇的合成

报道了非离子型Ｘ－ＣＴ造影剂磺海醇的化学合成。产物经元素分析、红外光谱、核磁共振谱、质谱和快原子轰击质谱等测定，与结构完全一致。     

头孢尼西钠杂质谱与市售品杂质谱的相似度研究

目的采用反相高效液相色谱法研究自制头孢尼西钠(CFNS)杂质谱和市售CFNS杂质谱的相似性。方法采用自身对照法对杂质谱进行定量测定,用相似度法比较自制CFNS杂质谱和市售CFNS杂质谱的相似性,并用UPLC-MS初步鉴定杂质种类。结果自制CFNS和市售CFNS的杂质谱均为9个共有杂质,两者杂质谱相似度均>0.99,自制CFNS杂质总含量略低于市售CFNS。结论自制CFNS杂质谱中杂质种类和总含量与市售CFNS杂质谱中杂质种类和总含量相当,中药指纹图谱相似度评价方法完全适合评价CFNS的杂质谱。     

L-甲基多巴的波谱学数据和结构确证

目的确证L-甲基多巴的结构。方法采用紫外、红外、氢谱、碳谱和质谱等方法进行结构解析。结果在0.1 mol·L-1氢氧化钠溶液中最大吸收峰发生红移;红外光谱表明分子中含有羟基、氨基、羰基和苯环等结构;碳谱显示结构中含有10个碳;质谱的分子离子峰m/z为211。结论通过上述方法可以确证L-甲基多巴的结构。     

盐酸度洛西汀的波谱学研究

报道并解析了盐酸度洛西汀的红外光谱、紫外光谱、质谱、氢-氢相关谱、碳谱(13C-NMR,DEPT)、碳氢相关谱、碳氢远程相关谱,对所有1HNMR和13CNMR谱的信号进行归属,同时讨论了红外特征吸收峰所对应的官能团的振动形式。     

不同降解方法制备褐藻胶甘露糖醛酸寡糖的结构特点

综述了以不同降解方法制备的甘露糖醛酸寡糖的结构特点,及其甘露糖醛酸寡糖在质谱、核磁共振氢谱及碳谱等谱图上的特征。     

胆红素IX_α的提取与纯化研究

用直接水解法从新鲜猪胆汁中提取胆红素IX_α,所得胆红素粗品用改良的氯仿抽提法进行纯化。通过元素分析、红外光谱和质谱等对胆红素的纯度进行确证。胆红素的质谱图上出现清晰的特征谱峰,这些谱峰可望在胆红素异构体和纯度的快速检验方面得到应用。     

假细锥香茶菜新二萜成分——假细锥甲素的结构

从假细锥香茶菜(Rabdosia coetsoides C.Y.Wu)叶分离得到新二萜成分,根据紫外光谱、红外光谱、质谱、核磁共振氢谱及碳谱等分析,推定了化学结构,并经X-射线衍射确证,命名为假细锥甲素。     

乳酸环丙沙星的波谱分析

介绍乳酸环丙沙星的红外光谱、紫外光谱、核磁共振谱（￣１Ｈ、￣（１３）Ｃ）和质谱的谱图和数据，并对其进行归属分析。     

L-甲基多巴的波谱学数据和结构确证

目的确证L-甲基多巴的结构。方法采用紫外、红外、氢谱、碳谱和质谱等方法进行结构解析。结果在0.1 mol·L^-1氢氧化钠溶液中最大吸收峰发生红移;红外光谱表明分子中含有羟基、氨基、羰基和苯环等结构;碳谱显示结构中含有10个碳;质谱的分子离子峰m/z为211。结论通过上述方法可以确证L-甲基多巴的结构。     

丹参中丹参螺旋缩酮内酯的结构

从丹参注射液水沉淀部分分得一结晶,经紫外光谱、红外光谱、核磁共振谱及质谱推断了其结构并经X射线衍射证实了该结构,命名为丹参螺旋缩酮内酯,为一新成分.     

Measurement of glomerular filtration rate and effective renal plasma flow in the conscious beagle dog by single intravenous bolus of iohexol and p-aminohippuric acid.

The objective of this study was to validate a kinetic approach for the simultaneous measurement of glomerular filtration rate (GFR) and effective renal plasma flow (ERPF) in the dog. Six healthy male Beagle dogs were randomly assigned in a three-period cross-over study of intravenous bolus administration of iohexol (64.7 mg/kg), PAH (10 mg/kg), and an iohexol/PAH mixture. PAH and iohexol were determined simultaneously by a validated high-performance liquid chromatographic method. The iohexol and PAH data obtained after intravenous administration were analyzed using noncompartmental and bicompartmental approaches. A simplified iohexol plasma clearance was also calculated from the terminal elimination phase of the plasma iohexol concentrations versus time profile. The total plasma clearance values for PAH and exo-iohexol were 13+/-2.3 mL/kg/min and 2.9+/-0.3 mL/kg/min, respectively. No significant (or biologically relevant) effect of coadministration of PAH and iohexol was observed on the pharmacokinetic parameters of either drug. The calculation of simplified plasma clearance led to an overestimation of the true plasma clearance. In conclusion, GFR and ERPF can easily and rapidly be measured in the dog by this approach which is relatively noninvasive.     

碘海醇药动学研究进展与应用

碘海醇注射液是一种非离子型含碘造影剂, 已广泛应用于临床造影。肾小球滤过率是肾功能评价的重要指标, 近年来, 碘海醇用于肾小球滤过率测定的研究报道颇多。碘海醇用药相对安全, 但其不良反应的发生时有报道, 合理的护理措施至关重要。碘海醇药动学研究可为临床合理用药提供参考, 准确、高效的测定方法是药动学研究的基础。本文对近几年碘海醇的测定方法、药动学研究、应用、不良反应的相应护理措施进行简单综述, 期望为碘海醇的基础研究, 临床合理用药以及进一步的开发利用提供参考资料。     

碘海醇与泛影葡胺在CT增强检查160例高危因素的副反应

对有造影剂反应高危因素80例(男44,女36,年龄44±SD 9yr)用非离子型碘海醇100mL(300gI/L)作CT增强检查;另外有造影剂反应高危因素80例(男39,女41,年龄38±SD11yr)用离子型60％泛影葡胺100mL作CT增强检查。结果碘海醇的总副反应、中度反应的发生率均低于泛影葡胺(P<0.01,P<0.05),证明碘海醇在高危因素患者应用的安全性及可靠性。     

低剂量碘海醇CT尿路造影应用在小儿肾积水检查中的价值

目的 研究低剂量碘海醇CT尿路造影应用在小儿肾积水检查中的价值.方法 50例肾积水患儿为研究对象,均接受低剂量碘海醇CT尿路造影和静脉尿路造影.以病理组织学诊断为最终诊断的金标准,比较两种检查方法的尿路显影率与假阴性率,不同程度肾积水患儿低剂量碘海醇CT尿路造影检查的图像评级.结果 低剂量碘海醇CT尿路造影检查的尿路显...     

Glomerular filtration and saturable absorption of iohexol in the rat isolated perfused kidney.

1. The renal handling of iohexol was examined in the rat isolated perfused kidney (IPK) over a perfusate concentration range of 5-20 micrograms ml-1. 2. At a concentration of 5 micrograms ml-1, a ratio of renal clearance over clearance by glomerular filtration (ClR/GF) of 0.63 +/- 0.06 could be determined. This ratio increased until 1.02 +/- 0.06 at 20 micrograms ml-1, indicating that a saturable mechanism is involved in the luminal disappearance of the drug. 3. Pretreatment of the kidneys with polylysine, probenecid or diatrizoate resulted in a significantly enhanced clearance of iohexol, probably due to inhibition of membrane binding. Renal clearance data were fitted to a kinetic model including filtration into the primary urine followed by saturable absorption at the luminal membrane. An absorption constant, KA, of 7.3 +/- 1.3 micrograms ml-1, and a maximum rate of absorption, VA,Max, of 1.4 +/- 0.1 micrograms min-1 were determined. 4. Iohexol accumulated in kidney tissue, reaching a concentration of 2 to 7.5 times the perfusate concentration. In freshly isolated proximal tubular cells and kidney cortex mitochondria, iohexol reduced the uncoupled respiratory rate at a concentration comparable to the highest tissue concentration found in the IPK. 5. In conclusion, iohexol is not only filtered by the kidney but also reabsorbed via a saturable mechanism, which results in tubular accumulation. Intracellularly sequestered iohexol may affect mitochondrial oxidative metabolism. Our results indicate that iohexol is not a true filtration marker.     

Neurotropic effects of non-ionic contrast media

Effects of non-ionic contrast media on the central nervous system were compared in order to clarify any differences due to the side-chain structures among iopamidol, iotrolan, iocibidol, iohexol, iopromide, iosimide and metrizamide. The study included a primary screening test based on Irwin's method, antielectric convulsive tests using mice, measurement of the blood pressure using rats and electroencephalography using rats and rabbits. The general behavior of mice in the primary screening test revealed that tolerance to iopamidol, iotrolan and iocibidol was excellent; that to iopromide and iohexol was moderate; and that to iosimide and metrizamide was poor. Iosimide and iohexol suppressed the transient increase of blood pressure upon intravenous administration in the normal rats but not in the pithed rats. Electric stimulus increased the mortality of mice pretreated with iosimide and iohexol. Abnormal EEG with epileptic seizures, slow wave and/or flattening were observed with the administration of iopromide, iosimide or metrizamide as well as ionic contrast media. From these results, it was concluded that iopromide and metrizamide were not well tolerated in general behavior and EEG; iohexol, in general behavior, electroshock and blood pressure; and iosimide, in all experiments, while iopamidol, iotrolan and iocibidol were well tolerated. Therefore, small differences in their side-chain structures among these contrast media are considered to cause different effects on the central nervous system.     

复方泛影葡胺与碘海醇在肾盂造影诊断中的毒副反应比较

目的 比较静脉肾盂造影诊断中常用的显影剂复方泛影葡胺与碘海醇引起的不良反应.方法 回顾性分析医院98例静脉肾盂造影患者(采用复方泛影葡胺显影剂者45例,采用碘海醇者53例)的一般资料、造影方法和不良反应.结果 采用复方泛影葡胺造影的45例患者中,出现毒副反应者39例(86.67%),其中第一级副反应31例(68.89%),第二级副反应5例(11.11%),第三级副反应3例(6.67%).采用碘海醇造影的53例患者中,出现毒副反应者有25例(47.17%),其中第一副反应22例(41.51%),第二级副反应3例(5.66%).结论 在静脉肾盂造影诊断中,应用碘海醇为显影剂的安全性优于复方泛影葡胺.     

<Emphasis Type="BoldItalic">In Vivo</Emphasis> Performance of a Liposomal Vascular Contrast Agent for CT and MR-Based Image Guidance Applications

Purpose This study evaluated the in vivo performance of a liposome formulation that co-encapsulates iohexol and gadoteridol as a multimodal contrast agent for computed tomography (CT) and magnetic resonance (MR)-based image guidance applications. Materials and Methods The pharmacokinetics and biodistribution studies were conducted in Balb-C mice using high performance liquid chromatography (HPLC) and inductively coupled plasma atomic emission spectrometry (ICP-AES) to detect iohexol and gadoteridol concentrations. The imaging efficacy of this liposome system was assessed in New Zealand White rabbits using a clinical CT and a clinical 1.5 Tesla MR scanner. Results The vascular half-lives of the liposome encapsulated iohexol and gadoteridol in mice were found to be 18.4 ± 2.4 and 18.1 ± 5.1 h. When administered at the same dose the distribution (α phase) half-lives for the free contrast agents were 12.3 ± 0.5 min (iohexol) and 7.6 ± 0.9 min (gadoteridol); while, the elimination (β phase) half-lives were 3.0 ± 0.9 h for free iohexol and 3.0 ± 1.3 h for free gadoteridol. The CT and MR signal increases were measured and correlated with the concentrations of iohexol and gadoteridol detected in plasma samples. Conclusion The long in vivo circulation lifetime and simultaneous CT and MR signal enhancement provided by this liposome system make it a promising agent for image guidance applications.     

An efficient approach for glomerular filtration rate assessment in older adults

Aims

Assessment of glomerular filtration rate (GFR) is crucial because the GFR value defines the stage of chronic kidney disease and determines the adjustment of drug dosage. The aim was to investigate a new method for the accurate determination of GFR in older adults based on the combination of an exogenous filtration marker, iohexol, and an endogenous marker, serum creatinine or cystatin C.

Methods

We combined variables for the estimation of GFR with a reduced set of measurements of the marker iohexol. In a population-based sample of 570 subjects (≥70 years old) from the Berlin Initiative Study (BIS), we investigated the following: (i) the BIS1 and BIS2 equations based on age, gender and serum creatinine with or without serum cystatin C; (ii) equations based on one or two iohexol measurements; and (iii) equations based on the combination of variables from BIS1 or BIS2 with iohexol measurements. The reference standard was based on eight iohexol measurements. The cut-off value of 60 ml min⁻¹ (1.73 m)⁻² was chosen to assess accuracy. Equations were constructed using a learning sample (n = 285) and an independent validation sample (n = 285).

Results

Misclassification rates were 17.2% (BIS1), 11.6% (BIS2), 14.7% [iohexol measurement at 240 min (iohexol₂₄₀)], 7.0% (iohexol₂₄₀ combined with variables included in BIS1) and 6.7% (iohexol₂₄₀ combined with variables included in BIS2). Misclassification rates did not decrease significantly after inclusion of two or three iohexol measurements.

Conclusions

Combined strategies for the determination of GFR lead to a relevant increase of diagnostic validity.     

碘海醇致严重不良反应65例文献分析

目的：了解碘海醇致严重不良反应（ADR）的情况,分析其特点和相关因素,促进临床合理用药。方法：采用文献学计量方法,对国内公开报道的65例碘海醇致严重ADR进行总结性分析。结果：碘海醇致严重ADR中,全身性损害41例,神经系统损害10例,呼吸系统损害8例,泌尿系统损害3例,皮肤附件、血液及消化系统损害各1例。结论：碘海醇致全身性、神经系统、呼吸系统损害较为多见,占总ADR分别为63.08%,15.38%,12.31%;碘海醇ADR前3位依次为过敏性休克、神经系统和呼吸系统损害,占总ADR78.46%。