Twenty-four-hour pharmacokinetics of rectal acetaminophen in children: an old drug with new recommendations

Oxidized low density lipoprotein (LDL) and acetyl LDL are recognized by the scavenger receptor class A type I/II (SR-AI/II) on macrophages and liver endothelial cells. Several investigators have suggested that there are additional receptors specific for oxidized LDL, but characterization of these alternate receptors for oxidized LDL and evaluation of their quantitative importance in uptake of oxidized LDL has been difficult because of overlapping ligand specificity with SR-AI/II. The purpose of this study was to determine the importance of SR-AI/II in the removal of modified LDL from the bloodstream in vivo. The clearance rate of oxidized LDL from plasma in normal mice was very rapid, and > 90% of injected dose was removed from the blood within 5 min. Clearance rates of oxidized LDL were equally high in SR-AI/II knockout mice, indicating that this receptor is not required for removal of oxidized LDL from plasma. Surprisingly, there was no difference in the clearance rate of acetyl LDL in wild-type and SR-AI/II knockout animals. The plasma clearance of radioiodinated acetyl LDL was almost fully blocked by a 50-fold excess of unlabeled acetyl LDL, but the latter only inhibited oxidized LDL clearance by approximately 5%. Both modified LDLs were cleared mostly by the liver, and there was no difference in the tissue distribution of modified LDL in control and knockout mice. Studies in isolated nonparenchymal liver cells showed that Kupffer cells accounted for most of the uptake of oxidized LDL. Extensively oxidized LDL and LDL modified by exposure to fatty acid peroxidation products were efficient competitors for the uptake of labeled oxidized LDL by SR-AI/II-deficient Kupffer cells, while acetyl LDL and malondialdehyde-modified LDL were relatively poor competitors.     

Synthesis and anticonvulsant activity of new thiazolidinone and thioxoimidazolidinone derivatives derived from furochromones

Various new thiazolidinone and thioxoimidazolidinone derivatives were synthesized starting from 4,9-dimethoxy-5 H-furo[3,2-g][1]benzopyran-5-on-7-carboxaldehyde. The anticonvulsant activity of the synthesized compounds was evaluated. Most of the compounds showed anticonvulsant activity equal or superior to phenobarbital.     

Evaluation of oral midazolam as pre-medication in day care surgery in adult Pakistani patients

A placebo controlled randomized double blind study was designed to assess the suitability of oral Midazolam as a premedication in day care surgery in adult Pakistani patients. Fifty ASA I and II patients aged between 20-60 years received either Midazolam 7.5 mg or a placebo approximately one hour prior to surgery. Midazolam 7.5 mg produced significant anxiolysis and sedation (p < 0.001) in comparison to placebo after one hour of premedication. There was a significant difference (p < 0.001) in the mean heart rate and blood pressure in both groups after 1 hour of premedication with a lesser rise in blood pressure and heart rate in the Midazolam group. Psychomotor performance assessed by 'n' deletion test was impaired by Midazolam (p < 0.001) and recall of pictures revealed differences (p < 0.05) in the groups at one hour after premedication. However, at four hours after surgery there were no differences in both groups. These findings indicate that rapidly acting oral Midazolam in doses of 7.5 mg provided safe and effective premedication in terms of anxiolysis, sedation, amnesia and psychomotor performance and is suitable for day surgery.     

Conversion of D-arabinose to D-erythroascorbic acid and oxalic acid in Sclerotinia sclerotiorum

D-glycero-Pent-2-enono-1,4-lactone (trivial name: D-erythroascorbic acid) occurs in the phytopathogen, Sclerotinia sclerotiorum (Lib.) de Bary, where it has a potential role as precursor of oxalic acid. On Glc/yeast/malt medium, S. sclerotiorum produces only nominal amounts of D-erythroascorbic acid but even partial replacement of Glc by D-Ara increases production of erythroascorbic acid and oxalic acid. Use of D-[1-14C]-, -[3-14C]-, or -[6-14C]Glc and D-[5-3H]-, -[2-14C,5-3H]-, or -[UL-14C]Ara provide additional information on erythroascorbic acid biosynthesis and cleavage. The latter process resembles that obtained by peroxygenation of erythroascorbic acid in alkaline solution. An unknown erythroascorbic acid-like compound also occurs in both Glc- and Ara-based cultures.     

Effect of maternally acquired Aujeszky's disease (pseudorabies) virus-specific antibody in pigs on establishment of latency and seroconversion to differential glycoproteins after low dose challenge

This study investigated whether (1) passively immune pigs could become latently infected after challenge with low doses of wild type pseudorabies virus (PRV) and (2) if seroconversion to PRV could be consistently detected using two commercially available differential diagnostic ELISAs. Three litters of piglets with passively acquired PRV serum neutralizing (SN) antibody (geometric mean titers 47.03 to 95.10) were challenged at 6 to 12 days of age with 236 to 500 TCID50 of Shope strain virus; pigs were vaccinated at 11 weeks of age with a commercially available genetically engineered vaccine (TK- gE- gG- Iowa S62 strain PRV). Vaccination was intended to reduce the risk of reactivation of latent infection resulting in spread of virulent PRV infection to previously uninfected pigs during the experiment. Vaccination at this age also approximated common field practices in infected herds. After 15 weeks, all challenged pigs were seropositive on the PRV glycoprotein (g or gp) E differential ELISA but were seronegative on the gG differential ELISA. All three challenge groups had pigs that were latently infected as evidenced by the detection of PRV DNA by polymerase chain reaction (PCR) assay of their trigeminal ganglia (TG). There was a significant inverse relationship observed for age at challenge and the proportion of PCR positive pigs in the group 15 weeks postchallenge (p = 0.0004). This trend was independent of the passively acquired PRV SN antibody titers at challenge. In this study, passively acquired antibody did not provide protection against establishment of latent infection in piglets after exposure to low doses of virulent PRV. These latent infections were detected serologically by only one of two available differential diagnostic ELISA.     

靶向型药物载体在抗肿瘤治疗中的研究进展

恶性肿瘤是一种严重威胁人类健康的常见病和多发病,是引起死亡的主要原因之一。近年来,抗肿瘤药物的靶向性研究越来越受到人们的重视。发展抗肿瘤药物的新型靶向载体,增加药物靶向性,提高生物利用度,降低毒副作用,是目前备受关注的课题。根据近年来文献,综述了一些新型的抗肿瘤药物载体,包括靶向的脂质体载药系统、纳米粒载药系统、微粒载药系统、胶束载药系统等,并分别总结了其颗粒大小、载药类型、载药模式及治疗效果等,为肿瘤的靶向给药研究提供思路。     

常用V型组合杆密封液压缸压盖螺钉断裂原因的分析

分析了常用V型组合杆密封液压缸压盖螺钉断裂的各种原因,提醒液压缸设计师注意完善设计细节、制造者应提高产品质量监控意识,液压缸用户应提供较为完善的订货工况描述.     

四苯基卟啉铟纳米材料的制备及其光学传感性能研究

在水/二甲基亚砜(DMSO)的混合溶液体系中,利用自组装方法,使5,10,15,20-四苯基卟啉铟(InTPP)分子聚集成纳米材料,并研究了其最优制备温度为50℃。通过场发射扫描电子显微镜(FE-SEM)对铟卟啉纳米材料的表面形貌进行了研究,可获得粒径为100～200nm的棒状铟卟啉纳米材料。利用紫外-可见光谱分析了铟卟啉单体与纳米材料光学性质的差别:在紫外-可见光谱中,铟卟啉纳米分散体系的Soret带吸收峰从原来的423nm分别红移到433和453nm,吸光值明显减小,峰形呈劈裂状且明显变宽。利用紫外-可见光谱对铟卟啉的光学检测性能进行了研究,将铟卟啉单体和纳米溶液体系对低浓度甲基膦酸二甲酯(DMMP)的检测效果进行了对比,结果显示铟卟啉纳米溶液体系的检测效果明显优于单体。