Anti-inflammatory,analgesic, antipyretic and related properties of meloxicam,a new non-steroidal anti-inflammatory agent with favourable gastrointestinal tolerance

The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs.With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenaninduced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration.Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain.In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeastinduced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid.Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm.Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam.The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.     

从脾论治磺脲类降糖药继发性失效

对 64例 2型糖尿病继发磺脲类降糖药失效患者 ,在继续口服磺脲类药的基础上加用健脾中药 ,结果显效 1 5例 ,有效 3 6例 ,无效 1 3例 ,总有效率 85 .2 4% ;治疗前后血糖明显下降 ,有显著性差异 ( P<0 .0 0 1 )     

芪月降脂片中黄芪甲苷的含量测定

[目的 ]研究芪月降脂片中黄芪甲苷的含量测定方法 .[方法 ]用甲醇提取、水饱和正丁醇萃取、大孔吸附树脂处理供试品后 ,以双波长薄层扫描法测定黄芪甲苷的含量 .[结果 ]黄芪甲苷的平均回收率为 10 4 18% ,RSD为 3 2 5% .[结论 ]双波长薄层扫描法较为简便、经济且重现性较好 ,可用于制剂中黄芪甲苷的质量控制     

临床医师处方抗菌药物前需思考的几个问题

2001年和2003年卫生部全国医院感染监测网调查结果均显示,医院横断面抗菌药物的平均使用率在54%以上,联合用药较为普遍.国内监测结果也表明细菌耐药性日益严重.针对上述问题,提出临床医师在面对病人开处方抗菌药物之前,须思考的问题:是否有使用抗菌药物的适用症?是否了解选用的抗菌药物,选用何种药物?是否有联合使用抗菌药物的指征?采用何种给药途径、给药剂量、给药时间?是否属于特殊宿主或针对特殊病原体的感染使用抗菌药物?密切观察抗菌药物治疗是否有效?针对局部感染是否需要穿刺或外科手术引流病灶?是否已出现抗菌药物的不良反应?是否存在药物相互作用?是否存在不合理使用抗菌药物情况?并且针对每个问题提出了建议.     

高效液相色谱法测定骨宁片中淫羊藿苷的含量

[目的 ]用高效液相色谱法测定骨宁片中淫羊藿苷的含量 .[方法 ]采用ZoobaxC18(4 6mm×2 5 0 0mm)色谱柱 ,乙腈 水 (体积比为 30∶70 )为流动相 ,检测波长为 2 70nm ,柱温为 4 0℃ ,流速为 1 0mL/min .[结果 ]线性范围为 0 0 80 4～ 0 4 82 4 μg ,线性关系良好 ,回归方程为Y =6 6 75 3 3X +110 2 7,相关系数为r =0 9999,平均回收率为 99 0 % ,RSD为 1 0 % .[结论 ]高效液相色谱法适合于测定骨宁片中淫羊藿苷的含量     

Luminal transport step of para-aminohippurate (PAH): transport from PAH-loaded proximal tubular cells into the tubular lumen of the rat kidney in vivo

 Proximal tubular cells were loaded for 10 s with [³H]para-aminohippurate ([³H]PAH) by microperfusing the peritubular capillaries with Ringer solution containing 0.05 mmol/l PAH. Immediately thereafter [³H]PAH influx from cells into a column of equilibrium solution injected into the oil-filled tubular lumen was measured by re-aspirating the fluid after 1–10 s of contact time. The rise of luminal PAH concentration within 2 s of contact time was almost linear, reaching a luminal / capillary concentation ratio of 1.6 after 2 s and of 3.2 after 5 s. The 2-s PAH concentration ratio was not changed when different manoeuvres were applied to depolarize proximal tubular cells. Also, the 2-s PAH concentration ratio was not influenced by varying the luminal pH from 6.0 to 8.0 or the luminal Cl^–concentration from zero to 134 mmol/l or when either 5 mmol/l urate or 25 mmol/l lactate was in the luminal perfusate. A decrease in the 2-s PAH concentration ratio, i.e. trans-inhibition, was observed when 25 or 50 mmol/l HCO₃ ^–(–50%) was in the luminal perfusate. Trans-inhibition was also seen with 5 mmol/l of the following substituted benzoates: 2-hydroxy-benzoate (–58%), 2-methoxy-benzoate (–46%), 2-hydroxy-benzoate-acetyl ester (–36%), 2-hydroxy-3,5-dinitro-benzoate (–48%), 3,5-dichloro-benzoate (–49%), and 2,3,5-trichloro-benzoate (–45%). No effect was seen with benzoate, 3-hydroxy-benzoate, 2-chloro-benzoate, 2-nitro-benzoate, 2,5-dinitro-benzoate, 3-sulfamoyl-benzoate and 4-sulfamoyl-benzoate. However, analogues of the latter two compounds possessing two additional side groups, such as furosemide and piretanide, or a hydrophobic moiety, such as probenecid, were inhibitory (by –62, –41 and –49% respectively). Phenoxyacetate had no effect; however, it inhibited if in addition it had three chloro groups, as in 2,4,5-trichlorophenoxyacetate (–71%) or a hydrophobic carbamoyl side group, as in mersalylic acid (salyrgan, –75%). Benzene-sulfonate trans-inhibited (–33%), as did phenolsulfonphthalein (phenol red, –39%) and sulfofluorescein (–55%). However, the trans-inhibitory effect of the corresponding carboxy-compounds was absent (phenolphthalein) or weaker (fluorescein, –42%). The trans-inhibitory effect of the uricosurics ethacrynic acid (–53%), tienilic acid (–55%) indacrinone (–72%) and benzbromarone (–42%) could be attributed to two chloro or bromo side groups on the benzene ring. Other trans-inhibiting uricosuric substances were indomethacin (–42%), sulfinpyrazone (–38%), losartan (–80%) its metabolite EXP 3174 (–55%), and AA 193 (–65%). These organic acids, with pKa values between 2.8 and 4.9, possess chloro and sulfin groups, as well as heterocyclic 5-ring and hydrophobic ring or chain areas. No significant effect was seen with 5 mmol/l PAH, 2-oxo-glutarate, DIDS, cGMP, prostaglandin E₂, cortisol, benzylamiloride, pyrazinoic acid and 25 mmol/l lactate. Our data indicate that in situ the secretory luminal PAH transport proceeds in a non-rheogenic fashion, per exclusionem by anion exchange. The observed trans-inhibition of PAH secretion seems to correlate with the affinity for the luminal PAH transporter and, for uricosuric substances, with their uricosuric potency. Received: 15 October 1996 / Received after revision: 17 December 1996 / Accepted: 18 December 1996     

Sensitivity of effect variables in rheumatoid arthritis: A meta-analysis of 130 placebo controlled NSAID trials controlled NSAID trials

In a meta-analysis of placebo controlled NSAID trials, the sensitivity of the effect variables was calculated as the correlation coefficient and as the difference between drug and placebo, divided by the placebo group standard deviation. The patient's global evaluation was the most sensitive variable overall. Pain was more sensitive than Ritchie's index. Several variables may be omitted from clinical trials, especially if two active drugs are being compared. For example, the best maximum estimate for the difference in ESR between NSAADs and placebo was 1.0 mm/hr (95% confidence interval −1.5 to 3.4 mm/hr), and for joint size 0.44% (−1.0 to 1.9%), corresponding to a quarter of a millimeter for each of the 10 joints usually measured. It is suggested to record only the patient's global evaluation, pain, and morning stiffness.     

化疗药物外渗后局部组织损伤处理的实验研究

目的根据化疗药物外渗后局部组织损伤的特点寻找理想的处理方法。方法制作化疗药物外渗的动物坏死模型,分别采用临床常用的三种处理方法进行动物实验,进行肉眼观察及组织学观察。结果1∶5 000呋喃西林加季德胜蛇药外敷对化疗药物外渗所致的局部组织坏死疗效最佳,其次为复方利多卡因,50%硫酸镁外敷疗效甚微,对照组无效。结论临床处理化疗药物外渗应根据其局部特点选择合理有效的方法。