吡罗昔康-β-环糊精包合物的研制

目的：研究制备吡罗昔康β环糊精包合物的方法。方法：采用饱和水溶液法制备吡罗昔康β环糊精包合物，并用Ｘ射线衍射进行鉴定。同时考察了其体外溶出性能。结果：吡罗昔康β环糊精包合物主客分子比为１∶１。吡罗昔康平均含量为（２２．３２±０．３１）％，平均收率（８０．６７±０．５８）％体外溶出时１５ｍｉｎ达８６．４％，为普通片剂的２．６倍。结论：制成包合物后，显著提高了吡罗昔康的溶出度。     

吡罗昔康搽剂治疗关节炎的临床研究

目的：探讨吡罗昔康搽剂与嘴罗普康片剂和消失痛搽剂的疗效对比情况，方法：采用随机对照方法，应用１％嘴罗昔康搽剂治疗３４例类风湿性关节炎，骨关节炎患者，疗程４周，并与１７例应用吡罗昔康片剂治疗，１７例应用消炎痛搽剂治疗的患者作比较，结果：吡罗昔康搽剂组的显效率为２９．４％，总有效率为８８．２％，片剂组分别为５．９％，８８．２％，消炎痛搽剂组分别为１１．８％，８２．４％，三组疗效差异无显著统计学意义，吡     

黄腐酸钠抗炎作用的初步研究

观察黄腐酸钠（ＳｏｄｉｕｍＦｕｌｖｉｃ，ＳＦ）对不同炎症模型的作用。结果表明，ＳＦ（０．５％，１％、２％）外用能明显抑制巴豆油所致的小鼠鼠耳肿胀，显著减轻角叉菜胶所致的大鼠足跖肿胀程度，对小鼠琼脂肉芽肿也有明显的抑制作用，以上结果表明ＳＦ具有抗炎作用，并经实验证明对皮肤不引起过敏反应。     

吡罗昔康致皮疹一例

吡罗昔康致皮疹一例吴强吡罗昔康为新的非甾体消炎镇痛药，其消炎作用略强于消炎痛，已广泛用于风湿及类风湿性关节炎等疾病的治疗，临床效果好，副作用较少。笔者曾遇见１例吡罗昔康致周身皮疹，现报道如下。患者，女性，４２岁，因双膝关节肿胀、疼痛半个月于１９９４年...     

吡罗昔康及其贴剂的体外经皮渗透性的研究

本文对吡罗昔康经由离体裸鼠皮肤的渗透性进行了测定，结果表明吡罗昔康的累积渗透量与时间存在线性关系（Ｑ＝２．２１１ｔ－１．２９，ｒ＝０．９９８），吡罗昔康在磷酸盐缓冲液（ｐＨ７．４）中经由离体裸鼠皮肤的渗透系数为７１９×１０－ｃｍ／ｓ，扩散系数为４．１６×１０－７ｃｍ２／ｓ，滞后时间为０．７２ｈ；本文另以小白鼠皮肤为渗透屏障研究了吡罗昔康贴剂的体外经皮渗透性，考察了具体外的释放行为，结果表明该贴剂体外经皮渗透为零级过程，体外释放为ｔ１／２级过程，该贴剂为皮控型局部用经皮吸收制剂。     

妇异通冲剂对实验性大鼠肿胀炎症的影响

探讨不同剂量的妇异通冲剂对因琼脂所致大鼠肿胀及大鼠棉球肉芽组织增生的影响；方法：给大鼠灌肠不同药物，每日一次，连续５天，于第５天灌药后３０分钟给大鼠右后肢足趾皮下注射１％琼脂溶液０．０５ｍｌ，致炎后１、３、５、２４小时测量足在节的周长变化，以左侧足对照。左右周长之差为肿胀炎症程度。     

新生儿黄疸

新生儿黄疸上海医科大学儿科医院（２０００３２）樊绍曾新生儿期黄疸相当常见，在我国汉族约９０％新生儿在生后１周内均出现黄疸，其中大部分并非病理性而是由于新生儿胆红素代谢特点所致的生理性黄疸。在诊断新生儿黄疸时要考虑下述各点。１黄疸足生理性还是病理性按公...     

吡罗昔康β-环糊精包合物的胃刺激性及生物利用度

本实验研究了吡罗昔康β-环糊精包合物对大鼠胃的刺激性,及其吡罗昔康β-环糊精包合物的胶囊的体外溶出速度和生物利用度。结果表明:吡罗昔康制成β-环糊精包合物后,刺激性远较吡罗昔康原料小。8名志愿者口服吡罗昔康β-环糊精包合物胶囊和吡罗昔康普通片后,用HPLC法测定血药浓度,经一室模型拟合,胺囊的AUC为片剂的110％,而吸收半衰期T_(1/2)(K_α)和达峰时T_m均小于片剂,这和体外溶出实验的结果,胶囊溶出速度显著大于片剂是相平行的。     

酒石酸锗复合物的抗炎作用及作用机理

灌胃酒石酸锗复合物２０ｍｇ·ｋｇ－１，明显地抑制二甲苯或巴豆油所致小鼠耳壳肿胀，抑制角叉菜所致大鼠足肿胀，抑制小鼠棉球肉芽肿增生及佛氏完全佐剂所致大鼠关节炎．这表明，酒石酸锗夏合物具有抑制急、慢性及免疫性炎症的作用，还降低小鼠毛细血管通透性，增强小鼠单核巨噬细胞系统的吞噬功能，抑制大鼠热烫足肿胀，减少大鼠炎症部位的ＰＣＥ２含量．提示，酒石酸锗复合物的抗炎作用与降低毛细血管通透性，增强单核巨噬细胞的吞噬功能和抑制炎症部位的激肽类、ＰＧＥ２的合成、释放有关．     

早期应用肌力平衡手术治疗婴幼儿期先天性马蹄内翻足疗效观察

目的；探讨婴和期先天性马蹄内翻足，早期肌力平衡手术疗效方法：自１９８７年以来对５个月￣３周岁的婴幼儿应用跟腱延长，胫前肌转移为主的肌力平衡手术治疗５９例；７２足。结果：经随访按陆裕朴标准，优为７３．１％，良为１７．３％，可为９．６％，优良率占９０．４％，其中５个月￣１周岁以内的病例，优良率为９３．８％，结论：婴幼儿期，尤其是１周岁以内的先天性马蹄内翻足，应用以肌力平衡为主的手术方法，可获得显著的临     

吡罗昔康贴片在大鼠体内的药代动力学研究

通过研究吡罗昔康在大鼠体内的药代动力学过程及其分布特点,探索其经皮给药系统的药物转运特性。方法高效液相色谱法(HPLC)测定吡罗昔康经皮给药后不同时间点大鼠血浆、关节中吡罗昔康的浓度;大鼠右肩部应用2、4、6mg吡罗昔康贴片后,用DAS软件处理时间-血药浓度数据,计算药代动力学参数。结果大鼠局部给药4mg后2、4、8h,关节中吡罗昔康质量分数分别为:(119±26)、(1 538±358)、(1 349±320)ng.g-1,血浆中吡罗昔康质量浓度分别为:(427±82)、(2 015±184)、(1 317±224)μg.L-1,它们的比值介于0.28和1.02之间;在2～6mg剂量范围内,大鼠局部应用吡罗昔康贴片,血浆中吡罗昔康质量浓度4h达峰值,药峰质量浓度(Cmax)分别为:(925±118)、(1 980±135)、(2 644±337)μg.L-1,药时曲线下面积(AUC0-∞)分别为:(29 976±10 845)、(63 871±58 534)、(85 389±15 352)μg.L-1.h-1,Cmax、AUC0-∞随剂量的增高成比例增大。结论吡罗昔康经皮给药后,可直接从用药部位渗透至局部深层的关节组织中并达到较高的质量浓度;在2～6mg内,吡罗昔康贴片于大鼠体内呈线性动力学特征。     

The effect of piroxicam in preventing surgically induced miosis.

The effect of an antiprostaglandin, piroxicam, in preventing surgically induced miosis is studied. Patients undergoing extracapsular cataract surgery were randomly divided into the piroxicam and placebo groups. Intra-operative measurements of the pupillary diameters were performed. The stages of procedure at which they were measured were at the beginning of operation (Stage 1), after anterior capsulotomy (Stage 2), after lens nucleus delivery (Stage 3) and at the end of irrigation and aspiration (Stage 4). It is noted in this Study that the pupillary diameters were larger at stages 2,3 and 4 in the piroxicam group. The increase in the mean pupillary areas of the piroxicam group were statistically significant for Stages 3 and 4.     

炎痛喜康贴剂制备及体外透皮吸收研究

研究了炎痛喜康贴剂的制备及其透皮吸收过程。透皮装置采用改进型Ｆｒａｎｚ扩散池。炎痛喜康能从贴剂中缓慢释放，在扩散介质中维持２４ｈ的恒定释药浓度。其平均透皮速率及平均透皮百分率分别与贴剂的处方配比、促渗剂含量、表面粘性、皮肤状况、工艺差异有关，而与贴剂的剥离粘性、含量差异无规律性联系。     

吡罗昔康提高γδT细胞杀伤胃癌细胞作用的机制研究

目的探讨吡罗昔康提高γδT细胞杀伤胃癌细胞作用的机制。方法按常规方法培养γδT细胞;在培养第9天的γδT细胞中加入不同浓度吡罗昔康（分别为0.01、0.02、0.04、0.08、0.16 mmol/L）诱导,24 h后收集培养上清液用于细胞因子γ干扰素（IFN-γ）、肿瘤坏死因子α（TNF-α）、白细胞介素12（IL-12）检测,沉淀细胞用流式细胞术测定穿孔素、粒酶B和NKG2D及用LDH法检测γδT细胞杀伤胃癌细胞活性。结果吡罗昔康浓度为0.04 mmol/L时诱导的γδT细胞穿孔素和粒酶B分别为78.7%和71.8%,明显高于对照组（分别为51.4%和60.9%）。吡罗昔康能显著抑制γδT细胞NKG2D的表达,并随着药物浓度的增加作用越明显。γδT细胞经吡罗昔康诱导24 h后,培养上清液中IFN-γ和IL-12浓度与对照组比较没有明显变化;但能抑制TNF-α的分泌,并且随着药物浓度的增加抑制作用越明显。γδT细胞杀伤胃癌细胞BCG-823的活性在0.04 mmol/L时最高（75%）,明显高于对照组（58%）。结论经吡罗昔康诱导后γδT细胞杀伤BCG-823活性明显增高的机制可能与γδT细胞表达较高浓度的穿孔素和粒酶B有关。     

P(AA-co-PEGLA)凝胶对吡罗昔康的控释作用

将两亲性大单体聚氧乙烯月桂醇醚丙烯酸酯（PEGLA）与丙烯酸（AA）通过UV引发聚合,制备了水凝胶P(AA-co-PEGLA)。以水难溶性吡罗昔康为模型药物,研究了凝胶中PEGLA含量对载药量的影响。结果表明：吡罗昔康的载药量随着PEGLA含量的增加而提高,当凝胶中的PEGLA的摩尔分数(x)从0增加到60%时,载药量从1.24 mg/g提高到17.36 mg/g。吡罗昔康体外释放研究表明：P(AA-co-PEGLA)凝胶可保护药物不被胃酸等破坏,而在肠中释放。药物的释放速率随着凝胶中PEGLA含量的增加而降低,表现出明显的缓释作用。用Weibull方程拟合释放曲线,指数因子(b)0.88~0.97,表明对吡罗昔康释放的控制是扩散和高分子链松弛协同作用的结果。     

Comparative efficacy and tolerability of nimesulide and piroxicam in osteoarthritis with specific reference to chondroprotection: a double blind randomised study

The aim of the study was to assess the efficacy, tolerability and chondroprotection afforded by nimesulide, a selective cyclooxygenase-2 inhibitor and piroxicam in a randomised, double blind, controlled clinical trial in 90 patients suffering from osteoarthritis of the knee joint. A significant improvement in the osteoarthritis severity index at 2 weeks (p < 0.01) and an improvement in physicians assessment of global arthritic condition at 4 weeks (p < 0.01) was seen with both the treatments. A significant decrease in articular index of joint tenderness (p < 0.05) at 8 weeks and in self assessment of handicap at 4 weeks (p < 0.05), in comparison to baseline, was observed only in patients receiving nimesulide. Rescue therapy was required by a greater percentage of patients being administered piroxicam. Functional capacity improved in 64% of the patients on nimesulide and 74.5% of the patients receiving piroxicam. Adverse effects were observed in 6 patients on nimesulide and 9 patients receiving piroxicam. No significant difference was found in any of the efficacy and tolerability parameters between the two treatment groups. Magnetic resonance imaging evaluation of the knee joint of 10 patients showed no significant change in the articular cartilage and associated joint structures after 6 months of therapy with both the treatments. The results show that nimesulide and piroxicam are comparable in efficacy and tolerability in patients suffering from osteoarthritis.     

吡罗昔康鼻粘膜吸收

目的 :研究吡罗昔康包合物混悬液的鼻粘膜吸收。方法 :将吡罗昔康包合 ,增加其在水中的溶解度 ,降低它对粘膜的刺激性 ,以大鼠在体鼻循环法为实验模型 ,考察循环液中不同吡罗昔康浓度对鼻粘膜吸收量的影响。结果 :循环液流速确定时 ,吡罗昔康通过鼻粘膜的吸收量随所考察的浓度的增大而有所增加 ;实验完毕后剖开大鼠鼻腔 ,发现鼻粘膜上粘附许多混悬液中的微粒。结论 :通过实验吡罗昔康可以通过鼻粘膜吸收 ;未见其包合物混悬液对鼻粘膜有明显刺激性。     

吡罗昔康对人γδT细胞和消化系统肿瘤细胞的作用比较

目的:探讨吡罗昔康对人γδT细胞杀伤消化系统肿瘤细胞株的影响。方法:用异戊烯焦磷酸法体外扩增人外周血γδT细胞。用不同浓度的吡罗昔康诱导γδT细胞和消化系统肿瘤SGC-7901、SW-1990、SW-480、SW-1116、LOVO细胞株,用MTT法检测吡罗昔康对这些细胞的抑制率和用乳酸脱氢酶法测定γδT细胞的杀伤活性,用流式细胞术检测诱导前后的γδT细胞和SGC-7901、SW-1990、SW-480、SW-1116和LOVO细胞凋亡百分率。结果:γδT细胞培养10d时从扩增前4.21%增加到70.35%。吡罗昔康各种浓度对SGC-7901、SW-1990、SW-480、SW-1116和LOVO细胞株抑制率明显高于γδT细胞。0.01~0.04mmol/L吡罗昔康诱导24h后的γδT细胞对5种肿瘤细胞的杀伤活性最高,浓度超过0.04mmol/L时杀伤活性呈下降趋势;SGC-7901、SW-1990、SW-480、SW-1116和LOVO细胞经不同浓度的吡罗昔康诱导24h后γδT细胞对其的杀伤活性与对照组比较无明显变化。0.16mmol/L吡罗昔康诱导24h对SGC-7901、SW-1990、SW-480、SW-1116和LOVO细胞株的凋亡率分别为12.26%、13.46%、14.59%、25.64%和39.36%,显著高于γδT细胞(8.16%)。结论:吡罗昔康在临床常规使用的药物浓度时可增强γδT细胞杀伤肿瘤细胞作用,超过这一浓度可明显抑制γδT细胞和肿瘤细胞的增殖能力和杀伤活性及增加细胞的凋亡率;吡罗昔康对肿瘤细胞株的抑制率明显高于γδT细胞。这一结果为临床吡罗昔康预防消化道肿瘤的用量提供了实验依据。     

A comparison of the effect of intramuscular diclofenac, ketorolac or piroxicam on postoperative pain following laparoscopy.

Sixty patients presenting for in-patient gynaecological laparoscopic surgery were randomly allocated to receive either diclofenac 75 mg (n = 20), ketorolac 30 mg (n = 20) or piroxicam 20 mg (n = 20) as an intra-muscular injection immediately after induction of anaesthesia. Postoperative visual analogue scores over the first 24 hours, using a 10 cm scale, ranged from 3.2-0.5 in the diclofenac group, 2.7-0.85 in the ketorolac group and 2.8-0.5 in the piroxicam group. The scores did not differ significantly between the three groups (p > 0.05). Mean time (SD) to first analgesia was 27(94) minutes in the piroxicam group, 16 (30) minutes in the diclofenac group and 62 (120) minutes in the piroxicam group. Six out of twenty patients in the diclofenac group required further analgesia compared to nine out of twenty in the other two drug groups. This difference was not significant. There were no reports of increased bleeding, bronchoconstriction, bleeding from the upper gastrointestinal tract, renal impairment or pain from the intra-muscular injection site in any of the groups. The administration of a non-steroidal anti-inflammatory drug to patients presenting for laparoscopic surgery reduces postoperative pain. There were no obvious differences between the agents used.     

Synthesis and electrochemical properties of environmental free l-glutathione grafted graphene oxide/ZnO nanocomposite for highly selective piroxicam sensing

A simple and reliable strategy was proposed to engineer the glutathione grafted graphene oxide/ZnO nanocomposite (glutathione-GO/ZnO) as electrode material for the high-performance piroxicam sensor. The prepared glutathione-GO/ZnO nanocomposite was well characterized by X-ray diffraction (XRD), Fourier transform infrared spectrum (FTIR), X-ray photoelectron spectroscopy (XPS), field emission scanning electron microscopy (FE-SEM), cyclic voltammetry (CV), electrochemical impedance spectroscopy (EIS) and differential pulse voltammetry (DPV). The novel nanocomposite modified electrode showed the highest electrocatalytic activity towards piroxicam (oxidation potential is 0.52 V). Under controlled experimental parameters, the proposed sensor exhibited good linear responses to piroxicam concentrations ranging from 0.1 to 500 μM. The detection limit and sensitivity were calculated as 1.8 nM and 0.2 μA/μM·cm², respectively. Moreover, it offered excellent selectivity, reproducibility, and long-term stability and can effectively ignore the interfering candidates commonly existing in the pharmaceutical tablets and human fluids even at a higher concentration. Finally, the reported sensor was successfully employed to the direct determination of piroxicam in practical samples.