二苯恶丙酸的抗炎作用及其机理

以多种炎症模型观察了二苯恶丙酸的抗炎作用。给动物灌服二苯恶丙酸，能抑制角叉菜胶致足跖肿胀和棉球致肉芽组织增生，对大鼠佐剂性关节炎也有明显的抑制作用。该药的抗炎作用强度与阿司匹林相似，但作用时间明显延长。探讨其作用机理表明，二苯恶丙酸能降低毛细血管通透性，抑制白细胞游走反应，但对血浆皮质醇的含量无明显影响。     

家蚕细胞基因工程人α—干扰素注射液抗I型单纯疱疹病毒作用

本文报导家蚕细胞基因工程人α－干扰素注射液具有明显抗ＨＳＶ－１的作用，在Ｖｅｒｏ细胞上，其有一定的细胞毒性，但随浓度降低而毒性减少，它能明显抑制ＨＳＶ－１致细胞病变，对ＨＳＶ－１的抑制指数为３．５－４．５，能有效地抑制ＨＳＶ－１在细胞内复制。在体实验表明该药对ＨＳＶ－１致小鼠脑炎，家兔角膜炎，豚鼠皮肤疱疹有明显治疗作用。     

胆乐胶囊的抗炎与镇痛作用研究

目的：研究胆乐胶囊的抗炎与镇痛作用。方法：采用蛋清致大鼠足跖肿胀，二甲苯致小鼠耳肿胀，醋酸致小鼠毛细血管通透性增加和扭体进行抗炎镇痛作用研究。结果：胆乐胶囊能明显抑制蛋清致大鼠足跖肿胀和二甲苯致小鼠耳肿胀，并能明显抑制醋酸致小鼠毛细血管通透性增加和扭体数。结论：胆乐胶囊具有较好的抗炎与镇痛作用。     

刺茎楤木根皮抗炎和免疫作用的研究

目的探讨刺茎楤木根皮的抗炎和免疫作用。方法抗炎实验采用巴豆油致小鼠耳廓肿胀等常规抗炎模型;免疫实验采用对小鼠体内碳粒廓清功能影响等的方法。结果刺茎楤木根皮提取物可明显抑制巴豆油致小鼠耳廊肿胀及角叉菜胶引起的大鼠足跖肿胀,能明显抑制大鼠棉球肉芽肿的增重及2,4二硝基氯苯(DNCB)致小鼠迟发型超敏反应(DTH),增强吞噬功能。结论刺茎楤木根皮有明显的抗炎和免疫调节作用。     

刺茎楤木根皮抗炎和免疫作用的研究

目的探讨刺茎楤木根皮的抗炎和免疫作用。方法抗炎实验采用巴豆油致小鼠耳廓肿胀等常规抗炎模型;免疫实验采用对小鼠体内碳粒廓清功能影响等的方法。结果刺茎楤木根皮提取物可明显抑制巴豆油致小鼠耳廊肿胀及角叉菜胶引起的大鼠足跖肿胀,能明显抑制大鼠棉球肉芽肿的增重及2,4二硝基氯苯(DNCB)致小鼠迟发型超敏反应(DTH),增强吞噬功能。结论刺茎楤木根皮有明显的抗炎和免疫调节作用。     

骨刺宁主要药效学研究

研究了骨刺宁的镇痛、抗炎、消肿和对微循环的影响。结果表明，该药对甲醛致小鼠痛反应有明显抑制，对小鼠热板前阈值显著提高；能明显抑制大、小鼠棉球肉芽肿和小鼠二甲本耳肿胀；使小鼠耳廓微静脉管径增粗、毛细血管开放数明显增加。     

头顶一棵珠抗炎和免疫作用的实验研究

目的探讨头顶一棵珠的抗炎和免疫作用.方法抗炎实验采用巴豆油致小鼠耳廓肿胀等常规抗炎模型;免疫实验采用对小鼠体内碳粒廓清功能影响等的方法.结果头顶一颗珠提取物可明显抑制巴豆油致小鼠耳廊肿胀及角叉菜胶引起的大鼠足跖肿胀,能显著抑制大鼠棉球肉芽肿的增重及2.4-二硝基氯苯致小鼠迟发型超敏反应,明显增加免疫器官重量及指数,增强吞噬功能.结论头顶一颗珠有明显的抗炎和免疫调节作用.     

云芝胞内多糖对特异性免疫功能的影响及其与免疫抑制剂合用时的免疫药理效果研究

25～50mg/kg/日的云芝胞内多糖(IPPV)对2,4-二硝基氯苯及绵羊红细胞所致小鼠迟发型超敏反应无明显影响,但可促进绵羊红细胞所致615小鼠血清溶血素抗体形成。当合并用药时,IPPV对环磷酰胺等多种免疫抑制剂所致小鼠特异性细胞免疫、体液免疫及网状内皮系统吞噬功能抑制有不同程度的拮抗作用,能使被抑制的免疫功能有所改善、恢复正常或高于正常,但IPPV对环磷酰胺、5-氟脲嘧啶的抑瘤效果却无拮抗作用。     

喻蟆油及其提取笺对肾虚和正常小鼠的抗疲劳作用

哈蟆油能抑制氢化可的松致肾虚小白鼠的体温下降及体重减轻，而对正常小白鼠体重无影响能，能延长肾虚小鼠的滚棒及游泳时间，常压耐缺氧的存活时间略有延长，以哈蟆油的作用最明显，石油醚提取物次之，甲醇提取物作用不明显。     

皮痒宁抗炎、抑菌、止痒药理研究

目的;研究皮痒宁的药理作用．方法：用巴豆油诱发小鼠耳部急性炎性水肿上,２,４－二硝基氯苯致小鼠Ⅳ（迟发）型超敏反应（ＤＴＨＲ）、磷酸组胺致痒耐受试验和体外抑菌试验等实验方法,观察皮痒宁与药效学相关的药理作用。结果：皮痒宁能明显抑制小鼠耳部急性炎症水肿（Ｐ ＜ ０．０１）;能明显提高豚鼠对组胺的致痒阈（Ｐ ＜ ０． ０１）;大剂量组的皮痒宁还有明显抑制小鼠 ＤＴＨＲ的作用（Ｐ＜０．０１）：抑菌作用明显． 上述作用呈正变的量效关系．结论：皮痒宁具有抗炎止痒、抑菌和桔抗ＤＴＨＲ等药理作用     

雷醇内酯的抗炎作用

雷醇内酯（Ｔ９）能抑制角叉菜胶、巴豆油和Ｆｒｅｕｎｄ完全佐剂引起的炎性水肿。减少急性胸膜炎渗液量．抑制白细胞游走和棉球肉芽增生。可降低血浆中ＰＧＥ２含量．对肾上腺重量及肾上腺ＶｉｔＣ含量无影响。其抗炎作用的治疗指数为９．８６。结果与雷公藤其它抗炎免疫活性成分的结果相似，证明其为有效成分之一。Ｐ＜０．０１２．３对佐剂致大鼠原发性关节肿胀的影响［６］大鼠随机分为４组，每组８只。分别ｉｐＴ９１．０、０．５ｍｇ·ｋｇ－１，强的松龙１０ｍｇ·ｋｇ－１及等量生理盐水。给药后０．５ｈ，大鼠有足跖ｓｃＦｒｅｕｎｄ完全佐剂０．１ｍｌ致炎，测量致炎前及致炎后１８ｈ的关节周长（ｃｍ），以周长差作为肿胀度指标。结果显示，Ｔ９１．０、０．５ｍｇ·ｋｇ－１均能明显抑制大鼠佐剂性关节肿胀，有量效关系（表３）。表１Ｔ９对角叉菜致大鼠关节肿胀的影响与对照组比较．＊Ｐ＜０．０５．Ｐ＜０．０１表３Ｔ９对大鼠１８ｈ佐剂关节肿胀的影响与对照组比较．＊Ｐ＜０．０５，Ｐ＜０．０１２．４对大鼠急性胸膜炎的影响［７］大鼠随机分为４组，分别ｉｐＴ９０．８、０．４ｍｇ·ｋｇ－１等量生理盐水及ｐｏ阿斯匹林３００ｍｇ·ｋｇ－１。ｉｐ后０．５ｈ或ｐｏ后１ｈ，在乙醚麻?     

奥沙普秦凝胶剂的体外渗透性及药效学

目的:研究奥沙普秦凝胶剂体外经皮渗透性及体外释药情况,观察其抗炎镇痛作用。方法:采用Franz扩散池,进行奥沙普秦凝胶剂体外渗透性和释放度实验。采用角叉菜胶致大鼠足肿胀、二甲苯致小鼠耳肿胀、大鼠棉球肉芽肿、醋酸扭体法和甲醛致痛法模型,观察奥沙普秦凝胶剂的抗炎、镇痛作用,同时考察了奥沙普秦凝胶剂皮肤用药的急性毒性、致敏性和刺激性。结果:奥沙普秦凝胶剂对角叉菜胶致大鼠足肿胀、二甲苯致小鼠耳肿胀和大鼠棉球肉芽肿均有明显的抑制作用,对醋酸、甲醛所致小鼠炎症性疼痛有明显抑制作用。急性毒性、致敏性和刺激性实验结果表明奥沙普秦凝胶剂皮肤用药无明显的毒性、致敏性及刺激性。结论:皮肤是奥沙普秦凝胶剂透皮吸收的主要屏障。奥沙普秦凝胶剂具有抗炎镇痛作用,无明显的不良反应。     

Anti-inflammatory activity of a non-steroidal anti-inflammatory agent, oxaprozin, in experimental models

Anti-inflammatory activity and mode of action of oxaprozin, a new non-steroidal anti-inflammatory agent, were investigated in experimental animal models and in vitro tests. Anti-inflammatory potency of oxaprozin was almost equal to that of aspirin in acetic acid vascular permeability, carrageenin hind paw edema, cotton pellet granuloma and adjuvant arthritis tests in rats. On the other hand, in mice, oxaprozin was more potent than aspirin, ibuprofen and phenylbutazone, and it was as potent as sulindac and fenbufen in acetic acid vascular permeability and carrageenin hind paw edema tests. In adrenalectomized rats, the anti-edema activity of oxaprozin in the carrageenin hind paw edema test was the same as that in intact rats. Oxaprozin inhibited erythema formation induced by ultra-violet rays in guinea pigs. The inhibitory potency of oxaprozin against prostaglandin E2 biosynthesis in vitro was equal to that of ibuprofen. Oxaprozin showed a concentration-dependent inhibition of heat-induced denaturation of bovine serum albumin and lysis of rabbit erythrocytes in vitro. However, oxaprozin did not inhibit rat hind paw edemas induced by dextran, formalin and serotonin. It was suggested from these results that the mode of action of oxaprozin is similar to those of other acidic non-steroidal anti-inflammatory drugs. Ulcerogenicity of oxaprozin was weaker than those of phenylbutazone and aspirin in rats. Species differences in the metabolic rate of oxaprozin were shown. The blood concentration of oxaprozin in rats is extremely low because the metabolic rate of oxaprozin is rapid in rats. Therefore, in rats, oxaprozin exhibited a weak anti-inflammatory effect. However, in mice, oxaprozin had a low metabolic rate, and the effect of oxaprozin was as potent as sulindac and fenbufen. The elimination half-life of oxaprozin is extended, 49 to 69 hr, in humans. It was suggested from these findings that oxaprozin is a potent and long acting anti-inflammatory drug in clinical use.     

奥沙普嗪对血小板聚集和血栓形成的影响

目的:研究奥沙普嗪对家兔和大鼠血小板聚集和血栓形成的影响.方法:麻醉动物颈动脉取血,制备富含血小板血浆(PRP),加入奥沙普嗪,用多功能血小板聚集仪测定二磷腺苷(ADP)诱导的血小板聚集作用.结果:奥沙普嗪能明显抑制ADP诱导动物体内外血小板聚集和降低胶原 肾上腺素静脉注射所致的小鼠死亡率.结论:初步证实奥沙普嗪具有类似阿司匹林抑制血小板聚集作用.     

Gastric irritation of oxaprozin, a new nonsteroidal, antiinflammatory drug, in comparison to acetylsalicylic acid and indomethacin: a gastric potential difference analysis

For the evaluation of gastric irritation of oxaprozin in comparison to indomethacin and acetylsalicylic acid, a study was carried out with eight healthy male volunteers, investigating doses of 600 and 1200 mg of oxaprozin compared to therapeutical equivalents of 50 mg indomethacin and 1000 mg acetylsalicylic acid. Gastric irritation was checked with the model of the transmural gastric potential difference. The model is based on the assumption that a change in electric tension caused by a lesion of the gastric mucosa, which leads to an increasing permeability of the cell membrane for electrolytes, is a sensitive parameter for cell disintegrity. The results of the study show that oxaprozin has less irritative potency than indomethacin and can thus be qualified as an antiinflammatory drug with a minimum of gastric irritation.     

牛黄消炎片的镇痛抗炎作用实验研究

用0.05g/ml和0.025g/ml12个剂量进行试验,均能明显抑制二甲苯引起的小鼠耳肿及角叉菜胶引起的大鼠足趾肿胀,对醋酸诱发的小鼠扭体反应也有明显的抑制作用,试验表明牛黄消炎片有明显的镇痛抗炎作用。     

Inhibitory effects of E-5110 on interleukin-1 generation from human monocytes

Effects of E-5110, a novel non-steroidal antiinflammatory drug, on interleukin-1 (IL-1) generation from human monocytes were studied in vitro. E-5110 reduced the amounts of extra- and intracellular IL-1 activity induced by lipopolysaccharide (LPS, 1 micrograms/ml) in a dose-dependent manner (1-10 microM). E-5110 also inhibited the IL-1 generation induced by antigen-antibody complexes, opsonized zymosan and silica particles. It was suggested that the inhibition of IL-1 generation by E-5110 was independent of the inhibitory effects on arachidonate cyclooxygenase and/or lipoxygenase because indomethacin, piroxicam, BW755C and AA861 had no effects on IL-1 generation. Hydrocortisone (IC50:0.084 microM), aurothioglucose (11.5 microM) and lobenzarit (75.0 microM), which are clinically effective antirheumatic drugs, also inhibited IL-1 generation, like E-5110 (1.21 microM). It is expected that E-5110 will be superior to classical non-steroidal antiinflammatory drugs in medical treatment of rheumatoid arthritis.     

促渗剂对奥沙普秦经皮渗透的促进作用

目的：考察几种促渗剂对奥沙普秦透皮作用的影响。方法：采取改良Franz直立式释放池,以离体小鼠皮肤为透皮屏障,计算含不同浓度和组合促透剂的奥沙普秦的累积渗透量Q及渗透速率K,结果;含不同促渗剂奥沙普秦的透皮速率有明显差别,其促进强度依次为油酸＞月桂氮Chuo酮＞薄荷脑;混合促渗剂的促渗效果均比单用时有不同程度的提高;丙二醇有明显的抑制作用,并且抑制油酸,月桂氮Chuo酮及薄荷脑的促渗作用。结论：奥沙普秦透皮吸收符合非极性通道释放的零级动力学方程,其中以10％油酸加1％月桂氮Chuo酮组成的混合促进剂作用最显著。     

尼美舒利对佐剂性关节炎大鼠的治疗作用研究

尼美舒利(Nime)0．6、30、15mg·kg^-1对佐剂性关节炎大鼠的原发性和继发性炎症反应均有明显的抑制作用，用药组继发性炎痘反应的全身症状也明显减轻，而Nime对佐剂性关节炎大鼠低下的脾细胞增殖反应和腹腔巨噬细胞产生过高的IL-1活性却无明显影响，提示Nime无明显的免疫作用，该结果表明，Nime对佐剂性关节炎大鼠有明显的治疗作用，这一作用可能与Nime有较强的抗炎作甩有关。     

Interaction of oxaprozin with acetaminophen,cimetidine, and ranitidine

Summary Twelve healthy male volunteers participated in a single-dose four-way crossover study to evaluate potential drug interactions with oxaprozin, a nonsteroidal antiinflammatory agent of the propionic class. The four modes of administration were:a. oxaprozin, 1200 mg alone;b. oxaprozin during concurrent acetaminophen, 500 mg 4 times daily;c. oxaprozin with cimetidine, 300 mg 4 times daily;d. oxaprozin with ranitidine, 150 mg every 12 hours. Acetaminophen, cimetidine, or ranitidine were begun 24 hours prior to oxaprozin dosage and continued for the 10-day duration of each trial. No significant differences existed among the four treatment conditions in peak plasma oxaprozin concentration (86 µg/ml), volume of distribution (0.23 l/kg), time of peak concentration (3.7 h after dosage), or elimination half-life (54 h). Oxaprozin oral clearance was significantly lower (by 20%) during both the cimetidine and ranitidine trials versus control (0.047 vs 0.047 vs 0.059 ml/min/kg), but clearance during acetaminophen was not significantly different from control. Thus acetaminophen, cimetidine or ranitidine has only a small influence on the pharmacokinetics of a single oral dose of oxaprozin. The reduction in oxaprozin clearance due to cimetidine or ranitidine is statistically significant but small in magnitude.Supported in part by Grants MH-34223 and AG-00106 and Biomedical Research Support Grant RR-05598 from the USPHS, and by a Grant-in-Aid from Wyeth Laboratories, Radnor, PA, USA