酮基布洛芬从Poloxamer凝胶中的释放

酮基布洛芬是一有效的非甾体消炎药,常用于治疗各种急、慢性关节炎。与其它非甾体抗炎药一样,酮基布洛芬口服可产生一系列严重的副作用。据报道,近年来酮基布洛芬的局部应用已取得成功,由于药物直接作用于炎症部位,不仅起效迅速且局部浓度高。本文采用聚氧乙烯-聚氧丙烯嵌段的聚合物Poloxamer 407(普流罗尼F-127,简写为PF-127)作为凝胶形成剂制备酮基布洛芬凝胶,并考察其体外释药特性及影响因素。制备方法称取酮基布洛芬和PF-127     

2.5%酮基布洛芬凝胶对急性痛风性关节炎疗效评价

痛风是长期嘌呤代谢紊乱及,或尿酸排泄减少所引起的一疾病,主要表现为单纯性血尿酸增高、关节炎和肾脏疾病发作。痛风性关节炎的治疗主要是卧床休息,多饮水,非甾体类抗炎药(NSAlDs)控制炎症和降低血尿酸。2.5％酮基布洛芬     

布洛芬与其它非甾体抗炎药的临床比较

布洛芬(lbuprofen)是一种较新的非甾体抗炎药,由于其副作用发生率较低,效果肯定,具有较大发展前途。本文对布洛芬临床应用情况与其它非甾体抗炎药进行一些比较。 1.治疗风湿性关节炎大量研究表明,布洛芬治疗风湿性关节炎与阿斯匹林和其它非甾体抗炎药效果相同。其常见副作用为消化不良、     

人重复经皮给酮基布洛芬后的药动学

近年来对应用经皮肤给抗炎药治疗风湿病逐渐引起兴趣,其主要优点为减少副作用发生率。本研究目的在测定非甾体抗炎药酮基布洛芬以凝胶剂型经皮肤吸收,评价每天两次给药10天的稳态。10名健康受试者(5男5女)参加试脸,平均年龄为23.2土2.5岁     

新型非甾体抗炎药——炎痛喜康

<正> 炎痛喜康(piroxicam)是一种新型非甾体抗炎药,对类风湿关节炎、风湿性关节炎及痛风性关节炎等有效;兼有明显镇痛作用;但副作用轻,故临床效应优于阿司匹林、消炎痛、布洛芬(ibuprofen)及萘普生(naproxen)等其他非甾体抗炎药。其结构式为     

非诺洛芬的合成路线图解

非诺洛芬(苯氧布洛芬,fenoprofen),化学名为α-甲基间苯氧基苯乙酸。本品钙盐(1)系良好的非甾体抗炎药。1976年美国     

2007—2009年非甾体抗炎药应用分析

目的:评估北京市朝阳区妇儿医院非甾体抗炎药的应用现状。方法:采用Excel软件对2007—2009年非甾体抗炎药的数据进行统计分析。结果:我院非甾体抗炎药的数量、金额等逐年递增;布洛芬、对乙酰氨基酚销售数量总量、DDDs在3年中居前2名;且在单方制剂中,3年来布洛芬占销售数量、DDDs皆位于首位。结论:布洛芬、对乙酰氨基酚在我院非甾体抗炎药治疗中居主导地位,该类药物使用是合理的。     

酮基布洛芬的药物动力学研究

酮基布洛芬(Ketoprofen)系非甾体类,具有苯丙酸基本结构的消炎、镇痛药物。因其药理作用较强,国内已广泛用于治疗风湿性关节炎,外伤、术后及癌症所致的疼痛。尽管本品临床药物动力学的研究国外已有报道,但就国内新近试制成功的本品,进     

酮代布洛芬:一种新型非甾体抗炎止痛药

<正> 酮代布洛芬是属于芳香烷类的非甾体抗炎药,同类的还有布洛芬,萘普酮等。本品主要用于治疗类风湿性关节炎、骨关节炎以及轻度钝痛,它的抗炎及止痛机制主要是:可逆性抑制环氧酶,脂氧酶等参与前列腺素及白三烯合成的酶。同时,它还是缓激肽的抑制剂,并阻止溶酶体酶     

非甾体抗炎药与肾脏毒性

<正> 非甾体抗炎药(nonsteroidal anti-in flammatory drugs,NSAIDs)原称解热镇痛药,是一大类不同质的化合物,包括水杨酸类的阿司匹林和氟苯水杨酸,多环酸类的吲哚美辛、苏灵大、萘普生、布洛芬、苯氧布洛芬、保泰     

Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83

Pharmacological properties of LFP83, a non-steroidal analgesic and antipyretic drug, were studied in mice, rats and rabbits. LFP83 is a prodrug of flurbiprofen (FP) which is its active major metabolite in vivo. In experimental models of acetic acid writhing, the Randall and Selitto method, arthritic pain, yeast fever, LPS fever, carrageenin edema and adjuvant arthritis, LFP83 (i.v.) showed remarkable analgesic, antipyretic and antiinflammatory activities; and it was more potent than ketoprofen (i.m.) and aspirin DL-lysine (i.v.). The analgesic activity of LFP83 was equal to or more potent than that of pentazocine, and its duration was longer than those of aspirin DL-lysine and pentazocine. In addition, the analgesic potency of LFP83 was approximately the same or more potent than that of FP (p.o.), and the onset of this analgesic effect began earlier. On the other hand, the ulcerogenic activity of LFP83 on rat gastric mucosa was less than that of FP (p.o.) in both single and consecutive (7 days) administrations. The safety index (UD50/ED50) of LFP83 was three to ten-fold higher than that of FP (p.o.). As mentioned above, LFP83 is a potent analgesic, antipyretic and antiinflammatory drug; and in comparison to oral FP, it has a more potent and immediate effect, weak gastric irritation and high safety index.     

AHR-10037, a non-steroidal anti-inflammatory compound of low gastric toxicity

AHR-10037 is an anti-inflammatory compound possessing analgesic and antipyretic properties and a high therapeutic index. AHR-10037 was comparable to indomethacin in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation. There was a delayed onset of antipyresis (yeast-induced hyperthermia in rats), analgesia (acetylcholine-induced abdominal constriction in mice) and inhibition of caster oil-induced diarrhea in rats. Antipyresis occurred 3 hours after administration of AHR-10037, 4 mg/kg, PO. vs 1 hour after administration of acetylsalicylic acid, 100 mg/kg, PO; maximum analgesic activity (ED50 = 4.1 mg/kg) occurred at 4 hours. AHR-10037 was inferior to indomethacin in suppressing castor oil-induced diarrhea in rats. The therapeutic index of AHR-10037 (relating acute anti-inflammatory potency to gastric toxicity potency relative to indomethacin) ranged from 56-91. The pharmacological profile suggests that AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor.     

The antiinflammatory profile of (5H-dibenzo[a,d]-cyclohepten-5-ylidene)acetic acid (WY-41,770), an agent possessing weak prostaglandin synthetase inhibitory activity that is devoid of gastric side effects

Wy-41,770 [(5H-dibenzo[a,d]cyclohepten-5-ylidene)acetic acid], a novel acrylic acid, was compared to indomethacin and aspirin in standard antiinflammatory, analgesic and antipyretic animal models. The acute antiinflammatory, analgesic and antipyretic activity of Wy-41,770 (oral ED50S 50-170 mg/kg) was similar to aspirin; however, it was considerably more potent orally in adjuvant arthritis in the rat (ED50, 16 mg/kg) and urate-induced synovitis in the dog (ED50, 4.5 mg/kg). Wy-41,770 was a weak inhibitor of prostaglandin biosynthesis and did not inhibit either 5- or 15-lipoxygenase. Furthermore, the cellular migration characteristic of carrageenan pleurisy was not affected by Wy-41,770. Unlike a majority of NSAIDs, it produced no gastric irritation in rats after either acute or chronic oral administration over the range 400-800 mg/kg. The major mechanism of action of Wy-41,770 has yet to be identified but does not seem to involve interference of arachidonic acid metabolism.     

Pharmacological studies of dl-2[3-(2'-chlorophenoxy)phenyl]propionic acid. I. Analgesic and antipyretic effects

Analgesic and antipyretic effects of dl-2[3-(2'-chlorophenoxy)phenyl] propionic acid (CPP) were studied in mice, rats and guinea-pigs. CPP produced a dose dependent inhibition of acetic acid-induced writhing syndrome. Its ED50 values 1 and 3 hr after oral administration were 47 and 31 mg/kg, respectively. CPP had a potent analgesic effect on bradykinin-induced nociceptive response in rats, and its ED50 value was 15 mg/kg 2 hr after oral administration. The analgesic activity of CPP in these experiments was less potent than that of indomethacin, but it was approximately equivalent to ibuprofen and 10 to 20 times as potent as aspirin. CPP had no analgesic effect on both the tail pinch and hot plate tests in mice, while CPP potentiated the analgesic effect of codeine on these tests. CPP had no effect on the nociceptive response induced by intradermal injection of bradykinin and/or EDTA in guinea-pigs. On the other hand, when CPP was given orally in a dose range of 1.25 to 5 mg/kg, it produced an antipyretic effect on yeast-induced fever in rats. The antipyretic activity of CPP was equivalent to ibuprofen and 10 to 15 times as potent as aspirin.     

Prostaglandin synthetase systems in rat and rabbit renal medulla and inhibition by non-steroidal anti-inflammatory drugs.

The properties of prostaglandin synthetase systems (PSSs) in the renal medulla of the rat and rabbit, and inhibition by ketoprofen, indomethacin, ibuprofen, phenylbutazone and aspirin were investigated in relation to their anti-inflammatory, analgesic, antipyretic and ulcerogenic activities. Rat and rabbit PSSs produced prostaglandin (PG)E and PGF from arachidonic and dihomo-gamma-linolenic acids and had an optimal pH of 8.5 and 7.5 for PGE formation, respectively. Only a slight loss of activity occurred with lyophilization. In the rat PSS, all drugs tested were inhibitory in the order of ketoprofen, ibuprofen, indomethacin and aspirin, respectively. In the rabbit PSS, the same potency relationship was also found. Drug sensitivity of the rat PSS was remarkably lower than that of the rabbit PSS. Significant correlations were noted between the inhibitory potencies of the drugs against both PSSs and other in vivo pharmacological activities within the same species.     

Pharmacological properties of a new non-steroidal anti-inflammatory drug: flunoxaprofen

The anti-inflammatory, analgesic and antipyretic activities of S-(+)-2(4-fluorophenyl)-alpha-methyl-5 benzoxazole acetic acid (flunoxaprofen: Flu), a new non-steroidal anti-inflammatory drug, were compared with those of indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDs) in experimental animals. Flu showed strong inhibitory activity on acute and subacute inflammation tests in rats, such as carrageenin hind paw oedema (oral: 6-25 mg/kg; rectal: 50-100 mg/kg); pellet-induced granuloma formation (5-20 mg/kg/day) and adjuvant-induced arthritis (10 mg/kg/day). Its potency was comparable with that of indomethacin (I) and higher than that of acetyl salicylic acid (ASA), ibuprofen (IBU) or phenylbutazone (P). The analgesic activity of Flu, evaluated by the hot plate method and tail pinching in mice, was slightly lower than that of I but higher than that of ASA and IBU. In pyretic rabbits Flu showed an antipyretic activity higher than that of ASA and IBU. The ability of Flu to affect platelet aggregation, mucopolysaccharide synthesis by fibroblasts and the proteolytic action of trypsin was also investigated.     

Pharmacological properties of the novel non-steroidal antiinflammatory agent N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2 -one

The antiinflammatory activity of the novel pyrrolidin-2-one derivative N-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-o ne (E-5110) was investigated and compared with those of indomethacin and piroxicam in various antiinflammatory, analgesic and antipyretic animal models. The acute antiinflammatory activity of E-5110 on the carrageenin paw edema was similar to that of indomethacin, and half that of piroxicam. The chronic inflammatory responses in established adjuvant- and type II collagen-induced arthritis, which are widely used models of rheumatoid arthritis, were suppressed as effectively by E-5110 as by indomethacin and piroxicam. E-5110 decreased the pleural exudate volume and inhibited leucocyte infiltration in a reversed passive Arthus reaction more potently than indomethacin, suggesting that mediators other than prostaglandin E2 may play an important role in this inflammatory process. The analgesic potency of E-5110 against inflammatory pain was similar to that of indomethacin or piroxicam, but the antipyretic activity of E-5110 was more potent than that of the reference drugs. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than those of indomethacin and piroxicam. In conclusion, E-5110 is a very potent antiinflammatory compound acting against various types of inflammation, and has a favorable therapeutic index.     

国产湿痛喜康的抗炎解热和镇痛作用

湿痛喜康对角叉菜胶诱发大鼠踝关节肿胀、二甲苯诱导小鼠耳水肿、大鼠佐剂性关节炎、酵母诱发大鼠发热、冰醋酸诱导小鼠扭体反应和“热板”致痛反应等实验模型,有明显的抗炎、解热和镇痛作用。对角叉菜胶性炎症模型和小鼠扭体反应的ED_(50)分别为5.26mg/kg和5.5mg/kg。     

Pharmacological studies of the new antiinflammatory agent 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-o ne. 1st communication: antiinflammatory, analgesic and other related properties.

The antiinflammatory, analgesic and antipyretic activities of 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-on e (T-614, CAS 123663-49-0) were investigated in various animal models and compared with those of nimesulide, indomethacin and ibuprofen. The antiinflammatory potency of T-614 on carrageenin-induced paw edema, paper disk granuloma and established adjuvant arthritis was greater than that of ibuprofen, but slightly lower than those of nimesulide and indomethacin. In acute inflammatory models, unlike indomethacin, T-614 suppressed the edemas provoked by dextran and bromelain in rats, but its inhibitory action on ultraviolet erythema in guinea-pigs was weak. Although the analgesic activity of T-614 was hardly demonstrated in writhing tests in mice, its potency against the inflammatory pain such as Randall-Selitto test, adjuvant-induced hyperalgesia and antigen-induced arthritic pain in rats was superior to that of ibuprofen. Moreover, it had a potent analgesic effect on urate-induced synovitis in dogs. T-614 exerted a prompt and strong antipyretic effect in both yeast-induced febrile rats and lipopolysaccharide-induced febrile rabbits. T-614 had virtually no gastrointestinal ulcerogenic action and did not affect water and sodium excretion in rats. T-614 is a novel antiinflammatory compound with different pharmacological properties from that of the reference drugs.     

The antiinflammatory activity of the immunomodulator Wy-18,251 (3-(p-chlorophenyl)thiazolo[3,2-a]benzimidazole-2-acetic acid)

The antiinflammatory activity of the immunomodulatory agent Wy-18,251 (3-(p-chlorophenyl)thiazolo-[3,2-a]benzimidazole-2-acetic acid) was examined using a variety of antiinflammatory, analgesic and antipyretic animal models in comparison to aspirin, levamisole and indomethacin. The acute antiinflammatory and analgesic activity of Wy-18,251 (ED50 = 100-200 mg/kg, p.o.) was similar to aspirin, but in contrast to aspirin Wy-18,251 failed to demonstrate antipyretic activity. Wy-18,251 (10-100 mg/kg, p.o.) also inhibited chronic inflammatory responses in the adjuvant- and collagen-induced arthritis models. Wy-18,251 was a modest inhibitor of prostaglandin biosynthesis but did not inhibit either 5- or 15-lipoxygenase enzymes. Wy-18,251 (up to 480 mg/kg, p.o.) produced little gastrointestinal pathology in 16 h fasted rats. The combined immunomodulatory and antiinflammatory activity of Wy-18,251 suggests that this agent may have therapeutic promise in certain immunoinflammatory diseases including rheumatoid arthritis.