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考察了离子导入和月桂氮酮预处理以及两法合用对4种非甾体抗炎药吡罗昔康、吲哚美辛、萘普生、双氯芬酸钠体外经皮渗透的促进作用。对4种药物的离子导入增渗倍数分别为37.2、9.7、6.4和7.5,合用月桂氮酮增渗倍数分别增达97.2、20.2、17.0和12.1,说明两法合用具协同作用。且对解离型药物促渗作用更强。 相似文献
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渗透促进剂对利多卡因经皮渗透的促进作用 总被引:1,自引:0,他引:1
考察了7种渗透促进剂对利多卡因游离碱的促渗作用,并提出了一促渗作用参数对油溶性和水溶性促渗剂的促渗作用进行系统比较,结果发现渍溶性促渗剂的促渗作用强于水溶性促渗剂(P<0.05),但对药物经皮渗透的滞后时间无改善作用,水溶性促渗剂可使滞后时间有所缩短。 相似文献
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<正> 近年来,越来越多的抗炎镇痛新药已经用于风湿病的治疗,这些药物临床作用的基础在于抑制前列腺素的合成,然而它们在不同的疾病中有不同的作用。由于它们精细的作用方式不尽相同,其药理作用和毒性也差异很大,特别是不同病人对不同的非甾体抗炎药(NSAID)有完全不同的反应。因此,试制多种药物以适应治疗的个体化,对各种病人寻求最有效的治疗方案是很有价值的,同时必须记住这些药物 相似文献
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2005年4月7日美国FDA发表了非甾体类抗炎药有增加心血管不良事件和胃肠道出血的潜在风险的声明;我国国家食品药品监督管理局随之也表示,将对这类药品的安全性问题予以“密切关注”。 相似文献
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Chiba T Sato K Kudara N Shinozaki H Ikeda K Sato K Endo M Orii S Suzuki K 《Inflammopharmacology》2008,16(1):16-20
Aims: We examined the characteristics of upper gastrointestinal disorders induced by non-steroidal anti-inflammatory drugs (NSAIDs).
Methodology: The questionnaire investigation was performed over a five year period.
Results: A study was performed on 354 patients (161 men and 193 women with mean ages of 66.0 and 70.7 years, respectively) who developed
NSAIDs associated upper GI disorders: 21 patients had AGML, 212 had gastric ulcer, 63 had duodenal ulcer, 17 had gastroduodenal
ulcers and 41 other cases. About 75 % of patients received NSAIDs for orthopedic conditions. Sixty percent of gastric disorders
induced by NSAIDs affected the antrum or angulus of the stomach. The incidence of disorders of the gastric antrum was significantly
higher in women than in men whilst the incidence of disorders on the gastric angulus was significantly higher in men than
in women (p < 0.05). The proportion of patients with abdominal pain was significantly lower in patients over 65 years old
than in those under 65 years old, and the proportion of patients with hematemesis or melena was significantly higher in patients
over 80 years old than in those under 80 years old (p < 0.05). The time taken to achieve the healing stage was significantly
longer in patients with greater than 3 months NSAIDs ingestion compared to patients that had received NSAIDs for less than
3 months (p < 0.05).
Conclusions: Patients 65 years old and over with continuous NSAIDs use had asymptomatic ulcers, and patients 80 years old and over had
hemorrhagic ulcers.
Received and accepted 20 September 2006 相似文献
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非水毛细管电泳法分离分析非甾体抗炎药物 总被引:1,自引:0,他引:1
目的建立一种非水毛细管电泳法(NACE)分离非甾体抗炎药物,并对奥沙普秦肠溶片进行定量分析。方法以含醋酸铵15mmol/L的甲醇-乙腈(3∶7)混合液为电泳缓冲液,运行电压20kV,柱温20℃,进样压力2.5kPa,进样时间10 s,UV检测波长200nm;内标法(内标:布洛芬)定量奥沙普秦肠溶片。结果NACE能有效分离布洛芬、萘普生、奥沙普秦、舒林酸和双氯芬酸钠五种非甾体抗炎药物。奥沙普秦与布洛芬的峰面积比对奥沙普秦浓度C(μg/mL)的线性回归方程为Y=0.0434C-7.1×10-3(R=0.999 9,n=9),线性范围0.8~80μg/mL,加样回收率99.05%~101.48%,日内、日间精密度分别为0.54%~0.83%,0.55%~0.92%。结论NACE用于奥沙普秦等非甾体抗炎药物的分离分析,选择性高,重现性好,准确,快速,可作为该类药物及其制剂的质量控制手段。 相似文献
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目的:以临床实例出发探讨非甾体抗炎药致重症药疹的特点和关联性,为临床用药安全提供参考。方法:通过检索1970-2017年国内外期刊数据库公开报道的非甾体抗炎药致重症药疹的病例,提取文献中患者年龄、性别、致ADR药物、重症药疹类型等信息进行统计和分析。结果:非甾体抗炎药致重症药疹文献49篇,共计病例49例。其中单一用药致重症药疹病例有27例,联合用药22例;49例非甾体抗炎药致重症药疹中发生率最高为对乙酰氨基酚,其次为吡罗昔康、布洛芬、依托考昔;非甾体抗炎药致重症药疹平均潜伏期为(7.88±10.42)d,其中致药物超敏反应综合征潜伏期最长,可长达(36.50±14.20)d;大部分患者停药后好转,1例因中毒性表皮坏死松解征死亡。结论:非甾体抗炎药致重症药疹具有潜在的危险性,临床应用时应提高警惕,以减少重症药疹给患者带来的危害。 相似文献
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《Expert opinion on investigational drugs》2013,22(8):1147-1168
Several epidemiological studies suggest that long-term use of non-steroidal anti-inflammatory drugs (NSAIDs) may protect against Alzheimer's disease (AD), especially for patients carrying one or more ?4 allele of the apolipoprotein E. The biological mechanism of this protection is not completely understood and may involve inhibition of COX activity, inhibition of β-amyloid1-42 (Aβ42) production and aggregation, inhibition of β-secretase activity, activation of PPAR-γ or stimulation of neurotrophin synthesis. Unfortunately, long-term, placebo-controlled clinical trials with both non-selective and COX-2 selective NSAIDs in AD patients produced negative results. A secondary prevention study with rofecoxib in patients with mild cognitive impairment and a primary prevention study with naproxen and celecoxib in elderly subjects with a family history of AD were also negative. All these failures have diminished the hope that NSAIDs could be beneficial in the treatment of AD. It is hypothesized that the chronic use of NSAIDs may be beneficial only in the normal brain by inhibiting the production of Aβ42. Once the Aβ deposition process has started, NSAIDs are no longer effective and may even be detrimental because of their inhibiting activity on activated microglia of the AD brain, which mediates Aβ clearance and activates compensatory hippocampal neurogenesis. 相似文献
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Non-steroidal anti-inflammatory drugs ( NSAIDs) can prevent or reduce the occurrence of colorectal cancers . Anti-carcinogenic properties of NSAIDs have been demonstrated in epidemiological studies of humans and experimental animals. In addition, clinical studies of familial adenomatous polyposis and sporadic adenomas have demonstrated that NSAIDs induce regression of colorectal adenomas and prevent formation of these tumors. NSAIDs thus induce early disruption of the adenoma-carcinoma sequence and may mainly suppress subsequent cancer formation at adenoma stage. The mechanism of the anti-carcinogenic effect of these drugs is not known, but results of most studies support that cyclooxygenase-2 (an inducible isoform of prostaglandin synthetase, COX-2) is a major target of NSAIDs in this effect. Recent immunohistochemical studies have revealed that COX-2 is expressed not in tumor cells but in interstitial cells of colonic adenomas. Accordingly, NSAIDs may exhibit anti-carcinogenic property through the inh 相似文献
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固相萃取-液相色谱法测定水环境中4种非甾体抗炎药物 总被引:1,自引:0,他引:1
目的建立专属、灵敏的固相萃取-液相色谱分析方法,测定水环境中4种非甾体抗炎药(酮洛芬、美洛昔康、双氯芬酸、布洛芬)的质量浓度。方法采用固相萃取技术进行样品前处理,用HPLC法测定。色谱柱:C18(200mm×4.6mm,5μm);流动相:乙腈-20mmol.L-1乙酸铵(60∶40),冰乙酸调pH至3.5;流速:1.0mL·min-1;检测波长:263nm。结果各目标分析物在0.5~50.0mg·mL-1范围内线性关系良好,定量下限均为0.5mg·mL-1。精密度(RSD)范围为0.6%~2.0%,萃取回收率大于78.0%,样品溶液在12h内稳定性良好。结论该法简单、灵敏、准确,可用于水环境中多种非甾体抗炎药的分析。 相似文献
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《Clinical Research and Regulatory Affairs》2013,30(2):27-33
Generic drugs play a very important role in health care. A study was undertaken to ascertain the equality or inequality between generics and branded generics. NSAIDs are the most commonly used drugs. So these drugs were chosen for the study. Selected branded generic and generic products of ibuprofen, nimesulide, and diclofenac sodium were tested by oral administration of their suspensions to different groups of rats. Freshly prepared drug suspensions equivalent to doses of 40, 10, and 5?mg/kg of ibuprofen, nimesulide, and diclofenac sodium, respectively, were administered orally to the rats and anti-inflammatory activity was measured by the carrageenan-induced rat paw edema model employing Zeitlin’s apparatus to measure the paw thickness. Statistical analysis by t-test, of the activity at the point of maximum difference indicated that with respect to anti-inflammatory activity generic ibuprofen and generic diclofenac sodium are better than branded generic ibuprofen and branded generic diclofenac sodium, respectively, and generic nimesulide is similar to branded generic nimesulide. All the products studied meet the Pharmacopoeial requirements. Hence it may be concluded that branded generic and generic NSAIDs, tested in this study, are of the same efficacy and inter-changeability among branded generics, and switching between branded generics and generics would not result in any difference in efficacy. 相似文献