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青蒿琥酯皮肤擦剂在小鼠和兔体内的药代动力学研究 总被引:1,自引:0,他引:1
将青蒿琥酯溶于苯二甲酸二甲酯,加适量氨酮制成皮肤擦剂。给兔脱毛后,皮肤涂抹此擦剂25mg/kg后,血药浓度达峰时间平均为2 h,峰浓度平均为1.80μg/ml。药物在兔体内平均驻留时间为3.54 h,清除半衰期约为2.46 h。给小鼠脱毛皮肤涂抹擦剂6.7,31.3和71.4 mg/kg,血药浓度在给药后0.5~4 h达高峰,峰浓度分别为0.82,2.05和7.11μg/ml,体内药物平均驻留时间为3.39,2.79及3.54 h,清除半衰期为2.35,1.93及2.45 h。可见,给兔及小鼠皮肤擦剂后,青蒿琥酯吸收良好,血药浓度维持时间较长。 相似文献
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Walter S Speidl Markus Exner Jasmin Amighi Wolfgang Mlekusch Schila Sabeti Stefan P Kastl Gerlinde Zorn Gerald Maurer Oswald Wagner Kurt Huber Erich Minar Johann Wojta Martin Schillinger 《Journal of endovascular therapy》2007,14(1):62-69
PURPOSE: To investigate whether balloon angioplasty of the superficial femoral artery (SFA) increases serum levels of C5a and whether C5a predicts risk of restenosis. METHODS: C5a antigen was measured at baseline and 8 hours after intervention in 131 consecutive patients (76 women; median age 72 years) with intermittent claudication who underwent successful primary SFA balloon angioplasty. Patients were followed for a median 10 months [interquartile range (IQR) 6 to 14] for the occurrence of >50% restenosis by duplex ultrasound. RESULTS: Median C5a levels increased significantly from 39.7 ng/mL (IQR 27.8 to 55.0) at baseline to 53.8 ng/mL (IQR 35.6 to 85.1, p<0.001) 8 hours post intervention. During the follow-up period, 70 (53%) patients developed restenosis. Increasing levels of C5a (quartiles) at baseline were significantly associated with an increased risk for restenosis (p=0.0092). Adjusted hazard ratios (95% confidence intervals) for restenosis with increasing quartiles of baseline serum C5a levels were 1.24 (0.60 to 2.58), 1.93 (0.95 to 3.93), and 2.08 (1.02 to 4.21), respectively, compared to the lowest quartile. This effect was independent of nonspecific inflammation as reflected by plasma levels of C-reactive protein. CONCLUSION: Inflammatory mechanisms play a major role in the development of restenosis after angioplasty. The complement component C5a exerts strong chemotactic and proinflammatory effects. Enhanced complement activation prior to PTA, as measured by higher levels of C5a, was significantly associated with restenosis after SFA balloon angioplasty. Pathways of complement inhibition thus may be worth investigating with respect to improving patency rates. 相似文献
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D H Russell N E Zorn A R Buckley P D Crowe M D Sauro E M Hadden R V Farese H E Laird 《European journal of pharmacology》1990,188(2-3):139-152
Prolactin (PRL) and other trophic factors rapidly activate a nuclear pool(s) of protein kinase C (nPKC) in purified splenocyte nuclei. The PRL also enhanced [2-3H]glycerol incorporation into nuclear mono- and triacylglycerol. An assay was devised which not only probed the ability of the hormone to activate protein kinase C (PKC) but also demonstrated the presence of nuclear substrates. Using this methodology, a biphasic concentration-response curve to PRL was observed. Heterologous species of PRL and various growth factors also activated nPKC. The PRL-induced nPKC stimulation was antagonized by various immunomodulators, G protein-coupling inhibitors, PKC inhibitors, a calmodulin inhibitor, and a peripheral benzodiazepine agonist and antagonist. A monoclonal antibody to PKC, anti-rat PRL antiserum and a monoclonal anti-rat PRL receptor antibody antagonized PRL-induced PKC-dependent nuclear phosphorylation, further implicating nPKC and a PRL receptor-mediated activation process. Nuclear PKC may be a major target for trophic regulation in response to both positive and negative growth signals. 相似文献
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The purpose of this study was to determine if early recovery of quadricep muscle strength post spinal cord injury (SCI) is a useful predictor of future ambulation. Seventeen C4-T10 motor incomplete (Frankel C) spinal cord injured patients admitted to our center between March 1988 and April 1990 were examined within 72 hours to one week post injury. All patients had initial quadricep strengths < or = 2/5 in both legs. Strength in the strongest quadricep was followed prospectively at intervals from admission to one year post injury. Recovery time to a > 3/5 quadricep was established for each patient. Patients were categorized into 2 groups: FA (n = 11) were those patients who achieved functional ambulation and NA (n = 6) were those subjects who were nonambulators. Functional ambulators were defined as those patients who were able to walk in the household and/or the community while non ambulators were those who either did not ambulate or did so only for exercise. All patients (n = 9) who achieved a > 3/5 quadricep by 2 months post SCI became functional ambulators whereas in the group of 8 patients who did not achieve a > 3/5 by 2 months, only 2 became functional ambulators. This result was found to be significant using a point-by-serial correlation with p < 0.05. In conclusion, motor incomplete spinal cord injured patients who recovered to a > 3/5 quadricep strength by 2 months post injury had an excellent prognosis for subsequent ambulation by 6 months post injury. 相似文献