International journal of clinical pharmacology, therapy, and toxicology最新文献_第5页

Efficacy of misoprostol in controlling indomethacin induced fecal blood loss in arthritic patients. 米索前列醇控制吲哚美辛致关节炎患者粪便失血的疗效。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

N S Jallad, A Cattan, D J Weidler

{"title":"Efficacy of misoprostol in controlling indomethacin induced fecal blood loss in arthritic patients.","authors":"N S Jallad, A Cattan, D J Weidler","doi":"","DOIUrl":"","url":null,"abstract":"Indomethacin, a nonsteroidal anti-inflammatory drug, may cause gastric mucosal damage as shown by fecal blood loss. A randomized, double-blind, placebo-controlled, parallel group study was conducted to determine the effects of 400 mcg b.i.d. misoprostol, a synthetic prostaglandin E1 analog, on intestinal blood loss caused by 50 mg t.i.d. indomethacin. Forty-two arthritic patients, mean age 59 years, received indomethacin for 14 days. Those with baseline blood loss of at least 1.5 ml/day during the first 7 days were randomized to 400 mcg of misoprostol or placebo (days 8 to 14). Fecal blood loss was measured using 51Cr labelled red blood cell technique. Success was defined as a reduction in mean daily blood loss of at least 50% during the treatment period compared to mean daily blood loss during the baseline (pre-treatment) phase. The mean daily blood loss on treatment days 9-15 was not significantly reduced from baseline in either group. These data neither confirm nor deny the effectiveness of misoprostol in reducing fecal blood loss caused by indomethacin. The results may have been confounded by the administration of misoprostol twice daily while indomethacin was administered three times daily. In addition, fecal blood loss as an indicator of gastrointestinal mucosal damage is not a sensitive measure; it is characterized by poor reproducibility and wide fluctuations within individual responses. Inappropriate laboratory techniques may have further reduced the sensitivity and reliability of this procedure.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"376-81"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19215824","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Potential pharmacokinetic interactions of nocloprost clathrate with retarded theophylline and enteric coated diclofenac after single and repeated premedication in healthy volunteers. 健康志愿者单次和多次预用药后诺氯前列素包合物与缓凝茶碱和肠溶双氯芬酸的潜在药代动力学相互作用

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

W Siegmund, E Scheuch, M Zschiesche, G Franke, E Stolz, I Amon

{"title":"Potential pharmacokinetic interactions of nocloprost clathrate with retarded theophylline and enteric coated diclofenac after single and repeated premedication in healthy volunteers.","authors":"W Siegmund, E Scheuch, M Zschiesche, G Franke, E Stolz, I Amon","doi":"","DOIUrl":"","url":null,"abstract":"Pharmacokinetic interactions of cytoprotective prostaglandin E2 analog nocloprost clathrate with theophylline and diclofenac were studied in two placebo controlled, single-blind studies with parallel groups (n = 8) in healthy male volunteers (age 20-32 years, body weight 63-95 kg, body height 169-193 cm, Broca index 0.81-1.18). Nocloprost (200 micrograms) or placebo tablets were given twice daily (07:00 h a.m. and p.m.) for 8 days. Thirty min after the first administration on the first day (single) and 30 min after the last administration in the morning of the 8th day (repeated premedication), pharmacokinetic examinations with retarded theophylline capsules (250 mg) or enteric coated tablets of diclofenac (50 mg) were performed. Theophylline was measured using an HPLC- and diclofenac with a GC-method. Both single and repeated premedication with nocloprost did not significantly change any pharmacokinetic parameter of theophylline. There was only a tendency towards lower AUC of theophylline after both regimens of premedication. As far as diclofenac is concerned, single premedication increased significantly the rate of absorption and total body clearance but lowered the AUC of the NSAID. After repeated premedication, no parameter was significantly influenced. All pharmacokinetic changes observed are most likely without any clinical importance.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"407-14"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19214499","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Steady-state pharmacokinetics of phentermine extended-release capsules. 芬特明缓释胶囊的稳态药动学研究。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

G Groenewoud, R Schall, H K Hundt, F O Müller, M van Dyk

{"title":"Steady-state pharmacokinetics of phentermine extended-release capsules.","authors":"G Groenewoud, R Schall, H K Hundt, F O Müller, M van Dyk","doi":"","DOIUrl":"","url":null,"abstract":"Twenty-one healthy, caucasian, male volunteers completed this randomized single blind, multiple-dose, crossover bioavailability study during which either phentermine HCl capsules (Minobese Forte, reference product) or phentermine base capsules (Duromine, test product) were ingested once daily for 14 days. A washout period of 14 days was allowed between the two treatment phases. On profile days (day 14 of each treatment phase) subjects remained recumbent for 24 hours after drug administration. Serial venous blood samples were drawn over the 24 hour dosing interval for plasma phentermine assay by gas chromatography. The 90% confidence intervals for the \"test/reference\" mean ratios of the pharmacokinetic variables Cmax,norm, Cmin,norm, AUCnorm (normalized for difference in the dose of phentermine base), %PTF and T75% Cmax, all fell within the bioequivalence range of 80% to 125%. With the aid of trough plasma phentermine concentrations, it was established that steady-state was reached after 14 days of once daily administration of either product. Adverse events experienced on both treatments included prolonged or recurrent episodes of insomnia, nausea, headache, dry mouth and dizziness. No clinically relevant changes in clinical chemistry or hematology variables occurred during the study.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"368-72"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19215822","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Covalent coupling of nucleosides to low density lipoprotein (LDL) generates macrophage specific (drug)-carriers. 核苷与低密度脂蛋白(LDL)的共价偶联产生巨噬细胞特异性(药物)载体。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

H von Baeyer, H Neitzel, M Nündel, E Riedel, H K Schultis

引用次数: 0

Five-year survival rate of fissure sealings and fissure restorations. 裂隙封闭与裂隙修复的5年存活率。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

P Städtler

引用次数: 0

Effect of free fatty acids on the binding kinetics at the benzodiazepine binding site of glycated human serum albumin. 游离脂肪酸对糖化人血清白蛋白苯二氮结合位点结合动力学的影响。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

Y Keita, W Kratzer, W Wörner, N Rietbrock

{"title":"Effect of free fatty acids on the binding kinetics at the benzodiazepine binding site of glycated human serum albumin.","authors":"Y Keita, W Kratzer, W Wörner, N Rietbrock","doi":"","DOIUrl":"","url":null,"abstract":"The effect of free fatty acids (FFA) and non-enzymatic glycation on the binding kinetics of dansylsarcosine (DS) to human serum albumin (HSA) was studied using the stopped-flow technique. The influence of FFA on the binding parameters of 25% glycated HSA depended on the type of fatty acid. The addition of stearic, oleic and linoleic acids in a concentration of 0.3 mmol/l showed no inhibitory effects on the association rate constant (k2) value for DS binding to 25% glycated HSA (k2 without FFA: 385 +/- 10 s-1, k2 with FFA > or = 385 +/- 10 s-1). In contrast, shorter chain fatty acids (hexanoic, octanoic, decanoic, lauric and myristic acids) showed marked inhibitory effects for 0.3 mmol/l FFA (k2 range: 233 +/- 32 to 69 +/- 5 s-1) and for 0.6 mmol/l FFA (k2 range: 125 +/- 3 to 20 +/- 4 s-1). The association rate constant (k2) as well as the affinity constant (KA) of DS were markedly affected by glycation: k2 was 686 +/- 61 s-1 for 7% glycated HSA, 385 +/- 10 s-1 for 25% glycated HSA and 209 +/- 12 s-1 for 50% glycated HSA. KA decreased from 6.1 +/- 2.9 x 10(5) M-1 for 7% glycated HSA, to 5.1 +/- 0.1 x 10(5) M-1 for 25% glycated HSA and to 1.3 +/- 0.6 x 10(5) M-1 for 50% glycated HSA.(ABSTRACT TRUNCATED AT 250 WORDS)","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 7","pages":"337-42"},"PeriodicalIF":0.0,"publicationDate":"1993-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"18693199","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

The analysis of plasma kinetics and beta-receptor binding and -blocking activity of timolol following its small intravenous dose. 替莫洛尔小剂量静脉注射后血浆动力学及β受体结合和阻断活性分析。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

T Kaila, S Karhuvaara, R Huupponen, E Iisalo

{"title":"The analysis of plasma kinetics and beta-receptor binding and -blocking activity of timolol following its small intravenous dose.","authors":"T Kaila, S Karhuvaara, R Huupponen, E Iisalo","doi":"","DOIUrl":"","url":null,"abstract":"Plasma kinetics and beta-receptor blocking and -binding activity of timolol was studied in six healthy volunteers following its intravenous 0.25 mg dose. Timolol concentrations were measured using radioreceptor assay (RRA), blocking activity by comparing the dose ratios (DRs) of the infusion rates of isoprenaline required to increase heart rate by 25 bpm (I25) and binding activity by determining the extent to which timolol occupied beta 1-receptors of rabbit lung and beta 2-receptors of rat reticulocytes in undiluted plasma samples. Timolol was eliminated from plasma with a mean half-life for the elimination phase of 2.6 hours. The dose antagonized potently isoprenaline-induced tachycardia at least for four hours. The effect was excellently correlated with the estimated beta 2-receptor binding activity of timolol in the circulating plasma. In conclusion, the small intravenous timolol dose was eliminated from plasma by a fashion, which was very similar to its eighty-fold higher oral doses reported earlier in the literature. The 0.25 mg dose was of considerable systemic beta-receptor blocking and -binding activity, that may help to explain its reported side-effects following ocular drug administration. The extent to which beta-blocking agents occupy rabbit lung beta 1- and rat reticulocyte beta 2-receptors in the circulation appears to predict the intensity and selectivity of their beta-blocking effects in healthy volunteers.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 7","pages":"351-7"},"PeriodicalIF":0.0,"publicationDate":"1993-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19096503","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of a high-fat meal on the bioavailability of phenytoin in a commercial powder with a large particle size. 高脂肪膳食对大粒径商业粉末中苯妥英生物利用度的影响。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

T Hamaguchi, D Shinkuma, T Irie, Y Yamanaka, Y Morita, B Iwamoto, K Miyoshi, N Mizuno

{"title":"Effect of a high-fat meal on the bioavailability of phenytoin in a commercial powder with a large particle size.","authors":"T Hamaguchi, D Shinkuma, T Irie, Y Yamanaka, Y Morita, B Iwamoto, K Miyoshi, N Mizuno","doi":"","DOIUrl":"","url":null,"abstract":"The effect of a high-fat meal on the bioavailability of free acid phenytoin (DPH) from Hydantol powder with a large particle size (mean particle size, 190 microns) was investigated in four healthy male subjects. The drug was administered as a single oral 5 mg/kg dose of free acid DPH in the fasting state, with a low-fat meal, or with a high-fat meal using a crossover study design. Seven blood samples were collected over a 34-h period following drug administration, and the drug plasma concentrations were determined by GLC. In comparison with the fasting state results, the mean area under the plasma concentration-time curve up to infinity after administration (AUC0-infinity) and the peak plasma concentration (Cmax) of DPH from Hydantol powder significantly increased about 2-fold with the intake of the high-fat meal and about 1.5-fold with the intake of the low-fat meal. The elimination rate constant was not significantly different among the three treatments. The increased bioavailability with the high-fat meal probably resulted from accelerated dissolution of the poorly soluble Hydantol powder due to the stimulation of bile flow or delay of the gastric emptying time caused by the fat intake.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 7","pages":"326-30"},"PeriodicalIF":0.0,"publicationDate":"1993-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19356571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Considerable cost savings through the analysis of pooled plasma samples in bioequivalence studies that fail to show bioequivalence. 通过在生物等效性研究中对未显示生物等效性的汇集血浆样本进行分析，可节省大量成本。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

H K Hundt, R Schall, H G Luus, F O Müller

引用次数: 0

Clinical evaluation of the effect of omeprazole, cimetidine, famotidine and ranitidine on histamine induced cutaneous wheal and flare response. 奥美拉唑、西咪替丁、法莫替丁和雷尼替丁对组胺致皮肤轮状和耀斑反应的临床评价。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-07-01

N Saha, A Sachdev, D K Bhasin, A Sankaranahyanan, P P Khosla, K Singh, P L Sharma

引用次数: 0