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Acta pharmaceutica Nordica最新文献

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Disposition of alprazolam in human volunteers. Differences between genders. 阿普唑仑在人类志愿者中的配置。性别差异。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
F Kristjánsson, S B Thorsteinsson
{"title":"Disposition of alprazolam in human volunteers. Differences between genders.","authors":"F Kristjánsson,&nbsp;S B Thorsteinsson","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The disposition of alprazolam in 16 young healthy volunteers (eight females and eight males) was investigated. All volunteers were given a 1 mg dose of alprazolam. Dose/kg was 13.3 micrograms/kg (SD +/- 0.89 micrograms/kg) on average for male volunteers and 17.5 micrograms/kg (SD +/- 1.84 micrograms/kg) for the female volunteers. Pharmacokinetic parameters were calculated separately for both sexes in order to detect possible gender-dependent differences. The elimination rate constant (beta) for alprazolam proved to be significantly higher in the female population 0.067 hr-1 vs. 0.053 hr-1 (p = 0.03). The closely related parameters, elimination half-life (t1/2) and clearance (Cl) were also significantly different. The total area under the serum concentration curve (AUCtot), maximum serum concentration (cmax) and volume of distribution (Vd) were not significantly different. AUCtot corrected for differences in dose/kg was on the other hand significantly higher in males (p = 0.003) while cmax corrected in the same manner was not.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 4","pages":"249-50"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12944067","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
Quantitation of diltiazem in human plasma by HPLC using an end-capped reversed-phase column. 用端盖反相柱高效液相色谱法定量人血浆中地尔硫卓。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
B H Jensen, C Larsen
{"title":"Quantitation of diltiazem in human plasma by HPLC using an end-capped reversed-phase column.","authors":"B H Jensen,&nbsp;C Larsen","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 3","pages":"179-80"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12956686","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
Synthesis and antiinflammatory activity of indole carboxylic acids and esters. 吲哚羧酸和酯的合成及其抗炎活性。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
A Andreani, M Rambaldi, A Locatelli, M Conti, S Malandrino
{"title":"Synthesis and antiinflammatory activity of indole carboxylic acids and esters.","authors":"A Andreani,&nbsp;M Rambaldi,&nbsp;A Locatelli,&nbsp;M Conti,&nbsp;S Malandrino","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>1-Phenylalkylindole-3-carboxylic acids 1-4, indole-1-acetic acids/esters 5-10 and the hydrazones 11-15 were prepared and submitted to the rat paw edema test using carrageenin. In the first two groups of compounds, the 2-chloro indoles were more active than the corresponding indole derivatives. In the third group the activity seemed to be determined largely by the substituent at the 1-position.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 1","pages":"5-8"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13016784","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
Stability of ketoprofen-dextran ester prodrugs in homogenates of various segments of the pig GI tract. 酮洛芬-葡聚糖酯前药在猪胃肠道各节段匀浆中的稳定性。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
C Larsen, B H Jensen, H P Olesen
{"title":"Stability of ketoprofen-dextran ester prodrugs in homogenates of various segments of the pig GI tract.","authors":"C Larsen,&nbsp;B H Jensen,&nbsp;H P Olesen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Initial velocities of ketoprofen formation from ketoprofen-dextran ester prodrugs incubated in homogenates of various segments of the pig GI-tract were determined. Enzyme-mediated drug release was found in caecum and colon homogenates with their contents, whereas release rates in the stomach, duodenum, jejunum and ileum homogenates were comparable to those determined in pure buffer solutions of identical pH. In colon homogenates adjusted to various pH values between 6.0 and 7.9, little variation in release rates was observed. However, the contribution of enzyme-catalyzed drug regeneration to the overall initial velocity of ketoprofen formation increased significantly as a function of decreasing pH. The presence of several antibiotics and betamethasone in colon homogenates did not affect the drug activation process, whereas the addition of various enzyme inhibitors slowed down the ketoprofen release rates. During incubation in colon homogenates the average molecular weight of the dextran esters decreased. The drug release may therefore involve an initial fragmentation of the drug-liganded dextran chains carried out by dextranases secreted from the microflora which reside in the pig's large bowel.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 1","pages":"41-4"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12876763","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
Gas chromatography and mass spectrometry of dimethylethylsilyl ether derivatives of norethisterone metabolites in plasma. 血浆中去甲睾酮代谢物二甲基乙基硅醚衍生物的气相色谱和质谱分析。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
M S Rizk, N A Zakhari, M I Walash, S S Toubar, C J Brooks, R Anderson
{"title":"Gas chromatography and mass spectrometry of dimethylethylsilyl ether derivatives of norethisterone metabolites in plasma.","authors":"M S Rizk,&nbsp;N A Zakhari,&nbsp;M I Walash,&nbsp;S S Toubar,&nbsp;C J Brooks,&nbsp;R Anderson","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Metabolites isolated from human plasma after oral administration of norethisterone were assayed as their novel dimethylethylsilyl ether derivatives by gas chromatography--mass spectrometry--ion selective monitoring. The major metabolite is 3 alpha, 5 alpha-tetrahydronorethisterone. The unchanged drug is present in a measurable amount even after 8 h of drug administration. The method is accurate, precise and highly sensitive.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 4","pages":"205-10"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12944063","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
Evaluation of the transdermal route for administration of narcotic analgesics: human skin permeability studies of methadone and pethidine. 麻醉镇痛药经皮给药途径的评价:美沙酮和哌替啶的人体皮肤渗透性研究。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
A Fullerton, L Christrup, H Bundgaard
{"title":"Evaluation of the transdermal route for administration of narcotic analgesics: human skin permeability studies of methadone and pethidine.","authors":"A Fullerton,&nbsp;L Christrup,&nbsp;H Bundgaard","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 3","pages":"181-2"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12956687","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
Metabolic study of pholcodine in urine using enzyme multiplied immunoassay technique (EMIT) and capillary gas chromatography. 利用酶倍增免疫分析技术(EMIT)和毛细管气相色谱法研究尿中福可定的代谢。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
M Johansen, K E Rasmussen, A S Christophersen, B Skuterud
{"title":"Metabolic study of pholcodine in urine using enzyme multiplied immunoassay technique (EMIT) and capillary gas chromatography.","authors":"M Johansen,&nbsp;K E Rasmussen,&nbsp;A S Christophersen,&nbsp;B Skuterud","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A study of pholcodine metabolism in man is reported. Three subjects received a single therapeutic oral dose of 50 mg pholcodine and urine samples were collected as long as a positive opiate response could be detected by EMIT (16-26 days). Pholcodine was found to conjugate with glucuronic acid and 15% (13-17%) of the pholcodine dose was excreted in urine as the glucuronide, and 29% (24-35%) as unconjugated pholcodine. Morphine was detected to be a metabolite of pholcodine and 0.5-1% of the pholcodine dose was excreted as morphine glucuronide. The identity of morphine was confirmed by capillary gas chromatography-mass spectroscopy (GC-MS).</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 2","pages":"91-4"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"13070718","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
High performance liquid chromatographic assays of the illicit designer drug "Ecstasy", a modified amphetamine, with applications to stability, partitioning and plasma protein binding. 非法设计药物“摇头丸”(一种改性安非他明)的高效液相色谱分析及其在稳定性、分配和血浆蛋白结合方面的应用。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
E R Garrett, K Seyda, P Marroum
{"title":"High performance liquid chromatographic assays of the illicit designer drug \"Ecstasy\", a modified amphetamine, with applications to stability, partitioning and plasma protein binding.","authors":"E R Garrett,&nbsp;K Seyda,&nbsp;P Marroum","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Specific, sensitive, reverse-phase high-performance liquid chromatographic (HPLC) assays of 3,4-methylenedioxymethamphetamine (MDMA) and 3,4-methylenedioxyamphetamine (MDA) have been devised with analytical sensitivities as low as 2.7 ng/ml of plasma for MDMA and 1.6 ng/ml for MDA, using spectrophotometric detection at 280 nm. The assays were used to determine some properties of MDMA and MDA. Both drugs were stable in aqueous 1 M HCl, and 1 M NaOH solutions at room temperature. The half-life for MDMA was 6.6 h and for MDA was 7.1 h under the extreme conditions of 90 degrees C and 6 M HCl. MDMA and MDA were highly stable for 28 h in plasma at 25 degrees and 39 degrees C. The concentrations of the drugs were unchanged in frozen plasma after 47 days. The apparent red blood cell-plasma partition coefficient determined from assayed concentrations of the drugs in plasma and erythrocytes was 1.45 for both MDMA and MDA. An equation is presented to correct drug concentration in erythrocytes for the trapped equilibrated plasma/buffer in the packed red blood cells. The fraction of MDMA and MDA bound to dog plasma proteins was determined by several methods and it is 0.34-0.40 for both drugs. The extent of protein binding was independent of the drugs' concentration.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 1","pages":"9-14"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12842226","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
Bioavailability of ketoprofen from orally administered ketoprofen-dextran ester prodrugs in the pig. 口服酮洛芬-葡聚糖酯前药酮洛芬在猪体内的生物利用度。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
C Larsen, B H Jensen, H P Olesen
{"title":"Bioavailability of ketoprofen from orally administered ketoprofen-dextran ester prodrugs in the pig.","authors":"C Larsen,&nbsp;B H Jensen,&nbsp;H P Olesen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The bioavailability of ketoprofen after oral administration of aqueous solutions of various ketoprofen-dextran ester prodrugs in pigs was assessed. Conjugates derived from dextran fractions in the molecular weight range 10,000-500,000 were employed. Compared to the administration of an oral solution of an equivalent dose of parent ketoprofen, the average absorption fractions for the different prodrugs ranged from 100 to 67%. Relatively small inter-individual variation of ketoprofen bioavailability was observed. Apparently, the molecular size of the employed dextran transport group only has a minor influence on the pharmacokinetic parameters. The ketoprofen plasma profiles for all the administered prodrugs exhibited a characteristic lag time of ketoprofen appearance in the blood (2-3 h). Quite similar results were obtained from identical experiments carried out in the pig, employing naproxen-dextran esters. Thus, the present study adds support to a more versatile application of the dextran ester prodrug approach to providing selective colon delivery of drugs possessing a carboxylic acid functional group.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 2","pages":"71-6"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12881152","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
Macromolecular prodrugs. IXX. Kinetics of hydrolysis of benzyl dextran carbonate ester conjugates in aqueous buffer solutions and human plasma. 大分子高活性化合物。IXX。碳酸苄葡聚糖酯缀合物在缓冲水溶液和人血浆中的水解动力学。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
H Weibel, L S Nielsen, C Larsen, H Bundgaard
{"title":"Macromolecular prodrugs. IXX. Kinetics of hydrolysis of benzyl dextran carbonate ester conjugates in aqueous buffer solutions and human plasma.","authors":"H Weibel,&nbsp;L S Nielsen,&nbsp;C Larsen,&nbsp;H Bundgaard","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Benzyl carbonate esters of dextran with varying degrees of substitution have been synthesized. The kinetics of the hydrolytic cleavage of the carbonate ester bond in aqueous solution within the pH range 0.44-10.46 (37 degrees C) has been investigated. The degradation reactions followed pseudo-first-order kinetics and a rate expression encompassing hydrogen ion-, hydroxide ion- and water-catalyzed hydrolysis of the dextran conjugates was derived. No influence of the degree of substitution on the reaction rates was observed. In alkaline solution a slightly enhanced lability of trifluorethyl benzyl carbonate ester compared to the benzyl dextran carbonate esters was observed, indicating a lack of any significant intramolecular catalytic effect in the hydrolysis of the dextran esters. Almost identical rates of liberation of benzyl alcohol were found in 80% human plasma and aqueous buffer of pH 7.4, indicating the lack of enzyme-mediated cleavage of the dextran carbonate ester bond.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 3","pages":"159-62"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12887788","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
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