发布求助
文献互助 智能选刊 最新文献

Acta pharmaceutica Nordica最新文献

筛选
英文 中文
Molecular and crystal structure of the hydrochloride monohydrate of (R)-N-[[1-(4-fluorobenzyl)-2-pyrrolidinyl]methyl]-5-bromo-2,3- dimethoxybenzamide, NCQ 115, a novel dopamine D2 receptor antagonist. 新型多巴胺D2受体拮抗剂(R)- n -[[1-(4-氟苄基)-2-吡咯烷基]甲基]-5-溴-2,3-二甲氧基苯甲酰胺NCQ 115盐酸盐一水合物的分子和晶体结构
Acta pharmaceutica Nordica Pub Date : 1992-01-01
I Csöregh, T Högberg
{"title":"Molecular and crystal structure of the hydrochloride monohydrate of (R)-N-[[1-(4-fluorobenzyl)-2-pyrrolidinyl]methyl]-5-bromo-2,3- dimethoxybenzamide, NCQ 115, a novel dopamine D2 receptor antagonist.","authors":"I Csöregh,&nbsp;T Högberg","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The structure and absolute configuration of the title compound have been determined by single crystal X-ray diffraction analysis. The space group symmetry is R21; the monoclinic unit cell contains two molecules and has the dimensions a = 12.4291(8), b = 7.4511(5), c = 12.7854(7) angstroms and beta = 102.295(7) degrees. The planar conformation of the benzamide moiety is stabilized by an intramolecular (N)H...O bond. Hydrogen bonds connect the chloride anion to the protonated pyrrolidine N atom, and also the crystal water to the carbonyl oxygen of the amide group. The molecule has a folded conformation in which the N-fluorobenzyl substituent of the pyrrolidine ring and the H-bonded pseudo ring of the benzamide moiety are arranged in a sandwich-like manner. In the crystal, intermolecular hydrogen bonds link the drug molecules via the chloride anion and the hydrate molecule into endless helical chains around the twofold axis. The absolute configuration was determined by comparison of the wRtot values, 0.037 and 0.040, calculated using all measured 2027 unique, non-zero reflections and assuming R and S configuration for the chiral center, respectively. Refinement of the structural model with an R configuration resulted in the final indices of R = 0.031 and wR = 0.033 for 1512 reflections with I/delta(I) greater than 3.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"1-4"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12558489","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
Relative bioavailability in man of noscapine administered in lozenges and mixture. 诺斯卡平在人体内的相对生物利用度。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
L N Jensen, L L Christrup, L Jacobsen, J Bonde, H Bundgaard
{"title":"Relative bioavailability in man of noscapine administered in lozenges and mixture.","authors":"L N Jensen,&nbsp;L L Christrup,&nbsp;L Jacobsen,&nbsp;J Bonde,&nbsp;H Bundgaard","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The bioavailability of noscapine base administered in lozenges in a dose of 100 mg to twelve healthy volunteers, in a study using an open balanced cross-over design, was compared with that of 100 mg of noscapine hydrochloride given perorally as a mixture. The bioavailability of noscapine after administration in lozenges was significantly higher than that after administration of the drug as a mixture. It is concluded that the lozenges containing noscapine base may be a valuable alternative to the conventional noscapine hydrochloride mixture.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 4","pages":"309-12"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12469303","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
Optimization of a matrix tablet formulation using a mixture design. 用混合设计优化基质片的配方。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
P J Waaler, C Graffner, B W Müller
{"title":"Optimization of a matrix tablet formulation using a mixture design.","authors":"P J Waaler,&nbsp;C Graffner,&nbsp;B W Müller","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The simplex centroid design was applied to the optimization of a modified release tablet formulation. A base granulation was made with the active ingredient naftidrofuryl. The variables investigated included fractions of the excipients microcrystalline cellulose, lactose and dicalcium phosphate dihydrate. The release rate, crushing strength, friability and weight variation were determined as response parameters. Mathematical models were fitted to the data obtained by the lattice method, described by Scheffé and by means of multiple linear regression. Regression analysis indicated a relatively good fit of the models. On the basis of the regression models, contour plots were constructed. An increase in the amount of dicalcium phosphate caused lower release rate and increased weight variation. An increase in the content of lactose showed lower strength and increased friability, whereas an increase in the amount of microcrystalline cellulose had the opposite effect.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"9-16"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12683777","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
Predictive animal sensitization assays. 预测性动物致敏试验。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
K E Andersen
{"title":"Predictive animal sensitization assays.","authors":"K E Andersen","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"127"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560678","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
A quantitative structure-activity relationship for some dopamine D2 antagonists of benzamide type. 苯甲酰胺型多巴胺D2拮抗剂的定量构效关系。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
U Norinder, T Högberg
{"title":"A quantitative structure-activity relationship for some dopamine D2 antagonists of benzamide type.","authors":"U Norinder,&nbsp;T Högberg","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A quantitative structure-activity relationship (QSAR) for some 6-methoxybenzamides having 1-ethyl-2-pyrrolidinylmethyl side chains with respect to the inhibition of [3H]spiperone binding is established using the PLS method. An experimental design approach to select the training set compounds is demonstrated. The established relationship between structure and in vitro activity indicates the dominating influence of the substituents in the 3-position as well as the importance of (S)-configuration in the side chain. A methoxy substituent in the 5-position is also beneficiary for high activity. Both salicylamides and non-salicylamides could be accommodated in the analysis, which supports the notion of a common binding site in the receptor.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 2","pages":"73-8"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12560680","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 alkaloids of the roots of Thalictrum flavum L. 黄沙锥根生物碱的研究。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
M Velcheva, H Dutschewska, G Samuelsson
{"title":"The alkaloids of the roots of Thalictrum flavum L.","authors":"M Velcheva,&nbsp;H Dutschewska,&nbsp;G Samuelsson","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The main alkaloid in the roots of Thalictrum flavum is berberine. The alkaloids glaucine, thalicsimidine, thaliglucine, thalidazine, hernandezine and thalfoetidine were also isolated.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"57-8"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12683775","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
Role of temperature and moisture, on monomer content of freeze-dried human albumin. 温度和水分对冻干人白蛋白单体含量的影响。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
T Moreira, L Cabrera, A Gutierrez, A Cádiz, M E Castellano
{"title":"Role of temperature and moisture, on monomer content of freeze-dried human albumin.","authors":"T Moreira,&nbsp;L Cabrera,&nbsp;A Gutierrez,&nbsp;A Cádiz,&nbsp;M E Castellano","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 1","pages":"59-60"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12683776","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
Degradation of tauromustine (TCNU) in aqueous solutions. 牛磺酸丁(TCNU)在水溶液中的降解。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
T Loftsson, J Baldvinsdóttir
{"title":"Degradation of tauromustine (TCNU) in aqueous solutions.","authors":"T Loftsson,&nbsp;J Baldvinsdóttir","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The stability of tauromustine in buffered aqueous solutions was investigated over the pH range 0.9-7.5. The pH rate profile at zero buffer concentration has a specific acid catalytic region at pH below 2, a plateau of pH-independent degradation between pH 2 and 4, and shows a sharp increase in the degradation rate at pH above 4. The activation parameters, the solvent isotope effect and the effect of the dielectric constant on the degradation rate were determined, and possible degradation mechanisms were discussed. The effects of six cyclodextrin (CD) derivatives on the stability of tauromustine in aqueous buffer solutions were investigated. All the CDs tested had some stabilizing effect on the drug at pH 1.98 and 4.06 but they had little or no effect at pH 6.38. Hydroxypropyl-alpha-cyclodextrin (HP alpha CD) had the largest stabilizing effect. Tauromustine degraded about 25 to 50% slower in aqueous buffer solutions containing 2% HP alpha CD compared to buffer solutions containing no CD.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 3","pages":"129-32"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12590841","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
Human skin permeability studies of desmopressin and some prodrug derivatives. 去氨加压素及一些前药衍生物的人体皮肤渗透性研究。
Acta pharmaceutica Nordica Pub Date : 1992-01-01
A H Kahns, J Møss, H Bundgaard
{"title":"Human skin permeability studies of desmopressin and some prodrug derivatives.","authors":"A H Kahns,&nbsp;J Møss,&nbsp;H Bundgaard","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"4 3","pages":"187-8"},"PeriodicalIF":0.0,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12590070","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
Removal of inhaled 99mTc-labelled particles of disodium cromoglycate from the lungs. 从肺中去除吸入的99mtc标记的甘糖二钠颗粒。
Acta pharmaceutica Nordica Pub Date : 1991-01-01
P Vidgren, M Vidgren, P Paronen, P Vainio, P Karjalainen, J Nuutinen
{"title":"Removal of inhaled 99mTc-labelled particles of disodium cromoglycate from the lungs.","authors":"P Vidgren,&nbsp;M Vidgren,&nbsp;P Paronen,&nbsp;P Vainio,&nbsp;P Karjalainen,&nbsp;J Nuutinen","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Disodium cromoglycate particles were labelled with 99mTc by spray-drying technique. The in vitro dissolution profile as well as the leakage of radioactivity from the drug particles were determined using a through-flow cell method. The radioactive drug particles were mixed with a lactose carrier and inhaled from a dry powder device by five healthy volunteers. The removal of the inhaled drug particles from the lungs was evaluated by a gamma camera. A close relationship between the dissolution of the drug as such and the leakage of radioactivity was noted. Gamma scintigraphy indicated a biphasic exponential removal of radioactivity from the lung region. The slow component with the halftime of about 55 min was mainly due to the dissolution of drug particles in the lungs. The halftime of the fast component describing mucociliary clearance was less than 10 min. This process was the dominating one for the removal of the drug from the lungs. The experiment thus showed that the main fraction of the inhaled dose was deposited in the tracheobronchial region. Accordingly, only a small portion of the dose initially deposited in the lung can be absorbed and induce a therapeutic effect.</p>","PeriodicalId":7082,"journal":{"name":"Acta pharmaceutica Nordica","volume":"3 3","pages":"155-8"},"PeriodicalIF":0.0,"publicationDate":"1991-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12956684","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
首页 上一页 下一页 尾页
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整，为了账户安全，请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们：info@booksci.cn Book学术提供免费学术资源搜索服务，方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号：604180095
Book学术官方微信
小红书