Arzneimittel-Forschung-Drug Research最新文献_第7页

In vitro and in vivo evaluation of Triptolide-loaded pluronic P105 polymeric micelles. 雷公藤甲素负载pluronic P105聚合物胶束的体内外评价。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-15 DOI: 10.1055/s-0032-1312602

H Li, X-S Wen, W Di

引用次数: 6

Synthesis and biological activities of some 1,3-benzoxazol-2(3H)-one derivatives as anti-quorum sensing agents. 反群体感应剂1,3-苯并恶唑-2(3H)- 1衍生物的合成及生物活性研究。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-15 DOI: 10.1055/s-0032-1312590

A M Miandji, S Ulusoy, Y Dündar, S Ozgen, F K Onurdağ, G Boşgelmez-Tınaz, N Noyanalpan

{"title":"Synthesis and biological activities of some 1,3-benzoxazol-2(3H)-one derivatives as anti-quorum sensing agents.","authors":"A M Miandji, S Ulusoy, Y Dündar, S Ozgen, F K Onurdağ, G Boşgelmez-Tınaz, N Noyanalpan","doi":"10.1055/s-0032-1312590","DOIUrl":"https://doi.org/10.1055/s-0032-1312590","url":null,"abstract":"Antibiotics are commonly used to treat microbial infections. Due to misuse or large-scale use of antibiotics, many pathogens have gained resistance which makes antibiotic treatments ineffective. The discovery that many bacteria use quorum sensing (QS) to regulate their virulence factor and pathogenicity production makes the QS system an attractive target for antimicrobial therapy. A series of 1,3-benzoxazol-2(3H)-one derivatives were designed and synthesized as QS inhibitors (QSIs) and tested for their QS inhibitory activities. In vitro quorum sensing inhibitor screen (QSIS) assay indicated that the 1,3-benzoxazol-2(3H)-one (compound 1), 5-chloro-1,3-benzoxazol-2(3H)-one (compound 6), 6-methyl-1,3-benzoxazol-2(3H)-one (compound 11), and 5-methyl-1,3-benzoxazol-2(3H)-one (compound 16), inhibit QS system in quorum sensing selector (QSIS)1 strain. These 4 QSIs also significantly reduced elastase production, biofilm formation and swarming motility of Pseudomonas aeruginosa PA01 strain. These results suggest that compound 1, 6, 11 and 16 may provide a starting point for the design and development of new anti-pathogenic drugs that restrict virulence of P. aeruginosa and possibly other clinically important human pathogens. In addition, these QSI molecules could potentially be used in combination with conventional antibiotics to increase the efficiency of disease control and to extend the life span of established antimicrobials.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"330-4"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1312590","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30620063","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: 13

The novel phenylpropiophenone derivates induced relaxation of isolated rat aorta. 新型苯丙烯酮衍生物诱导离体大鼠主动脉舒张。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-24 DOI: 10.1055/s-0032-1312617

B Ivković, S Vladimirov, R Novaković, V Cupić, H Heinle, L Gojković-Bukarica

{"title":"The novel phenylpropiophenone derivates induced relaxation of isolated rat aorta.","authors":"B Ivković, S Vladimirov, R Novaković, V Cupić, H Heinle, L Gojković-Bukarica","doi":"10.1055/s-0032-1312617","DOIUrl":"https://doi.org/10.1055/s-0032-1312617","url":null,"abstract":"Our aim was to define how different chemical properties of newly developed phenylpropiophenone derivates (PhPds) influenced their potency and efficacy to relax rat aorta. A contribution of ion channels in the PhPds and propafenone mechanism of vasodilatation was tested. PhPds were syntethysed by substitution in the benzyl moiety with -F, -CH3 or -CF3 groups on the ortho or para position. The vasodilatation by PhPds was examined on the rings of rat aorta precontracted with phenylephrine. In order to test involvement of voltage-gated Na+ and K+ channels and L-type Ca2+ channels in a mechanism of action of PhPds, we used their blockers: lidocaine, nifedipine and 4-aminopiridine, respectively. Aorta was more sensitive to 5-ortho-trifluoromethyl derivate than to propafenone and other PhPds. The 5-para-methyl derivate had lower potency and efficacy than propafenone and other PhPds. Lidocaine did not influenced relaxation induced by PhPds, but slightly inhibited the effect of propafenone. The 4-aminopiridine only inhibited relaxation induced by 5-para-methyl derivate. Nifedipine inhibited relaxation of the rat aorta induced by 5-ortho-trifluoromethyl derivate and by propafenone. Introduction of 5-ortho-trifluoromethyl and 5-para-methyl group in the benzyl moiety of propafenone molecule changed its potency, efficacy and mechanism of action in the rat aorta. The 4-aminopiridine- and nifedipine sensitive ion channels are involved in mechanism of action of 5-para-methyl and 5-ortho-trifluoromethyl derivate. The introduction of other tested groups in the benzyl moiety does not affect pharmacological properties of the PhPds in relation to propafenone.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"345-50"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1312617","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30642848","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: 3

Anti-nociceptive and anti-inflammatory effects of cyanocobalamin (vitamin B12) against acute and chronic pain and inflammation in mice. 氰钴胺素(维生素B12)对小鼠急性和慢性疼痛和炎症的抗伤害和抗炎作用。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-15 DOI: 10.1055/s-0032-1311635

H Hosseinzadeh, S A Moallem, M Moshiri, M S Sarnavazi, L Etemad

{"title":"Anti-nociceptive and anti-inflammatory effects of cyanocobalamin (vitamin B12) against acute and chronic pain and inflammation in mice.","authors":"H Hosseinzadeh, S A Moallem, M Moshiri, M S Sarnavazi, L Etemad","doi":"10.1055/s-0032-1311635","DOIUrl":"https://doi.org/10.1055/s-0032-1311635","url":null,"abstract":"In this study, the anti-nociceptive and anti-inflammatory effects of cyanocobalamin (Vit B12) against acute and chronic pain and inflammation were evaluated in mice. Vit B12 (0.87, 1 and 1.77 mg/kg) were injected intraperitoneally. The anti-nociceptive effects against acute pain were examined using hot-plate and writhing tests. The chronic pain was examined 14 days after sciatic nerve ligation using the hot-plate test. Morphine (10 mg/kg) was used as a positive control. Anti-inflammatory effects of Vit B12 against acute and chronic inflammation were assessed using xylene-induced edema in ears and granuloma caused by compressed cotton implantation, respectively. In these tests, sodium diclofenac (15 mg/kg) was used as a positive control. Vit B12 showed a dose related effect in acute anti-nociceptive test and increased the anti-nociceptive effect of morphine in chronic treatment. Vit B12 demonstrated an anti-nociceptive effect in chronic studies as single or continues daily treatment and increased significantly the anti-nociceptive effect of morphine. All doses of Vit B12 significantly decreased xylene-induced ear edema. Maximum anti-inflammatory effect (37.5%) was obtained at dose of 1 mg/kg. In chronic inflammation, Vit B12 significantly decreased granuloma formation in mice. In conclusion our work presents some experimental evidence supporting the administration of cyanocobalamin in controlling acute and chronic neuropathic pain. Cyanocobalamin may have anti-inflammatory effect. It may reduce tolerance to anti-nociceptive effect of morphine as well.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"324-9"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1311635","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30619643","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: 42

Synthesis and Biological Activities of Some 1,3-Benzoxazol-2(3H)-One Derivatives as Anti-Quorum Sensing Agents. 抗群体感应剂1,3-苯并恶唑-2(3H)- 1衍生物的合成及其生物活性

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-25 DOI: 10.1055/s-0032-1315825

A M Miandji, S Ulusoy, Y Dündar, S Ozgen, F K Onurdağ, G Boşgelmez-Tınaz, N Noyanalpan

引用次数: 1

Pharmacokinetics and cardiovascular effect of etoricoxib in the absence or presence of St. John's Wort in rats. 在没有或存在圣约翰草的大鼠体内，依托昔布的药代动力学和心血管效应。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-04-27 DOI: 10.1055/s-0032-1309043

M A Radwan, N A A Baky, I Zaghloul, H Y Aboul-Enein

{"title":"Pharmacokinetics and cardiovascular effect of etoricoxib in the absence or presence of St. John's Wort in rats.","authors":"M A Radwan, N A A Baky, I Zaghloul, H Y Aboul-Enein","doi":"10.1055/s-0032-1309043","DOIUrl":"https://doi.org/10.1055/s-0032-1309043","url":null,"abstract":"The effect of chronic administration of etoricoxib (EXB), in the absence or presence of St. John's Wort (SJW), on its pharmacokinetic parameters and blood pressure was investigated in rats.Rats were divided into 3 groups, each group received daily different oral treatment for 3 weeks. Rats' blood pressures were monitored initially, after 1 and 3 weeks of treatment, and after 1 week of discontinuing dosing of both drugs. EXB pharmacokinetic parameters in the absence or presence of SJW were calculated after 3 weeks.SJW was significantly affected EXB pharmacokinetic parameters. The steady state peak plasma concentration and terminal half-life were reduced by 32% and 91%, respectively, due to a > 3 fold increase in its apparent clearance which is a concentration and time dependent effect. EXB was significantly increased (P<0.001) Rats' blood pressure while, co-administration of EXB and SJW was not significantly affect (P>0.05) rats' blood pressure as compared to the control.Monitoring blood pressure of patients anticipated taking EXB for extended period should be advised. The co-administration of SJW with EXB should be avoided since SJW would greatly reduce EXB concentrations by inducing its metabolism.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":" ","pages":"313-8"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1309043","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40194913","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: 3

Comparative in vitro dissolution and in vivo bioequivalence of 2 pentoxifylline sustained release formulations. 2己酮茶碱缓释制剂体外溶出度及体内生物等效性比较。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-30 DOI: 10.1055/s-0032-1312600

P Zakeri-Milani, S Ghanbarzadeh, H Valizadeh

{"title":"Comparative in vitro dissolution and in vivo bioequivalence of 2 pentoxifylline sustained release formulations.","authors":"P Zakeri-Milani, S Ghanbarzadeh, H Valizadeh","doi":"10.1055/s-0032-1312600","DOIUrl":"https://doi.org/10.1055/s-0032-1312600","url":null,"abstract":"Pentoxifylline is a xanthine derivative that is indicated for the treatment of patients with intermittent claudication on the basis of chronic occlusive arterial disease of the limbs. In the present study, prior to the in vivo study, an in vitro comparative dissolution test was performed by the paddle method for 2 oral sustained release pentoxifylline tablets (400 mg) following the bioequivalence guidance of FDA. Metrics of peak exposure (Cmax) and total exposure to 24 h (AUC24) were compared using a randomized, single oral, open-label, 2-period, 2-sequence, 2 treatments crossover study in 24 healthy male volunteers under fasted conditions. After an overnight fast, the volunteers received 400 mg pentoxifylline and the blood samples were collected over a 24-h period following drug administration. Plasma drug concentrations were measured by a reverse-phase HPLC method with ultraviolet detection. In vitro dissolution tests requirements were met by both formulations. Observed exposure metrics for test and reference products were 140.6±51.5 and 132.6±48.5 ng/ml for Cmax and 986.4±350.7 and 1 035.8±350.3 ng.h/ml for AUC0-24 respectively. The confidence intervals (90%) around ratios (test/reference) of least squares means derived from logarithmic transformed exposure metrics were 0.9912-1.1564% for Cmax and 0.8886-1.0535% for AUC0-24. Therefore it can be concluded that both products are bioequivalent in terms of peak and total exposure and therefore interchangeable.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"335-9"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1312600","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30655665","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: 5

Validated LC-MS/MS method for the determination of mirodenafil in rat plasma and its application to a comparative pharmacokinetic study of the free base and hydrochloride salt forms of mirodenafil. hplc -MS/MS法测定大鼠血浆中美洛地那非的含量，并应用于美洛地那非游离碱和盐酸盐两种形式的药代动力学比较研究。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-06-12 DOI: 10.1055/s-0032-1312665

T K Kim, H H Yoo, J H Park

引用次数: 0

Bioequivalence of two formulations of escitalopram. 艾司西酞普兰两种制剂的生物等效性。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-05-24 DOI: 10.1055/s-0032-1309042

S Almeida, P Pedroso, A Filipe, R I Neves, M Tanguay, A Torns

{"title":"Bioequivalence of two formulations of escitalopram.","authors":"S Almeida, P Pedroso, A Filipe, R I Neves, M Tanguay, A Torns","doi":"10.1055/s-0032-1309042","DOIUrl":"https://doi.org/10.1055/s-0032-1309042","url":null,"abstract":"Escitalopram, CAS registry number 128196-01-0 is an orally administrated selective serotonin reuptake inhibitor (SSRI).The objective of this trial was to assess bioequivalence between an escitalopram formulation manufactured by Grupo Tecnimede and that of a European reference formulation, while evaluating both formulations' tolerability as a secondary objective.24 healthy subjects were enrolled in a single centre, randomised, single-dose, open-label, 2-way crossover study. Drug levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection, LC-MS/MS method. Pharmacokinetic parameters used for bioequivalence assessment were determined from the drug concentration data using non-compartmental analysis.Mean±Standard deviation (SD) Cmax values were 18.89±5.06 ng/mL and 18.45±5.05 ng/mL for reference and test, respectively. AUClast was 577.16±196.20 ng · h/mL after the administration of the reference and 577.69±220.88 ng · h/mL for the test. AUCinf was 595.66±203.80 ng · h/mL after the administration of the reference 596.19±235.47 ng · h/mL for the test.The 90% confidence intervals obtained by analysis of variance were 92.38-103.38% for Cmax, 94.10-104.37% for AUClast and 93.80-104.09% for AUCinf, which were within the predefined acceptable range of 80.00-125.00%. Both formulations were well tolerated, with no major side effects and no relevant differences in safety profiles observed between the preparations.The design of the study was adequate to determine the pharmacokinetic parameters of the test and the reference formulations. Bioequivalence between formulations was concluded both in terms of rate and extent of absorption.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"307-12"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1309042","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30642847","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: 3

Formulation and comparative bioavailability of 2 ciprofloxacin sustained release tablets. 2环丙沙星缓释片的处方及比较生物利用度。

Arzneimittel-Forschung-Drug Research Pub Date : 2012-07-01 Epub Date: 2012-04-27 DOI: 10.1055/s-0032-1311609

A N Zaid, A Qaddomi, S Khammash

{"title":"Formulation and comparative bioavailability of 2 ciprofloxacin sustained release tablets.","authors":"A N Zaid, A Qaddomi, S Khammash","doi":"10.1055/s-0032-1311609","DOIUrl":"https://doi.org/10.1055/s-0032-1311609","url":null,"abstract":"Background and the purpose of the study: The aim of this study is to formulate and evaluate the quality of ciprofloxacin (CAS number: 85721-33-1) sustained release tablet (Ciprocare®XR) 1 000 mg ciprofloxacin (test formulation) by comparing its pharmacokinetic parameters with Cipro®XR sustained release tablet (reference formulation). For this purpose ciprofloxacin SR tablets were developed using the 2-layer method. To assess the quality of the produced sustained release tablets a randomized, 2-way, crossover, bioequivalence study was performed in 24 healthy, male volunteers. The selected Middle Eastern volunteers were divided into 2 groups of 12 subjects. One group was treated with the reference formulation and the other one with the test formulation, with a cross-over after a drug washout period of 7 days. Blood samples were collected at fixed time intervals and Ciprofloxacin concentrations were determined by a validated HPLC assay method. The pharmacokinetic parameters AUC0-48, AUC0-∞, Cmax, Tmax, Ke and T1/2 were determined for both sustained release tablets and were compared statistically to evaluate the bioequivalence between the 2 formulations of ciprofloxacin, using the statistical model recommended by the FDA. The analysis of variance (ANOVA) did not show any significant difference between the 2 formulations and 90% confidence intervals (CI) fell within the acceptable range for bioequivalence. According to the obtained results it was concluded that the test and reference formulations are bioequivalent, since they exhibit comparable pharmacokinetic parameters.","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":" ","pages":"319-23"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1311609","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40196067","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: 3