Arzneimittel-Forschung-Drug Research最新文献

筛选
英文 中文
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,&nbsp;S A Moallem,&nbsp;M Moshiri,&nbsp;M S Sarnavazi,&nbsp;L Etemad","doi":"10.1055/s-0032-1311635","DOIUrl":"https://doi.org/10.1055/s-0032-1311635","url":null,"abstract":"<p><p>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.</p>","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
{"title":"Synthesis and Biological Activities of Some 1,3-Benzoxazol-2(3H)-One Derivatives as Anti-Quorum Sensing Agents.","authors":"A M Miandji,&nbsp;S Ulusoy,&nbsp;Y Dündar,&nbsp;S Ozgen,&nbsp;F K Onurdağ,&nbsp;G Boşgelmez-Tınaz,&nbsp;N Noyanalpan","doi":"10.1055/s-0032-1315825","DOIUrl":"https://doi.org/10.1055/s-0032-1315825","url":null,"abstract":"","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"e2"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1315825","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30649813","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: 1
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,&nbsp;S Ghanbarzadeh,&nbsp;H Valizadeh","doi":"10.1055/s-0032-1312600","DOIUrl":"https://doi.org/10.1055/s-0032-1312600","url":null,"abstract":"<p><p>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.</p>","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
{"title":"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.","authors":"T K Kim,&nbsp;H H Yoo,&nbsp;J H Park","doi":"10.1055/s-0032-1312665","DOIUrl":"https://doi.org/10.1055/s-0032-1312665","url":null,"abstract":"<p><p>In this study, the pharmacokinetics of 2 forms of mirodenafil, namely the base form and the hydrochloride salt form, were investigated in rats. The 2 forms were orally administered to rats and the plasma concentrations of mirodenafil were determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The mirodenafil base and hydrochloride salt forms showed similar pharmacokinetic profiles in terms of their maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC). The time to peak concentration (Tmax) of the base form was slightly greater than that of the salt form, but this difference was not statistically significant. These results suggest that the mirodenafil base and hydrochloride forms are pharmacokinetically equivalent in rats, and thus the base form could be used in various mirodenafil formulations as a substitute for the existing mirodenafil hydrochloride form.</p>","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 7","pages":"351-4"},"PeriodicalIF":0.0,"publicationDate":"2012-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1312665","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30686386","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
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,&nbsp;P Pedroso,&nbsp;A Filipe,&nbsp;R I Neves,&nbsp;M Tanguay,&nbsp;A Torns","doi":"10.1055/s-0032-1309042","DOIUrl":"https://doi.org/10.1055/s-0032-1309042","url":null,"abstract":"<p><p>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.</p>","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,&nbsp;A Qaddomi,&nbsp;S Khammash","doi":"10.1055/s-0032-1311609","DOIUrl":"https://doi.org/10.1055/s-0032-1311609","url":null,"abstract":"<p><strong>Background and the purpose of the study: </strong>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.</p>","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
Effect of triptolide on progesterone production from cultured rat granulosa cells. 雷公藤甲素对培养的大鼠颗粒细胞产生孕酮的影响。
Arzneimittel-Forschung-Drug Research Pub Date : 2012-06-01 Epub Date: 2012-05-16 DOI: 10.1055/s-0032-1309041
J Zhang, Z Jiang, X Mu, J Wen, Y Su, L Zhang
{"title":"Effect of triptolide on progesterone production from cultured rat granulosa cells.","authors":"J Zhang,&nbsp;Z Jiang,&nbsp;X Mu,&nbsp;J Wen,&nbsp;Y Su,&nbsp;L Zhang","doi":"10.1055/s-0032-1309041","DOIUrl":"https://doi.org/10.1055/s-0032-1309041","url":null,"abstract":"<p><p>Triptolide(CAS 38748-32-2), a major active component of Tripterygium wilfordii Hook F (TWHF), is known to have multiple pharmacological activities. However, studies have also shown that triptolide is highly disrupt to the reproductive system by disrupting normal steroid hormone signaling. In the present study, we investigated the effect of triptolide (5, 10, or 20 nM for 24 h) on progesterone production by rat granulosa cells. Triptolide inhibited both basal and human chorionic gonadotropin (HCG)- and 8-bromo-cAMP-stimulated progesterone production as revealed by RIA assay. Furthermore, the HCG-evoked increase in cellular cAMP content was also inhibited by triptolide, indicating that disruption of the cAMP/PKA signaling pathway may mediate the deleterious effects of triptolide on progesterone regulation. In addition, triptolide inhibited 25-OH-cholesterol-stimulated progesterone production, suggesting that activity of the P450 side chain cleavage (P450scc) enzyme was also be inhibited by triptolide. Western blot and quantitative real-time PCR (qRT-PCR) assays further revealed that triptolide decreased mRNA and protein expression of P450scc and the steroidogenic regulatory (StAR) protein in granulosa cells. In contrast, cell viability tests using 3-(4,5-dimethyl-thiazol-2-yl)-2,5- diphenyl-tetrazolium bromide (MTT) indicated that triptolide did not cause measurable cell death at doses that suppressed steroidogenesis. The reproductive toxicity of triptolide may be caused by disruption of cAMP/PKA-mediated expression of a number of progesterone synthesis enzymes or regulatory proteins, leading to reduced progesterone synthesis and reproductive dysfunction.</p>","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 6","pages":"301-6"},"PeriodicalIF":0.0,"publicationDate":"2012-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1309041","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30622876","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: 17
Determination of norcantharidin in mouse tissues by liquid chromatography coupled to tandem mass spectrometry and its tissue distribution study. 液相色谱-串联质谱法测定小鼠组织中去甲斑蝥素的含量及组织分布研究。
Arzneimittel-Forschung-Drug Research Pub Date : 2012-06-01 Epub Date: 2012-04-02 DOI: 10.1055/s-0032-1308980
R Zhang, J Wang, G Yuan, C Wei, X Liu, B Wang, H Gao, R Guo
{"title":"Determination of norcantharidin in mouse tissues by liquid chromatography coupled to tandem mass spectrometry and its tissue distribution study.","authors":"R Zhang,&nbsp;J Wang,&nbsp;G Yuan,&nbsp;C Wei,&nbsp;X Liu,&nbsp;B Wang,&nbsp;H Gao,&nbsp;R Guo","doi":"10.1055/s-0032-1308980","DOIUrl":"https://doi.org/10.1055/s-0032-1308980","url":null,"abstract":"<p><p>The purpose of this study is to determine the concentrations of norcantharidin (CAS NO: 5442-12-6) in mouse tissues and investigate its tissue distribution after intragastric administration of disodium norcantharidate solution. A highly sensitive and specific liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed and validated, using ribavirin (CAS NO: 36791-04-5) as the internal standard (IS). Norcantharidin and IS were extracted from 0.3 mL tissue homogenates using protein precipitation with acetone under acid condition. The analyte was separated on a C18 reverse phase column and analyzed by MS/MS in the multiple reaction monitoring (MRM) mode using ESI with positive ionization, m/z 169→123 for norcantharidin and m/z 267→135 for IS. The developed method was validated over a linear range of concentrations 0.01~5 μg·mL - 1 in liver, lung, kidney, stomach, small intestine, uterus and testis, 0.005~0.5 μg·mL - 1 in heart, spleen and brain, the correlation coefficients (r2) were between 0.9918 and 0.9976. The tissue distribution study result was as follows: The AUC0-t of norcantharidin in tissues was in the order as follows: small intestine, stomach, uterus, kidney, testis, liver, lung, spleen, heart, brain.</p>","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":" ","pages":"290-4"},"PeriodicalIF":0.0,"publicationDate":"2012-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1308980","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39971686","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: 1
Novel brain targeting prodrugs of naproxen based on dimethylamino group with various linkages. 基于多键二甲基氨基的萘普生新脑靶向前药。
Arzneimittel-Forschung-Drug Research Pub Date : 2012-06-01 Epub Date: 2012-03-09 DOI: 10.1055/s-0032-1306273
Q Zhang, Z Liang, L Y Chen, X Sun, T Gong, Z R Zhang
{"title":"Novel brain targeting prodrugs of naproxen based on dimethylamino group with various linkages.","authors":"Q Zhang,&nbsp;Z Liang,&nbsp;L Y Chen,&nbsp;X Sun,&nbsp;T Gong,&nbsp;Z R Zhang","doi":"10.1055/s-0032-1306273","DOIUrl":"https://doi.org/10.1055/s-0032-1306273","url":null,"abstract":"<p><p>As a preventive and treatment drug for Alzheimer's disease (AD), naproxen's clinical application is hampered by its limited distribution in the brain. To increase the delivery of naproxen across the blood-brain barrier (BBB), 3 prodrugs (P1, P2 and P3) of naproxen were synthesized through either ester bond or amido bond using the dimethylamino moiety as a brain-targeting ligand. The in vitro release of naproxen from the 3 prodrugs was studied in PBS, rat plasma and brain homogenate. P3 with an amido bond appeared to be highly stable in all incubation media, whereas P1 and P2 with ester bonds were partially hydrolyzed in alkaline environment and brain homogenate to yield the parent drug. After i. v. administration to rats, the brain concentration of total naproxen (summation of released and bound naproxen, TN) of P1, P2 and P3 groups were 28.81, 24.51 and 15.54 times greater than that of the control naproxen group at 5 min, respectively, and the brain AUC0-t were 6.94, 10.06 and 6.70 times greater than that of the control naproxen group. In addition, the Cmax of TN in the brain after the administration of prodrugs with ester bonds (P1 and P2) was higher than that of the amide prodrug (P3). The results highlighted the possibility of brain delivery of naproxen using prodrug strategies based on the brain-targeting ligand with dimethylamino moiety, in which the linkage between drug and targeting group might play an important role in modulating the in vivo behaviors of these prodrugs.</p>","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":" ","pages":"261-6"},"PeriodicalIF":0.0,"publicationDate":"2012-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1306273","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40155749","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: 12
Phase IV study comparing diurnal glycemic profile following the administration of 2 NPH plus regular human DNA recombinant insulin regimens in type 1 diabetes mellitus (T1DM) adult patients. 比较1型糖尿病(T1DM)成年患者服用2种NPH和常规人DNA重组胰岛素方案后的日血糖谱的IV期研究。
Arzneimittel-Forschung-Drug Research Pub Date : 2012-06-01 Epub Date: 2012-03-21 DOI: 10.1055/s-0032-1306274
E C Feleder, G A Yerino, E K Halabe, J L Tombazzi, J M Farias
{"title":"Phase IV study comparing diurnal glycemic profile following the administration of 2 NPH plus regular human DNA recombinant insulin regimens in type 1 diabetes mellitus (T1DM) adult patients.","authors":"E C Feleder,&nbsp;G A Yerino,&nbsp;E K Halabe,&nbsp;J L Tombazzi,&nbsp;J M Farias","doi":"10.1055/s-0032-1306274","DOIUrl":"https://doi.org/10.1055/s-0032-1306274","url":null,"abstract":"<p><p>Intensive insulin therapy (IIT) based on multiple daily injections of long plus rapid-acting insulin has been demonstrated to reduce mortality and morbidity associated with chronic hyperglycemia in T1DM patients. The objective of this study was to assess and compare the postprandial glycemic profile over a diurnal 12 h-period produced by the administration of a new NPH plus regular human DNA recombinant IIT (test regimen) relative to the reference IIT in T1DM patients. A phase IV, single-center, open-label, randomized, multiple-dose, balanced, cross-over study in 12 T1DM patients was conducted. Patients were assigned to receive either the test (Densulin® N (NPH) plus Densulin® R (regular),100 UI/ml, Denver Farma, Argentina) followed by the reference (InsulatardHM® (NPH) plus ActrapidHM®,100 UI/ml, Novo Nordisk Pharma Argentina) regimens or viceversa, according to a random sequence. Each treatment regimen consisted of 2 phases of an ambulatory run-in period of 7 days followed by 12 h confinement period. Blood glucose levels were measured. Glycemic profile was evaluated through glycemic plasma-concentration time curves, area under the time-concentration glycemic curves from basal to 2 h (GlyAUC0-2) and to 12 h (GlyAUC0-12) postprandial, and maximum glycemic postprandial concentration (GlyCmax). 12 hour glycemic concentration-time curves were similar for both test and reference regimens. Geometric least square means ratios Test/ref regimens and their 90% confidence interval for GlyAUC0-2, GlyAUC0-12 and GlyCmax were 94.33 (81.13-125.09), 107.75 (94.05-123.45) and 105 (92.89-118.68), respectively. Both regimens presented similar safety profile. This study demonstrated that the new human DNA recombinant NPH and regular insulin is equally effective to the reference regimen for postprandial diurnal glycemic profile.</p>","PeriodicalId":56084,"journal":{"name":"Arzneimittel-Forschung-Drug Research","volume":"62 6","pages":"267-73"},"PeriodicalIF":0.0,"publicationDate":"2012-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0032-1306274","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30520609","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
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
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