Pharmazie (PHARMAZIE)

Publisher: Pharmazeutische Gesellschaft der DDR; Deutsche Arzneibuch-Kommission

Journal description

DiePharmazie is one of the world's leading pharmaceutical journals. As a peer-reviewed scientific journal, DiePharmazie is regularly indexed in Current Contents/Life Sciences, Excerpta Medica, Analytical Abstracts, International Pharmaceutical Abstracts, Beilstein Current Facts in Chemistry, Chemical Engineering and Biotechnology Abstracts (CEABA) and Science Citation Index. The journal DiePharmazie publishes reviews, experimental studies, letters to the editor, as well as book reviews. The following fields of pharmacy are covered: Pharmaceutical and medicinal chemistry, pharmaceutical analysis and drug control, pharmaceutical technolgy, biopharmacy (biopharmaceutics, pharmacokinetics, biotransformation), experimental and clinical pharmacology, pharmaceutical biology (pharmacognosy), history of pharmacy.

Current impact factor: 1.05

Impact Factor Rankings

2016 Impact Factor Available summer 2017
2014 / 2015 Impact Factor 1.052
2013 Impact Factor 1.003
2012 Impact Factor 0.962
2011 Impact Factor 1.006
2010 Impact Factor 0.869
2009 Impact Factor 0.812
2008 Impact Factor 0.858
2007 Impact Factor 0.775
2006 Impact Factor 0.606
2005 Impact Factor 0.677
2004 Impact Factor 0.587
2003 Impact Factor 0.696
2002 Impact Factor 0.74
2001 Impact Factor 0.498
2000 Impact Factor 0.471
1999 Impact Factor 0.446
1998 Impact Factor 0.419
1997 Impact Factor 0.504
1996 Impact Factor 0.487
1995 Impact Factor 0.466
1994 Impact Factor 0.334
1993 Impact Factor 0.34
1992 Impact Factor 0.309

Impact factor over time

Impact factor
Year

Additional details

5-year impact 1.06
Cited half-life >10.0
Immediacy index 0.19
Eigenfactor 0.00
Article influence 0.22
Website Pharmazie website
Other titles Pharmazie
ISSN 0031-7144
OCLC 1779245
Material type Periodical, Internet resource
Document type Journal / Magazine / Newspaper, Internet Resource

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: In principle, RNA interference (RNAi) allows for the inhibition of any oncogene of choice, thus leading to novel concepts in tumor therapy. For their delivery, the RNAi-inducing small RNA molecules (small interfering RNAs, siRNAs) can be formulated in various nanoparticle systems, prior to testing them in preclinical animal models. The same is true for miRNAs that have more recently been explored in therapeutic miRNA replacement strategies. This puts high demands on the properties of the nanoparticles. This review article discusses various nanoparticulate systems for RNA delivery in vivo and gives an overview of preclinical studies on siRNA- or miRNA-based tumor therapy.
    No preview · Article · Jan 2016 · Pharmazie
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    ABSTRACT: RNA-based effector molecules (nucleic acid effectors) are important tools in molecular medicine because they offer a strategy to address therapeutically interesting targets that are not "druggable" with classic small molecule inhibitors. However, for in vivo applications, RNA-based effectors require specific chemical modifications to improve their stability and pharmacokinetic properties, as well as to minimize toxic and unspecific off-target effects.
    No preview · Article · Jan 2016 · Pharmazie
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    ABSTRACT: The pharmaceutical industry is currently faced with increasing pressure due to patent expirations for block busters, healthcare reforms with strained budgets and growing demands for approval by administrative organizations like the FDA and the EMA. High attrition rates especially in the later expensive stages of the drug development process ask for thoroughly validated drug targets at the beginning of such projects. The great potential of RNA interference strategies toward reaching this goal is outlined in this article.
    No preview · Article · Jan 2016 · Pharmazie
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    ABSTRACT: The development of malignant tumors from healthy tissues is associated with profound changes in expression profiles of a large number of mRNAs, miRNAs and IncRNAs. These changes on the one hand permit insights into the biology of individual tumors; on the other hand, tumor-derived RNAs can also be detected in circulating blood and serve as specific markers for differential diagnosis and patient prognosis.
    No preview · Article · Jan 2016 · Pharmazie
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    ABSTRACT: Non-coding RNAs (ncRNAs) in eukaryotes have recently developed to a very active research area in RNA biology, opening up new strategies for diagnosis and therapies of human disease. Here we introduce and describe the most important classes of eukaryotic ncRNAs: microRNAs (miRNAs), long non-coding RNAs (IncRNAs), and circular RNAs (circRNAs). We further discuss new RNA-based diagnostic and therapeutic concepts.
    No preview · Article · Jan 2016 · Pharmazie
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    ABSTRACT: Sixteen 2-substituted ethenesulfonic acid ester derivatives were designed, synthesized and evaluated for the inhibitory activity against tyrosine phosphatase 1B (PTP1B) and T-Cell protein tyrosine phosphatase (TCPTP). The structural activity relationship (SAR) of these compounds demonstrated that the hydrophilic head, aromatic center and the hydrophobic tail affected the inhibitory activities against PTP1B and the selectivity over TCPTP. Most of the compounds exhibited excellent inhibitory activity against PTP1B with IC50 value of 1.0 mu M - 31.2 mu M. SAR analysis revealed that the hydrophilic head was indispensable in the maintain of inhibitory activity against PTP1B, the aromatic center significantly altered the selectivity of PTP1B over TCPTP, and the hydrophobic tail significantly altered the inhibitory activity against PTP1B.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: Platelet Glycoprotein IIb/IIIa inhibitors are approved for the treatment of acute coronary syndromes and percutaneous coronary interventions due to their effects on the final common pathway of platelet aggregation. Z4A5 is a new hexapeptide IIb/IIIa inhibitor with antiplatelet and antithrombotic effects. This study was performed to assess the characteristics of Z4A5 compared with another IIb/IIIa inhibitor eptifibatide. Light-transmission aggregonnetry was used to measure platelet aggregation to assess the antiplatelet efficacy of Z4A5 in vitro and ex vivo in beagles. The time course of platelet inhibition and bleeding time prolongation during i.v. bolus plus infusion and after infusion of the Z4A5 were evaluated in beagles following two 2 x 2 Latin square designs. We also compared the antithrombotic activity of Z4A5 with eptifibatide in arterial thrombosis and arteriovenous shunt thrombosis model in beagles. Our data showed that Z4A5 completely inhibited adenosine diphosphate (ADP)-, thrombin- and arachidonic acid-induced in vitro platelet aggregation with values of IC50 of 260 nM, 128.6 and 56.4 n respectively. Z4A5 also markedly and stably prevented ADP-induced ex vivo platelet aggregation and prolonged the bleeding time throughout the 8-hour infusion. Both platelet function and bleeding time returned to normal sooner after cessation of Z4A5 infusion than after eptifibatide. Z4A5 inhibited thrombosis and had the same potent antithrombotic activity as eptifibatide. In conclusion, Z4A5 has the same potent antiplatelet effect and antithrombotic activity with the advantage of a faster on and off time compared to eptifibatide.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: This study investigated the most suitable surfactant medium for the dissolution testing of a poorly soluble basic drug, namely, carvedilol reflecting the in vivo behavior. Sodium lauryl sulfate (SLS), hexadecyltrimethylannmonium bromide (CTAB) and polysorbate 80 were used as anionic, cationic and nonionic surfactants, respectively. Saturation solubilities of carvedilol were determined in the presence of SLS, CTAB and polysorbate 80 (0.5, 1 and 2% (w/v)) at pH 1.2 and 6.8. Dissolution behaviors of the commercial tablets were studied using USP apparatus II in pH 1.2, 4.5 and 6.8 buffers and pH 6.8 dissolution media with 0.5% (w/v) SLS, polysorbate 80 and CTAB. Polysorbate 80 enhanced the solubility of carvedilol irrespective of pH, while SLS and CTAB exhibited larger solubilization effect than polysorbate 80 depending on pH and the ionic nature of the surfactant. Based on in vitro dissolution profile similarity, pH 6.8 dissolution medium with 0.5% (w/v) polysorbate 80 was found to be the most biorelevant medium, which probably reflects the bioequivalence of test products to the reference product of carvedilol.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a well-known natural polyphenol compound. It is reported that resveratrol possesses strong anti-oxidative, anti-inflammatory, cardiovascular protective and cancer chemo-preventive effects. Therefore, there has been a considerable interest in its biological activity, pharmacological activity and also synthetic resveratrol analogues in recent years. Up to now, many new resveratrol derivatives have been synthesized and some new biological activities of these compounds have been found, so in the treatment of Alzheimer's disease and the inhibition of influenza H1N1 neuraminidase. Structure-activity studies revealed that crucial elements of parental components are required for specific effects. This review summarizes the available literatures on the structure-activity relationships and pharmacological properties of resveratrol analogues.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: The poor water solubility of many candidate drugs remains a major obstacle to their development and clinical use, especially for oral drug delivery. Nanocrystal technology can improve the solubility and dissolution rates of many poorly water-soluble drugs very effectively, significantly improving their oral bioavailability and decreasing the food effect. For this reason, this technology is becoming a key area of drug delivery research. This review presents much of the recent progress in nanocrystal drug pharmaceuticals, including the characteristics, composition, preparation technology, and clinical applications of these drugs. Finally, the effect of nanocrystal technology on insoluble drugs is quantified and described.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: Junctophilin2 (JP2) is a critical protein associated with cardiogenesis. lcariin (ICA) facilitated the directional differentiation of murine embryonic stem (ES) cells into cardiomyocytes. However, little is known about the effects of ICA on JP2 during cardiac differentiation. Here, we explored whether ICA has effects on the expression and Ca2+ related function of JP2 during cardiomyocyte differentiation of ES cells in vitro. Embryonid bodies (EBs) formed by hanging drop were treated with 10(-7) rinol/L ICA from day 5 to promote the cardiac differentiation. Percentage of beating EBs and number of beating area within EBs were monitored. Cardiomyocytes were purified by discontinuous percoll gradient centrifugation from EBs. The expression of JP2, a-actinin and troponin-T within EBs or isolated cardiomyocytes were analyzed by immunocytochemistry, western blot and flow cytometry. The transient Ca2+ release was characterized in cardiomyocytes treated with/without 10 mmol/L caffeine and 8 mmol/L Ca2+. Our results showed that ES cell-derived cardiomyocytes were well characterized with JP2 proteins. ICA promoted cardiomyocyte differentiation as indicated by an increased percentage of beating EBs and number of beating area within EBs. The expression of JP2, a-actinin and troponin-T were up-regulated both in EBs and isolated cardiomyocytes from EBs. Furthermore, ICA-induced JP2 expression was accompanied by a remarkable increase of the amplitude of Ca2+ transients in cardiomyocytes before/after caffeine and Ca2+ stimulating. In conclusion, ICA promotes in cardiac differentiation partly through regulating JP2 and improved the Ca2+ modulatory function of cardiomyocytes.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: This study aimed to develop a dry suspension formulation of raloxifene (RLX) using its HP-p-cyclodextrin inclusion complexes to enhance the oral bioavailability. Dry suspensions loading RLX/HP-p-cyclodextrin inclusion complexes (RLX-HICs) were prepared by solvent evaporation followed by a standard wet granulation process. The inclusion complexes were characterized by scanning electron microscopy, differential scanning calorimetry, and Fourier transform infrared spectroscopy. The features of dry suspensions such as dispersibility, flowability and dissolution were compared with conventional suspensions. Dry suspensions containing RLX-HICs dramatically increased the dissolution of RLX. Pharmacokinetic studies in rats showed that dry suspensions with RLX-HICs significantly enhanced the oral bioavailabilities of RLX. The absolute and relative bioavailabilities were up to 13.04% and 413.97% compared with the solution formulation (i.v.) and conventional suspensions (Lg.), respectively. The bioavailability improvement for dry suspensions with RLX-HICs can be attributed to improved dissolution and physiochemical properties of RLX, by which the overall absorption was enhanced. Dry suspensions prepared from RLX-HICs may be an attractive formulation for the oral delivery of RLX.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: Caco2 cells are a human adenocarcinoma cell line that forms tight junctions and are widely used to examine bidirectional drug transport as well as P-glycoprotein mediated efflux. Unfortunately Caco2 cell lines can be very heterogeneous in nature. Our aim was to improve the Caco2 cell model for determination of P-glycoprotein mediated drug transport. Young passage Caco2 from ATCC had inadequate expression of P-glycoprotein, therefore three approaches were adopted to upregulate Caco2 P-glycoprotein expression to mimic that in vivo; a) incubation of mature Caco2 monolayer with rifannpicin, b) prolonged exposure of Caco2 cells to vinblastine (generating the Caco2 VIN line), and c) splitting cells every 7 to 9 days until late passage numbers (over P80) were available. Upon development of the models, P-gp expression and activity was determined using western blotting and bidirectional transport studies of rhodamine123. All four models exhibited P-gp mediated efflux transport for rhodamine123. Incubation with rifannpicin did not alter bidirectional transport compared to passage 44 cells. Increased passage number altered P-glycoprotein expression and the efflux ratio increased to 4.7 for passage 80 from 1.4 of passage 44. The highest basolateral to apical transport was observed for both passage 89 Caco2 and the Caco2 VIN model with an efflux ratio of 13 to 14. Western blot images confirmed the increased P-glycoprotein expression of late passage and Caco2 VIN. Caco2 cells are not ready for P-gp related research when first acquired from ATCC (Passage 18). Late passage Caco2 cell nnonolayers or Caco2 VIN models are needed to determine P-gp mediated efflux transport.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: An endogenous CYP3A4 biomarker for in vivo metabolism of cyclosporine should be useful for optimizing individual dosage. We aimed to investigate if the combined ratio of endogenous 6 beta-hydroxycortisol and 6 beta-hydroxycortisone to cortisol and cortisone (HOM) in urine could be used as an endogenous probe for the prediction of cyclosporine dosage requirements in renal transplant recipients. 54 medically stable kidney transplant recipients participated in this study. Morning spot blood and urine samples were gathered. The multiple regression analysis including urinary HOM and body mass index accounted for 73.1% of variability in blood concentration/dose ratio (C/D) of cyclosporine, in which urinary HOM and body mass index contributed 64.9% and 8.2%, respectively. Based on the present approach, individual dosage regimen of CsA could be acquired without therapeutic drug monitoring and the results showed that all of the observed stable doses of CsA were within the predicted range during different post-operative periods. In summary, there is a significant relationship between endogenous CYP3A4 biomarker (assessed by urinary HOM) and in vivo metabolism of cyclosporine in renal transplant recipients. Urinary HOM and body mass index are important predictors of cyclosporine metabolism. Our findings provide clinical implications that the predictive algorithm based on a simple, safe and non-invasive CYP3A4 phenotyping can be anticipated.
    No preview · Article · Dec 2015 · Pharmazie
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    ABSTRACT: Due to the recent advances in molecular biology, there are promising gene therapy studies for prevention and treatment of cancer, genetic and infectious diseases. Many technologies in molecular biology and biotechnology were developed, and among those technologies, ‘antisense technology’ has become prominent in recent years. In this study, non-viral gene delivery systems such as solid lipid and chitosan nanoparticles were developed for improving intercellular delivery of siRNA. Commercially available Bcl-2 siRNA which is specific for Bcl-2 mRNA was used as a genetic material. Particle size, zeta potential, siRNA binding abilities and cytotoxic properties of the systems were evaluated and transfection assay was performed on among the prepared formulations. When the results of those studies were compared with Lipofectamine® 2000, prepared formulations were found to show usable results. A novel method was developed in this study for producing solid lipid nanoparticles (SLNs) with highly efficient siRNA encapsulation. The results of this study showed that the genetic materials can be encapsulated in SLNs and SLNs have the potential to be used as a transfection agents.
    No preview · Article · Nov 2015 · Pharmazie
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    ABSTRACT: APO866 is a potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), and inhibits nicotinamide adenine dinucleotide (NAD) synthesis. Our previous study showed that APO866 inhibits the proliferation of C6 glioblastoma cells, but failed to induce apoptosis. Since APO866 inhibits cellular metabolism and such metabolic stress is closely related with autophagy, thus we determined whether APO866 can induce autophagy in C6 glioblastoma cells and whether the autophagy induced by APO866 is pro-death or prosurvival. Using LC3 immunofluorescence imaging and transmission electron microscopy detection, we found that APO866 at 1-100 nM induced autophagy in C6 glioblastoma cells. APO866 at 1 nM mainly induced initial autophagic vacuoles. Whereas APO866 at 100 nM induced degrading autophagic vacuoles, as well as induced nuclei malformation and mitochondria swelling. In addition, APO866 concentration-dependently decreased the cell viability of C6 glioblastoma cells, and this effect was attenuated by autophagy inhibitors, including 3-methyladenine and LY294002. APO866 concentration-dependently decreased intracellular NAD level. Interestingly, APO866 at 1 nM slightly decreased intracellular NAD level, but dramatically increased autophagy-positive cells. The dramatical cell viability decreasing required the decreasing of intracellular NAD level to a very low threshold. Thus, our results indicated that APO866 induced pro-death autophagy in C6 glioblastoma cells by decreasing intracellular NAD, and low concentration of APO866 can be used as an autophagy inducer in autophagic-death sensitive glioblastoma.
    No preview · Article · Oct 2015 · Pharmazie
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    ABSTRACT: 3'4'7-Trihydroxyflavone is a flavonoid from ladino clover, alfalfa, and Albizzia julibrissin. In the present study, we found that 3'4'7-trihydroxyflavone markedly inhibited the receptor activator of nuclear factor kappa B ligand (RANKL) induced osteoclastic differentiation from mouse bone marrow derived macrophages (BMMs). 3'4'7-trihydroxyflavone also reduced the mRNA expression level of osteoclastic marker genes including calcitonin receptor (CTR), Cathepsin K, v-ATPase V0 subunit d2 (ATP6v0d2), and dendritic cell-specific transmembrane protein (DC-STAMP). In addition, 3'4'7-trihydroxyflavone decreased the bone resorption activity of osteoclasts on dentin slices. We found that 3'4'7-trihydroxyflavone inhibited RANKL-induced expression of nuclear factor of activated T cells c1 (NFATc1), a key transcription factor of osteoclast differentiation. Furthermore, 3'4'7-trihydroxyflavone attenuated RANKL-induced activation of p38 mitogenactivated protein kinase (MAPK) and expression of B lymphocyte-induced maturation protein 1 (Blimp1), a repressor of negative regulators of NFATc1. Taken together, our data suggest that 3'4'7-trihydroxyflavone inhibits osteoclastogenesis via NFATc1.
    No preview · Article · Oct 2015 · Pharmazie
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    ABSTRACT: Here we examined the effects of a DNA methylation inhibitor, 5-azacytidine, on melanogenesis in Mel-Ab cells. We found that 5-azacytidine decreased the melanin content and tyrosinase activity in these cells in a dose-dependent manner; importantly, 5-azacytidine was not cytotoxic at the concentrations used in these experiments. On the other hand, 5-azacytidine did not affect tyrosinase activity in a cell-free system, indicating that 5-azacytidine is not a direct tyrosinase inhibitor. Instead, 5-azacytidine decreased the protein levels of microphthalmia-associated transcription factor (MITF) and tyrosinase. Thus, we investigated the effects of 5-azacytidine on signal transduction pathways related to melanogenesis. However, 5-azacytidine did not have any effect on either Akt or glycogen synthase kinase 3β (GSK3β) phosphorylation. The phosphorylation of cAMP response element-binding protein (CREB) is well known to regulate MITF expression, thereby also regulating tyrosinase expression. We found that 5-azacytidine decreased the phosphorylation of CREB. Therefore, we propose that 5-azacytidine may decrease melanin synthesis by downregulating MITF and tyrosinase via CREB inactivation.
    No preview · Article · Oct 2015 · Pharmazie
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    ABSTRACT: Rituximab (RTX), a monoclonal antibody against CD20, is known to cause fewer side effects than conventional anti-cancer drugs; however, infusion reaction (IR), which is specific to monoclonal antibody therapy, is frequently triggered by RTX. Therefore, we designed this study to identify risk factors based on clinical test values for developing IR after RTX administration. Eighty-nine patients with B-cell non-Hodgkin's lymphoma who had received RTX for the first time between February 2010 and March 2013, at the Gifu Municipal Hospital were enrolled as subjects. Analysis of data was conducted for 87 patients, after excluding patients whose data were missing. Univariate analysis showed significant differences in the number of patients exhibiting a soluble interleukin-2 receptor (sIL-2R) level > 2,000 U/L and hemoglobin (Hb) < lower standard limit (LSL) between the IR and non-IR groups. Multivariate analysis showed significant differences with respect to sIL-2R > 2,000 U/L [odds ratio (OR), 4.463; 95% confidence interval (Cl), 1.262-15.779; P=0.020], Hb < LSL [OR, 3.568; 95% Cl, 1.071-11.890; P=0.038], and steroid administration [OR, 0.284; 95% CI, 0.094-0.852; P= 0.025]. Our findings show that sIL-2R >2,000 U/L, Hb < LSL, and a lack of steroid premedication are risk factors for developing IR following RTX treatment.
    No preview · Article · Oct 2015 · Pharmazie