Pharmazie Journal Impact Factor & Information

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

2015 Impact Factor Available summer 2016
2014 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

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: Schisandrin B (Sch B), the most abundant dibenzocyclooctadiene lignan isolated from the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill, possesses various biological activities, such as hepatic protection, anti-tumor, anti-inflammatory and anti-cardiovascular properties. However, the effect of Sch B on inflammatory bowel disease (IBD) is not yet known. The aim of this study was to investigate whether Sch B has protective effect against dextran sulfate sodium (DSS)-induced colitis in a mouse model. The acute mouse model of IBD was induced by drinking 2.5% DSS water for 5 days. Sch B was administered orally in doses of 10, 40, and 100 mg/kg respectively. It significantly reduced concentration of TNF-α, IL-1β, INF-γ and IL-6 in colon tissue as well as the mRNA expression levels. In addition, we demonstrated that Sch B blocked the phosphorylation of IκBα, nuclear factor-κB (NF-κB) p65, p38 mitogen-activated protein kinase (MAPK), c-Jun NH2-terminal kinase, and extracellular signal regulated kinase in DSS-induced acute colitis. In conclusion, these results indicated that Sch B could exert beneficial effects on experimental IBD induced by DSS and may represent a novel treatment strategy for IBD.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5561
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    ABSTRACT: Rapamycin, a classical inhibitor of the mammalian target of rapamycin (mTOR), has been intensively studied for its role in metabolism and verified to induce metabolic defects through mTORC2/Akt pathway. However, disparity of the results exists depending on the differences of the animal models or the detailed procedures. Moreover, data regarding the effect of rapamycin treatment in diabetic models are sparse. Therefore, we investigated its influence on glucose and lipid metabolism, and further analyzed its effect on the mTORC2/Akt pathway in a high-fat diet- and streptozotocin-induced diabetic mice model. Three-weeks old C57BL/6J mice were fed with a high fat diet (60 kcal% fat) and intraperitoneally injected with streptozotocin (100 mg/kg) at 6 weeks of age. Rapamycin (2 mg/kg) was orally given to the mice daily for consecutive 6 weeks. Body weight, blood lipid parameters and HbA1c% values were evaluated. Oral glucose test and insulin tolerance test were performed. Furthermore, western blot assay was applied to investigate the protein epression levels of Akt and PKC , two key targets of the mTORC2/Akt pathway. Rapamycin-treated diabetic mice demonstrated less weight gain, more profound symptoms of polydipsia, polyphagia and polyuria, significant liver fat accumulation and exacerbated metabolic disorders including insulin resistance, hyperglycemia and dyslipidemia. Contrary to what have been expected, though significantly inhibiting mTORC1/S6K1 signaling, chronic rapamycin treatment failed to down-regulate mTORC2/Akt pathway. Our findings provide evidence that chronic rapamycin treatment may exacerbate metabolism in diabetic subjects and does not down-regulate mTORC2/Akt signialing in a high-fat diet- and streptozotocin- induced diabetic mice model.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.4847
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    ABSTRACT: Breviscapine (BE) is a standardized Chinese herbal medicine extracted from Erigeron breviscapus (Vant.) Hand.-Mazz. It has been widely used to treat cardiovascular and cerebrovascular diseases. However, there are no reports on the protective effects and underlying molecular mechanisms of BE action on myocardial ischemia/reperfusion (MI/R)-induced cardiomyocyte apoptosis. In the present study, we aimed to confirm the cardioprotective effect of BE from MI/R injury in vivo, and investigate the potential molecular mechanisms against simulated ischemia/reperfusion (SI/R)-induced cardiomyocyte apoptosis in vitro. The rat model of MI/R injury was induced by 30 min of transient vessel occlusion followed by 3 h of reperfusion. BE significantly reduced the myocardium infarct size and production of cardiac troponin (cTnI) in serum. In an in vitro experiment, H9c2 cardiomyocytes were incubated with vehicle or ischemic buffer during hypoxia; then, they were reoxygenated with or without BE. BE markedly improved the cell viability and decreased lactate dehydrogenase (LDH) release. We confirmed the anti-apoptotic effect of BE with the Hoechst 33258 staining assay, and this effect was associated with an increase in Bcl-2 and a decrease in active caspase-3 expression. Western blot analysis also showed that BE increased the phosphorylation of Akt and eNOS in H9c2 cells, and the protective effects of BE were partially inhibited by the phosphatidylinositol 3'-kinase (PI3K) specific inhibitor LY294002. Our results suggested that BE could provide significant cardioprotection against MI/R injury, and the potential mechanisms might involve suppression of cardiomyocyte apoptosis through activating the PI3K/Akt/eNOS signaling pathway.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5552
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    ABSTRACT: Historical research may be able to contribute to the exploration of traditional knowledge about medicinal plants and promising attempts have been made investigating Byzantine texts, Early Modern herbals, and writings of Christian missionaries. In this pilot study it should be explored if publications, travel reports, diaries or correspondence of the botanical explorers of the 19th and early 20th centuries may serve a source of ethnopharmacological information as well and may be able to guide modern phytopharmacological research. Writings of Berthold Seemann (1825-1871), a German investigator exploring the botany of Middle America, the Fiji islands and other regions, are investigated as a first example. It could be shown that Seemann’s heritage mainly kept at Kew Garden Archives, does contain ethnopharmacological information which in part has already been confirmed by recent study results indicating some reliability of his observations. However, there are also reports about traditional medicinal plants scarcely investigated so far, including Schultesia stenophylla Mart. (syn. S. guainensis (Aubl.) Malme), Trixis inula Crantz,Waltheria glomerata Presl., Gonophlebium attenuatum (Humb. & Bonpl. Es Willd) C. Presl., or Pseudoelephantopus spicatus (Juss ex Aubl.) C.F. Baker. It is suggested to further explore their potential as medicinal plants. In general, as Seemann’s example has shown, publications and correspondence of botanical explorers of the past seem to be a valuable and hitherto almost neglected source of information to be considered in further historical and ethnopharmacological research.
    Pharmazie 09/2015; 70(9):616-626. DOI:10.1691/ph.2015.5601
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    ABSTRACT: Endonuclease G (Endo G) is a novel determinant of cardiac hypertrophy. Here, we report the characterization of Endo G and mitochondria-sarcoplasmic reticulum-related proteins during cardiac hypertrophy, and hypothesize that Endo G regulate mitochondrial function partly through Mfn2 and Jp2 during cardiac hypertrophy. Our results show that Endo G levels gradually increased at the beginning of phenylephrine-induced cardiac hypertrophy, accompanied by an abnormal mitochondrial membrane potential. The up-regulation of Mfn2, Jp2, and Endo G appeared at an early stage of cardiac hypertrophy, whereas PGC1 was not up-regulated until a later stage. Abolishing Endo G with siRNA led to the uncoupling of the mitochondrial electron transport chain from ATP production and decreased PGC1 expression, likely by affecting the juxtaposition of the mitochondria and the sarcoplasmic reticulum via Mfn2 and Jp2. Furthermore, abolishing Jp2 altered the expression of Endo G expression and induced mitochondrial dysfunction, suggesting that mitochondrial abnormalities in cardiac hypertrophy are most likely caused by Endo G. Taken together, our study established a link between Endo G and mitochondrial function during cardiac hypertrophy, partly through the effects of Endo G on Mfn2 and Jp2, and revealed a role for Endo G in the crosstalk between the processes controlled by Mfn2 and Jp2 in maladaptive cardiac hypertrophy.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5559
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    ABSTRACT: Niemann-Pick C1-like 1 (NPC1L1) protein is the key transporter responsible for dietary cholesterol absorption. Recent studies indicated that several functional polymorphisms of NPC1L1 were associated with coronary heart disease (CHD) and response to ezetimibe therapy. The aim of the present study was to analyze the allele frequency and haplotype distribution of NPC1L1 polymorphisms in Chinese Hans and to compare them with those of other ethnic populations reported before. Blood samples were collected from 424 unrelated Chinese Hans (246 males and 178 females). Ten NPC1L1 polymorphisms (-762T > C, -133A > G, -18C > A, 1721C > T, 1735C > G, 1764T > C, 1767G > A, 27677T > C, 25342A > C and 28650A > G) were genotyped by direct sequencing or polymerase chain reaction–restriction fragment length polymorphism (PCR-RFLP) assay. Among the variants, the minor allele frequency of -762T > C and 1735C > G were 35.0% and 37.0%, respectively. Furthermore, these two polymorphisms were highly linked with a D' value of 0.80. The observed frequencies of two major haplotypes were 59.1% for T-762/C1735 and 30.1% for C-762/G1735, respectively. The frequencies of the rest variants were extremely low (1.8% for-133G, 1.5% for -18A, 0.9% for 1721T and only 0.2% for 27677C allele, respectively) or even not detected (1764T > C, 1767G > A, 25342A > C and 28650A > G) in our study population. Comparison with other ethnic populations revealed a remarkable genetic variability in the incidences of NPC1L1 polymorphisms. The frequencies of NPC1L1 polymorphisms in Chinese Hans are comparable to Japanese population but totally different from Caucasians, African-Americans and Hispanic individuals. This is the first study to report the ethnic difference in the frequencies of NPC1L1 functional polymorphisms in detail. -762T > C and 1735C > G are two prevalent NPC1L1 variants which need further studies to explore their clinical impact on CHD prevalence and response to ezetimibe therapy in Chinese Hans.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5582
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    ABSTRACT: A capillary zone electrophoresis method for quantitative determination of doripenem in synthetic matrix was developed. The stability-indicating capability was performed applying stress testing protocols. The selected analytical conditions include 100 mM sodium borate buffer (pH 8.0) as run electrolyte, voltage of + 15 kV, hydrodynamic injection of 5 s (50 mBar), detection at 298 nm and temperature of analysis of 25 °C. The electrophoretic separation was carried out in a fused silica capillary (effective length 40 cm, 50 μm i.d.), using procainamide hydrochloride as internal standard. The proposed method showed quickness and reproducibility, with an analytical run in a total time of 5 min. The percentage of drug amount estimated was 101.33% (RSD=0.80), with satisfactory intra-day and inter-day precision. In the recovery test, the method was found to be reliable and accurate in the drug quantitation (mean recovery = 101.86%). The robustness was performed applying the Plackett–Burman experimental design which confirmed the assay reliability. Based on results from forced degradation study, the stability-indicating capability was established, being observed a major degradation in alkaline, photolytic and thermal conditions. In comparison to HPLC method previously developed, the proposed capillary electrophoresis assay is statistically equivalent.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5008
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    ABSTRACT: Several natural compound interfere with microtubules or the actin cytoskeleton. Compounds interfering with the microtubules like Vinca-alkaloids or taxanes, are extensively used for cancer therapy. In contrast, knowledge about pharmacological properties of actin binding drugs is poor and drugs interfering with actin are far from clinical use. Rhizopodin is a natural compound that strongly affects the actin cytoskeleton at nanomolar concentrations. Initial work revealed interesting anti-bacterial and cytotoxic effects, but the cellular effects and pharmacological properties of rhizopodin have not been characterized. We hypothesized that rhizopodin might exert anti-cancer activity. Therefore, the aim of this study was to characterize the cellular and pharmacological effects of rhizopodin in cancer. Effects of rhizopodin demonstrated prominent effects on the actin cytoskeleton as shown in the actin-pyrene assay and by immunostaining of cancer cells. To investigate cellular effects of rhizopodin, we analyzed cell proliferation, cell death induction by propidium iodide exclusion and western blot, as well as migration by impedance measurement using the xCELLligence device in MDA-MB-231 breast cancer and T24 bladder cancer cell lines. Rhizopodin inhibited proliferation and induced cell death of MDA-MB-231 and T24 cells at nanomolar concentrations. PARP cleavage by rhizopodin suggests caspase-dependent cell death induction. Importantly, rhizopodin potently inhibited MDA-MB-231 and T24 cancer cell migration at subtoxic doses where no actin aggregation was observed, indicating a specific underlying signaling of rhizopodin. In summary, our study elucidates rhizopodin as actin-binding natural compound that exerts potent anti-cancer effects. Therefore, our work provides the basis for further in depth characterization of rhizopodin as an antitumoral agent.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5579
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    ABSTRACT: Willow bark extracts are used for the treatment of fever, pain and inflammation. Recent clinical and pharmacological research revealed that not only the salicylic alcohol derivatives, but also the polyphenols significantly contribute to these effects. Quantitative analysis of the European Pharmacopoeia still focuses on the determination of the salicylic alcohol derivatives. The objective of the present study was the development of an effective quantification method for the determination of as many flavanone and chalcone glycosides as possible in Salix purpurea and other Salix species as well as commercial preparations thereof. As Salix species contain a diverse spectrum of the glycosidated flavanones naringenin, eriodictyol, and the chalcone chalconaringenin, a subsequent acidic and enzymatic hydrolysis was developed to yield naringenin and eriodictyol as aglycones, which were quantified by HPLC. The 5-O-glucosides were cleaved with 11.5% TFA before subsequent hydrolysis of the 7-O-glucosides with an almond β-glucosidase at pH 6-7. The method was validated with regard to LOD, LOQ, intraday and interday precision, accuracy , stability, recovery, time of hydrolysis, robustness and applicability to extracts. All 5-O- and 7-O-glucosides of naringenin, eriodictyol and chalconaringenin were completely hydrolysed and converted to naringenin and eriodictyol. The LOD of the HPLC method was 0.77 M of naringenin and 0.45 M of eriodictyol. The LOQ was 2.34 M of naringenin and 1.35 M for eriodictyol. The method is robust with regard to sample weight, but susceptible concerning enzyme deterioration. The developed method is applicable to the determination of flavanone and chalcone glycosides in willow bark and corresponding preparations.
    Pharmazie 09/2015; 70(9). DOI:10.1691/ph.2015.5555
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    ABSTRACT: There is - apart from clinical trials - an ongoing discussion on how to demonstrate therapeutic equivalence for locally applied and locally acting products in the gastrointestinal tract. Possibly, among other alternatives, in vitro drug release models could be considered surrogates of drug release and availability at the site of action. However, to date the conditions in which in vitro models provide valid surrogates of in vivo release and availability at the site of action would have to be defined. To demonstrate the potential applicability of in vitro test methods for screening therapeutic equivalence of locally applied and locally acting gastrointestinal products and also to get an idea of which would be the right dosage form for an individual patient a series of in vitro studies was performed comparing a variety of in vitro release methods ranging from pharmacopoeial methods to “patient-specific” release methods in examining drug release of four mesalazine tablet formulations intended for local drug delivery in the gastrointestinal tract. Results from this study indicated that pharmacopoeial quality control methods are hardly applicable to predict the therapeutic equivalence of such products. Moreover, comparison of the results obtained with the different in vitro methods reveal that a prediction of the therapeutic equivalence for locally acting products in the gastrointestinal tract is unlikely based on release profiles obtained in a single drug release experiment. However, results from the study also indicated that a set of individualized biorelevant in vitro test scenarios might be very useful for both demonstrating therapeutic equivalence and selecting the appropriate drug product for a particular patient.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5556
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    ABSTRACT: Herein we present a novel synthetic procedure for the synthesis of imidazo[1,2-a]pyridines in a modified Groebke-Blackburn fashion. In a sequential three-step one-pot protocol the commercially hardly available isocyanide-component is formed in situ using standard reagents. Cyclization to the desired products can be afforded in the same reaction mixture. The absent need of isolation of the isocyanide in this protocol eases its handling considerably and workup is only needed to finally furnish the imidazo[1,2-a]pyridines via coloumn chromatography. This protocol is a convenient way to more diverse libraries of imidazo[1,2-a]pyridines extending the functionality of the Groebke-Blackburn synthesis.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5580
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    ABSTRACT: Resveratrol, for example widely present in the Chinese herbal medicine Polygonum cuspidatum, it is a natural phytoalexin, and has many biochemical activities, such as anti-tumor, anti-cardiovascular diseases, anti-bacterial, anti-inflammatory, anti-aging and other effects. This article will concentrate on the physical and chemical properties of resveratrol, the biological and pharmacological effects for its anticancer activities. An outlook is given to the development and application prospects in this drug.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5571
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    ABSTRACT: The aim of this study was to show the potential impact of services directed by clinical pharmacists, including medication reconciliation and medication review, on the hospital admission process for elderly patients. This study was conducted in an internal medicine ward between April 24 and July 25, 2014. Patients hospitalized due to any reason were eligible if they were 65 years or older and regularly used at least one medication at home. The clinical pharmacist evaluated potentially inappropriate medications (PIM), medication related problems (MRPs) and medication discrepancies at the time when these eligible elderly patients were admitted to the hospital. The physician acceptance rate as related the clinical pharmacist's recommendation was evaluated retrospectively. A total of 133 elderly patients (mean age 76.62±8.12 years old; 70 female) were included in the study. Out of 394 medication discrepancies, 88.32% were found to be unintended discrepancies among 111 elderly patients upon hospital admission. PIM was found in 19.55% of these cases. A total of 396 MRPs among 115 patients were identified, with the most common being that the drug had not been taken/administered at all. The doctor acceptance rate of the clinical pharmacist's recommendation was found to be 85.60%. In conclusion, it was found that medication related problems and inappropriate medication utilization at admission could be prevented at a high rate of success by clinical pharmacist-driven medication reconciliation and medication review services.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5510
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    ABSTRACT: Medicinal products obtained by recombinant DNA technology are complex molecules and demonstrate a high degree of molecular heterogeneity. Charge heterogeneity and isoform pattern of this class of medicines, are parameters important for their quality, safety, and efficacy. In this study we report the application of two-dimensional gel electrophoresis (2-D electrophoresis) for the quality assessment, identification, charge heterogeneity and isoform pattern study of recombinant protein, CTLA4-Ig (abatacept), which has been selected as an example of the drug class, known as Fc-fusion proteins. In order to achieve an efficient separation of this complex analyte,2-D electrophoresis was optimized employing different experimental conditions regarding the selection of an immobilized pH gradient (IPG), sample pretreatment, presentation and detection procedure. Experimental datadocumented that 2-D electrophoresis is a suitable method for the assessment of identity, purity, structural integrity, isoform pattern and to monitor charge heterogeneity and post-translational glycosylation of the Fc-fusion protein, abatacept.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5012
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    ABSTRACT: A stability-indicating RP-LC method for the determination of prasugrel in tablets was developed and validated. Stress testing of prasugrel was carried out in accordance with ICH guidelines, where the drug was submitted to acidic and basic hydrolysis, oxidative, thermal and photolytic conditions. Prasugrel was unstable under all the conditions and the degradations products were analyzed by HPLC-UV. Furthermore, two main degradation products found under alkaline and thermal conditions were investigated by LC-MS. Based on the fragmentation patterns, two products resulted from hydrolysis of the acetate ester moiety of prasugrel were observed. Due the chemical equilibrium, tautomerism occurs between the ketone and alcohol functions justifying the similar molecular weight and fragment pattern obtained in degradation products analysis. Successful separation was achieved on a RP-18 octadecyl silane column using acetonitrile and triethylamine 0.5% mixture (50:50, v/v) as the mobile phase at 25 °C. The flow rate was 1.0 mL/min and the detector wavelength was 263 nm. The method proposed in this work was successfully applied to quality control of prasugrel and contribute to stability assessment of pharmaceutical products containing this drug.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.4185
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    ABSTRACT: Five indolin-2-one derivatives bearing piperazinylbutyl side chains attached to the amide nitrogen were synthesized from 2-indolinone. 1-(4-Bromobutyl)-indolin-2-one was reacted with 1-piperazinecarboxaldehyde to form 1-(4-(4-formyl-1-piperazinyl)butyl)indolin-2-one (2). In the presence of H2SO4, the aldehyde moiety was removed from 1-(4-(4-formyl-1-piperazinyl)butyl)indolin-2-one and then 1-(4-(1-piperazinyl)butyl)indolin-2-one (3) was obtained, this compound was reacted with benzaldehyde derivatives to give the target compounds 4 a-e by N-alkylation reaction. The structures of the intermediates and the target compounds were characterized by 1H NMR, ESI-MS spectra and elemental analyses. In vitro receptor binding assays at D2, D3, D4 receptor subtypes of the target compounds were performed and the five compounds showed selectivity towards D2-like receptors. Among them, 1-(4-(4-(4-hydroxybenzyl)-1-piperazinyl)butyl) indolin-2-one (4c) exhibited a remarkable affinity and selectivity to D4 receptor with K i value of 0.5 nM. The results indicated that 1-(4-(4-(4-hydroxybenzyl)-1-piperazinyl)butyl)indolin-2-one might be a potential dopamine D4 receptor ligand.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5549
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    ABSTRACT: Cyclosporine A is a narrow therapeutic indexed immunosuppressant used after organ transplantation. Several herbs have been reported to alter its pharmacokinetics. Myrrh, dried oleogum resin obtained from Commiphora myrrha (Burseraceae) has been used for many common ailments. The present study was carried out to investigate the effect of myrrh on the pharmacokinetics of cyclosporine A. The rats of the control group received 60 mg/kg, p.o. cyclosporine A, and blood samples were collected at predetermined time intervals. Rats of the test group were treated with an aqueous suspension of myrrh (380 mg/kg p.o.) for eight days and on 8th day a single dose of cyclosporine A was administered to the treated group after 1 h of myrrh administration. Blood samples were drawn at predetermined time points and the drug was analyzed in whole blood by using H-Class UPLC-TQD. Pharmacokinetic profiles of control and test group were compared. Statistically significant differences were observed between the pharmacokinetic parameters of control and treated groups. In the myrrh treated group, the AUC0-t and Cmax of cyclosporine A was decreased by about 45% and 48%, respectively. The time to reach maximum concentration (Tmax) remained almost unchanged in both groups. Results indicated that the bioavailability of cyclosporine A was reduced by about 45% when co-administered with myrrh. This observation suggests that concurrent consumption of myrrh and cyclosporine A should be avoided. To confirm the clinical relevance of these findings, P-gp and CYP3A based molecular investigations can be performed along with a well-planned clinical study.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5551
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    ABSTRACT: Lanthanum carbonate has the same phosphorus depressant effect as the other phosphorus adsorbents, and is expected to decrease digestive symptom onset such as constipation in Japanese patients undergoing hemodialysis compared to sevelamar hydrochloride. In this study, we investigated the short- and long-term changes in digestive symptoms in these patients after substituting sevelamar hydrochloride with lanthanum carbonate. We studied 16 patients (4 men, 12 women) and evaluated their gastrointestinal symptoms before administration, at the time of administration, and 2, 4, 8, and 12 weeks after administration, using the Gastrointestinal Symptom Rating Scale. In addition, we conducted repeat evaluations 52 weeks after administration for the patients in whom lanthanum carbonate was administered continuously for 52 weeks. Fourteen (87.5%) out of the 16 patients could tolerate continuous administration for 12 weeks. The constipation score was 3.21 ± 1.74 before administration, 2.07 ± 0.83 2 weeks after administration, 1.76 ± 0.83 4 weeks after administration, 1.57 ± 0.56 8 weeks after administration, and 11.41 ± 0.48 12 weeks after administration. The scores improved significantly 4 weeks after administration (p < 0.05) and even 12 weeks after continuous administration. Among the 16 study patients, 9 patients (1 men, 8 women) were received lanthanum carbonate continuously for 52 weeks. The constipation score was 3.74 ± 1.92 at the start of administration, 1.37 ± 0.56 12 weeks after administration, and 1.85 ± 0.63 52 weeks after administration, with significant improvement even 52 weeks after administration (p < 0.05). This study shows that substituting sevelamar hydrochloride with lanthanum carbonate improves constipation symptoms in hemodialysis patients from an early stage, which indicates its usefulness in improving constipation symptoms caused by sevelamar hydrochloride.
    Pharmazie 08/2015; 70(8). DOI:10.1691/ph.2015.5573