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    17843 results match your criteria Arzneimittel-Forschung Drug Research[Journal]

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    Leave-one-out procedure in the validation of elimination rate constant analysis.
    Arzneimittelforschung 2012 Dec 30;62(12):682-9. Epub 2012 Nov 30.
    Polpharma Biologics, Gdańsk, Poland.
    Many registration agencies and other organizations define how to calculate the elimination rate constant (kel) value. No validation procedures have been introduced to verify the correct selection of the concentration-time (C-T) points used for the kel calculation. The purpose of this paper is to discover whether kel analysis can be subjected to the condensed validation procedure and what acceptance criteria should be adopted for such a procedure. Read More

    Pharmacokinetic and myocardial enzyme profiles of two administration routes of epirubicin in breast cancer patients.
    Arzneimittelforschung 2012 Dec 30;62(12):677-81. Epub 2012 Nov 30.
    Chemotherapy Research Center, Kunming Medical University, Kunming, China.
    To evaluate the changes in myocardial enzymes and plasma epirubicin concentration following administration by micro-pump (MP) and intravenous drip (ID) in breast cancer patients.11 self-controlled breast cancer patients were recruited for a trial with epirubicin administration by MP for 48 h and by ID for 1 h during 2 cycles of treatment. Plasma concentration of epirubicin at different time points was determined using LC-MS/MS. Read More

    Synthesis, anti-hypertensive effect of a novel angiotensin II AT1 receptor antagonist and its anti-tumor activity in prostate cancer.
    Arzneimittelforschung 2012 Dec 30;62(12):637-43. Epub 2012 Nov 30.
    Department of Pharmaceutical Science and Technology, Donghua University, Shanghai, China.
    Since the first non-peptide Ang II receptor antagonist was originally reported, it has become the most common target in the development of new treatments for hypertension. In recent years, all components of the classical RAS have been reported in the prostate, these results suggest the possibility that ARB is a novel therapeutic class of agents for prostate cancer. In this study, a new compound 2-(4-((2-propyl-5-nitro-1H-benzo[d]imidazol-1-yl) methyl)-1H-indol-1-yl) benzoic acid was synthesized and evaluated as a novel angiotensin II AT1 receptor antagonist by radioligand binding assays, anti-hypertensive assays in vivo and oral acute toxicity test. Read More

    Effect of zeolite nano-materials and artichoke (Cynara scolymus L.) leaf extract on increase in urinary clearance of systematically absorbed nicotine.
    Arzneimittelforschung 2012 Dec 29;62(12):650-4. Epub 2012 Nov 29.
    Department of Inorganic Chemistry, Razi University, Kermanshah, Iran.
    Nicotine, the main pharmacologically active component in tobacco and cigarette, has some toxic effects and also high potential for addiction. In this study, the effect of artichoke (Cynara scolymus L.) and zeolite nano-materials on urinary excretion of nicotine and consequently elimination of systematically absorbed nicotine was investigated. Read More

    Fluorescence detection of etoposide-loaded nanoparticles by HPLC and pharmacokinetics study.
    Arzneimittelforschung 2012 Dec 28;62(12):661-5. Epub 2012 Nov 28.
    Department of Respiratory, Changsha Central Hospital, Changsha, China.
    A simple HPLC with fluorescence detection method was developed for determination and pharmacokinetic study of Etoposide in dog plasma.Plasma sample pretreatment involved liquid-liquid extraction of 500 µL plasma. The chromatographic separation was carried out on a Gemini C18 column with a mixture of methanol (A) and water (B) (0~5 min, volume of A was 45-50%, 5~10 min, volume of A was 50-90%) used as mobile phase at a flow rate of 0. Read More

    Pharmacokinetics and potential advantages of a new oral solution of levothyroxine vs. other available dosage forms.
    Arzneimittelforschung 2012 Dec 15;62(12):631-6. Epub 2012 Nov 15.
    Faculté de pharmacie, Université de Montréal, Montreal, Quebec, Canada.
    To better understand the pharmacokinetics and potential advantages of a levothyroxine oral solution vs. tablets and soft gel capsules.4 randomized, 2-treatment, single-dose (600 mcg levothyroxine), 2-way crossover bioequivalence studies in 84 healthy subjects were analyzed. Read More

    A validated HPLC method for the determination of eriocalyxin B in plasma and its application to pharmacokinetic studies.
    Arzneimittelforschung 2012 Dec 15;62(12):666-9. Epub 2012 Nov 15.
    Department of General Surgery, Shanghai Jiao tong University School of Medicine, Shanghai, China.
    The purpose of this study was to determine EriB in plasma by using the method of HPLC and collect the preclinical pharmacokinetic parameters of EriB.The analysis involved a simple liquid-liquid extraction. After making alkaline with NaOH, plasma was extracted with diethyl ether and the organic extract was then evaporated. Read More

    Synthesis, biological activity and molecular modeling of 4-fluoro-N-[ω-(1,2,3,4-tetrahydroacridin-9-ylamino)-alkyl]-benzamide derivatives as cholinesterase inhibitors.
    Arzneimittelforschung 2012 Dec 15;62(12):655-60. Epub 2012 Nov 15.
    Department of Pharmaceutical Chemistry and Drug Analyses, Medical University, Lodz, Poland.
    The aim of this study was to synthesize and determine the biological activity of new derivatives of 4-fluorobenzoic acid and tetrahydroacridine towards inhibition of cholinesterases. Compounds were synthesized in condensation reaction between 9-aminoalkyl-tetrahydroacridines and the activated 4-fluorobenzoic acid. Properties towards inhibition of acetyl- and butyrylcholinesterase were estimated according to Ellman's spectrophotometric method. Read More

    Repeated administration of centhaquin to pregnant rats did not affect postnatal development and expression of endothelin receptors in the brain, heart or kidney of pups.
    Arzneimittelforschung 2012 Dec 15;62(12):670-6. Epub 2012 Nov 15.
    Department of Pharmaceutical Sciences, Midwestern University Chicago College of Pharmacy, IL, USA.
    The effect of repeated administration of centhaquin to pregnant rats on postnatal development, and expression of ETA and ETB receptors was determined. Pregnant rats were treated daily with either saline or centhaquin for 2 weeks. Male rat pups were sacrificed on day 1, 7, 14 and 28 of birth. Read More

    Simultaneous determination of methotrexate, dasatinib and its active metabolite N- deshydroxyethyl dasatinib in rat plasma by LC-MS/MS: method validation and application to pharmacokinetic study.
    Arzneimittelforschung 2012 Dec 8;62(12):624-30. Epub 2012 Nov 8.
    Incozen Therapeutics Private Limited, Andhra Pradesh, India.
    Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. Methotrexate is an antimetabolite and antifolate drug. Clinical trials utilizing a combination of dasatinib and methotrexate in patients with Philadelphia chromosome positive and/or Bcr-Abl positive acute lymphoblastic leukemia are currently ongoing. Read More

    A parallel design study to assess the bioequivalence of generic and branded hydroxychloroquine sulfate tablets in healthy volunteers.
    Arzneimittelforschung 2012 Dec 8;62(12):644-9. Epub 2012 Nov 8.
    Shanghai Xuhui Central Hospital, Shanghai, China.
    Hydroxychloroquine (HCQ) is a racemic 4-aminoquinoline derivative that was first introduced as an antimalarial, and subsequently applied to the treatment of autoimmune diseases such as rheumatoid arthritis and systemic lupus erythematosus. Information on the pharmacokinetics of HCQ in healthy volunteers, especially in a Chinese population is limited, and this study was conducted to provide support for a generic product to obtain marketing authorization in China.The aim of the present study was to compare the pharmacokinetics and assess bioequivalence of a new generic test and the branded reference hydroxychloroquine sulfate tablets in healthy volunteers. Read More

    The effect of ethyl alcohol on the function of spatial memory in rats.
    Arzneimittelforschung 2012 Dec 31;62(12):614-23. Epub 2012 Oct 31.
    Department of Pharmacoeconomics and Social Pharmacy, Poznan University of Medical Sciences.
    Alcoholism is a mental disease in the course of which depression, anxiety, and cognitive function deficits may appear, and these symptoms can be aggravated by comorbid schizophrenia.The aim of this study was to find whether spatial memory (Morris Water Maze) function impairment is found in prenatally stressed rats (PSG) (prenatal stress paradigm - animal model of schizophrenia) and whether aripiprazole ARI and olanzapine OLA modify these functions. It was also important to study the effect of ethyl alcohol administered to rats. Read More

    Neuroprotective action and free radical scavenging activity of Guttiferone-A, a naturally occurring prenylated benzophenone.
    Arzneimittelforschung 2012 Dec 31;62(12):583-9. Epub 2012 Oct 31.
    Centro de Investigación y Desarrollo de Medicamentos, La Habana, Cuba.
    Reactive oxygen species (ROS) are important mediators in a number of neurodegenerative diseases and molecules capable of scavenging ROS may be a feasible strategy for protecting neuronal cells. We previously demonstrated a powerful iron-chelating action of Guttiferone-A (GA), a naturally occurring polyphenol, on oxidative stress injuries initiated by iron overload. Here we addressed the neuroprotective potential of GA in hydrogen peroxide and glutamate-induced injury on rat's primary culture of cortical neurons and PC12 cells, respectively, and antioxidant properties concerning scavenging and anti-lipoperoxidative activities in cell-free models. Read More

    Pharmacokinetics of ginkgolide B injection in beagle dogs.
    Arzneimittelforschung 2012 Dec 23;62(12):595-8. Epub 2012 Oct 23.
    Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, People's Republic of China.
    A liquid chromatography-mass spectrometry method was developed, validated, and applied to the pharmacokinetic study with doses of 0.68, 2.73 and 10. Read More

    LC-MS/MS method for determination of epothilone B in rat plasma and its application in pharmacokinetic study.
    Arzneimittelforschung 2012 Dec 23;62(12):609-13. Epub 2012 Oct 23.
    Department of Oncology, Shanghai Jiaotong University, Shanghai, China.
    A simple LC-MS/MS method was developed for determination and pharmacokinetic study of Epothilone B in rat plasma.Plasma sample pretreatment involved a one-step liquid-liquid extraction of 100 µL plasma. The chromatographic separation was carried out on a Agilent Zobax SB C18 column with a mobile phase consisting of 10 mmol/L ammonium acetate-acetonitrile (35:65, v/v) at a flow rate of 0. Read More

    In vitro dissolution and in vivo bioequivalence evaluation of two brands of isosorbide 5-mononitrate sustained release tablets.
    Arzneimittelforschung 2012 Dec 23;62(12):576-82. Epub 2012 Oct 23.
    Kolon Pharmaceuticals Inc., Korea.
    The purpose of the present study was to test a sustained release-tablet newly formulated with synthetic paraffin and compare its bioequivalence to that of the Imdur® Long-Acting tablet, based on the guidelines of the Korean Food and Drug Administration.Dissolution test was performed in 4 different dissolution media. A LC/MS/MS method of isosorbide 5-mononitrate in human plasma was validated. Read More

    Interaction of 5-amino-1,3,4-thiadiazole-2-thiol and its violuric acid adduct with Pt(II) - crystals structures, spectroscopic properties and cytotoxic activity.
    Arzneimittelforschung 2012 Dec 23;62(12):599-602. Epub 2012 Oct 23.
    Department of Chemistry, Medical University, Sofia, Bulgaria.
    The coordination properties of Pt(II) with 5-amino-1,3,4-thiadiazole-2-thiol [CAS 2349-67-9] (L 1 ) and its novel violurate adduct (L 2 ), both in solution and in solid state, are studied by means of conventional IR-spectroscopy, single crystal X-ray diffraction and thermal methods. The complex compounds of L 1 and L 2 , with general formulas [Pt(C2H2N3S2)2] and [Pt(C6H4N6S2O3)(Cl)]Cl respectively, are obtained. Quantum chemical calculations of the ligands are performed with a view to obtain electronic structure and optical properties of the ligands L 1 and L 2 , respectively. Read More

    Ketorolac tromethamine improves the analgesic effect of hyoscine butylbromide in patients with intense cramping pain from gastrointestinal or genitourinary origin.
    Arzneimittelforschung 2012 Dec 23;62(12):603-8. Epub 2012 Oct 23.
    Escuela Superior de Medicina, Instituto Politécnico Nacional, Mexico, Mexico.
    The symptomatic treatment of pain associated with spasm of gastrointestinal or genitourinary origin can include the use of spasmolytic agents and/or non-steroidal anti-inflammatory drugs. However, the evidence of a superior effectiveness of combination in comparison with individual drugs is scarce and controversial. A double-blind, randomised, clinical trial study was designed to characterize the analgesic effect and safety of ketorolac and hyoscine butylbromide against hyoscine butylbromide alone in patients with ambulatory acute cramping pain of gastrointestinal and genitourinary origin. Read More

    Antimicrobial and cytotoxicity potential of acetamido, amino and nitrochalcones.
    Arzneimittelforschung 2012 Dec 19;62(12):590-4. Epub 2012 Oct 19.
    Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Vale do Itajaí, Itajaí, Brazil.
    Chalcones constitute one of the major classes of natural products belonging to the flavonoid family, and they have been reported as having a range of important therapeutic activities, including some chalcones are effective as antimicrobial agents. Currently, the search for new structures with antimicrobial activity has been intensified due to the emergence of many strains resistant to antibiotics currently used to treat infectious diseases.3 chalcone series (amino, acetamido and nitrochalcones) were prepared (23 compounds) and evaluated for their antimicrobial and cytotoxic potential. Read More

    Microwave-assisted synthesis of 1,3-benzothiazol-2(3H)-one derivatives and analysis of their antinociceptive activity.
    Arzneimittelforschung 2012 Dec 19;62(12):571-5. Epub 2012 Oct 19.
    Department of Pharmaceutical Chemistry, Gazi University, Ankara, Turkey.
    A rapid and efficient method was developed for synthesis of 6-acyl-1,3-benzothiazol-2(3H)-one derivatives under microwave irradiation (MWI) conditions. The reaction times were shortened compared to conventional heating. Additionally, we synthesized acetic acid and acetamide derivatives of 1,3-benzothiazol-2(3H)-one, 6-acyl-1,3-benzothiazol-2(3H)-one, 5-chloro-1,3-benzothiazol-2(3H)-one and 6-acyl-5-chloro-1,3-benzothiazol-2(3H)-one with the microwave-assisted method and analyzed their antinociceptive activity with the tail flick, tail clip, hot plate and writhing tests. Read More


    Pharmacokinetics and bioequivalence evaluation of two brands of ciprofloxacin 500 mg tablets in Iranian healthy volunteers.
    Arzneimittelforschung 2012 Dec 9;62(12):566-70. Epub 2012 Oct 9.
    Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
    In the present study pharmacokinetics and bioequivalence of 2 brands of ciprofloxacin 500 mg were evaluated in 24 healthy male volunteers after a single dose oral administration in an open, randomized, 2-way crossover study.Blood samples were taken before and within 12 h after the administration of the drug. Plasma concentrations of ciprofloxacin were determined by a simple HPLC method with ultraviolet detection. Read More

    Pharmacokinetics and safety of eszopiclone in healthy Chinese volunteers.
    Arzneimittelforschung 2012 Dec 4;62(12):561-5. Epub 2012 Oct 4.
    Department of Clinical Pharmacology, Capital Medical University, Beijing, China.
    The main objective of this study was to investigate the pharmacokinetic characters of eszopiclone (CAS: 138729-47-2) after single and multiple-dose oral administration in healthy adult Chinese volunteers.In single-dose study, 12 subjects were given oral administrations of 1.5, 3 and 6 mg eszopiclone in an open-label, randomized, crossover fashion. Read More

    Dapson in heterocyclic chemistry part VI: synthesis and molecular docking of some novel sulfonebiscompounds of expected anticancer activity.
    Arzneimittelforschung 2012 Nov 21;62(11):497-507. Epub 2012 Sep 21.
    Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
    To discover new bioactive lead compounds for medicinal purposes, herein, sulfone biscompounds bearing dihydrothiazoles (3-9, 14, 15), acrylamide (11), thiazolidinones (12, 13, 20), thiophenes (16, 17) and benzothiophene (19) were prepared and tested for their anticancer activity. The structures of the products were confirmed from elemental analysis as well as spectral data. All the synthesized compounds showed remarkable anticancer activity against human breast cancer cell line especially, compound (3) with IC50 value 23. Read More

    Virtual screening and synthesis of new chemical scaffolds as VEGFR-2 kinase inhibitors.
    Arzneimittelforschung 2012 Dec 21;62(12):554-60. Epub 2012 Sep 21.
    Department of Pharmaceutical Chemistry, Ainshams University, Abbasia, Cairo, Egypt.
    VEGFR-2 tyrosine kinase inhibitors are currently receiving high interest in drug discovery process as anticancer agents. We have used virtual screening techniques in order to discover new scaffolds that can be used for developing new VEGFR-2 kinase inhibitors.Similarity ensemble approach was used to reduce the chemical space of ZINC database to select a subset of compounds. Read More

    Synthesis and biological evaluation of a 6-aminofuro[3,2-c]pyridin-3(2H)-one series of GPR 119 agonists.
    Arzneimittelforschung 2012 Nov 12;62(11):537-44. Epub 2012 Sep 12.
    Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd., Hokusei-cho, Inabe, Mie, Japan.
    G protein-coupled receptor 119 (GPCR 119 (GPR119)) agonists have received considerable attention as a promising therapeutic option for treatment of type 2 diabetes mellitus. GPR119 is one of the GPCRs expressed in pancreatic islet β-cells and its activation enhances stimulation of insulin secretion in a glucose-dependent manner. We have recently described a series of 6-amino-1H-indan-1-ones as potent, selective, and orally bioavailable GPR119 agonists with an amino group that plays important roles not only in their drug-like properties, such as high aqueous solubility, but also in their potent agonistic activity. Read More

    Some novel anticonvulsant agents derived from phthalazinedione.
    Arzneimittelforschung 2012 Nov 6;62(11):532-6. Epub 2012 Sep 6.
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Boys) Al-Azhar University, Cairo, Egypt.
    A series of phthalazinedione bearing substituted oxadiazole moiety derivatives X(1-7) were synthesized in good yield and evaluated for their possible anticonvulsant activity. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. Their anticonvulsant activities were evaluated by the maximal electroshock induced seizure (MES) and subcutaneous pentylenetetrazole (PTZ) tests. Read More

    Pharmacokinetics of febuxostat in healthy Chinese volunteers.
    Arzneimittelforschung 2012 Oct 6;62(10):463-9. Epub 2012 Sep 6.
    Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, PR China.
    Background: Febuxostat is a novel non-purine selective inhibitor of xanthine oxidase developed for the management of hyperuricemia in patients with gout.

    Objective: To investigate the pharmacokinetics and also evaluate the effects of gender and food on the pharmacokinetics of febuxostat in healthy Chinese volunteers.

    Methods: A phase I, 3-period study was performed in healthy Chinese male and female subjects. Read More

    The preventive oral supplementation of a selenium nanoparticle-enriched probiotic increases the immune response and lifespan of 4T1 breast cancer bearing mice.
    Arzneimittelforschung 2012 Nov 3;62(11):525-31. Epub 2012 Sep 3.
    Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran.
    The immunomodulatory effects of lactic acid bacteria have been demonstrated previously. In this study, a Lactobacillus plantarum strain was selected and enriched with selenium nanoparticles for use as a new immunomodulating agent in a breast cancer murine model. 30 female inbred BALB/c mice were equally divided into a test group and a control group. Read More

    Ibudilast, a phosphodiesterase inhibitor, in combination with low-dose aspirin potently inhibits guinea pig carotid artery thrombosis without extending bleeding time and causing gastric mucosal injury.
    Arzneimittelforschung 2012 Dec 3;62(12):545-53. Epub 2012 Sep 3.
    Development Research Laboratories, Kyorin Pharmaceutical Co., Ltd. Tochigi, Japan.
    A combination of low-dose aspirin (ASA) and a phosphodiesterase inhibitor has been clinically tried for the secondary prevention of atherothrombotic diseases. The in vivo antithrombotic property of ibudilast (CAS 50847-11-5), a phosphodiesterase 4 (PDE4) inhibitor, was evaluated in a photochemically-induced guinea pig carotid artery thrombosis model in combination with low-dose ASA. The time required to decrease the carotid artery blood flow to the reading "zero" was defined as the time to occlusion (TTO) of the artery through thrombogenesis. Read More

    CYP2C9*3(1075A>C), MDR1 G2677T/A and MDR1 C3435T are determinants of inter-subject variability in fluvastatin pharmacokinetics in healthy Chinese volunteers.
    Arzneimittelforschung 2012 Nov 31;62(11):519-24. Epub 2012 Aug 31.
    Department of Pharmacy, the 2nd Affiliated Hospital, School of Medicine, Zhejiang University, Zhejiang, Zhejiang Province, China.
    To evaluate the impact of single-nucleotide polymorphisms (SNPs) in CYP2C9, MDR1, SLCO1B1 and ABCG2 on the pharmacokinetics of fluvastatin in Chinese participants.A pharmacokinetic study of fluvastatin (single dose 40 mg) was conducted in 12 healthy Chinese volunteers. Plasma concentrations of fluvastatin were determined by a high-performance liquid chromatography with fluorescence detection. Read More

    The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy)caffeine analogues.
    Arzneimittelforschung 2012 Nov 31;62(11):513-8. Epub 2012 Aug 31.
    Pharmaceutical Chemistry, School of Pharmacy, North-West University, Potchefstroom, South Africa.
    Previous studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an IC50 value of 0.383 µM towards MAO-B. Read More

    Development and validation of a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of acrivastine and pseudoephedrine in human plasma and its application in pharmacokinetics.
    Arzneimittelforschung 2012 Oct 30;62(10):449-56. Epub 2012 Aug 30.
    Department of Pharmacy, Kunming General Hospital of Chengdu Military Command, Kunming, Yunnan, PR China.
    A specific, sensitive and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed for the simultaneous determination of acrivastine and pseudoephedrine in human plasma samples. Plasma samples were processed and analyzed on a Phenomenex Luna 3 μ CN 100A column (150 mm×2.0 mm) eluted with the mobile phase consisting of methanol and 0. Read More

    Bioequivalence of lamotrigine 50-mg tablets in healthy male volunteers: a randomized, single-dose, 2-period, 2-sequence crossover study.
    Arzneimittelforschung 2012 Oct 29;62(10):470-6. Epub 2012 Aug 29.
    Clinical Pharmacology Center (FLENI-mrc/ Centralab CR), Buenos Aires, Argentina.
    Unlabelled: OBEJCTIVE: To compare the bioavailability of two 50-mg lamotrigine dispersible tablet formulations (Epilepax®, Ivax-TEVA Argentina Laboratories, Argentina, as a test formulation, and Lamictal®, GlaxoSmithKline, UK, as a reference formulation) in 24 healthy male volunteers.

    Material And Methods: This study was a randomized, 2-period, 2-sequence crossover design that was open for subjects and investigators, but blind for the bioanalytical lab. Serum samples were obtained over a 120-h interval. Read More

    Pharmacokinetics and bioequivalence of 2 tablet formulations of olanzapine in healthy Chinese volunteers: a randomized, open-label, single-dose study.
    Arzneimittelforschung 2012 Nov 29;62(11):508-12. Epub 2012 Aug 29.
    Central Laboratory, Shanghai Xuhui Central Hospital, Shanghai, China.
    Olanzapine is a widely used agent for the treatment of schizophrenia.The aim of this study was to evaluate bioequivalence of two 10-mg tablet formulations of olanzapine following single oral dose in adult male volunteers.This was a randomized, single-dose, open-label, crossover bioequivalence study. Read More

    Synthesis and pharmacological investigation of 5-substituted-3-methylsulfanyl-1H-pyrazole-4-carboxylic acid ethyl esters as new analgesic and anti-inflammatory agents.
    Arzneimittelforschung 2012 Oct 29;62(10):457-62. Epub 2012 Aug 29.
    Department of Pharmaceutical Chemistry, Vinayaka Mission's College of Pharmacy, Sankari Main Road, Ariyanoor, Salem, India.
    Purpose: To synthesize a new series of 5-substituted-3-methylsulfanyl-1H-pyrazole-4-carboxylic acid ethyl esters for their analgesic and anti-inflammatory activity.

    Methods: The title compound synthesized by reacting the amino group of 5-amino-3-methylsulfanyl-1H-pyrazole-4-carboxylic acid ethyl ester with acid anhydrides, acid chlorides and phenyl dithiocarbamates. The synthesized compounds were characterized by IR, 1H-NMR and mass spectral data; the purity of the compounds was determined by elemental analysis. Read More

    Effects of milk casein derived tripeptides on endothelial enzymes in vitro; a study with synthetic tripeptides.
    Arzneimittelforschung 2012 Oct 23;62(10):477-81. Epub 2012 Aug 23.
    Institute of Biomedicine, Pharmacology, University of Helsinki, Helsinki, Finland.
    In the fermentation of milk by certain lactic acid bacteria, casein is degraded into bioactive tripeptides shown to lower blood pressure in experimental animal models and in mildly hypertensive humans. This effect is suggested to result mainly in inhibition of angiotensin converting enzyme 1 (ACE-1).Due to the complexity of renin-angiotensin system (RAS), several other enzymes than ACE-1 can participate in the production of vasoactive components. Read More

    Development of a subcutaneous formulation for trastuzumab - nonclinical and clinical bridging approach to the approved intravenous dosing regimen.
    Arzneimittelforschung 2012 Sep 23;62(9):401-9. Epub 2012 Aug 23.
    F. Hoffmann-La Roche Ltd., Clinical Pharmacology, Basel, Switzerland.
    A subcutaneous (SC) formulation has been developed for the humanized monoclonal antibody (mAb) trastuzumab as an alternative to established intravenous (IV) infusion. The ready-to-use liquid SC formulation is injected as a fixed dose in approximately 5 min, which is expected to increase patient's convenience, reduce pharmacy preparation time, and administration costs overall.The trastuzumab dose as well as the dose of recombinant human hyaluronidase (rHuPH20), an enzyme that enables SC administration of volumes larger than 2 mL, was selected based on nonclinical xenograft, pharmacology, and pharmacokinetics mouse and minipig studies. Read More

    Metronidazole immediate release formulations: a fasting randomized open-label crossover bioequivalence study in healthy volunteers.
    Arzneimittelforschung 2012 Oct 23;62(10):490-5. Epub 2012 Aug 23.
    Department of Pharmacy, College of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil.
    Metronidazole is a BCS (Biopharmaceutics Classification System) class 1 drug, traditionally considered the choice drug in the infections treatment caused by protozoa and anaerobic microorganisms. This study aimed to evaluate bioequivalence between 2 different marketed 250 mg metronidazole immediate release tablets. A randomized, open-label, 2×2 crossover study was performed in healthy Brazilian volunteers under fasting conditions with a 7-day washout period. Read More

    Bioequivalence study of 2 orodispersible formulations of zolmitriptan 5 mg in healthy volunteers.
    Arzneimittelforschung 2012 Oct 23;62(10):482-6. Epub 2012 Aug 23.
    Laboratorios Lesvi, S.L.- Invent Farma Group, Sant Joan Despí, Barcelona, Spain.
    A bioequivalence study of 2 zolmitriptan (CAS 139264-17-8) orodispersible tablet formulations was carried out in 26 healthy volunteers according to an open label, randomized, 2-period, 2-sequence, crossover, single dose and fasting conditions design. The test and reference formulations were administered in 2 treatment days, separated by a washout period of 7 days. Plasma concentrations of zolmitriptan and its active metabolite (N-desmethyl-zolmitriptan) were obtained by LC/MS/MS method. Read More

    Pharmacokinetic study of a new derivative of sulfamethoxazole.
    Arzneimittelforschung 2012 Oct 23;62(10):487-9. Epub 2012 Aug 23.
    Deparment of Chemistry, Forman Christian College, Lahore, Pakistan.
    The study was aimed at determination of pharmacokinetic parameters of a previously synthesized salicylidine-sulfamethoxazole-Zn(II) monohydrate in normal humans. This new derivative of sulfamethoxazole was reported to be more active and less toxic than the parent drug by our group. 10 volunteers received a 200 mg dose of the drug orally. Read More

    Vasodilation and hypotension of CZ454, an analogue of lacidipine through inhibiting extracellular calcium influx.
    Arzneimittelforschung 2012 Sep 9;62(9):439-45. Epub 2012 Aug 9.
    Department of Pharmacology, Xi'an Jiaotong University College of Medicine, Xi'an, Shaanxi, China.
    The aim of this study was to evaluate the effects of an analogue of lacidipine, CZ454 in in vitro and in vivo. The isometric tension of Sprague-Dawley rat arterial ring segments was recorded by a myography system. Intracellular calcium of vascular smooth muscle was determined by the confocal laser microscopy. Read More

    Paracetamol (acetaminophen) - a popular and widely used nonopioid analgesic.
    Arzneimittelforschung 2012 Aug 1;62(8):355-9. Epub 2012 Aug 1.
    Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart and University of Tuebingen, Germany.
    For several decades paracetamol has proven its clinical efficacy and safety in the treatment of various acute and chronic pain states. Whereas its pharmacokinetic properties (high oral bioavailability, good penetration into the brain, relative rapid hepatic elimination) are well known, its exact central mode of action remains to be elucidated. According to many international guidelines/recommendations paracetamol is a drug of first choice for relieving mild to moderate pain. Read More

    Design and synthesis of novel 3-(4-chlorophenyl)-2-(3-substituted propyl thio) quinazolin-4-(3H)-ones as a new class of H1-antihistaminic agents.
    Arzneimittelforschung 2012 Sep 1;62(9):433-8. Epub 2012 Aug 1.
    Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy, Hyderabad, Andhra Pradesh, India.
    A series of novel 3-(4-chlorophenyl)-2-(3-substituted propyl) quinazolin-4-(3H)-ones have been synthesized and tested for their in vivo H1-antihistaminic activity on conscious guinea pigs. All the test compounds have protected the animals from histamine induced bronchospasm significantly. Compound 3-(4-chlorophenyl)-2-(3-(4-methylpiperazin-1-yl) propylthio) quinazolin-4(3H)-one (PC5) emerged as the most active compound (77. Read More

    Liquid chromatography - tandem mass spectrometry for the simultaneous quantitation of glipizide, cilostazol and its active metabolite 3, 4-dehydro-cilostazol in rat plasma: application for a pharmacokinetic study.
    Arzneimittelforschung 2012 Sep 20;62(9):425-32. Epub 2012 Jul 20.
    Incozen Therapeutics Private Limited, Andhra Pradesh, India.
    A liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS) method for the simultaneous quantitation of glipizide, cilostazol and 3, 4-dehydro-cilostazol in rat plasma was developed and validated. Glimepride was used as an internal standard (IS). The analytes were extracted by using liquid-liquid extraction procedure and separated on a reverse phase C18 column (50 mm×4. Read More

    Comparative pharmacokinetics and bioequivalence of two 50 mg atenolol tablet formulations in healthy Korean male volunteers.
    Arzneimittelforschung 2012 Sep 12;62(9):410-3. Epub 2012 Jul 12.
    College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, South Korea.
    Atenolol is a selective β1 receptor antagonist that is available as a racemic mixture. The objective of this study was to compare the pharmacokinetics and evaluate the bioequivalence of 50 mg atenolol test and reference formulations in 24 healthy Korean male volunteers.This study was a single-dose, randomized, open-label, 2 period crossover study. Read More

    Comparative fasting bioavailability and pharmacokinetic properties of 2 formulations of glucosamine hydrochloride in healthy Chinese adult male volunteers.
    Arzneimittelforschung 2012 Aug 12;62(8):367-71. Epub 2012 Jul 12.
    Department of Pharmacology, School of Pharmaceutical Sciences, China Medical University, Shenyang, People's Republic of China.
    Glucosamine (CAS 66-84-2) hydrochloride is an amino monosaccharide indicated for the treatment of arthrosis, especially osteoarthritis of the knee joint. This study was conducted to assess and compare the pharmacokinetic (PK) properties, bioavailability of a newly developed dispersible tablet formulation (test) of glucosamine hydrochloride with those of an established branded capsule formulation (reference) in healthy Chinese adult male volunteers.This single-dose, randomized, open-label, 2-period crossover study was conducted in 18 healthy Chinese adult male volunteers under fasting condition. Read More

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