Arzneimittel Forsch
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Arzneimittel Forsch · Jan 2011
Randomized Controlled Trial Comparative StudyTruncated areas under the curve in the assessment of pioglitazone bioequivalence. Data from a single-center, single-dose, randomized, open-label, 2-way cross-over bioequivalence study of two formulations of pioglitazone 45 mg tablets under fasting conditions.
Pioglitazone (CAS 112529-15-4 for the HCl form) is an oral antidiabetic agent that is a member of the group of drugs known as thiazolidinediones. It is indicated for the treatment of type 2 diabetes mellitus. ⋯ Bioequivalence between test and reference formulations, both in terms of rate and extension of absorption, under fasting conditions was concluded according to European guidelines. Both formulations were well tolerated. The conclusion of bioequivalence was also supported using the truncated AUCs approach.
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Arzneimittel Forsch · Jan 2011
Randomized Controlled TrialPharmacokinetics and bioequivalence study of two mosapride citrate formulations after single-dose administration in healthy Chinese male volunteers.
The pharmacokinetics and relative bioavailability/bioequivalence of two formulations of mosapride citrate (CAS 112885-42-4) were assessed in this study. The study was conducted in 20 healthy Chinese male volunteers according to an open, randomized, single-blind, 2-way crossover study design with a wash-out phase of 7 days. Blood samples for pharmacokinetic profiling were taken up to 12 h post-dose, and mosapride citrate plasma concentrations were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. ⋯ Bioequivalence between test and reference formulations was demonstrated for both parameters, AUJCo-infinity and AUCo-t. The 90% confidence intervals of the T/R-ratios of logarithmically transformed data were in the generally accepted range of 80-125%. That means that the test formulation is bioequivalent to the reference formulation of mosapride citrate.
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Arzneimittel Forsch · Jan 2011
Assessment of the extent of oxidative stress induced by intravenous ferumoxytol, ferric carboxymaltose, iron sucrose and iron dextran in a nonclinical model.
Intravenous (i.v.) iron is associated with a risk of oxidative stress. The effects of ferumoxytol, a recently approved i.v. iron preparation, were compared with those of ferric carboxymaltose, low molecular weight iron dextran and iron sucrose in the liver, kidneys and heart of normal rats. In contrast to iron sucrose and ferric carboxymaltose, low molecular weight iron dextran and ferumoxytol caused renal and hepatic damage as demonstrated by proteinuria and increased liver enzyme levels. ⋯ Inflammatory markers were also significantly higher with ferumoxytol and low molecular weight iron dextran rats than iron sucrose and ferric carboxymaltose. Polarographic analysis suggested that ferumoxytol contains a component with a more positive reduction potential, which may facilitate iron-catalyzed formation of reactive oxygen species and thus be responsible for the observed effects. Only low molecular weight iron dextran induced oxidative stress and inflammation in the heart.
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Arzneimittel Forsch · Jan 2011
Randomized Controlled TrialInhibitory effect of procaterol on exercise dynamic lung hyperinflation during the 6-min walk test in stable patients with chronic obstructive pulmonary disease.
The purpose of this study was to evaluate the inhibitory effect of procaterol (procaterol hydrochloride, CAS 62929-91-3) on exercise dynamic lung hyperinflation during the 6-min walk test (6MWT) in stable chronic obstructive disease (COPD) patients. Fourteen patients with stable COPD who were referred to our clinic between July 2008 and October 2009 were evaluated in this study. After the inhalation of procaterol, values for the lung function test, including vital capacity, inspiratory capacity, forced vital capacity, and FEV1/FEV1pred showed a significant improvement. ⋯ The Borg scale increased significantly during the 6MWT and was attenuated after inhaling procaterol hydrochloride, though the difference between the two groups was not statistically significant. In the present study, there was a significant attenuation in exercise dynamic lung hyperinflation, suggesting the important role of the beta2-receptor agonist procaterol in the treatment of COPD. It is therefore likely that most patients with COPD may derive considerable benefit from bronchodilator therapy with procaterol.
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Arzneimittel Forsch · Jan 2011
Randomized Controlled Trial Comparative StudyComparative in vitro dissolution and in vivo bioequivalence of two diclofenac enteric coated formulations.
The aim of this study was the comparison of in vitro dissolution and in vivo bioavailability of two different brands of diclofenac sodium (CAS 15307-86-5) enteric coated tablets in healthy male Iranian volunteers in a single-dose, randomized, open-label, single blind study, which was conducted according to a crossover design in healthy volunteers. A washout interval of two weeks was selected between administrations to each subject in this study. Serial venous blood samples over 10 h after each administration to measure diclofenac sodium concentration in serum were obtained, and placed into tubes containing sodium heparin. ⋯ Results show that the 90% confidence intervals for the ratio of test and reference products in Cmax (101.4-114.9%), AUC(0)tau (96.3-109.1%) and AUC(0)infinity (94.7-107.3%) were all within the 80-125% interval proposed by the FDA and EMA. Both formulations released > 80% of drug within 30 min in buffer pH = 6.8 medium. Therefore the diclofenac sodium enteric coated tablets of the test and reference formulations are bioequivalent in terms of rate and extent of absorption.