Arzneimittel Forsch
-
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.
-
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.
-
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.
-
Arzneimittel Forsch · Jan 2010
Randomized Controlled TrialPharmacokinetics, safety and tolerability of intravenous ferric carboxymaltose: a dose-escalation study in volunteers with mild iron-deficiency anaemia.
Iron-deficiency anaemia (IDA) represents a major burden to public health worldwide. The therapeutic aim for patients with IDA is to return iron stores and haemoglobin (Hb) levels to within the normal range using supplemental iron therapy and erythropoiesis-stimulating agents. Oral and previous intravenous (i.v.) iron formulations have a number of disadvantages, including immunogenic reactions, oxidative stress, low dosages, long administration times and the requirement for a test dose. ⋯ This study satisfactorily characterized the PK/PD parameters of single doses of 100, 500, 800 and 1000 mg iron as FCM. The majority of FCM was utilized or eliminated within 24 h of administration of a 100 mg dose and within 72 h of a 500-1000 mg dose. FCM was generally well tolerated across all doses in patients with mild IDA.
-
Arzneimittel Forsch · Jan 2010
Randomized Controlled TrialPharmacokinetics and bioequivalence study of valacyclovir hydrochloride capsules after single dose administration in healthy Chinese male volunteers.
The aim of the present study was to compare the bioavailability of valacyclovir (CAS 124832-26-4; INN: valaciclovir) from two valacyclovir hydrochloride (CAS 214832-27-5) capsules (150 mg/capsule as test preparation and 150 mg/capsule commercially available original capsule of the drug as reference preparation) in 20 Chinese healthy male volunteers, aged between 20 and 27. The study was conducted 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 24 h post-dose. ⋯ Bioequivalence between test and reference preparation was demonstrated for both parameters, AUC(0-infinity) and AUC(0-t). The 90% confidence intervals of the T/R-ratios of logarithmically transformed data were in the generally accepted range of 80-125%. It meant that the test formulation was bioequivalent to the reference formulation for valacyclovir hydrochloride.