Search results for "kinetics"
showing 10 items of 2224 documents
Enriched cereal bars are more effective in increasing plasma quercetin compared with quercetin from powder-filled hard capsules
2011
The flavonol quercetin, is one of the major flavonoids found in edible plants. The bioavailability of quercetin in humans may be influenced by the food matrix in which it is consumed as well as by its chemical and physical form. The objective of the present study was to investigate the biokinetics of quercetin from quercetin-enriched cereal bars and quercetin powder-filled hard capsules. In a randomised, single-blinded, diet-controlled cross-over study, six healthy women aged 22–28 years took a single oral dose of approximately 130 mg quercetin equivalents from either quercetin-enriched cereal bars (containing 93·3 % quercetin aglycone plus 6·7 % quercetin-4′-glucoside) or quercetin powder-…
Transfer of aciclovir from plasma to human breast milk.
2011
Aciclovir (CAS 59277-89-3) is frequently used in herpes simplex virus diseases, but administration to lactating women occurs only rarely. Therefore, information about the pharmacokinetics of aciclovir in human breast milk is limited. The concentration in breast milk is 2 to 3 fold increased compared to plasma. The reason for this increase is unknown until now. An active transport mechanism has been assumed. The aim of this study was to prove whether the higher concentration of aciclovir in human breast milk is due to only a passive transfer. Two chambers separated by a semipermeable membrane were used. The first chamber contained plasma with aciclovir, the second chamber breast milk without…
Oral versus intravenous vinorelbine: clinical safety profile
2005
The availability of chemotherapeutic drugs administrable by oral route represents a step forward in the management of cancer patients. Among oral agents, vinorelbine is particularly interesting for its pharmacological characteristics and clinical efficacy. Oral vinorelbine is rapidly absorbed (1.5-3 hours) with an elimination half-life of approximately 40 hours. It shows a low level of binding to plasma proteins (13%), is highly bound to platelets (78%) and has a hepatic metabolism and an absolute bioavailability of 40% with a moderate and similar interpatient variability for the two forms. Food has no influence on the pharmacokinetic profile of oral vinorelbine even if nausea/vomiting is l…
Pharmacokinetics of Droloxifene and Its Metabolites in Breast Cancer Patients
1991
Pharmacokinetics and metabolism of droloxifene, a new antiestrogenic drug, have been investigated by single- and multiple-dose studies in postmenopausal patients with advanced breast cancer. Short terminal elimination half-life, low accumulation, and improved drug tolerability are the most striking features of this safe and effective new antiestrogen. Bioequivalence of film-coated tablet, tablet, and standard solution of droloxifene has been shown. The concentrations of droloxifene and its metabolites have been determined by a highly selective HPLC method.
Cervical carcinoma: standard and pharmacokinetic analysis of time-intensity curves for assessment of tumor angiogenesis and patient survival
1999
Since detailed knowledge regarding the pathophysiological properties—which in turn are responsible for differences in contrast enhancement—remain fairly undetermined, it was the aim of this study (i) to examine the association of standard and pharmacokinetic analysis of time-intensity curves in dynamic MRI with histomorphological markers of tumor angiogenesis (microvessel density [MVD]; vascular endothelial growth factor [VEGF]) and (ii) to determine the ultimate value of a histomorphological and a dynamic MRI approach by correlation of those data with disease outcome in patients with primary cancer of the uterine cervix. Pharmacokinetic parameters (amplitude A, exchange rate constantk 21) …
A first-in-human study of PDC31 (prostaglandin F2 receptor inhibitor) in primary dysmenorrhea
2014
What is the safe and pharmacodynamically active dose range for PDC31 (prostaglandin F2α receptor inhibitor) in patients with primary dysmenorrhea (PD)?The 1 mg/kg/h dose of PDC31 appears to be safe and potentially effective in reducing intrauterine pressure (IUP) and pain associated with excessive uterine contractility when given as a 3-h infusion in patients with PD.PDC31 has previously been shown to reduce the duration and strength of PGF2α-induced contractions in human uterine myometrial strip models and to delay delivery in animal models of preterm labor.This was a prospective, multi-center, dose-escalating first-in-human Phase I study conducted from March 2011 to June 2012. A total of …
Enzyme replacement therapy in heterozygous females with Fabry disease: results of a phase IIIB study.
2003
Summary: Fabry disease is an X-linked glycosphingolipid storage disorder caused by a deficiency of α-galactosidase A. Affected patients experience debilitating neuropathic pain and have premature mortality due to renal failure, cardiovascular disease or cerebrovascular complications. The disease may be X-linked dominant, since most females heterozygous for Fabry disease are affected clinically. We evaluated the safety, efficacy and pharmacokinetics of agalsidase alfa (Replagal) administered intravenously to female patients with Fabry disease in an open-label, single-centre study. Fifteen severely affected patients received agalsidase alfa at 0.2 mg/kg every other week for up to 55 weeks. Ag…
Myelosuppressive effects of cytosine arabinoside (Ara‐C) on growth factor‐dependent human long‐term bone marrow cultures (LTBMC)
1992
Freshly isolated human mononuclear cells (5 × 106) were incubated in a Dexter-type long-term bone marrow culture (LTBMC) system to study myelosuppressive effects of cytosine arabinoside (Ara-C) in combination with granulocyte-macrophage colony-stimulating factor (GM-CSF) or interleukin 3 (IL-3). Differential counts (dc) of the nonadherent cell (nac) populations, starting with culture initiation, were performed weekly. After one week of simultaneous incubation of LTBMCs with either cytokine (100 ng/ml) and Ara-C (1 mg/ml), nac numbers were markedly reduced compared to controls. Dc after week 1 of culture demonstrated significant decreases of all myeloid cell fractions except for macrophages,…
Elevated risperidone serum concentrations during acute inflammation, two cases
2015
Inflammation-mediated changes in drug metabolism may lead to alterations in the absorption, distribution, and clearance of psychotropic drugs and thus elevate drug levels in blood and lead to intoxications. We report about two patients who developed an up to threefold increase of dose-related serum concentrations of risperidone’s active moiety (risperidone plus 9-hydroxyrisperidone) during acute inflammation indicated by elevated C-reactive protein. The two female patients (aged 56 and 38 years, respectively) had the diagnoses of paranoid schizophrenia and schizoaffective disorder. For both patients, there was a close time-dependent parallel fluctuation of drug levels and C-reactive protei…
Clinical benefits of a Bayesian model for plasma-derived factor VIII/VWF after one year of pharmacokinetic-guided prophylaxis in severe/moderate hemo…
2021
Abstract Introduction Individual pharmacokinetic (PK) profiling in hemophilia A (HA) helps to individualize prophylaxis using population PK models (popPK). A specific popPK model for plasma-derived factor VIII containing von-Willebrand Factor (pdFVIII/VWF) was developed. Aim To compare standard versus PK-driven prophylaxis, using a generic or a specific popPK model for pdFVIII/VWF. Materials and methods A prospective study conducted in HA patients in prophylaxis with pdFVIII/VWF (Fanhdi®) comparing three one-year study periods: (1) standard prophylaxis, (2) PK-guided prophylaxis using a generic pdFVIII popPK model which described FVIII activity irrespective of FVIII concentrate, and (3) PK-…