The pharmacokinetics and metabolism of the l-threo isoleucine thiazolidide dipeptidyl peptidase IV inhibitor, di-[2S,3S]-2-amino-3-methyl-pentanoic-1,3-thiazolidine fumarate (ILT-threo) and its allo stereoisomer (ILT-allo) were evaluated in rats, dogs, and monkeys. Both compounds were well absorbed (>80%) in all species, and most of the dose (>60%) was recovered in urine. Metabolites identified...

Insulin glargine is processed in vivo into soluble 21(A) -Gly-human insulin (M1), the principal moiety responsible for metabolic effects, and subsequently into M2. This sub-study compared metabolism and metabolite pharmacokinetic (PK) profiles of investigational new insulin glargine U300 (Gla-300) with insulin glargine 100 U/ml (Gla-100, Lantus®, Sanofi-Aventis Deutschland GmbH, Frankfurt am Ma...

The metabolism and excretion of trovafloxacin was investigated in four healthy male volunteers after a single oral administration of 200 mg of [14C]trovafloxacin (118 microCi). Mean values of 23.1 and 63.3% of the administered dose were recovered in the urine and feces, respectively, after 240 hr. The Cmax of total radioactivity and unchanged trovafloxacin in serum was 3.2 micrograms-equiv/ml a...

The pharmacokinetics of intravenous ciprofloxacin and its metabolites were characterized in 42 subjects with various degrees of renal function (group 1, Clcr (mL/min/1.73 m2) > 90, n = 10; group 2, Clcr 61-90, n = 11; group 3, Clcr 31-60, n = 11; group 4, Clcr < or = 30, n = 10). The dosage regimens were-groups 1 and 2: 400 mg i.v. at 8 hourly intervals; group 3: 400 mg i.v. at 12 hourly interv...

Human peripheral-blood monocytes are used as an established in vitro system for generating macrophages. For several reasons, monocytic cell lines such as THP-1 have been considered as a possible alternative. In view of their distinct developmental origins and phenotypic attributes, we set out to assess the extent to which human monocyte-derived macrophages (MDMs) and phorbol-12-myristate-13-ace...

While silica nanoparticles have enabled numerous industrial and medical applications, their toxicological safety requires further evaluation. Macrophages are the major cell population responsible for nanoparticle clearance in vivo. The prevailing macrophage phenotype largely depends on the local immune status of the host. Whereas M1-polarized macrophages are considered as pro-inflammatory macro...

We investigate the expressive power of memory logics. These are modal logics extended with the possibility to store (or remove) the current node of evaluation in (or from) a memory, and to perform membership tests on the current memory. From this perspective, the hybrid logic HL(↓), for example, can be thought of as a particular case of a memory logic where the memory is an indexed list of elem...

The main aim of this study was to find a suitable rabies vaccination protocol which would allow usage of lower volumes of vaccine, fewer clinical visits and above all, enough serological effectiveness for high-risk individuals requiring pre-exposure immunization. Human diploid cell rabies vaccine was administered intradermally and intramuscularly in 60 previously unvaccinated volunteers, aged 1...

the main aim of this study was to find a suitable rabies vaccination protocol which would allow usage of lower volumes of vaccine, fewer clinical visits and above all, enough serological effectiveness for high-risk individuals requiring pre-exposure immunization. human diploid cell rabies vaccine was administered intradermally and intramuscularly in 60 previously unvaccinated volunteers, aged 1...

Metabolism of a new antitumor agent, CAI (NSC 609974), was investigated in human liver tissue in vitro and in plasma and urine of patients receiving CAI. Metabolites identified by HPLC following C-labeled CAI incubation with human liver microsomes and reported as percentage of total metabolites formed were M1 (0-3.4%), M2 (4. 5-33%), M3 (60-79%), and M4 (7.2-19%). Ketoconazole, an inhibitor of ...