Comparative bioavailability study of two oral omeprazole formulations after single and repeated administrations in healthy volunteers.

Objective: Two oral enteric-coated pellet formulations of omeprazole, Pepticum((R)) (test formulation) and Mopral((R)) (reference), were administered to 24 healthy volunteers for 5 days at a daily dose of 20mg omeprazole in order to investigate the comparative bioavailability of the two formulations.

Results: The data obtained in this study demonstrated the bioequivalence of the two formulations. No statistical differences were observed for the area under the plasma concentration-time curve (AUC(0-t)), the parameter to which the inhibition of acid secretion induced by omeprazole is directly related.

Sensitive method for the quantitative determination of bromocriptine in human plasma by liquid chromatography-tandem mass spectrometry.

A sensitive LC-MS-MS assay for the quantitative determination of bromocriptine has been developed and validated and is described in this work. The assay involved the extraction of the analyte from 1 ml of human plasma using a solid phase extraction on Oasis MCX cartridges. Chromatography was performed on a Symmetry C18 (2.

Population pharmacokinetics of ibuprofen enantiomers in very premature neonates.

The objective of the present study was to evaluate the pharmacokinetic parameters for both S- and R-ibuprofen enantiomers in very premature neonates (gestational age strictly inferior to 28 weeks) and possible relationships between the pharmacokinetic parameters and various covariates. Newborns were randomized to receive ibuprofen or placebo for the prophylactic treatment of patent ductus arteriosus (PDA) at an initial dose of 10 mg/kg ibuprofen within 6 hours after birth, followed by two 5-mg/kg doses at 24-hour intervals (n = 52). If a PDA was still present afterwards, a curative course of ibuprofen using the same dosage regimen was administered (n = 10).

Pharmacokinetics and tolerability of prulifloxacin after single oral administration.

The pharmacokinetic properties and tolerability of three different strengths of prulifloxacin (CAS 123447-62-1), a new antibacterial agent prodrug of AF3013 (CAS 112984-60-8), have been investigated in a randomized, cross-over study performed in 12 Caucasian male subjects (age range 19-34 years). Prulifloxacin was administered as a single oral dose at the dosages of 300, 450 and 600 mg. Plasma concentrations of the active metabolite AF3013 were determined in blood samples collected before the administration (pre-dose) and at 15, 30, 45 min, 1, 1.

Multiple-dose pharmacokinetics and excretion balance of gatifloxacin, a new fluoroquinolone antibiotic, following oral administration to healthy Caucasian volunteers.

The multiple-dose pharmacokinetics and excretion balance of gatifloxacin were evaluated in 42 healthy Caucasian volunteers. Following multiple oral doses of 400 and 600 mg, the pharmacokinetics of gatifloxacin were similar on days 1 and 15, suggesting no therapeutically relevant time-dependent changes in the pharmacokinetics of gatifloxacin at the doses and duration of dosing studied. Gatifloxacin was rapidly absorbed and a favourable elimination half-life of 7-8 h was evaluated.

Comparison of plasma pharmacokinetics and bioavailability of ceftiofur sodium and ceftiofur hydrochloride in pigs after a single intramuscular injection.

Ceftiofur sodium, a broad-spectrum cephalosporin, is active against gram-positive and gram-negative pathogens of veterinary importance. Two studies were designed to compare the intramuscular bioavailability of the current sodium salt and the new hydrochloride salt in pigs at doses of either 3 mg or 5 mg ceftiofur equivalents (CE)/kg body weight. Twenty-six healthy young pigs were selected for these two-period, two-treatment crossover studies, 12 for the 3 mg/kg study and 14 for the 5 mg/kg study.

High-performance liquid chromatographic determination of baclofen in human plasma.

A reversed-phase isocratic HPLC method is described for the determination of baclofen in human plasma. Solid-phase extraction using a SCX Bond Elut column is used followed by derivatization with o-phthalaldehyde-tert.-butanethiol and electrochemical detection.

Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites.

The pharmacokinetics of terbinafine and its inactive metabolites SDZ 86-621 (the N-demethyl form), SDZ 280-027 (the carboxybutyl form), and SDZ 280-047 (N-demethyl- carboxybutyl form) in plasma were characterized for 10 healthy male subjects receiving 250 mg of terbinafine orally once a day for 4 weeks and in the subsequent 8-week washout phase. Terbinafine concentrations were also measured in sebum, hair, nail, and stratum corneum samples. Concentrations of the parent compound and metabolites were determined by validated high-performance liquid chromatography methods.

Determination of ceftiofur and its desfuroylceftiofur-related metabolites in swine tissues by high-performance liquid chromatography.

An HPLC method was developed and validated for the determination of ceftiofur-related metabolites that have the potential to be microbiologically active in swine muscle, kidney, liver and fat. Its performance was evaluated against incurred-residue swine tissues. This method is based on the cleavage of the disulfide and/or thioester bonds between the metabolites and their conjugate sulfur containing moiety using dithioerythritol to yield desfuroylceftiofur, and further stabilization to desfuroylceftiofur acetamide.

Levels of terbinafine in plasma, stratum corneum, dermis-epidermis (without stratum corneum), sebum, hair and nails during and after 250 mg terbinafine orally once daily for 7 and 14 days.

In earlier skin pharmacokinetic studies we have shown that terbinafine is rapidly delivered to the stratum corneum, nails and hair both through sebum and by direct diffusion through dermis-epidermis. In the present study the skin pharmacokinetic profile of terbinafine was studied in two groups of eight human male volunteers during and after 250 mg orally once daily for 7 and 14 days. In the 7-day study high terbinafine levels were found in sebum (19.

Levels of terbinafine in plasma, stratum corneum, dermis-epidermis (without stratum corneum), sebum, hair and nails during and after 250 mg terbinafine orally once per day for four weeks.

The distribution of terbinafine in stratum corneum dermis-epidermis (without stratum corneum), sebum, hair, nails and plasma was studied in human male volunteers during and after 250 mg orally once daily for 28 days. The highest concentration was seen in sebum, 56.07 micrograms/g, after 14 days of therapy.

Pharmacokinetics of cefotiam administered intravenously and intramuscularly to healthy adults.

We studied the pharmacokinetics of cefotiam, a parenteral cephalosporin, at intravenous doses of 0.5, 1, and 2 g and intramuscular doses of 0.5 and 1 g in two groups of eight healthy adult volunteers.

Relationship between a spleen-derived immunosuppressive peptide 'SDIP' and the 'Facteur thymique sérique' (FTS): biochemical and biological comparison of the two factors.

A spleen-derived immunosuppressive peptide (SDIP) has been purified to homogeneity. Its physicochemical properties (electrophoretic mobility, u.v.

New insight into lymphocytic chalone research. The 'facteur thymique Sérique' might be responsible for part of the immunosuppressive activity detected in the 'chalone fraction'.

Immunosuppressive activities have been detected in bovine spleen extracts and attributed to the presence of a 'lymphocytic chalone'. Following the immunosuppression of a T cell-dependent humoral response in mice as assay, we purified a peptide to homogeneity present at a concentration of 10-50 ng/kg of spleen whose properties were identical to those of the serum thymic factor. This factor appeared to be a regulator of the humoral immune response in the splenic extract and as such might be responsible for part of the immunosuppressive activities detected in the splenic 'chalone' fraction.

Further study on the humoral response of a highly-purified spleen-derived immunosuppressive peptide (SDIP).

Some biological properties of a highly-purified non-cytotoxic spleen-derived immunosuppressive peptide (SDIP) have been investigated. SDIP was shown to inhibit the primary anti-sheep red blood cell (SRBC) response at the last step of differentiation of the lymphocyte. In the present study we demonstrated that this response seemed to be T- and adherent spleen-cell dependent as no inhibition was noticed either in the response to TNP-LPS, a T-independent antigen, or in the response to SRBC in adherent spleen cell-depleted cultures.

[From the search for a lymphocytic chalone to the rediscovery of serum thymic factor (FTS)].

Looking for a "lymphocytic chalone" in Bovine spleen extracts, we isolated an immunosuppressive peptide, whose biochemical and biological properties are identical to those of the serum thymic factor FTS. This factor appeared to be a regulator of the humoral immune response.

Influence of a bovine spleen extract on immunological responses in mice.

The presence of immunological stimulatory and inhibitory activities has been detected in a bovine spleen extract F prepared by acetic extraction of an acetonic powder. F was fractioned after water dilution, by ultrafiltration on an Amicon PM-10 membrane. Two successive ultrafiltrates (mol.