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S Mészáros

Publications and source records attributed to S Mészáros.

8 recordsLinked to original sources
PubMed2004

Anti-inflammatory effect and soft properties of etiprednol dicloacetate (BNP-166), a new, anti-asthmatic steroid.

In vitro and in vivo anti-inflammatory properties and soft characteristics of etiprednol dicloacetate (BNP-166) a new steroid, which has been developed for the treatment of asthma, were investigated in this study. The compound effectively decreased cytokine production in lipopolysaccharide stimulated lymphocytes and attenuated lectin-induced proliferation of blood mononuclear cells in tissue culture. In an animal model of allergen sensitized and challenged Brown Norway rats, using topical treatment, etiprednol dicloacetate substantially attenuated the extent of allergen induced bronchoalveolar fluid eosinophilia. At every examined parameter its pharmacological effects were comparable to those of budesonide. By means of in vitro biological and analytical methods the soft character of BNP-166 was also investigated. The anti-inflammatory effect of etiprednol dicloacetate in vitro was shown to be the function of the quantity of serum components, present in the assay. This loss of activity was most likely the result of the fast metabolism of etiprednol dicloacetate, which in the presence of sera could have been demonstrated by LC/MS/MS. Our data indicate that the significant local effect of the compound will very likely be accompanied with a drastically reduced systemic activity indicating an encouraging selectivity of the pharmacological action of etiprednol dicloacetate.

Adrenal Cortex Hormones↗
PubMed1994

Pharmacokinetic study on a new antiischaemic agent (BRLP-42).

In the present study the pharmacokinetics of BRLP-42--a new antiischaemic agent--was investigated in dogs and rats. Plasma concentrations were measured by HPLC. After intravenous application the curves can be characterized by a two-compartment open pharmacokinetic model. The central volume of distribution (Vcentr.) is large (1.07 +/- 0.14 l/kg in dogs and 2.74 l/kg in rats), the first elimination half-life (t1/2 alpha) is 5.47 +/- 1.67 min in dogs and 13.7 min in rats. These facts indicate rapid and large tissue distribution. The excretion and/or metabolic elimination of BRLP-42 resulted in short second elimination half-life (t1/2 beta = 41.45 +/- 2.34 min in dogs and 43.8 min in rats). After oral application high individual variability can be seen. This fact may be due to the different rate and/or extent of absorption process. The plasma level curves can be characterized by a one-compartment open pharmacokinetic model. The absorption seems to conceal the distribution phase of the kinetic curve. The absorption half-life was short (t1/2a = 17.36 +/- 5.90 min in dogs and 2.7 min in rats). The bioavailability was 40 +/- 8% in dogs and 28% in rats. The elimination half-life (t1/2e = 28.77 +/- 0.88 min in dogs and 30.1 min in rats) is connected dominantly with metabolic elimination and/or excretion of BRLP-42. In the cases of intravenous as well as oral administrations the plasma concentrations decreased under the limit of quantitation by 4-6 hours in dogs and 4 hours in rats after treatments.

Administration, Oral↗
PubMed1993

[Pharmacokinetic studies of epervudine in rats using HPLC].

Pharmacokinetic properties of active substance of Hevizos ointment (Epervudine) were studied in rats after intravenous, oral and dermal applications. The animals received 10 mg/kg of Epervudine intravenously and orally. For checking of dermal absorption 220 mg of ointment (containing 0.8% of Epervudine) was applied. An HPLC method was developed for determination of Epervudine concentrations in serum. The method meets the requirements of precision and accuracy of the kinetic measurements (i.e. CV% is less than 20%) within the concentration range of 50-10,000 ng/ml. The mean serum concentration-time curve after i.v. administration can be characterized by a two-compartment open pharmacokinetic model. The first and second elimination half-lives (t1/2 alpha and t1/2 beta) are 0.14 and 0.31 hours, respectively. These values indicate fast distribution and elimination of compound studied. In the case of oral administration the absorption process conceals the fast distribution, so the mean serum concentration-time curve can be characterized by a one-compartment open pharmacokinetic model. The absorption of Epervudine starts practically prompt. The absorption half-life (t1/2a) is 0.11 hours. Highest serum concentrations were measured from 20 to 90 minutes after treatment. The elimination half-life (t1/2e) is 1.53 hours. The ratio of areas under serum level curves following oral and intravenous administration proves a good bioavailability (90%) of Epervudine. After dermal application Epervudine does not absorb.

Administration, Oral↗
PubMed1992

Pharmacokinetic and metabolism studies on girisopam by chromatographic and spectrometric methods in humans.

Girisopam possesses selective anxiolytic action without muscle relaxant and anticonvulsive activity. After a 100-mg oral dose of 14C-labelled girisopam to seven male subjects, the mean recovery of 14C radioactivity was 51% in urine and 33% in faeces. A high-performance liquid chromatographic method has been developed for studying girisopam in single-dose pharmacokinetic studies. The serum extract was chromatographed on a normal-phase column using a mobile phase of hexane-ethanol-diethyl ether (66:9:25, v/v) and ultraviolet detection at 235 nm. The recovery was 60% and the detection limit was 3 ng/ml, using 1 ml of serum. After a 20-min delay, girisopam is rapidly absorbed. After reaching a mean serum level of 178 ng/ml at a mean time of 2.0 h, the serum concentration of girisopam decreased with a mean elimination half-time of 22.2 h. The metabolites were separated by high-performance liquid chromatography, radio thin-layer chromatography and gas chromatography. Their structures were determined by liquid chromatography-mass spectrometry, mass spectrometry and gas chromatography-mass spectrometry. Their chemical structures were confirmed by comparison with synthesized reference compounds. The major urinary metabolites were 7-demethylgirisopam (I), 4'-hydroxygirisopam (II) and 4-hydroxymethyl-4-demethylgirisopam (III), which were in conjugated form, and 4-carboxy-4-demethylgirisopam (V), a compound with an open-chain structure (VII) and traces of 4-demethyl-4-oxogirisopam (VIII) and 4-hydroxymethyl-4-demethylgirisopam (III), which were in non-conjugated form. The metabolic profile in the serum consisted predominantly of the glucuronides of I, II and III. The non-conjugated metabolites were the metabolite with the open-chain structure (VII), III and V. Besides the parent compound, the faeces sample contained conjugates of I and II.

Adult↗
PubMedDate not supplied

[In vivo bioequivalence study of Sulpirid (GYKI-Alkaloida) and Dogmatil fort (Delagrange) 200 mg sulpiride tablets in healthy volunteers].

A single-dose, "crossover" bioequivalence study was conducted in healthy volunteers by comparing sulpiride serum levels after oral administration of the Test Product Sulpiride (200 mg) (GYKI-Alkaloida) in fasting subjects with those produced after oral administration of a marketed reference product (200 mg) (Delagrange Co., France). Statistical comparisons of Cmax, Tmax and AUC0-infinity have been performed utilizing ANOVA with subject, group, subject within group, period and product as sources of variance. No significant differences between the Test Drug and the Reference Drug considering the pharmacokinetic parameters Cmax, Tmax and AUC0-infinity were found. The 95% confidence intervals were as follows: AUC0-infinity: -20.46% and 31.19%, Cmax: -28.05% and 26.65% and Tmax: -43.53% and 20.67%. In the study for the analysis of Sulpiride a specific HPLC procedure with uv detection (lambda = 228 nm) and an internal standard were applied according to P. Nicolas et al. with modification. Sulpiride levels in serum reached a maximum at 4.4 hr +/- 1.5 (S.D.) following administration of Sulpiride tablet and at 5.0 hr +/- 0.8 (S.D.) after Dogmatil fort tablet. The maximal serum concentrations were 506.1 ng/ml +/- 87.2 (S.D.) and 509.1 ng/ml +/- 101.9 (S.D.) for Sulpiride and Dogmatil fort, respectively. The half-life of Sulpiride in serum was 9.9 hr +/- 1.3 (S.D.) following dosing with Dogmatil fort tablet and 12.2 hr +/- 3.0 (S.D.) following dosing with Sulpiride tablet.

Adult↗