Bioequivalence study of 8 mg ondansetron film-coated tablets in healthy Caucasian volunteers.

The aim of the study was to investigate the bioequivalence of a generic product of 8 mg film-coated tablets (test) to the branded product (reference) at the same strength in order to apply for regulatory approval. The secondary objective of the study was to compare the tolerability of both products. A double blinded, randomized, cross-over, 2-period, comparative study was conducted in healthy Caucasian volunteers under fasting conditions. A single oral dose administration of the test or reference product was followed by a 7-day wash-out period. The ondansetron concentration was determined using a validated high performance liquid chromatography with a UV detection method. The 90% confidence interval of the point estimate (test over reference products) for C(max) and AUC(0-t) fell within the 80.00-125.00% acceptance range. The results of the study indicate that the film-coated tablets of Ondatron 8 mg manufactured by Tarchominskie Zaklady Farmaceutyczne Polfa S.A. (test product) are bioequivalent to those of Zofran manufactured by GlaxoSmithKline Export Ltd (reference product). Both products were well tolerated.

Enantioselectivity of 3-amino-2-oxazolidinone derivatives with potential psychotropic activity on cellulose tris(4-methylbenzoate) chiral selector.

The behavior of a series of 3-amino-2-oxazolidinone derivatives with a potential hypnotic activity on achiral (octadecylsilane) and chiral (cellulose tris(4-methylbenzoate)) stationary phases was examined. The compounds differed in the composition of a substituted aromatic ring containing different substituents in different positions. It was possible to resolve all the compounds with selectivity 1.11 < or = alpha < or = 2.74. The enantiodifferentiating power of substituents was correlated to their electron donating ability and position in the aromatic ring.

Synthesis and anti-microbial activities of some pyridinium salts with alkoxymethyl hydrophobic group.

A novel class of functionalized cationic surfactant has been obtained. The work-up procedure of synthesis is very simple, the yield is high and the pyridinium salts with alkoxymethyl hydrophobic group are easily purified. All the salts examined showed anti-microbial activities. Some of them exhibited strong activity and wide anti-bacterial spectra similar to the activity of benzalkonium chloride. The relationship between chemical structure and anti-microbial activity was analysed by the QSAR method.

Enantioselective separation of 1,4-disubstituted piperazine derivatives on two cellulose chiralcel OD and OJ and one amylose chiralpak AD chiral selectors

A series of 1,4-disubstituted piperazine derivatives with hypnotic activity were examined on three polysaccharide-based chiral stationary phases, namely, Chiracel OD, Chiracel OJ and Chiralpak AD. It was possible to resolve all the compounds on all the phases examined (1.13

Application of chiral chromatographic parameters in quantitative structure-activity relationship analysis of homologous malathion derivatives.

The conditions of the chiral resolution of the racemic malathion O,O-di-n-alkyl derivatives on cellulose tris(3,5-dimethylphenylcarbamate) are described. Quantitative relationships between chromatographic parameters obtained on chiral and achiral stationary phases and acute toxicity of the compounds towards house fly are derived and discussed.

Buspirone analogues as ligands of the 5-HT1A receptor. II: Capacity factors as chromatographic parameter of lipophilicity evaluation in a series of 5-HT1A and 5-HT2A receptor ligands.

The lipophilicity of a series of buspirone related agents was studied by means of reversed-phase HPLC using an octadecylsilane stationary phase a mixture of aqueous solution of sodium phosphate and methanol as a mobile phase. Comparison of the measured capacity factors with log P values has shown very good correlations with regression correlation coefficients in the range of 0.994-0.996.