Solid state investigation of mefloquine hydrochloride.

Mefloquine hydrochloride was crystallized under different conditions and the products were studied by thermal analysis, IR spectroscopy and X-ray diffraction. It was demonstrated that different conditions of crystallization resulted in different crystal structures. The alpha- and delta-modifications were hydrates, the beta- and gamma-forms were polymorphs, the epsilon-form was an acetone solvate and theta-mefloquine was tetrahydrofuran solvate. During long storage at room temperature, the alpha-, delta- and theta-forms of mefloquine hydrochloride were transformed. By heat treatment of the delta-, epsilon and theta-modifications, a new crystal structure was obtained.

[Synthesis and analytical characterization of dansyl derivatives of morphine-like substances]. / Morfin alkaloidok danzil-származékainak elöállítása és analitikai jellemzése.

Dansyl derivatives of morphine-like substances were prepared using dansyl-chloride in acetone in the presence of sodium hydrogen carbonate. The reaction was selective for the phenolic hydroxyl group and was also quantitative. The purity of crystalline dansyl derivatives was checked by thin layer chromatography. Their structure was confirmed by PMR and MS spectra. Characteristic chemical shifts and MS fragments of the new derivatives were determined. UV spectra of the parent compounds and the dansyl derivatives were recorded. It was found that the absorbance of dansyl derivatives at 286 nm increased four-fold and a new band appeared at 320 nm. Some thin-layer chromatographic systems were elaborated to detect and separate dansyl derivatives. HPLC studies were done using normal as well as reversed phase. Parent compounds and their dansyl derivatives were separated easily by HPLC.

[Analytic and biological standardization of Prunus avium extracts]. / Prunus avium extraktumok analitikai és farmakológiai standardizálása.

Novicardine, the acetonic extract of P. avium peduncle which has advantageous cardiotonic effect, was standardized chemically and biologically. Flavonones, flavones, isoflavones and their glycosides were (methanolbuffer solution eluent, gradient elution) detected by reverse phase HPLC technique. It has been found that substances produced from different varieties of cherry peduncle originated from various lands, have the same components and their ratios are similar, but a contradictory statement could be made in the case of sour cherry. The allowed area ratios belonging to some ingredients were stated with reference to dihydrowogonine-7-O-glucoside. The biological experiments were performed on isolated heart preparations. In the organ bath with Locke's solution content the suspended left atrium and the papillary muscle were driven by rectangular electric impulses of 1 msec duration and of 1.7 Hz frequency, whereas the right atria were beating spontaneously. The result of experiments demonstrated that the standard Novicardine improves the contraction force of heart muscle by some 20-25%, and at the same time doesn't exert influence on the basic electrophysiological parameters and doesn't cause significant changes in heart rate. On the basis of investigation of substances having modified componentratio it was stated that extracts could be isolated which have cardiotonic effect four times stronger than that of Novicardine, on the other hand there were some extracts having negative inotropic effect. These effects were brought into connection with families of compounds (mainly glycosides and aglycones). It seems that the big variety of Novicardine can be assigned to the individual sensitivity of heart preparations, and the ratios of the above mentioned compounds.