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Biomedical subjects

J Szejtli

Publications and source records attributed to J Szejtli.

At least 19 recordsLinked to original sources
PubMed1990

13C-N.M.R. spectra of cyclomalto-oligosaccharides (cyclodextrins), their derivatives, and complexes with azo dyes.

The nature of the inclusion complexes of several cyclomalto-oligosaccharides (cyclodextrins, CDs) with azo dyes has been studied on the basis of 13C-n.m.r. chemical shifts, relaxation times, correlation times, and broadening and doubling of the n.m.r. signals. All CDs show the azo dye-induced shifts at the narrow-rim side of the CD, indicating that the azo dyes protrude from the cavity. CD-induced shifts of azo dyes depend on the hydrophobic nature of the cavity, van der Waals forces, as well as ring-current and deformation effects, and suggest inclusion essentially from the hydrophobic site. The broadening and the doubling of the 13C-n.m.r. signals, the altered relaxation and correlation times, as well as the temperature dependence for these phenomena, also provide particular information about the characteristic host-guest interactions.

Azo Compounds↗
PubMed1989

Aggregation of amphotericin B in the presence of gamma-cyclodextrin.

The macrolide antibiotic amphotericin B (AmB) forms an inclusion complex with gamma-cyclodextrin (gamma-CDx), resulting in a molecularly dispersed state of the drug. The state of aggregation of AmB in different solvents has been studied by absorption (uv-vis) and CD spectroscopy. While in aqueous solutions AmB forms colloid-like multimolecular aggregates, in the presence of gamma-CDx true solutions can be prepared, which show similar spectral properties as AmB dissolved in organic solvents. The AmB-gamma-CDx complex can be isolated as an amorphous, stable, water-soluble powder, indicating that gamma-CDx is a good carrier for the solubilization of this antibiotic. Using gamma-CDx as a carrier, the danger of precipitation of the drug during parenteral or intravenous administration can be largely reduced.

Amphotericin B↗
PubMed1988

Resolution of chiral barbiturates into enantiomers by reversed-phase high-performance liquid chromatography using methylated beta-cyclodextrins.

The correlation between the capacity factors of enantiomers of chiral barbiturates and the concentrations of beta-cyclodextrin, heptakis(2,6-di-O-methyl)-beta-cyclodextrin and heptakis(2,3,6-tri-O-methyl)-beta-cyclodextrin dissolved in the mobile phase was studied using LiChrosorb RP-18 as the stationary phase. Owing to the very strong adsorption of permethylated beta-cyclodextrin on the ODS surface a chiral stationary phase is generated dynamically and forms complexes with the solutes; this mechanism has been found to be the only factor responsible for the chiral recognition of the investigated compounds at all applied concentrations. The inclusion of barbiturates in the cavities of permethylated beta-cyclodextrin involves a distinct and entirely new kind of enantioselectivity compared with that observed for beta-cyclodextrin and its dimethyl derivative. Using permethylated beta-cyclodextrin baseline resolutions have been obtained with barbiturates containing a chiral centre in the heterocyclic ring or in the aliphatic side-chain.

Barbiturates↗
PubMed1987

Enhanced percutaneous absorption of homogenized tolnaftate/beta-cyclodextrin polymer ground mixture.

The absorption of tolnaftate after external application of tolnaftate-cyclodextrin polymer homogenized ground mixtures was investigated in comparison with that of tolnaftate alone and non-homogenized mixtures. To evaluate their percutaneous absorption, samples were applied to the shaved back skin of mice. It was found that homogenized ground mixture samples showed the highest level of percutaneous absorption, and also resulted in the highest blood level concentrations.

Animals↗
PubMed1985

Cyclodextrins: a new group of industrial basic materials.

Adequate toxicological studies, discovery of numerous potential fields of utilization and last but not least, the production of cyclodextrins on industrial scale with high homogeneity and low price led to their recognition as a new group of industrial basic materials. Until now cyclodextrins were considered merely as agents for molecular encapsulation, however intensive research of the past few years revealed quite new and unexpected aspects: cyclodextrins, their derivatives and polymers can be applied--not exclusively due to their complexing ability--in foods, cosmetics, pharmaceuticals, chromatography, pesticide formulations, in photochemistry, etc.

Catalysis↗
PubMed1985

Quantitative structure-stability relationships among inclusion complexes of cyclodextrins. I: Barbituric acid derivatives.

Quantitative structure-stability relationships (QSSRs) are formulated for the inclusion complexation of 17 barbituric acid derivatives with alpha- and beta-cyclodextrin. The variation in the complex stability constants K alpha and K beta is found to be partly accounted for by the molar refractivity or the hydrophobicity of the substituent R1 at position 5 of the barbiturate ring. In addition, K alpha also depends upon whether or not R1 is branching or cyclic, and K beta also depends upon whether the guest molecule is a barbiturate or a thiobarbiturate. The results suggest that in alpha-cyclodextrin-barbiturate complexes the cyclodextrin cavity includes only R1, while in beta-cyclodextrin complexes both R1 and (part of) the barbiturate ring are included. This complexation model is compared with those proposed by other authors.

Barbiturates↗
PubMed1985

Suppositories containing cyclodextrin complexes. Part 2: Dissolution and absorption studies.

The dissolution and absorption of poorly water-soluble drugs from rectal suppositories can be enhanced by complexing these substances (e.g., essential oils, indomethacin) with beta-cyclodextrin. Preliminary in vivo studies showed, that the application of cyclodextrin complexes to suppositories, the same as to oral applications, resulted in an increased blood level.

Absorption↗
PubMed1985

Absorption, distribution, excretion and metabolism of orally administered 14C-beta-cyclodextrin in rat.

The absorption, distribution, excretion and metabolism of orally administered universally labelled 14C-beta-cyclodextrin and 14C-glucose were compared in rat. The maximum radioactivity of the blood derived from 14C-beta-cyclodextrin was observed between 4th and 11th h and the value of the maximum in different experiments ranged between 5 and 17 0/00 of the total administered radioactivity. Following 14C-glucose treatment radioactivity reached the maximum within half-an-hour, with values of 15 to 82 0/00. In the 8th h after a high dose (313.5 mg/kg) of beta-cyclodextrin no more than 3-50 ppm beta-cyclodextrin was detectable in the blood by HPLC. After 14C-beta-cyclodextrin treatment 4.2-4.8% of the administered total radioactivity was excreted by the urine and about the same quantity (2-3.6%) in case of 14C-glucose. No specific accumulation was observed after 14C-beta-cyclodextrin treatment in the different organs. The large intestine contained 10-15% of the cyclodextrin radioactivity while this value was only 2% in case of 14C-glucose. Following p.o. administration of different doses of 14C-beta-cyclodextrin the radioactivity peak was detected in the exhaled air between the 4-6th and 6-8th h, respectively, depending on the administered doses, while in case of 14C-glucose treatment it was observed within 2 h. The total radioactivity exhaled by 14C-beta-cyclodextrin treated animals in 24 h was 55 to 64% of the administered radioactivity and 58% in case of 14C-glucose. It is assumed that beta-cyclodextrin is metabolized in rats slower but similarly to glucose, therefore p.o. administered beta-cyclodextrin cannot induce toxic symptoms.

Administration, Oral↗
PubMed1984

Cyclodextrin polymer, a new tablet disintegrating agent.

Cyclodextrin (CD) polymer, a type of crosslinked cyclodextrin, has been evaluated as a new tablet disintegrating agent in comparison with four common disintegrants (crosslinked polyvinylpyrrolidone, crosslinked carboxymethyl cellulose, formaldehyde casein and corn starch). Physical properties of the disintegrants have been studied. Tablets made by direct compression using microcrystalline cellulose as binder, magnesium stearate as lubricant and talc as antiadherent have been compared. The parameters evaluated were disintegration time, hardness and friability. CD polymer performs well as a tablet disintegrating agent with results paralleling those of crosslinked carboxymethyl cellulose (Ac-Di-Sol) and superior to the other three.

Cellulose↗
PubMed1984

Cyclodextrin-stabilized volatile substances for inhalation therapy.

Diapulmon (Chinoin) which comprise camphor, 1-menthol, eucalyptus oil and quinine dissolved in sunflower oil (Oleum helianthi) is marketed in ampoules of 2 ml but utilized almost exclusively for inhalation therapy. Complexing the active ingredients of Diapulmon with beta-cyclodextrin (beta-CD) a stable non hygroscopic microcrystalline substance is obtained. When this powder sprinkled on hot water, the included volatile compounds are gradually released and the desired pharmacological effect can be brought about.

Camphor↗