[Organic solvents for determination of bacterial endotoxin index in water-insoluble pharmaceutical substances].

Substances for manufacture of parenteral drugs require control by the "Bacterial Endotoxin" (BE) index with the LAL-test. The aim of the study was to show possible applicability of organic solvents in BE determination by the gel-thromb test in case of water-insoluble pharmaceutical substances. The results confirmed that ethyl alcohol practically had no effect on the endotoxin activity.

[Pharmacokinetics of n-(5-oxynicotinoyl)-L-glutamic acid calcium salt upon bolus administration in rats and rabbits: interspecies extrapolation].

The pharmacokinetics of N-(5-oxynicotinoyl)-L-glutamate (ONG) was studied in rats (doses, 20, 100 and 500 mg/kg) and rabbits (50 mg/kg) after bolus administration of calcium salt of N-(5-oxynicotinoyl)-L-glutamic acid (Ampasse preparation). The ONG concentration in the blood serum was determined by HPLC assay with fluorimetric detection. The lower limit of accurate detection for ONG was 100 ng/ml.

[Estimation of the efficacy of screened natural hypolipidemic compounds in a model of rabbit hypercholesterolemia].

Thirteen strains producing hydrophobic compounds with high hypolipidemic activity were screened among 657 tested strains of fungi, actinomycetes and bacteria with the use of 2 models. The further aim of the study was to estimate the efficacy of the compounds with respect to their ability to inhibit cholesterol synthesis in vivo. For that purpose a model of hyperlipidemia in rabbits was used.

[Implantation with natursil as a method for repair of dental defects and normalization of oral homeostasis].

Parameters of homeostasis in the oral liquid during adentia, after implantation of titanium implants gated in generally accepted way and also with usage of natursilum from Silybum marianum were studied. Application of natursilum in surgery and in postoperative period promoted optimization of an implant osteointegration and normalized physicochemical and metabolic parameters of the oral liquid.

[Aprotinin antiviral aerosol: study of the local irritating and allergenic action after inhalation].

The aerosol of aprotinin, a natural low molecular weight polypeptide (m.w. about 160 kD) inhibiting a wide range of serine proteases may be used as an antiviral drug.

[The antiviral aerosol aprotinin. General effect on the body after inhalation administration].

A new medicine for the treatment of respiratory viral infections is described. It contains aprotinin, a natural inhibitor of proteases, and is used in the form of a fine aerosol for inhalation or intra-respiratory instillation. To estimate its innocuousness, the inhalation effect of the aerosol was studied on animals of two species.

[Experimental study of human recombinant insulin].

The experimental study of recombinant human insulin revealed its high specific activity. The kinetics of the hypoglycemic effect of various dosage forms of the insulin developed at the National Research Centre of Antibiotics and the dosage forms manufactured by Eli Lilly was similar. The pharmacological investigation of the dosage forms showed that they had no side effects on the vitally important organs and systems.

[Study of general toxic and organotropic properties of clindamycin in long-term experiments].

The action of clindamycin monohydrate on the general state and weight rise, liver and kidney functions, peripheral blood count and pathomorphological state of the viscera was studied on rats in chronic experiments. Clindamycin was administered to laboratory animals orally in doses of 50, 100, 150 and 300 mg/kg. It was shown that some adverse reactions to the drug and in particular disorders in blood coagulation and morphological changes in the intestine did not depend on its dose and were due to duration of the drug use and probable development of dysbacteriosis.

[Study of general toxic and organotropic properties of ampicillin combined with sulbactam].

The effect of sulacillin, a combination of sulbactam and ampicillin (1:2), on the functions of the liver and kidneys, peripheral blood count, cardiovascular and central nervous systems was studied in acute and chronic experiments on animals of various species. The allergenic and local irritating properties of the combination were also studied. It was shown that the combination was low toxic and the interaction of sulbactam and ampicillin by the lethal effect was additive.

[Biologic activity and tolerance of a preparation of polyunsaturated fatty acids, obtained by a microbiological route ["biopolyene"]].

Biopolyene is a mixture of ethyl ethers of polyunsaturated fatty acids isolated from biomass of Entomophthora virulenta, a mycelial fungus. Its acute and chronic toxicity was studied on rats and guinea pigs. After oral administration of the preparation in single doses exceeding 50 g/kg there were no disorders in the general state of the rats.

[Experimental study of protease C--proteolytic enzyme of microbial origin].

The specific activity of protease C, a proteolytic enzyme isolated from Acremonium chrysogenum was studied under experimental conditions. Protease C was shown to lyse necrotic biological substrates (dry crusts of burn wounds) and blood clots. By the nature of the effect protease C was analogous to terrilytin and by the level of the effect it was superior in some experiments.

[Experimental study of a novel formulation for local application based on gentamicin, erythromycin and protease C].

A novel formulation for local application based on an enzyme of microbial origin, C protease, and two antibiotics, gentamicin and erythromycin, was studied on various experimental models in rats with respect to its effect on necrotic tissues and recovery of the skin and hypodermic tissue defects due to wounds. It was found that even within the first days of the application the formulation induced lysis of the primary crust, lowered exudation and promoted debridement, reduced the wound size and completely closed it. By its effect the formulation was similar to iruxol.

[Tolerance of gentacycol--a local dosage form of gentamicin based on collagen--animal experiments].

Gentacycol is a local dosage form of gentamicin based on collagen for implantation to wounds in treatment of patients with infections of soft tissues and prevention of contamination of open injuries of the bones and soft tissues. General toxic and organotropic properties of gentacycol were studied on animals with subcutaneous implantation of the dosage form in doses equivalent to the therapeutic dose for man and exceeding it 2-fold. The study showed that the dosage form had no unfavourable side effects on the animal general state, hearing, the functional state of the liver and kidneys and the peripheral blood.

[Hypotension caused by intravenous infusion of rifampicin and its relation to the administration schedule].

It was shown in studies on animals that bolus administration of rifampicin induced hypotension whose severity depended on the rate of the antibiotic administration. When the antibiotic was administered in the 5-, 10- or 15-minute regimen in a dose of 10 mg/kg the maximum decrease in blood pressure was 44, 34 or 21% of the initial level and the maximum antibiotic concentration attained in the blood was 34.4, 27.

[General toxic and organotropic properties of cefotaxime in acute and chronic experiments].

The action of cefotaxime on the functions of the liver and kidneys, the peripheral blood count, growth and development of young animals, blood circulation, respiration and the central nervous system was studied in acute and chronic experiments on mice and rats. Allergenic, immunomodulating, embryotoxic and teratogenic properties of the antibiotic were also studied. Cefotaxime was shown to be low toxic.

[Mechanism of hypotension induced by rifampicin during intravenous administration].

In vivo and in vitro experiments showed that the mechanism of hypotension induced by rifampicin was not associated with its effect on peripheral m- and n-cholinoreactive and adrenoreactive systems. It was due to the direct action of the drug on the vessel muscular wall and its mediated effect on the histaminergic systems participating in vascular tension control.

[General toxic and organotropic properties of azlocillin in acute and chronic experiments].

The general toxic and organotropic properties of azlocillin were studied in acute and chronic experiments with various animal species. By the body surface area the doses of azlocillin were equivalent to the drug average and maximum course doses for humans. The aim of the study was to determine the drug dose inducing certain side effects.

[Pharmacokinetics of amikacin in the perilymph and blood serum. An approach to the comparative evaluation of the potential ototoxicity of aminoglycoside antibiotics].

The pharmacokinetics of amikacin in serum and perilymph was studied on guinea pigs treated with its single subcutaneous administrations in doses of 100, 200, 400 and 800 mg/kg. Proportional relation between the values of the areas under the concentration against time curves of the antibiotic in serum and perilymph was shown. It suggested that the level of the antibiotic penetration into the internal ear might be predicted by the area under the concentration against time curve of the aminoglycoside.

[Sisomycin pharmacokinetics in the perilymph and blood serum--an approach to predicting its ototoxic effect].

To elucidate the possibility of predicting the level of aminoglycoside antibiotic penetration into the fluids of the internal ear by the antibiotic blood levels, the pharmacokinetics of sisomicin in the perilymph and blood serum was studied on guinea pigs. The antibiotic was administered to the animals subcutaneously in doses of 50, 100 and 200 mg/kg. On the basis of the comparison of the sisomicin concentrations in the perilymph normalized against the dose it was concluded that the pharmacokinetics of sisomicin in the perilymph and blood serum of the animals was linear.