[Sulfalene kinetics in the blood and cerebrospinal fluid in arachnoiditis]. / Kinetika sul'falena v krovi i spinnomozgovoi zhidkosti bol'nykh arakhnoiditom.

The kinetics of free sulfalene in the blood and cerebrospinal fluid was studied in patients suffering from chronic arachnoiditis without marked inflammation signs on the part of arachnoid after a single intake of 2 g of the drug. It was found that administration of the drug in this dose once a week is quite justified and that sulfalene penetrates well in the cerebrospinal fluid. Upon administering large doses of the drug its absorption from the gastrointestinal tract declines. Sulfalene is eliminated from the cerebrospinal fluid more slowly than from the blood. High enough drug concentration is maintained in the cerebrospinal fluid for 7 days.

[Mechanism of the effect of proteolytic enzymes on antibiotic pharmacokinetics]. / Mekhanizm vliianiia proteoliticheskikh fermentov na farmakokinetiku antibiotikov.

Possible relation between the changes in the penicillin pharmacokinetics and coagulograms under the effect of trypsin in rats and man was analysed. It was found that parenteral administration of the enzyme was accompanied by a simultaneous increase in the penicillin blood level, oliguria, a decrease in the antibiotic amount excreted with urine and drop of the fibrinogen level in plasma. The latter is consequent on intravascular coagulation which results in temporary impairment of the excretion function of the kidneys defining the changes in the penicillin pharmacokinetics under the effect of trypsin.

[Human pharmacokinetic characteristics of sulfamonomethoxine depending on the drug form]. / Osobennosti farmakokinetiki sul'famonometoksina ud cheloveka v zavisimosti ot lekarsvennoi formy.

Comparative study of sulfamonomethoxin pharmacokinetics in the man given the drug per os or parenterally in the form of methylglucaminate showed that the latter favours higher blood concentrations of the drug 12 hours following injection. Sulfamonomethoxinmeglumin is absorbed more rapidly and has a greater bioavailability. The drug is mainly excreted with urine, more than a half being excreted in an acetylated form. It is recommended that the initial and maintenance doses be not less than 1000 and 500 mg for both dosage forms respectively. The interval between sulfanilamide administrations should not exceed 24 hours.

[Trypsin and lipase activity in the presence of antibiotics]. / Aktivnost' tripsina i lipazy v prisutstvii antibiotikov.

Effect of penicillin, kanamycin and streptomycin on the proteolytic activity of trypsin using hemoglobin and casein as substrates as well as effect of these antibiotics and oxacilin, methycillin and tetracycline on the lipase activity were studied in vitro. Penicillin, kanamycin and streptomycin (5 mg, 20 mg and 80 mg of the antibiotic per 1 mg of trypsin, respectively) did not inhibit the proteolytic activity of the enzyme. Kanamycin slightly activated the trypsin activity in reaction with hemoglobin and streptomycin -- in reaction with casein. Penicillin, oxacillin and methycillin inhibited the lipase activity, when 80-100 mg of the antibiotics were used per 1 mg of the enzyme.

[Pharmacokinetics of sulfamonomethoxine and ite N-methylglucamine salt in rats]. / Farmakokinetika sul'famonometoksina i ego N-metilgliukaminovoi soli u krys.

Tests conducted with albino rats demonstrated that after intramuscular administration of N-methylglucaminic salt of sulphamonomethoxine there are built up higher concentrations of the compound in the blood and organs than with its enteral introduction. The maximal sulphamonomethoxine concentrations in rats with the compound administered by mouth are observed in 3-6 hours and with its intramuscular injection--over a space of 30 minutes-1 hour. Doubling the dose of injectable sulphamonomethoxine resulted in a higher content of the compound in the organism of rats by comparison with its administration by mouth.

[Effect of proteolytic enzymes on the antitrypsin activity of blood serum in the postoperative period]. / Vliianie proteoliticheskikh fermentov na antitripticheskuiu aktivnost' syvorotki krovi operirovannykh bol'nykh

An antitryptic activity and effect of trypsin and chymotrypsin, administered parenterally, on the activity were studied in blood serum of patients, subjected to surgical operations. The antitryptic activity and content of alpha1- and alpha2-globulins were shown to increase in blood serum of patients within 5 days of the postoperative period. Intramuscular administration of the proteolytic enzymes within 5 days decreased the anti-tryptic activity and content of alpha1- and alpha2-globulins in blood serum.

[Penetration of antibiotics into experimental foci of inflammation under the influence of proteolytic enzymes]. / Proniknovenie antibiotikov v éksperimental'nye ochagi vospaleniia pod vliianiem proteoliticheskikh fermentov

The effect of trypsin or chemotrypsin on the levels of benzylpenicillin, ampicillin, oxacillin, kanamycin or tetracycline in the peritoneal inflammation fluid, as well as the effect of trypsin on penetration of these antibiotics into the granulemas of 2 types was studied. It was found that intramuscular administration of the enzymes to animals in a dose of 10 mg/kg resulted in increased levels of penicillins and kanamycin in the inflammation peritoneal fluid. An analogous effect of trypsin was observed with respect to experimental granulemas. The levels of tetracycline in restricted inflammatory foci increased only after intraperitoneal administration of trypsin to rats. Increased penetration of benzylpenicillin into the peritoneal fluid and connective tissue granulema under the effect of the enzymes was observed. The effect of trypsin on penetration of benzylpenicillin into granulema according to Selie did not differ from the effect of the enzyme on penetration of semisynthetic penicillins and kanamycin into it.

[Effect of chymotrypsin on the urinary excretion of antibiotics in rabbits]. / Vliianie khimotripsina na vyvedenie antibiotikov s mochoi u krolikov

The effect of cymotrypsin on excretion of penicillin, methicillin, oxacillin, streptomycin and gentamycin with urine including the kidney clearance was studied on rabbits. It was found that the enzyme introduced intramuscularly in a dose of 20 mg/kg increased excretion of penicillin, methicillin, oxacillin and gentamycin by 37, 24, 26 and 16 per cent respectively. The only exclusion was streptomycin. Chymotrypsin increased the kidney clearance of penicillin, methicillin, oxacillin, streptomycin and gentamycin by 1.7, 1.9, 2.2, 1.2 and 1.5 times respectively.

[Antibiotic interaction with proteolytic enzymes]. / K voprosu o vzaimodeistvii antibiotikov s proteoliticheskimi fermentami

The effect of penicillin, tetracycline, aminoglucozide antibiotics and streptomycin on BAEE-esterase activity of trypsin was studied. It was found that benzylpenicillin in amounts of 50, 100 and 300 mg, ampicillin in an amount of 25 mg, methicillin in an amount of 12 mg and tetracycline in an amount of 2.5 mg as calculated per 1 mg of trypsin had no effect in vitro on the esterase activity of the enzyme. Neomycin, kanamycin and streptomycin in amounts of 5, 10, 100 or 300 mg per 1 mg of trypsin catalyzed splitting of BAEE by trypsin. When the antibiotics were added to the bile, its esterase activity increased. Preliminary intramuscular administration of trypsin and kanamycin to the rats had no effect on the ampicillin levels in the blood serum and brain and did not affect the permeability of the hemato-encephalic barrier as compared to the use of trypsin alone.

[Comparison of the effect of trypsin and chymotrypsin on the pharmacokinetics of penicillins in the body of rats]. / Sravnenie vliianiia tripsina i khimotripsina na farmakokinetiku penitsillinov v organizme krys

Trypsin and chemotrypsin administered intramuscularly to rats in doses of 2 and 10 mg/kg respectively prior to benzylpenicillin, ampicillin or oxacillin administered also intramuscularly were studied with respect to their effect on the pharmacokinetics of the antibiotics. The latter 2 antibiotics were additionally studied after their oral administration. It was found that trypsin and chemotrypsin had almost the same effect on the pharmacokinetics of the penicillins in the animals, when administered intramuscularly and the effect did not depend on the doses of trypsin and chemotrypsin (2 and 10 mg/kg). No significant differences in the effect of the enzymes on the pharmacokinetics of ampicillin and oxacillin administered orally was registered. Combination of prior injection of every of the enzymes followed by oral administration of the semisynthetic penicillins resulted in a more pronounced increase in the levels of the antibiotics in the blood serum and organs of the rats as compared to that after intramuscular administration of the antibiotics.