ABSTRACT
The influence of the rate of administration was examined during the test "Abnormal toxicity" on the quality control of ceftriaxone in a comparative experimental study on the basis of the methodologies Rus. Ph. XII and Eur. Ph. Recommendations are issued for conducting study entitled "Abnormal toxicity" for the formulations of ceftriaxone.
Subject(s)
Anti-Bacterial Agents/adverse effects , Ceftriaxone/adverse effects , Animals , Anti-Bacterial Agents/administration & dosage , Ceftriaxone/administration & dosage , Female , MiceABSTRACT
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. In the routine assays it is advisable to test solutions of the substances at the alcohol concentration of 6% below.
Subject(s)
Endotoxins/analysis , Limulus Test , Pharmaceutical Preparations/analysis , Quality Control , Sensitivity and Specificity , SolubilitySubject(s)
Injections, Intraperitoneal/methods , Injections, Intravenous/methods , Pharmaceutical Preparations/administration & dosage , Toxicity Tests, Acute/standards , Animals , Anti-Bacterial Agents/administration & dosage , Cefepime , Cephalosporins/administration & dosage , Dose-Response Relationship, Drug , Injections, Intraperitoneal/standards , Injections, Intravenous/standards , Mice , Time FactorsSubject(s)
Anti-Bacterial Agents/toxicity , Animals , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/standards , Cefazolin/administration & dosage , Cefazolin/standards , Cefazolin/toxicity , Cefoperazone/administration & dosage , Cefoperazone/standards , Cefoperazone/toxicity , Ceftriaxone/administration & dosage , Ceftriaxone/standards , Ceftriaxone/toxicity , Drug Contamination , Lethal Dose 50 , Mice , Pharmacopoeias as Topic , Toxicity Tests, AcuteSubject(s)
Biotransformation , Acetylation , Aging , Amines/metabolism , Amines/pharmacology , Animals , Diabetes Mellitus/metabolism , Diabetes Mellitus, Experimental/metabolism , Glucuronates/metabolism , Glucuronic Acid , Hormones/metabolism , Hormones/pharmacology , Humans , Hydrolysis , Kinetics , Liver/metabolism , Male , Rats , Structure-Activity Relationship , Vitamins/metabolism , Vitamins/pharmacologyABSTRACT
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.
Subject(s)
Sulfamonomethoxine/blood , Sulfanilamides/blood , Adult , Aged , Biopharmaceutics , Blood Proteins/metabolism , Humans , In Vitro Techniques , Injections, Intramuscular , Injections, Intravenous , Kinetics , Middle Aged , Protein Binding/drug effects , Sulfamonomethoxine/administration & dosage , Tablets , Time FactorsSubject(s)
Sulfanilamides/analysis , Acetylation , Animals , Chemical Phenomena , Chemistry , Indicators and Reagents , Methods , Rats , Sulfonic AcidsABSTRACT
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.
