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In vivo and in vitro studies with sulfamate sweeteners
Journal of Pharmaceutical Sciences
|June 1, 1982
Summary
Metabolism of methylcyclohexyl and cyclohexenylsulfamates in rats yielded low metabolite levels. In vitro bacterial studies showed some correlation with in vivo findings, with preliminary mutagenicity tests conducted on related amines.
Area of Science:
- Metabolomics
- Toxicology
- Microbiology
Background:
- Sulfamates are artificial sweeteners with varying metabolic profiles.
- Understanding the in vivo and in vitro metabolism of sulfamates is crucial for safety assessment.
- Previous studies have investigated the metabolism of cyclamate and other sulfamate derivatives.
Purpose of the Study:
- To investigate the metabolic fate of novel sulfamate compounds (2-methylcyclohexyl-, 3-methylcyclohexyl-, and 2-cyclohexenylsulfamates) in Wistar albino rats.
- To compare the in vivo metabolism of these compounds with previously studied sulfamates.
- To conduct complementary in vitro studies using bacterial extracts and assess preliminary mutagenicity of related amines.
Main Methods:
- Administration of sulfamate compounds to Wistar albino rats.
- Analysis of rat urine and feces for amine, ketone, and alcohol metabolites.
- In vitro incubation of sweet sulfamates (cyclamate, cycloheptyl-, cyclooctyl-, cyclopentylsulfamates) with fecal bacterial extracts.
- Preliminary Ames test for mutagenicity of corresponding amines.
Main Results:
- Low overall percentages of metabolites were detected for the tested sulfamates.
- 2-Cyclohexenylsulfamate yielded a particularly small quantity of metabolites.
- A correlation was observed between in vitro bacterial metabolism and previous in vivo findings for sulfamates.
Conclusions:
- The in vivo metabolism of 2-methylcyclohexyl-, 3-methylcyclohexyl-, and 2-cyclohexenylsulfamates in rats is limited.
- In vitro bacterial incubations provide insights that correlate with in vivo metabolic data.
- Further investigation into the safety and metabolic pathways of these sulfamate compounds is warranted, including mutagenicity assessments.