Design and Optimization of a Novel Strategy for the Local Treatment of Helicobacter pylori Infections
| Autor: | Werner Siegmund, Franziska Schindele, Philipp Schick, Mirko Koziolek, Werner Weitschies, Felix Schneider, Taddese Mekonnen Ambay, Rainer Haas, Maximilian Sager, Michael Grimm |
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| Rok vydání: | 2021 |
| Předmět: |
Helicobacter pylori infection
medicine.drug_class Antibiotics Pharmaceutical Science Penicillin G Sodium Microbial Sensitivity Tests 02 engineering and technology 030226 pharmacology & pharmacy Helicobacter Infections Microbiology 03 medical and health sciences Minimum inhibitory concentration 0302 clinical medicine medicine Humans Helicobacter pylori biology Gastric fluid Treatment regimen Chemistry 021001 nanoscience & nanotechnology biology.organism_classification Anti-Bacterial Agents Extended release 0210 nano-technology |
| Zdroj: | Journal of Pharmaceutical Sciences. 110:1302-1309 |
| ISSN: | 0022-3549 |
| Popis: | Infections with Helicobacter pylori are a global challenge. Currently, H. pylori infections are treated systemically, but the eradication rates of the different therapy regimens are declining due to the growing number of bacterial strains resistant to major antibiotics. Here, we present a strategy for the local eradication of H. pylori by the use of Penicillin G sodium (PGS). In vitro experiments revealed that PGS shows high antibiotic activity against resistant strains of Helicobacter pylori with a minimum inhibitory concentration (MIC) of 0.125 μg/ml. In order to provide luminal concentrations above the MIC for longer periods of time, an extended release tablet was developed. Alkalizers were included to prevent acidic degradation of PGS within the tablet matrix. Out of the tested alkalizers MgO, l -Lysine, NaHCO3, and Na2CO3 NaHCO3 provided the strongest rise in pH inside the hydrated matrix when tested in simulated gastric fluid. Better PGS stability can mainly reasoned from that, addition of MgO resulted in high pH values within the matrix, causing basic degradation of PGS. This work is a first step towards the use of extended release tablets containing PGS for the local treatment of H. pylori as a safe and cost-effective alternative to common systemic treatment regimens. |
| Databáze: | OpenAIRE |
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