The evaluation of some pharmaceutically acceptable excipients as permeation enhancers for amoxicillin
| Autor: | Igor Legen, Janez Kerc, Matjaž Kračun, Mateja Salobir |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Sodium
Pharmaceutical Science Excipient chemistry.chemical_element In Vitro Techniques Excipients chemistry.chemical_compound Sodium sulfate Benzbromarone medicine Animals Rats Wistar Antibacterial agent Chromatography Dose-Response Relationship Drug Chemistry Electric Conductivity Amoxicillin Sodium Dodecyl Sulfate Permeation Hydrogen-Ion Concentration Bioavailability Anti-Bacterial Agents Rats Glucose Jejunum Intestinal Absorption Drug delivery Multidrug Resistance-Associated Proteins medicine.drug |
| Zdroj: | International journal of pharmaceutics. 308(1-2) |
| ISSN: | 0378-5173 |
| Popis: | The aim of the present study was to evaluate different pharmaceutically acceptable excipients as permeation enhancers for a low permeability drug, amoxicillin. As a model for the intestinal epithelium excised rat jejunum, mounted in side-by-side diffusion cells, was used. Amoxicillin was actively transported across the intestine in the serosal-to-mucosal direction, but only if glucose was present at the mucosal side. This effect of glucose was abolished by a multridrug resistance associated protein (MRP) inhibitor benzbromarone (0.04 mM), but not by verapamil (0.2 mM). Among the tested pharmaceutically acceptable excipients only sodium lauryl sulfate (0.2 mg/ml) increased the permeability of amoxicillin in the mucosal-to-serosal direction, which was accompanying with the abolishment of the secretory oriented transport of amoxicillin. Other excipients (0.07 2mg/ml Pluronic F68, 0.2 mg/ml Lutrol F127, 0.2 mg/ml Cremophor EL or 0.2 mg/ml Carbopol 934) have no influence on the permeability of amoxicillin. The effect of sodium lauryl sulfate on the active secretion of amoxicillin was mainly attributed to the reversible cellular ATP depletion. We concluded that sodium lauryl sulfate can be considered as a relatively safe permeation enhancer for amoxicillin in drug delivery systems intended to improve oral bioavailability of this drug. |
| Databáze: | OpenAIRE |
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