pectins and stearyl-alcohol

The purpose of this study was to prepare wax-incorporated pectin-based emulsion gel beads using a modified emulsion-gelation method. The waxes in pectin-olive oil mixtures containing a model drug, metronidazole, were hot-melted, homogenized and then extruded into calcium chloride solution. The beads formed were separated, washed with distilled water and dried for 12 h. The influence of various types and amounts of wax on floating and drug release behavior of emulsion gel beads of calcium pectinate was investigated. The drug-loaded gel beads were found to float on simulated gastric fluid if the sufficient amount of oil was used. Incorporation of wax into the emulsion gel beads affected the drug release. Water-soluble wax (i.e. polyethylene glycol) increased the drug release while other water-insoluble waxes (i.e. glyceryl monostearate, stearyl alcohol, carnauba wax, spermaceti wax and white wax) significantly retarded the drug release. Different waxes had a slight effect on the drug release. However, the increased amount of incorporated wax in the formulations significantly sustained the drug release while the beads remained floating. The results suggest that wax-incorporated emulsion gel beads could be used as a carrier for intragastric floating drug delivery.

Topics: Administration, Oral; Anti-Infective Agents; Calcium Chloride; Chemistry, Pharmaceutical; Drug Carriers; Drug Compounding; Emulsions; Fatty Acids; Fatty Alcohols; Gastric Juice; Gels; Glycerides; Hydrophobic and Hydrophilic Interactions; Kinetics; Metronidazole; Olive Oil; Particle Size; Pectins; Plant Oils; Polyethylene Glycols; Solubility; Surface Properties; Technology, Pharmaceutical; Waxes