Wax-incorporated Emulsion Gel Beads of Calcium Pectinate for Intragastric Floating Drug Delivery

Abstract

Abstract. 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 waterinsoluble 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.

Utilization of ionotropic gelation technique for bioavailability enhancement of cinnarizine: in-vitro optimization and in-vivo performance in human

“…The emulsion gel calcium pectinate beads could float immediately with no lag time and remained floating for 8 h (Sriamornsak et al, 2008) as shown in Figure 8. The beads floated with an oil amount of 30% (w/w).…”

“…The floating properties of the emulsion gel beads may be attributed to the low-apparent density of the beads containing oils (Sriamornsak et al, 2004). This implied that the beads will have the tendency to exhibit a good in-vivo floating effect (Sriamornsak et al, 2008).…”

“…Ionotropic gelation is based on the ability of polyelectrolytes to cross link in the presence of counter ions to form beads. In a work by Sriamornsak et al (2008), a new emulsion gelation method was used to prepare oil-entrapped calcium pectinate gel (CaPG) beads as a carrier for intragastric floating drug delivery.…”

“…A pharmacokinetic study was carried out on healthy human volunteers to compare the optimized CNZ emulsion gel calcium pectinate beads and Stugeron Õ as the marketed reference product. Preparation of CNZ-loaded emulsion gel calcium pectinate beads using ionotropic gelation method CNZ-emulsion gel calcium pectinate beads were prepared by ionotropic gelation according to Sriamornsak's method (Sriamornsak et al, 2008). Briefly, LM-pectin 101, LMpectin 104, GMO, LL and distilled water were well stirred on a magnetic stirrer (model SP 72220-26, Barnstead/ Thermolyne, Dubuque, IA) at 500 rpm, an o/w emulsion was formed and then CNZ was dispersed.…”

Flocculating and suspending properties of commercial citrus pectin and pectin extracted from pomelo (Citrus maxima) peel

“…Thirawong, Nunthanid, Puttipipatkhachorn, & Sriamornsak, 2007;Thirawong, Thongborisute, Takeuchi, & Sriamornsak, 2008), as a carrier for floating drug delivery (e.g. Sriamornsak, Thirawong, & Puttipipatkhachorn, 2005;Sriamornsak et al, 2008), and as a carrier for colonic drug delivery (e.g. Sriamornsak, 1999;Sriamornsak, Nunthanid, Wanchana, & Luangtana-anan, 2003), etc.…”