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Research Article

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

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Pages 2736-2746 | Received 12 May 2015, Accepted 16 Jun 2015, Published online: 13 Jul 2015

Figures & data

Table 1. Independent and dependent variables of the D-optimal mixture design.

Table 2. The formulations of the mixture design and their characterization results.

Table 3. Regression results of the measured responses.

Table 4. The selected equations describing each response of floating CNZ emulsion gel calcium pectinate beads.

Figure 1. In-vitro release profile of CNZ from emulsion gel calcium pectinate beads formulae in 0.1 N HCL.

Figure 1. In-vitro release profile of CNZ from emulsion gel calcium pectinate beads formulae in 0.1 N HCL.

Figure 2. The 3D surface plot of floating CNZ calcium pectinate bead formulations at different time intervals.

Figure 2. The 3D surface plot of floating CNZ calcium pectinate bead formulations at different time intervals.

Figure 3. The 2D contour plot describing the percent of drug entrapped.

Figure 3. The 2D contour plot describing the percent of drug entrapped.

Table 5. The observed and predicted values for the optimized formulation.

Figure 4. Release of CNZ from the optimized floating emulsion gel calcium pectinate beads formulation.

Figure 4. Release of CNZ from the optimized floating emulsion gel calcium pectinate beads formulation.

Figure 5. 3D surface plot showing swelling index of CNZ-loaded calcium pectinate beads.

Figure 5. 3D surface plot showing swelling index of CNZ-loaded calcium pectinate beads.

Table 6. Floating CNZ emulsion gel calcium pectinate beads in the mixture design and optimized formula with their % SI.

Figure 6. A light photo for the optimized CNZ-loaded calcium pectinate beads.

Figure 6. A light photo for the optimized CNZ-loaded calcium pectinate beads.

Figure 7. SEM micrographs of CNZ-loaded calcium pectinate beads at different magnification powers. (a,b) Before release in 0.1 N HCl. (c,d) after 8 h release in 0.1 N HCl.

Figure 7. SEM micrographs of CNZ-loaded calcium pectinate beads at different magnification powers. (a,b) Before release in 0.1 N HCl. (c,d) after 8 h release in 0.1 N HCl.

Figure 8. CNZ-loaded calcium pectinate beads in 0.1 N HCL at zero time, after 4 and 8 h.

Figure 8. CNZ-loaded calcium pectinate beads in 0.1 N HCL at zero time, after 4 and 8 h.

Figure 9. LC-MS/MS chromatograms of blank human plasma.

Figure 9. LC-MS/MS chromatograms of blank human plasma.

Figure 10. LC-MS/MS chromatograms of human plasma after oral administration of CNZ optimized formula.

Figure 10. LC-MS/MS chromatograms of human plasma after oral administration of CNZ optimized formula.

Figure 11. Plasma concentration–time curve of Stugeron® tablets and optimized CNZ emulsion-loaded calcium pectinate beads.

Figure 11. Plasma concentration–time curve of Stugeron® tablets and optimized CNZ emulsion-loaded calcium pectinate beads.

Table 7. Mean pharmacokinetic parameters of Stugeron® tablets and optimized CNZ calcium pectinate beads.

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