Preparation and in vitro/in vivo evaluation of esomeprazole magnesium-modified release pellets

Figures & data

Table 1. Studies schedule in rats for different formulations.

Subject	First week	Second week	Third week
1	A	B	C
2	B	C	A
3	C	A	B
4	B	A	C
5	A	C	B
6	C	B	A

Figure 1. Release profiles of EMZ pellets coated with different curing time at the blend ratios ERS/ERL of 5:5 and the same coating weight of 5% (n = 3).

Figure 2. Release profiles of EMZ pellets coated with different blend ratios of ERS/ERL at the same coating weight of 5% (n = 3).

Figure 3. Effects of the coating weight on drug release from pellets coated with ERS/ERL of 7/3 (n = 3).

Figure 4. The release profiles of EMZ-MRPs with fixed film curing time of 6 h, ERS/ERL ratio of 7/3 and coating weight of 10% in different pH medium. Each point represents the mean ± SD (n = 3).

Figure 5. In vitro release profiles of EMZ-MRPs and EMZ-ECPs. Each point represents the mean ± SD (n = 3).

Table 2. Mathematical modeling and drug release kinetics from EMZ-MRPs.

Mathematical model	Equation	r^b
Zero order	Q^a = 0.031 + 0.124t	0.9231
First order	Q^a = 100 × [1 − exp(−0.001t)]	0.8332
Higuchi	Q^a = −0.3 + 0.44t^0.5	0.7883
Korsmeyer–Peppas	Q^a = −0.053 + 0.199t^0.8	0.9894

^aFraction released ($M_t/M_{\infty }$).

^bDetermination coefficient.

Figure 6. SEM photographs of EMZ-MRPs. (A: × 50, B: × 90 and C: × 400) (0: sugar starter cores; 1: drug layer; 2: isolated layer; 3: sustained release polymer layer; 4: isolated layer; 5: enteric polymer layer).

Figure 7. EMZ plasma concentration curves. Each point represents the mean ± SD (n = 6).

Table 3. The pharmacokinetic parameters of EMZ for EMZ-ECPs and EMZ-MRPs after single oral administration in model rats (n = 6).

Parameters (unit)	EMZ-ECPs	EMZ-MRPs
Tmax (h)	1.45 ± 0.735	6.00 ± 0.526
Cmax (ng/ml)	1354.50 ± 98.769	364.89 ± 19.739
MRT (h)	2.73 ± 0.119	7.36 ± 0.391
AUC0–t (ng h/ml)	2774.93 ± 77.430	2733.13 ± 94.419^a
AUC0–∞ (ng h/ml)	2842.61 ± 83.409	2942.15 ± 142.071^a

^ap < 0.01 verus EMZ-ECPs.