Natural gum as mucoadhesive controlled release carriers: evaluation of Cefpodoxime Proxetil by D-Optimal design technique

Figures & data

Figure 1. (a) FTIR spectrum of Cefpodoxime Proxetil; (b) FTIR spectrum of drug–excipients mixture; (c) FTIR spectrum of excipients mixture.

Figure 2. (a) DSC thermogram of Cefpodoxime Proxetil; (b) DSC thermogram of drug–excipients mixture.

Figure 3. In vitro dissolution of Cefpodoxime Proxetil mucoadhesive tablets (S1 to S9).

Figure 4. In vitro dissolution of Cefpodoxime Proxetil mucoadhesive tablets (C1 to C9).

Table 1. Composition of Cefpodoxime Proxetil mucoadhesive tablets (S1–S9).

Ingredient (in mg) ↓	S1	S2	S3	S4	S5	S6	S7	S8	S9
Cefpodoxime Proxetil	330	330	330	330	330	330	330	330	330
Sodium alginate	16.50	21.45	26.40	16.50	21.45	26.40	16.50	21.45	26.40
HPMC K100 LV	26.40	26.40	26.40	33.00	33.00	33.00	39.60	39.60	39.60
MCC KG-100	24.65	19.70	14.75	18.05	13.10	8.15	11.45	6.50	1.55
Magnesium stearate	2.45	2.45	2.45	2.45	2.45	2.45	2.45	2.45	2.45
Total weight	400	400	400	400	400	400	400	400	400

Table 2. Composition of Cefpodoxime Proxetil mucoadhesive tablets (C1–C9).

Ingredient (in mg) ↓	C1	C2	C3	C4	C5	C6	C7	C8	C9
Cefpodoxime Proxetil	330	330	330	330	330	330	330	330	330
Karaya gum	16.50	21.45	26.40	16.50	21.45	26.40	16.50	21.45	26.40
HPMC K100 LV	26.40	26.40	26.40	33.00	33.00	33.00	39.60	39.60	39.60
MCC KG-100	24.65	19.70	14.75	18.05	13.10	8.15	11.45	6.50	1.55
Magnesium stearate	2.45	2.45	2.45	2.45	2.45	2.45	2.45	2.45	2.45
Total weight	400	400	400	400	400	400	400	400	400

Table 3. Evaluation of powder blend of Cefpodoxime Proxetil mucoadhesive tablets (S1–S9).

Parameters ↓	S1	S2	S3	S4	S5	S6	S7	S8	S9
LOD (%)*	1.78 ± 0.50	1.95 ± 0.40	1.98 ± 0.60	1.99 ± 0.70	1.78 ± 0.80	1.88 ± 0.50	1.89 ± 0.60	1.98 ± 0.90	1.56 ± 0.70
Bulk density (g/cc)*	0.205 ± 0.12	0.199 ± 0.14	0.203 ± 0.16	0.210 ± 0.16	0.205 ± 0.17	0.215 ± 0.18	0.198 ± 0.17	0.199 ± 0.18	0.201 ± 0.17
Tapped density (g/cc)*	0.238 ± 0.16	0.234 ± 0.17	0.244 ± 0.18	0.242 ± 0.19	0.238 ± 0.14	0.247 ± 0.16	0.239 ± 0.13	0.237 ± 0.15	0.237 ± 0.19
Carr’s compressibility index (%)*	13.86 ± 1.00	14.95 ± 1.90	16.80 ± 2.00	13.22 ± 1.80	13.86 ± 2.30	12.95 ± 1.70	17.15 ± 1.50	16.03 ± 1.70	15.18 ± 1.80
Hausner’s ratio*	1.14 ± 0.16	1.17 ± 0.19	1.20 ± 0.17	1.15 ± 0.18	1.14 ± 0.20	1.19 ± 0.18	1.20 ± 0.17	1.19 ± 0.18	1.17 ± 0.16
Angle of repose (degree)*	34.68 ± 2.00	41.38 ± 1.90	36.69 ± 2.0	37.68 ± 2.10	39.32 ± 1.70	40.50 ± 1.80	42.39 ± 2.00	42.50 ± 2.20	41.60 ± 2.30

*All values are mean ± SD of three determinations.

Table 4. Evaluation of powder blend of Cefpodoxime Proxetil mucoadhesive tablets (C1–C9).

Parameters ↓	C1	C2	C3	C4	C5	C6	C7	C8	C9
LOD (%)*	1.98 ± 1.00	1.75 ± 1.00	1.56 ± 1.00	1.47 ± 1.00	1.58 ± 1.00	1.59 ± 1.00	1.98 ± 1.00	1.75 ± 1.00	1.68 ± 1.00
Bulk density (g/cc)*	0.198 ± 0.10	0.207 ± 0.15	0.202 ± 0.15	0.215 ± 0.16	0.210 ± 0.10	0.199 ± 0.12	0.215 ± 0.11	0.205 ± 0.14	0.201 ± 0.17
Tapped density (g/cc)*	0.239 ± 0.14	0.239 ± 0.14	0.245 ± 0.14	0.250 ± 0.17	0.242 ± 0.17	0.237 ± 0.19	0.247 ± 0.17	0.249 ± 0.17	0.237 ± 0.15
Carr’s compressibility index (%)*	17.15 ± 1.50	13.39 ± 1.90	17.55 ± 1.50	14.00 ± 1.80	13.22 ± 1.40	16.03 ± 1.80	12.95 ± 1.00	17.67 ± 1.40	15.18 ± 1.70
Hausner’s ratio*	1.20 ± 0.15	1.15 ± 0.19	1.21 ± 0.20	1.16 ± 0.18	1.15 ± 0.19	1.19 ± 0.17	1.19 ± 0.15	1.21 ± 0.19	1.17 ± 0.16
Angle of repose (degree)*	38.61 ± 1.50	39.58 ± 1.90	34.88 ± 2.00	39.03 ± 1.90	40.74 ± 2.00	42.02 ± 1.80	43.30 ± 1.70	39.21 ± 2.50	42.23 ± 2.00

*All values are mean ± SD of three determinations.

Table 5. Evaluation parameters of Cefpodoxime Proxetil mucoadhesive tablets (S1–S9).

Parameters ↓	S1	S2	S3	S4	S5	S6	S7	S8	S9
Average weight (mg)	400 ± 1.20	400 ± 0.58	400 ± 1.10	400 ± 1.20	400 ± 1.32	400 ± 0.68	400 ± 1.20	400 ± 0.84	400 ± 0.95
Thickness (mm)*	5.86 ± 0.07	5.85 ± 0.09	5.85 ± 0.08	5.87 ± 0.05	5.85 ± 0.09	5.82 ± 0.07	5.87 ± 0.05	5.80 ± 0.09	5.89 ± 0.10
Hardness (kg/cm^2)*	5.0 ± 1.00	5.0 ± 1.00	4.5 ± 1.00	4.5 ± 1.00	5.0 ± 1.00	4.5 ± 1.00	5.0 ± 1.00	4.5 ± 1.00	5.5 ± 1.00
Friability (%)	0.53	0.56	0.55	0.54	0.59	0.52	0.57	0.52	0.49
Drug content (%)*	98.00 ± 1.45	98.52 ± 1.25	99.30 ± 1.14	99.95 ± 1.52	99.85 ± 1.22	100.11 ± 1.47	99.71 ± 1.44	100.14 ± 1.51	100.46 ± 1.37
Mucoadhesive strength (g)*	8.30 ± 0.34	12.2 ± 0.48	15.5 ± 0.39	18.3 ± 0.54	21.5 ± 0.47	23.15 ± 0.52	35.0 ± 2.90	30.4 ± 0.47	32.2 ± 0.39
Mucoadhesion force (N)*	0.81 ± 0.24	1.19 ± 0.37	1.52 ± 0.44	1.79 ± 0.54	2.10 ± 0.35	2.27 ± 0.42	3.43 ± 0.24	2.98 ± 0.32	3.15 ± 0.50

*All values are mean ± SD of three determinations.

Table 6. Evaluation parameters of Cefpodoxime Proxetil mucoadhesive tablets (C1–C9).

Parameters ↓	C1	C2	C3	C4	C5	C6	C7	C8	C9
Average weight (mg)*	400 ± 1.20	400 ± 0.67	400 ± 0.84	400 ± 1.20	400 ± 1.00	400 ± 0.50	400 ± 1.10	400 ± 1.12	400 ± 1.50
Thickness (mm)*	5.82 ± 0.08	5.81 ± 0.05	5.8 ± 0.02	5.79 ± 0.05	5.78 ± 0.08	5.82 ± 0.09	5.79 ± 0.06	5.78 ± 0.08	5.85 ± 0.10
Hardness (kg/cm^2)*	5.0 ± 1.00	5.0 ± 1.00	5.0 ± 1.00	6.0 ± 1.00	6.0 ± 1.00	4.5 ± 1.00	5.0 ± 1.00	5.0 ± 1.00	6.0 ± 1.00
Friability (%)*	0.43	0.32	0.45	0.42	0.39	0.32	0.47	0.56	0.32
Drug content (%)*	99.26 ± 1.45	99.57 ± 1.65	99.84 ± 1.87	99.89 ± 1.97	100.79 ± 1.58	99.71 ± 1.45	99.00 ± 1.96	99.75 ± 1.79	100 ± 1.67
Mucoadhesive strength (g)*	9.10 ± 0.20	15.20 ± 0.31	18.10 ± 0.34	20.15 ± 0.39	23.20 ± 0.42	25.19 ± 0.47	27.21 ± 0.46	30.30 ± 0.62	35.19 ± 0.54
Mucoadhesion force (N)*	0.89 ± 0.25	1.49 ± 0.30	1.77 ± 0.24	1.97 ± 0.30	2.27 ± 0.41	2.47 ± 0.55	2.66 ± 0.12	2.97 ± 0.15	3.45 ± 0.18

*All values are mean ± SD of three determinations.

Figure 5. Response surface plots for (a) T4; (b) T8; (c) T12.

Figure 6. Swelling index of Cefpodoxime Proxetil mucoadhesive tablets (S1 to S9).

Figure 7. Swelling index of Cefpodoxime Proxetil mucoadhesive tablets (C1 to C9).

Figure 8. X-ray photographs of Cefpodoxime Proxetil mucoadhesive tablets at different time intervals. (a) at 0 h; (b) after 2 h; (c) after 4 h; (d) after 6 h; (e) after 8 h; (f) after 10 h.

Table 7. Evaluation of Cefpodoxime Proxetil mucoadhesive tablets (S7) kept for stability at 40 °C/75% relative humidity.

Parameters ↓	Initial	1 Month	2 Months	3 Months
Average weight (mg)*	400 ± 1.20	400 ± 1.50	400 ± 1.30	400 ± 1.2
Thickness (mm)*	8.83 ± 0.075	8.83 ± 0.078	8.83 ± 0.076	8.83 ± 0.075
Hardness (kg/cm^2)*	4–5	4–5	4–5	4–5
Mucoadhesive strength (g)*	27.3 ± 0.62	28.3 ± 2.90	27.2 ± 3.10	28.1 ± 3.50
Total mucoadhesion time (h)	12	12	12	12
Drug content (%)*	99.85 ± 1.22	99.75 ± 1.11	99.75 ± 1.21	99.75 ± 0.98
% drug released*	97.22 ± 0.21	96.90 ± 0.60	96.80 ± 0.60	96.50 ± 0.60

*All values are mean ± SD of three determinations.