Matrix Polymeric Excipients: Comparing a Novel Interpolyelectrolyte Complex with Hydroxypropylmethylcellulose

Figures & data

TABLE 1 Formulations (F1–F12) of the different matrix tablets

	Concentration (% w/w)
Ingredient	F 1	F 2	F 3	F 4	F 5	F 6	F 7	F 8	F 9	F10	F11	F12
Sinomenine HCl	20	20	20	20	20	20
Ranitidine HCl							20	20	20	20	20	20
IPEC	80	64.5					80	64.5
HPMC K100M			80	64.5					80	64.5
HPMC K100LV					80	64.5					80	64.5
Avicel, pH101		10		10		10		10		10		10
Explotab		5		5		5		5		5		5
Mg-stearate		0.5		0.5		0.5		0.5		0.5		0.5

FIG. 1 Infrared spectra of chitosan, polycarbophil, and the IPEC prepared between these two polymers.

TABLE 2 Physical characteristics and drug content of the different matrix tablets

Formulation	Thickness (mm) n = 20	Hardness (N) n = 10	Friability (%) n = 20	Weight (mg) n = 20	Drug content (% w/w) n = 3
F 1	3.64 ± 0.02	63 ± 10	0.25	82.5 ± 2.3	19.14 ± 0.32
F 2	3.50 ± 0.04	81 ± 11	0.39	84.3 ± 5.3	19.18 ± 0.29
F 3	3.52 ± 0.08	82 ± 8	0.21	80.3 ± 6.9	20.01 ± 0.31
F 4	3.50 ± 0.04	95 ± 14	0.21	80.2 ± 5.8	20.07 ± 0.09
F 5	3.46 ± 0.04	90 ± 12	0.05	78.9 ± 4.0	19.84 ± 0.25
F 6	3.46 ± 0.04	87 ± 14	0.15	78.1 ± 3.4	20.09 ± 0.11
F 7	3.67 ± 0.04	91 ± 11	0.20	87.9 ± 4.0	18.82 ± 0.41
F 8	3.40 ± 0.04	84 ± 8	0.26	75.8 ± 2.3	19.85 ± 0.21
F 9	3.70 ± 0.06	85 ± 11	0.11	86.1 ± 5.6	19.23 ± 0.12
F 10	3.54 ± 0.04	87 ± 15	0.05	80.3 ± 3.5	18.81 ± 0.35
F 11	3.50 ± 0.06	94 ± 12	0.06	81.3 ± 4.8	19.88 ± 0.09
F 12	3.50 ± 0.06	89 ± 18	0.11	77.6 ± 3.9	19.90 ± 0.26

*n is the number of measurements.

FIG. 2 Swelling index profiles of the matrix tablets containing sinomenine HCl (formulations F1–F6) at pH 7.4.

FIG. 3 Swelling index profiles of the matrix tablets containing ranitidine HCl (formulations F7–F12) at pH 7.4.

FIG. 4 Percentage erosion of sinomenine HCl-containing matrix tablets (formulations F1–F6) at pH 7.4.

FIG. 5 Percentage erosion of the ranitidine HCl-containing matrix tablets (formulations F7–F12) at pH 7.4.

TABLE 3 Release kinetics and mean dissolution times (MDT) values (formulations F 1–F 12) at pH 7.4

Formulation	MDT (min)	Release constant (K1)	Release exponent (n)	Correlation coefficient (R^2)
F 1	269.75 ± 8.04	0.382 ± 0.058	0.877 ± 0.027	0.996
F 2	181.13 ± 5.46	1.418 ± 0.225	0.696 ± 0.027	0.993
F 3	207.70 ± 6.25	2.921 ± 0.373	0.535 ± 0.021	0.990
F 4	194.41 ± 2.18	3.389 ± 0.468	0.510 ± 0.023	0.987
F 5	174.88 ± 17.19	3.166 ± 0.756	0.553 ± 0.040	0.971
F 6	165.75 ± 15.04	3.191 ± 0.634	0.560 ± 0.034	0.981
F 7	215.10 ± 1.82	1.186 ± 0.123	0.708 ± 0.018	0.997
F 8	41.81 ± 2.73	4.840 ± 5.701	0.651 ± 0.262	0.824
F 9	150.08 ± 7.67	4.937 ± 0.817	0.484 ± 0.029	0.981
F 10	143.68 ± 2.85	6.754 ± 0.966	0.433 ± 0.025	0.981
F 11	123.06 ± 4.72	4.091 ± 1.095	0.542 ± 0.048	0.967
F 12	122.70 ± 4.30	4.432 ± 1.024	0.526 ± 0.041	0.973

FIG. 6 Sinomenine HCl release profiles from the different matrix tablets at pH 7.4.

FIG. 7 Ranitidine HCl release profiles from the different matrix tablets at pH 7.4.

TABLE 4 Calculated difference factor (f₁) and similarity factor (f₂) values for comparison of the dissolution profiles of the matrix-type tablets

Comparison	Difference factor (f1)	Similarity factor (f2)
F 1 vs. F 3	14.10	52.18
F 1 vs. F 5	20.79	40.91
F 2 vs. F 4	28.99	47.84
F 2 vs. F 6	4.63	67.11
F 7 vs. F 9	13.20	48.91
F 7 vs. F 11	19.71	39.21
F 8 vs. F 10	19.28	28.81
F 8 vs. F 12	16.09	31.10