Controlled release effervescent buccal discs of buspirone hydrochloride: in vitro and in vivo evaluation studies

Figures & data

Table 1. Composition of designed buccal discs (75 mg) and results of physical characterization.

B. No.^a	HPMC (%w/w)	Sodium Bicarbonate (%w/w)	Citric acid (%w/w)	Lactose (%w/w)	Assay (%)	Friability (%)	Thickness (mm)	Bioadhesion (N)
F1	26.67	0.00	0.00	51.33	98.76 ± 0.57	0.61	2.47 ± 0.02	0.867 ± 0.17
F2	26.67	28.00	0.00	23.33	100.56 ± 0.48	0.43	2.49 ± 0.01	0.812 ± 0.36
F3	26.67	0.00	9.33	42.00	99.63 ± 0.74	0.19	2.51 ± 0.02	0.784 ± 0.13
F4	26.67	16.00	5.33	30.00	98.89 ± 0.83	0.32	2.51 ± 0.03	0.689 ± 0.11
F5	26.67	24.00	8.00	19.33	98.16 ± 0.41	0.57	2.50 ± 0.04	0.694 ± 0.08
F6	26.67	28.00	9.33	14.00	99.01 ± 0.29	0.51	2.52 ± 0.03	0.671 ± 0.18

^a2% (w/w) magnesium stearate, 6.67% (w/w) of MCC and 13.33% (w/w) of drug was added in all the batches.

Figure 1. Drug release profiles from the designed buccal discs (n = 3).

Table 2. Mathematical treatment of drug release data for prediction of drug release kinetics and drug release mechanism from designed HPMC buccal discs.

	Zero order		First order		Higuchi		Korsmeyer-Peppas
B. No	R^2	k0 (mg%/h)	R^2	k1 (h^−1)	R^2	kH (h^−0.5)	R^2	kKP (h^−n)	n
F1	0.909	13.488	0.981	0.199	0.974	25.557	0.993	21.964	0.633
F2	0.833	15.194	0.957	0.246	0.984	29.152	0.988	27.578	0.549
F3	0.866	23.879	0.994	0.588	0.976	45.564	0.985	41.239	0.588
F4	0.724	19.659	0.956	0.416	0.989	38.188	0.991	39.712	0.465
F5	0.702	30.001	0.980	0.874	0.991	52.442	0.995	54.714	0.452
F6	0.691	39.896	0.995	1.167	0.989	60.700	0.993	62.298	0.455

Table 3. Pharmacokinetic parameters of BS when administered intravenously and via buccal route.

Pharmacokinetic parameters	10 mg BS solution via i.v	10 mg non-effervescent buccal disc (F1)	10 mg effervescent buccal disc (F5)
AUC0–∞ (ng h/mL)^a	5153.90 ± 430.81	1662.27 ± 745.26	2687.07 ± 912.32
F	–	0.32 ± 0.11	0. 55 ± 0.06
C max (ng/mL)^a	1384.68 ± 467.21	219.22 ± 36.47	329.31 ± 31.78
t max (h)	–	3.00	2.50
T1/2^a (h)	2.53 ± 0.12	4.78 ± 0.26	5.76 ± 0.23

^aValues are mean ± SD. n = 3.

Figure 2. Mean plasma concentration time profile of BS following intravenous and buccal administration (n = 3).