Development of Mucoadhesive Dosage Forms of Buprenorphine for Sublingual Drug Delivery

Figures & data

1 Schematic of modified tensiometer used for mucoadhesion studies.

2 Dependence of the polymer film thickness on volume of gel cast and drying conditions. The drug-free formulation represented here contained 2.5% w/w Carbopol 974P and 0.5% w/w PEG 400.

Physical characteristics of mucoadhesive tablet formulations

Composition (% w/w)					Thickness	Hardness	Disintegration	Tensile strength
Carbopol	Carbopol	Noveon			(mm);	(kg);	time (hr);	(Newtons)
934P	974P	AA-1	PEG 3350	Lactose	n = 3	n = 3	n = 3	n = 1
100					1.78 ± 0.06	9.8 ± 0.6	9.0 ± 1.0	13.7
95			5		1.79 ± 0.04	10.0 ± 0.8	9.0 ± 0.75	13.0
85			10	5	1.81 ± 0.05	9.8 ± 0.6	8.5 ± 0.75	13.1
80			5	15	1.84 ± 0.10	8.8 ± 0.6	7.0 ± 0.75	11
60			10	30	1.86 ± 0.10	7.4 ± 0.6	5.0 ± 0.5	8.3
40			10	50	1.94 ± 0.12	6.2 ± 0.8	3.0 ± 0.5	5.2
30			10	60	1.98 ± 0.14	5.6 ± 1.0	2.0 ± 0.2	3.9
	100				1.68 ± 0.04	9.6 ± 0.6	8.5 ± 0.75	16.2
	95		5		1.68 ± 0.04	10.0 ± 0.8	8.0 ± 0.75	16.8
	85		10	5	1.71 ± 0.05	9.2 ± 0.6	7.5 ± 0.5	16.1
	80		5	15	1.72 ± 0.08	7.8 ± 0.4	6.0 ± 0.5	14.0
	60		10	30	1.76 ± 0.10	6.8 ± 0.4	4.0 ± 0.4	11.2
	40		10	50	1.76 ± 0.10	5.4 ± 0.8	2.5 ± 0.3	8.8
	30		10	60	1.78 ± 0.12	5.2 ± 1.0	2.0 ± 0.3	7.3
		100			1.89 ± 0.02	10.6 ± 0.6	10.0 ± 1.0	15.0
		95	5		1.82 ± 0.04	10.8 ± 0.8	10.0 ± 0.75	15.5
		85	10	5	1.82 ± 0.02	10.4 ± 0.8	9.5 ± 1.0	14.8
		80	5	15	1.80 ± 0.04	9.6 ± 0.6	8.0 ± 0.75	12.8
		60	10	30	1.86 ± 0.04	8.2 ± 0.8	6.0 ± 0.5	10.1
		40	10	50	1.88 ± 0.12	7.8 ± 1.0	4.0 ± 0.5	8.1
		30	10	60	1.90 ± 0.14	7.6 ± 1.2	3.0 ± 0.5	6.8

3 Dependence of the film diameter on volume of gel cast and drying conditions. The drug-free formulation represented here contained 2.5% w/w Carbopol 974P and 0.5% w/w PEG 400.

4 Differential scanning calorimetry scans for Carbopol 974P, lactose PEG 3350, and buprenorphine, compared with a tablet compact made from these ingredients.

5 Release profiles of buprenorphine from various formulations, each containing 8 mg buprenorphine; ▪ = tablet formulation containing 60% lactose, 10% PEG 3350, and 30% Carbopol 974P; • = tablet formulation containing 60% lactose, 10% PEG 3350, and 30% Noveon AA-1; ▴ = Carbopol 974P polymer film containing 0.5% PEG 400 as plasticizer.