Transbuccal Delivery of Chlorpheniramine Maleate from Mucoadhesive Buccal Patches

Figures & data

TABLE 1 Formulation ingredients of mucoadhesive buccal patches of chlorpheniramine maleate

	Formulation
Ingredients	AA1	AA2	AA3	AA4	AA5
HEC 10 (mg)	1000	1250	1500	1750	2000
CPM (mg)	205	205	205	205	205
Propylene glycol (μl)	150	188	225	263	300
Distilled water (ml)	25	25	25	25	25

HEC = hydroxyethylcellulose; CPM = chlorpheniramine maleate

FIG. 1 In vitro permeation of CPM (4.0 mg) through porcine buccal mucosa; values represented as mean ± S.D. (n = 4).

FIG. 2 Buccal absorption of CPM (4.0 mg) in healthy human volunteers; values represented as mean ± S.D. (n = 8).

FIG. 3 Release profiles of CPM from mucoadhesive buccal patches in phosphate buffer pH 6.6. AA1 = (—); AA2 = (▪); AA3 = (▴); AA4 = (•); AA5-(□); values represented as mean ± S.D. (n = 6).

TABLE 2 Moisture absorption and mechanical properties of mucoadhesive buccal patches of chlorpheniramine maleate

Formulation	Moisture absorbed (% w/w)^a	Tensile strength (Kg.mm^−2)^b	Elongation at break (% mm^−2)^b
AA1	Deformed	3.12 ± 0.90	86.44 ± 5.28
AA2	148.34 ± 7.60	4.86 ± 1.32	37.36 ± 5.13
AA3	170.12 ± 9.36	7.94 ± 2.03	26.53 ± 3.09
AA4	190.34 ± 12.32	8.73 ± 2.34	28.82 ± 4.12
AA5	205.31 ± 7.54	11.34 ± 1.32	19.24 ± 3.73

^aValues represented as mean ± S.D. (n = 6)

^bValues represented as mean ± S.D. (n = 4)

FIG. 4 Serum levels of chlorpheniramine administered by oral (♦) and buccal (▪) routes; values represented as mean ± S.D. (n = 6).

TABLE 3 Pharmacokinetic parameters of chlorpheniramine maleate (CPM) (4.0 mg) administered by oral and buccal routes in human volunteers

Route	Cmax(ng/ml)^a	Tmax (h)^a	AUC0 −n (ng.h/ml)^a
Oral	5.73 ± 1.08	2.17 ± 0.41	57.85 ± 15.50
Buccal	6.16 ± 0.99	3.33 ± 0.82	84.99 ± 17.96

^aValues represented as mean ± S.D. (n = 6)