Development and evaluation of a sublingual film of the antiemetic granisetron hydrochloride

Figures & data

Table I. Influence of polymer ratio on film uniformity.

Formulation code	HPMCK4M/PVPK30	PEG (ml)	Mannitol (mg)	Drug (mg)	Observation
GSF1	10/2	1	20	50	Film breaking/non-uniform weight of film
GSF2	10.1/5	1	20	50	Film breaking/ Non-uniform weight of film
GSF3	100/2.2	1	20	50	Film breaking/non-uniform weight of the film
GSF4	100/2.2	1.5	20	50	No film breaking/uniform weight of the film
GSF5	150/2.2	2	20	50	Film forming/uniform weight, but not able to sustain its integrity, breakage after some time

Bold row signifies optimized formulation and selected for further studies.

Table II. Physical characterization of the optimized drug-loaded film.

Formulation code	Weight variation (mg)	Thickness	% Drug content	Folding endurance	Tensile strength (Kg/mm^2)
GSF1	64.8 ± 1.00	0.54 ± 0.081	72.63 ± 2.32	280.0	1.141 ± 0.3
GSF2	74.73 ± 1.527	0.56 ± 0.008	76.46 ± 4.23	246.6	0.846 ± 0.2
GSF3	64.16 ± 2.516	0.46 ± 0.052	73.18 ± 3.27	238.3	1.023 ± 0.7
GSF4	59.1 ± 1.00	0.43 ± 0.009	86.73 ± 4.13	291.6	1.444 ± 0.1
GSF5	94.2 ± 2.516	0.74 ± 0.015	80.07 ± 2.56	270.0	1.151 ± 0.3

Bold row signifies optimized formulation and selected for further studies.

Figure 1. Entrapment efficiency of the different formulations.

Figure 2. In vitro drug release profiles of developed formulation and marketed formulation.

Figure 3. Ex vivo permeability study of the developed and marketed formulations.

Figure 4. Comparison of plasma drug concentration vs time profile of developed and marketedformulation.

Table III. Comparison of pharmacokinetic parameters.

Pharmacokinetic parameters	Developed formulation	Marketed formulation (MHRA)
AUC (ng.h/ml)	146.60	140.10
Cmax (ng/ml)	23.3	10.6
t1/2 (h)	4.81	11.3
Tmax (h)	3.56	2.42