A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets

Figures & data

Table 1 Percentage composition of the orally disintegrating tablet formulations investigated

Component	Form of SH	Microcrystalline cellulose (%)^a	Carboxymethyl starch sodium (%)^a	Mannitol (%)^a	Xylitol (%)^a	Lactose (%)^a	Magnesium stearate (%)^a
Function	Active drug	Deaggregant	Deaggregant	Sweetener	Corrigent	Diluent	Lubricant
Formulation A	Original SH	35	10	45	1	5	0.5
Formulation B	SH-NiMS	35	10	45	1	5	0.5
Formulation C	SH microparticles	35	10	45	1	5	0.5

Note:

a The percentage stands for weight ratio of one component to total (w/w).

Abbreviations: NiMS, nanoparticles-in-microparticles system; SH, scopolamine hydrobromide.

Figure 1 Transmission electron microscope photograph of scopolamine hydrobromide-loaded chitosan nanoparticles (×30,000) prepared by ionotropic gelation process.

Figure 2 Scanning electron microscopy microphotographs of chitosan (CS) microparticles prepared by the spray-drying method: A) without tripolyphosphate pentasodium (TPP) and B) crosslinked with TPP (CS/TPP weight ratio of 6:1, w/w).

Figure 3 In vitro drug release profiles for noncrosslinked and crosslinked chitosan microparticles (n = 3).

Table 2 Disintegration times of orally disintegrating tablets with different drug dispersion states (n = 6)

Orally disintegrating tablets	Disintegration time (mean ± standard deviation) (seconds)
Conventional (free drug)	31 ± 2.6
With noncrosslinked microparticles	35 ± 2.0
With crosslinked microparticles	42 ± 1.7

Figure 4 In vitro drug release profiles for orally disintegrating tablets (ODTs) formulated with different drug dispersion states (n = 3).

Abbreviation: ODMT, orally disintegrating microparticle tablet.