Preparation and evaluation of Vinpocetine self-emulsifying pH gradient release pellets

Figures & data

Figure 1. Transepithelial cumulative percent across Caco-2 monolayers at 37 °C.

Figure 2. Particle size distribution.

Figure 3. DSC thermograms of (a) VIN (b) blank self-emulsifying pellets (c) physical mixture (d) VIN self-emulsifying pH gradient release pellets.

Figure 4. Scanning electron micrographs of pellets (A) pellet coated with HPMC (B) pellet coated with Eudragit L30D-55 (C) pellet coated with Eudragit FS30D.

Figure 5. The release curve in the simulated gastrointestinal pH conditions (n = 6).

Figure 6. Profiles of mean plasma concentration-time after oral administration of VIN commercial tablet, liquid SEDDS, and self-emulsifying pH gradient release pellet (n = 6).

Table 1. Studies schedule in Beagle dogs for different formulations.

	Dog number
Period	1	2	3	4	5	6
1	A	A	B	B	R	R
2	B	R	R	A	A	B
3	R	B	A	R	B	A

A: liquid SEDDS; B: self-emulsifying pH gradient release pellet; R: commercial tablet.

Table 2. Pharmacokinetic parameters of commercial tablet, liquid SEDDS and self-emulsifying pellets after oral administered.

Parameters	Commercial tablet	Liquid SEDDS	Self-emulsifying pellet
Tmax (h)	1.667 ± 0.258	2.167 ± 0.258*	2.083 ± 0.376*
Cmax (ng/mL)	110.340 ± 8.715	242.296 ± 41.700*	110.614 ± 10.385
AUC0–t (ng/mL·h)	349.155 ± 37.813	630.942 ± 41.616*	476.937 ± 20.374*

* p < .05 compared with commercial tablets.