Sustained-release solid dispersion of pelubiprofen using the blended mixture of aminoclay and pH independent polymers: preparation and in vitro/in vivo characterization

Figures & data

Table 1. Composition of pelubiprofen loaded-solid dispersions.

	Ratio (w/w/w)
Formulation	Pelubiprofen	Eudragit® RL PO	Eudragit® RS PO	Aminoclay (%)
F1	1	1	8	5
F2	1	1	6	5
F3	1	1	2	5
F4	1	2	2	5
F5	1	0	2	5
F6	1	1	2	1
F7	1	1	2	0

Figure 1. Dissolution profiles of PEL from different formulations (F1-F7) at pH 6.8 (Mean ± SD, n = 3). (A) Effect of Eudragit® RS PO, (B) effect of Eudragit® RL PO, (C) effect of aminoclay.

Figure 2. Dissolution profiles of PEL from SRSD (F6) in the different dissolution media (Mean ± SD, n = 3). (A): in buffer transition system, (B): in FaSSIF and FeSSIF.

Figure 3. Structural characteristics of SRSD (F6). DSC thermograms (A), PXRD patterns (B), and FT-IR spectra (C).

Figure 4. Pharmacokinetic profiles of PEL and PEL-transOH after oral administration of PEL in different formulations to rats ((Mean ± SD, n = 3). Untreated drug (3 mg/kg) was given orally three times and SRSD (F6) was given orally once at the dose equivalent to 9 mg/kg of PEL.

Table 2. Pharmacokinetic parameter of PEL and PEL-transOH after oral administration of PEL in different formulations to rats ((Mean ± SD, n = 3).

	PEL		PEL-transOH
Pharmacokinetics parameters	Untreated drug	SRSD (F6)	Untreated drug	SRSD (F6)
Cmax (ng/mL)	30.5 ± 21.1	30.9 ± 21.1	5886.2 ± 717.32	3380.2 ± 983.73*
Tmax (h)	0.25	0.42 ± 0.29	0.25	2.7 ± 1.2*
AUC (ng/mL)	40.7 ± 21.7	62.2 ± 37.9	33998 ± 9603.5	37299 ± 8759.6

* p < .05, Compared to untreated drug.