Pulsatile systems for colon targeting of budesonide: In vitro and in vivo evaluation

Figures & data

Table 1.  Compositions of different spray-coated and pulsatile capsules.

Formula	Tablet plug						Spray coat (20 mg)
	Effervescent mixture (mg)	CAB (%)	HPMC (%)	Pectin (%)	Guar gum (%)	Anhydrous lactose (%)
F1	—	—	—	—	—	—	EUD L100
F2	—	—	—	—	—	—	EUD S100
F3	—	—	—	—	—	—	Ethyl cellulose
F4	—	50	—	—	—	50	—
F5	50	50	—	—	—	50	—
F6	—	25	—	—	—	75	—
F7	—	25	—	—	—	75	EUD S100
F8	—	—	50	—	—	50	—
F9	—	—	25	—	—	75	—
F10	—	—	25	—	—	75	EUD S100
F11	—	—	—	100	—	—	—
F12	—	—	—	75	—	25	—
F13	—	—	—	50	—	50	—
F14	—	—	—	50	—	50	EUD S100
F15	—	—	—	—	50	50	—
F16	—	—	—	—	25	75	—
F17	—	—	—	—	25	75	EUD S100

Figure 1.  Release profile of BUD from spray coated capsules in 0.1N HCl for 2 hours, phosphate buffer (pH 6.8) for another 3 hours and phosphate buffer (pH 7.4) till the end of 24 hours.

Figure 2.  Percentage of BUD released before the target area, in the target area and total percentage released after 24 hrs from spray coated capsules.

Figure 3.  Release profile of BUD from pulsatile capsules using time dependent polymers in tablet plugs in 0.1N HCl for 2 hours, phosphate buffer (pH 6.8) for another 3 hrs and phosphate buffer (pH 7.4) till the end of 24 hours.

Figure 4.  Percentage of BUD released before the target area, in the target area and total percentage released after 24 hrs from pulsatile capsules using time dependent polymers in tablet plugs.

Figure 5.  Release profile of BUD from pulsatile capsules using enzyme dependent polymers in tablet plugs in 0.1N HCl for 2 hours, phosphate buffer (pH 6.8) for another 3 hrs and phosphate buffer (pH 7.4) till the end of 24 hours.

Figure 6.  Percentage of BUD released before the target area, in the target area and total percentage released after 24 hrs from pulsatile capsules using enzyme dependent polymers in tablet plugs.

Figure 7.  Localization of F2 throughout the GIT: A- Stomach after 20 min. B- Transverse colon after 3 hrs.

Table 2.  Position of different formulas at different time intervals as detected by x-ray imaging.

	F2	F14	F17
20 min	Stomach
	Intact
3 h	Transverse colon	Ileum	Ileum
	Opened	Intact	Intact
5 h		Ascending colon	Ascending colon
		Intact	Opened
8 h		Rectum	Transverse colon
		Intact	Opened
24 h		Disappeared	Disappeared

Figure 8.  Localization of F14 throughout the GIT: A: Stomach after 20 min. B: Ileum after 3 hrs. C: Transverse colon after 5 hrs. D: Rectum after 8 hrs.

Figure 9.  Localization of F17 throughout the GIT: A: Stomach after 20 min. B: Ileum after 3 hrs. C: Ascending colon after 5 hrs. D: Transverse colon after 8 hrs. E- Disappeared.

Figure 10.  Histological appearance of colonic tissues (A) normal group, (B) TNBS induced colitis group, (C) Spray coated capsules treated group, (D) F17 pulsatile capsules treated group and (E) commercial capsules treated group.