Colon-specific drug delivery systems based on cyclodextrin prodrugs: In vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates

Table 3 Recovery (%) of γ-CyD-5-ASA, 5-ASA, and Ac-5-ASA in GIT, plasma, urine, feces, and liver after oral administration of γ-CyD-5-ASA to rats (mean±SD)

Time	Stomach			Small intestine			Cecum			Colon
(h)	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA
4	19.8±9.4	0.0±0.0	0.0±0.0	46.4±28.7	0.2±0.3	0.0±0.0	10.0±10.1	0.9±0.3	5.4±4.8	8.4±14.6	6.4±5.4	2.2±1.8
8	3.2±5.0	0.0±0.0	0.0±0.0	16.2±3.3	2.4±1.5	0.0±0.0	18.2±24.8	15.7±9.4	2.2±2.7	4.0±4.2	20.2±8.2	7.7±4.2
12	0.0±0.0	0.2±0.0	0.6±0.6	2.1±1.2	0.8±0.3	0.0±0.0	7.6±7.0	4.9±2.5	14.1±12.2	7.9±5.2	7.2±1.5	34.6±20.8
24	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.8±0.7	5.3±5.8	2.1±1.8	40.5±35.4	15.0±22.3	19.4±15.6	5.1±4.0
	Plasma			Urine			Feces			Liver			Total
	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA	Prodrug	5-ASA	AC-5-ASA	recovery
4	0.0±0.0	0.0±0.0	0.2±0.2	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	76.8±12.2
8	0.0±0.0	0.2±0.1	2.5±2.4	0.0±0.0	1.1±0.2	1.8±1.8	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	2.9±2.2	1.7±1.8	61.9±22.0
12	0.0±0.0	1.8±1.7	3.8±3.5	0.0±0.0	0.1±0.0	6.4±6.6	0.5±0.8	2.2±0.8	0.0±0.0	0.0±0.0	0.9±0.6	4.3±0.2	48.5±6.8
24	0.0±0.0	1.3±1.4	0.6±0.1	0.0±0.0	0.1±0.0	2.5±2.4	3.7±4.1	0.3±0.0	3.4±1.3	0.0±0.0	0.0±0.0	0.0±0.0	17.2±2.4

Total recovery=100×(amount of the intact prodrugs, 5-ASA, and Ac-5-ASA recovered from stomach, small intestine, cecum, colon, blood, urine, liver, and feces)/dose.