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

doi:10.3748/wjg.v11.i47.7457

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World Journal of Gastroenterology

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1007-9327

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World J Gastroenterol. Dec 21, 2005; 11(47): 7457-7460
Published online Dec 21, 2005. doi: 10.3748/wjg.v11.i47.7457

Table 1 Recovery (%) of α-CyD-5-ASA, 5-ASA and Ac-5-ASA in the GIT, plasma, urine, feces, and liver after oral administration of α-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±4.8	0.0±0.0	0.0±0.0	41.6±30.8	0.0±0.0	0.0±0.0	7.7±7.6	14.7±17.3	7.3±12.6	6.3±11.0	0.8±1.0	1.8±1.6
8	2.8±4.3	0.0±0.0	0.0±0.0	14.3±6.5	0.7±0.4	0.0±0.0	11.3±14.0	20.2±22.4	6.1±5.8	7.2±9.9	9.1±7.7	18.4±13.6
12	0.0±0.0	0.1±0.1	0.4±0.5	1.7±0.4	0.5±0.7	2.5±3.9	9.4±11.8	4.7±7.4	6.2±6.4	17.2±24.0	17.3±23.7	16.6±17.9
24	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	22.8±24.2	9.2±9.0	0.3±0.5	7.9±13.6	13.3±15.6	1.4±1.1	23.4±15.6
	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	0.0±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	0.0±0.0	69.3±29.0
8	0.0±0.0	0.5±0.3	4.0±2.6	0.0±0.0	0.2±0.1	2.0±1.3	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.3±0.1	3.0±2.2	65.0±11.9
12	0.0±0.0	0.4±0.5	4.7±4.0	0.0±0.0	0.3±0.4	2.8±2.4	0.3±0.5	7.1±8.2	7.1±8.0	0.0±0.0	0.2±0.3	0.4±0.8	50.5±20.0
24	0.0±0.0	1.4±1.2	1.9±1.9	0.0±0.0	0.0±0.0	0.0±0.0	4.3±7.4	1.3±1.3	9.3±11.8	0.0±0.0	1.4±1.3	2.1±2.5	12.6±7.6

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.

Table 2 Recovery (%) of β-CyD-5-ASA, 5-ASA, and Ac-5-ASA in GIT, plasma, urine, feces, and liver after oral administration of 9 9 β-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	26.7±3.2	0.0±0.0	0.0±0.0	47.0±27.6	0.0±0.0	0.0±0.0	13.2±13.7	1.0±0.6	0.3±0.3	9.7±16.9	1.2±1.4	0.9±1.4
8	8.5±12.9	0.0±0.0	0.0±0.0	14.9±6.6	2.4±3.4	0.0±0.0	30.6±35.8	7.5±11.6	3.8±3.8	12.3±17.0	9.1±4.4	4.3±2.9
12	0.0±0.0	0.0±0.0	0.7±1.2	6.6±7.9	0.4±0.3	3.0±0.8	8.4±7.4	18.7±13.1	11.7±12.8	16.1±12.6	13.5±12.4	7.9±7.3
24	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	0.0±0.0	2.9±4.4	16.6±16.1	10.3±16.7	17.4±15.2	27.2±45.2	11.0±12.9	5.3±5.9
	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	0.0±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	0.0±0.0	64.0±14.3
8	0.0±0.0	0.7±0.7	2.4±3.0	0.0±0.0	0.1±0.0	0.4±0.4	0.0±0.0	0.1±0.0	0.1±0.1	0.0±0.0	1.9±2.5	1.1±1.6	40.6±14.7
12	0.0±0.0	1.2±0.5	4.1±4.6	0.0±0.0	2.4±3.5	2.3±2.2	0.3±0.9	0.0±0.0	1.1±1.8	0.0±0.0	0.5±0.7	0.8±1.2	35.6±10.7
24	0.0±0.0	2.3±2.6	1.7±2.2	0.0±0.0	0.0±0.0	0.0±0.0	4.6±7.9	0.2±0.2	0.7±0.9	0.0±0.0	0.0±0.0	0.0±0.0	14.8±6.5

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.

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.

Citation: Zou MJ, Cheng G, Okamoto H, Hao XH, An F, Cui FD, Danjo K. Colon-specific drug delivery systems based on cyclodextrin prodrugs: In vivo evaluation of 5-aminosalicylic acid from its cyclodextrin conjugates. World J Gastroenterol 2005; 11(47): 7457-7460
URL: https://www.wjgnet.com/1007-9327/full/v11/i47/7457.htm
DOI: https://dx.doi.org/10.3748/wjg.v11.i47.7457