Atenolol Cyclosporine

Figure 3 Correlation between the fraction absorbed and the membrane permeability in Caco-2 cells. Papp represents the membrane permeability of following 20 compounds, and was obtained by measuring the transcellular transport from the apical-to-basal side in Caco-2 cells. The fraction absorbed was obtained from literature. A amoxicillin, B antipyrine, C atenolol, D caffein, E cephalexin, F cyclosporin A, G enalaprilate, H L-glutamine, I hydrocortisone, J inulin, K D-mannitol, L metoprolol, M L-phenylalanine, N PEG-400, O PEG-4000, P propranolol, Q sucrose, R taurocholate, S terbutaline, T testosterone. Source From Ref. 37.

Relationship between rat intestinal absorption clearance and lipid solubility. The results shown with the squares represent the relationship between intestinal absorption clearance (ka) observed from the in situ jejunum loop in the presence ( ) and absence ( ) of cyclosporin A in rats and octanol-buffer (pH 7.0) partition coefficients (log D) determined in this study. The numbers refer to 1, atenolol 2, nadolol 3, acetamide 4, celiprolol 5, acebutolol 6, doxorubicin 7, timolol 8, sulfathiazole 9, quinidine 10, sulfamethoxazole 11, digoxin 12, cyclosporin A 13, vinblastine 14, b-estradiol 15, verapamil. Modified from A.Tsuji and I. Tamai. Pham. Res., 13 963—977 (1996). 

Figure 6.3 Plot of the fraction of dose absorbed (in %) of various drugs as a function of the permeability estimates in the Caco-2 system. Key 1 D-glucose 2 verapamil 3 piroxicam 4 phenylalanine 5 cyclosporin 6 enalapril 7 cephalexim 8 losartan 9 lisinopril 10 amoxicillin 11 methyldopa 12 naproxen 13 an-tipyrine 14 desipramine 15 propanolol 16 amiloride 17 metoprolol 18 terbu-taline 19 mannitol 20 cimetidine 21 ranitidine 22 enalaprilate 23 atenolol 24 hydrochlorothiazide.

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