In Situ Perfusion Model in Rat Colon for Drug Absorption Studies: Comparison with Small Intestine and Caco-2 Cell Model

Journal of Pharmaceutical Sciences

Volumn 104, Issue 9, 2015, Pages 3136-3145

  Lozoya Agullo, Isabel ^a,b   González Álvarez, Isabel ^a   González Álvarez, Marta ^a   Merino Sanjuán, Matilde ^b   Bermejo, Marival ^a  

^a MIGUEL HERNÁNDEZ UNIVERSITY   (Spain)

^b UNIVERSITY OF VALENCIA   (Spain)

Author keywords

absorption; Caco 2 cells; colon absorption; colonic drug delivery; fraction absorbed; in vitro models; permeability; site specific absorption

Indexed keywords

AMOXICILLIN; ATENOLOL; CAFFEINE; CARBAMAZEPINE; CIMETIDINE; CODEINE; COLCHICINE; FUROSEMIDE; METOPROLOL; NAPROXEN; PHENAZONE; RANITIDINE; TERBUTALINE; THEOPHYLLINE; VALSARTAN; VERAPAMIL; DELAYED RELEASE FORMULATION;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CACO 2 CELL LINE; COLON FRACTION ABSORBED; COMPARATIVE STUDY; CONTROLLED RELEASE FORMULATION; DRUG ABSORPTION; DRUG PENETRATION; DRUG SCREENING; DRUG TISSUE LEVEL; DRUG TRANSPORT; FRACTION ABSORBED; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN TISSUE; IN SITU CLOSED LOOP PERFUSION MODEL; INTESTINE PERFUSION; MALE; MODEL; NONHUMAN; ORAL FRACTION ABSORBED; RAT; SMALL INTESTINE; WATER ABSORPTION; ANIMAL; COLON; DELAYED RELEASE FORMULATION; INTESTINE ABSORPTION; METABOLISM; PERFUSION; PERMEABILITY; PHYSIOLOGY; PROCEDURES; TRANSPORT AT THE CELLULAR LEVEL; TUMOR CELL LINE; WISTAR RAT;

ANIMALS; BIOLOGICAL TRANSPORT; CACO-2 CELLS; CELL LINE, TUMOR; COLON; DELAYED-ACTION PREPARATIONS; HUMANS; INTESTINAL ABSORPTION; INTESTINE, SMALL; MALE; MODELS, ANIMAL; PERFUSION; PERMEABILITY; RATS; RATS, WISTAR;

EID: 84939264285     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.24447     Document Type: Article

References (57)

1. Tannergren C, Bergendal A, Lennernas H, Abrahamsson B,. 2009. Toward an increased understanding of the barriers to colonic drug absorption in humans: Implications for early controlled release candidate assessment. Mol Pharm 6 (1): 60-73.
2. Wilson CG,. 2010. The transit of dosage forms through the colon. Int J Pharm 395 (1-2): 17-25.
3. Yuasa H,. 2008. Drug absorption from the colon in situ. In Drug absorption studies;, Ehrhardt C, Kim K-J, Eds. Springer US, New York, pp 77-88.
4. Lennernas H,. 2014. Regional intestinal drug permeation: Biopharmaceutics and drug development. Eur J Pharm Sci 57: 333-341.
5. Meier Y, Eloranta JJ, Darimont J, Ismair MG, Hiller C, Fried M, Kullak-Ublick GA, Vavricka SR,. 2007. Regional distribution of solute carrier mRNA expression along the human intestinal tract. Drug Metab Dispos 35 (4): 590-594.
6. Estudante M, Morais JG, Soveral G, Benet LZ,. 2013. Intestinal drug transporters: An overview. Adv Drug Deliv Rev 65 (10): 1340-1356.
7. Drozdzik M, Groer C, Penski J, Lapczuk J, Ostrowski M, Lai Y, Prasad B, Unadkat JD, Siegmund W, Oswald S,. 2014. Protein abundance of clinically relevant multidrug transporters along the entire length of the human intestine. Mol Pharm 11 (10): 3547-3555.
8. Drozdzik M, Groer C, Penski J, Lapczuk J, Ostrowski M, Lai Y, Prasad B, Unadkat JD, Siegmund W, Oswald S,. 2014. Protein abundance of clinically relevant multidrug transporters along the entire length of the human intestine. Mol Pharm 11 (10): 3547-3555.
9. Sousa T, Paterson R, Moore V, Carlsson A, Abrahamsson B, Basit AW,. 2008. The gastrointestinal microbiota as a site for the biotransformation of drugs. Int J Pharm 363 (1-2): 1-25.
10. Sousa T, Yadav V, Zann V, Borde A, Abrahamsson B, Basit AW,. 2014. On the colonic bacterial metabolism of azo-bonded prodrugsof 5-aminosalicylic acid. J Pharm Sci 103 (10): 3171-3175.
11. Gramatte T,. 1994. Griseofulvin absorption from different sites in the human small intestine. Biopharm Drug Dispos 15 (9): 747-759.
12. Masaoka Y, Tanaka Y, Kataoka M, Sakuma S, Yamashita S,. 2006. Site of drug absorption after oral administration: Assessment of membrane permeability and luminal concentration of drugs in each segment of gastrointestinal tract. Eur J Pharm Sci 29 (3-4): 240-250.
13. Sjogren E, Abrahamsson B, Augustijns P, Becker D, Bolger MB, Brewster M, Brouwers J, Flanagan T, Harwood M, Heinen C, Holm R, Juretschke HP, Kubbinga M, Lindahl A, Lukacova V, Munster U, Neuhoff S, Nguyen MA, Peer A, Reppas C, Hodjegan AR, Tannergren C, Weitschies W, Wilson C, Zane P, Lennernas H, Langguth P,. 2014. In vivo methods for drug absorption-Comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for formulation/API/excipient characterization including food effects. Eur J Pharm Sci 57: 99-151.
14. Ungell AL, Nylander S, Bergstrand S, Sjoberg A, Lennernas H,. 1998. Membrane transport of drugs in different regions of the intestinal tract of the rat. J Pharm Sci 87 (3): 360-366.
15. Kararli TT,. 1995. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos 16 (5): 351-380.
16. Davis SS, Hardy JG, Fara JW,. 1986. Transit of pharmaceutical dosage forms through the small intestine. Gut 27 (8): 886-892.
17. Pagliara A, Reist M, Geinoz S, Carrupt PA, Testa B,. 1999. Evaluation and prediction of drug permeation. J Pharm Pharmacol 51 (12): 1339-1357.
18. Amidon GL, Lennernas H, Shah VP, Crison JR,. 1995. A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12 (3): 413-420.
19. Corrigan OI,. 1997. The biopharmaceutic drug classification and drugs administered in extended release (ER) formulations. Adv Exp Med Biol 423: 111-128.
20. Sutton SC, Evans LA, Fortner JH, McCarthy JM, Sweeney K,. 2006. Dog colonoscopy model for predicting human colon absorption. Pharm Res 23 (7): 1554-1563.
21. Wilding IR,. 1999. Evolution of the biopharmaceutics classification system (BCS) to oral modified release (MR) formulations; what do we need to consider? Eur J Pharm Sci 8 (3): 157-159.
22. Michael M, Cullinane C, Hatzimihalis A, O'Kane C, Milner A, Booth R, Schlicht S, Clarke SJ, Francis P,. 2012. Docetaxel pharmacokinetics and its correlation with two in vivo probes for cytochrome P450 enzymes: The C(14)-erythromycin breath test and the antipyrine clearance test. Cancer Chemother Pharmacol 69 (1): 125-135.
23. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR,. 1999. Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res 16 (3): 408-414.
24. Faassen F, Vogel G, Spanings H, Vromans H,. 2003. Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm 263 (1-2): 113-122.
25. Owen A, Pirmohamed M, Tettey JN, Morgan P, Chadwick D, Park BK,. 2001. Carbamazepine is not a substrate for P-glycoprotein. Br J Clin Pharmacol 51 (4): 345-349.
26. Ufer M, Mosyagin I, Muhle H, Jacobsen T, Haenisch S, Hasler R, Faltraco F, Remmler C, von Spiczak S, Kroemer HK, Runge U, Boor R, Stephani U, Cascorbi I,. 2009. Non-response to antiepileptic pharmacotherapy is associated with the ABCC2 -24C>T polymorphism in young and adult patients with epilepsy. Pharmacogenet Genomics 19 (5): 353-362.
27. Neuhoff S, Ungell AL, Zamora I, Artursson P,. 2003. pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: Implications for drug-drug interactions. Pharm Res 20 (8): 1141-1148.
28. Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y,. 2002. Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res 19 (2): 147-153.
29. Ozvegy-Laczka C, Hegedus T, Varady G, Ujhelly O, Schuetz JD, Varadi A, Keri G, Orfi L, Nemet K, Sarkadi B,. 2004. High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. Mol Pharmacol 65 (6): 1485-1495.
30. Ekins S, Bravi G, Wikel JH, Wrighton SA,. 1999. Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther 291 (1): 424-433.
31. Takara K, Kakumoto M, Tanigawara Y, Funakoshi J, Sakaeda T, Okumura K,. 2002. Interaction of digoxin with antihypertensive drugs via MDR1. Life Sci 70 (13): 1491-1500.
32. Skolnik S, Lin X, Wang J, Chen XH, He T, Zhang B,. 2010. Towards prediction of in vivo intestinal absorption using a 96-well Caco-2 assay. J Pharm Sci 99 (7): 3246-3265.
33. Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, Sawada Y,. 2002. Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun 296 (3): 644-650.
34. Pavek P, Merino G, Wagenaar E, Bolscher E, Novotna M, Jonker JW, Schinkel AH,. 2005. Human breast cancer resistance protein: Interactions with steroid drugs, hormones, the dietary carcinogen 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine, and transport of cimetidine. J Pharmacol Exp Ther 312 (1): 144-152.
35. Tzvetkov MV, dos Santos Pereira JN, Meineke I, Saadatmand AR, Stingl JC, Brockmoller J,. 2013. Morphine is a substrate of the organic cation transporter OCT1 and polymorphisms in OCT1 gene affect morphine pharmacokinetics after codeine administration. Biochem Pharmacol 86 (5): 666-678.
36. Amidon G, Sinko P, Fleisher D,. 1988. Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds. Pharm Res 5 (10): 651-654.
37. Dahan A, Amidon GL,. 2009. Grapefruit juice and its constituents augment colchicine intestinal absorption: Potential hazardous interaction and the role of p-glycoprotein. Pharm Res 26 (4): 883-892.
38. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A,. 1999. Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): Its pharmacological and toxicological relevance. J Pharmacol Exp Ther 291 (2): 778-784.
39. Hasegawa M, Kusuhara H, Adachi M, Schuetz JD, Takeuchi K, Sugiyama Y,. 2007. Multidrug resistance-associated protein 4 is involved in the urinary excretion of hydrochlorothiazide and furosemide. J Am Soc Nephrol 18 (1): 37-45.
40. Ito N, Ito K, Ikebuchi Y, Kito T, Miyata H, Toyoda Y, Takada T, Hisaka A, Honma M, Oka A, Kusuhara H, Suzuki H,. 2014. Organic cation transporter/solute carrier family 22a is involved in drug transfer into milk in mice. J Pharm Sci 103 (10): 3342-3348.
41. Challa VR, Babu PR, Challa SR, Johnson B, Maheswari C,. 2013. Pharmacokinetic interaction study between quercetin and valsartan in rats and in vitro models. Drug Dev Ind Pharm 39 (6): 865-872.
42. Poirier A, Cascais AC, Funk C, Lave T,. 2009. Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn 36 (6): 585-611.
43. Doluisio JT, Billups NF, Dittert LW, Sugita ET, Swintosky JV,. 1969. Drug absorption. I. An in situ rat gut technique yielding realistic absorption rates. J Pharm Sci 58 (10): 1196-1200.
44. Martin-Villodre A, Pla-Delfina JM, Moreno J, Perez-Buendia D, Miralles J, Collado EF, Sanchez-Moyano E, del Pozo A,. 1986. Studies on the reliability of a bihyperbolic functional absorption model. I. Ring-substituted anilines. J Pharmacokinet Biopharm 14 (6): 615-633.
45. Mangas-Sanjuan V, Gonzalez-Alvarez I, Gonzalez-Alvarez M, Casabo VG, Bermejo M,. 2014. Modified nonsink equation for permeability estimation in cell monolayers: Comparison with standard methods. Mol Pharm 11 (5): 1403-1414.
46. Lunn G, Schmuff NR,. 1997. HPLC methods for pharmaceutical analysis. New York: John Wiley & Sons, Inc.
47. Lentz KA, Hayashi J, Lucisano LJ, Polli JE,. 2000. Development of a more rapid, reduced serum culture system for Caco-2 monolayers and application to the biopharmaceutics classification system. Int J Pharm 200 (1): 41-51.
48. Sjoberg A, Lutz M, Tannergren C, Wingolf C, Borde A, Ungell AL,. 2013. Comprehensive study on regional human intestinal permeability and prediction of fraction absorbed of drugs using the Ussing chamber technique. Eur J Pharm Sci 48 (1-2): 166-180.
49. Rozehnal V, Nakai D, Hoepner U, Fischer T, Kamiyama E, Takahashi M, Yasuda S, Mueller J,. 2012. Human small intestinal and colonic tissue mounted in the Ussing chamber as a tool for characterizing the intestinal absorption of drugs. Eur J Pharm Sci 46 (5): 367-373.
50. Salphati L, Childers K, Pan L, Tsutsui K, Takahashi L,. 2001. Evaluation of a single-pass intestinal-perfusion method in rat for the prediction of absorption in man. J Pharm Pharmacol 53 (7): 1007-1013.
51. Haslam IS, O'Reilly DA, Sherlock DJ, Kauser A, Womack C, Coleman T,. 2011. Pancreatoduodenectomy as a source of human small intestine for Ussing chamber investigations and comparative studies with rat tissue. Biopharm Drug Dispos 32 (4): 210-221.
52. Varma MV, Sateesh K, Panchagnula R,. 2005. Functional role of P-glycoprotein in limiting intestinal absorption of drugs: Contribution of passive permeability to P-glycoprotein mediated efflux transport. Mol Pharm 2 (1): 12-21.
53. Zakeri-Milani P, Valizadeh H, Tajerzadeh H, Azarmi Y, Islambolchilar Z, Barzegar S, Barzegar-Jalali M,. 2007. Predicting human intestinal permeability using single-pass intestinal perfusion in rat. J Pharm Pharm Sci 10 (3): 368-379.
54. Kim JS, Mitchell S, Kijek P, Tsume Y, Hilfinger J, Amidon GL,. 2006. The suitability of an in situ perfusion model for permeability determinations: Utility for BCS class I biowaiver requests. Mol Pharm 3 (6): 686-694.
55. Dahan A, Wolk O, Zur M, Amidon GL, Abrahamsson B, Cristofoletti R, Groot DW, Kopp S, Langguth P, Polli JE, Shah VP, Dressman JB,. 2014. Biowaiver monographs for immediate-release solid oral dosage forms: Codeine phosphate. J Pharm Sci 103 (6): 1592-1600.
56. Ungell A., 2002. Transport studies using intestinal tissue ex-vivo. In Cell culture models of biological barriers: In vitro test systems for drug absorption and delivery;, Lehr CM, Ed. New York: Taylor & Francis, pp 164-188.
57. Lozoya-Agullo I, Zur M, Wolk O, Beig A, Gonzalez-Alvarez I, Gonzalez-Alvarez M, Merino-Sanjuan M, Bermejo M, Dahan A,. 2015. In-situ intestinal rat perfusions for human F prediction and BCS permeability class determination: Investigation of the single-pass vs. the Doluisio experimental approaches. Int J Pharm 480 (1-2): 1-7.