Site-specific drug delivery to the middle-to-lower region of the small intestine reduces food-drug interactions that are responsible for low drug absorption in the fed state

Journal of Pharmaceutical Sciences

Volumn 97, Issue 12, 2008, Pages 5341-5353

  Tanno, Fumié K ^a   Sakuma, Shinji ^b   Masaoka, Yoshie ^b   Kataoka, Makoto ^b   Kozaki, Toshio ^c   Kamaguchi, Ryosei ^c   Ikeda, Yutaka ^a   Kokubo, Hiroyasu ^a   Yamashita, Shinji ^b  

^a SHIN ETSU CHEMICAL CO LTD   (Japan)

^b SETSUNAN UNIVERSITY   (Japan)

^c Morishita Jintan Co Ltd   (Japan)

Author keywords

Enteric coating; Food drug interaction; Hypromellose acetate succinate; pH dependent dissolution; Site specific drug delivery

Indexed keywords

HYDROXYPROPYLMETHYLCELLULOSE ACETATE SUCCINATE; TRIENTINE;

ANIMAL EXPERIMENT; AQUEOUS SOLUTION; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DESIGN; ENTERIC COATED TABLET; FOOD DRUG INTERACTION; MALE; NONHUMAN; PH; SMALL INTESTINE ABSORPTION; TABLET DISINTEGRATION TIME; TABLET HARDNESS;

EID: 57349135350     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21382     Document Type: Article

References (45)

1. Schmidt LE, Dalhoff K. 2002. Food-drug interactions. Drugs 62:1481-1502.
2. Singh BN. 1997. Effects of food on clinical pharmacokinetics. Clin Pharmacokinet 37:213-255.
3. Gauthier I, Malone M. 1998. Drug-food interactions in hospitalized patients. Methods of prevention. Drug Saf 18:383-393.
4. Sakuma S, Tanno FK, Masaoka Y, Kataoka M, Kozaki T, Kamaguchi R, Kokubo H, Yamashita S. 2007. Effect of administration site in the gastrointestinal tract on bioavailability of poorly absorbed drugs taken after a meal. J Control Release 118:59-64.
5. Lange H, Eggers R, Bircher J. 1988. Increased systemic availability of albendazole when taken with a fatty meal. Eur J Clin Pharmacol 34:315-317.
6. Crounse RG. 1961. Human pharmacology of griseofulvin: The effect of fat intake on gastrointestinal absorption. J Invest Dermatol 37:529-533.
7. Charman WN, Rogge MC, Boddy AW, Berger BM. 1993. Effect of food and a monoglyceride emulsion formulation on danazol bioavailability. J Clin Pharmacol 33:381-386.
8. Colburn WA, Gibson DM, Wiens RE, Hanigan JJ. 1983. Food increases the bioavailability of isotretinoin. J Clin Pharmacol 23:534-539.
9. Kenyon CJ, Brown F, McClelland GR, Wilding IR. 1998. The use of pharmacoscintigraphy to elucidate food effects observed with a novel protease inhibitor (saquinavir). Pharm Res 15:417-422.
10. Gertz BJ, Holland SD, Kline WF, Matuszewski BK, Freeman A, Quan H, Lasseter KC, Mucklow JC, Porras AG. 1995. Studies of the oral bioavailability of alendronate. Clin Pharmacol Ther 58:288-298.
11. Laitinen K, Patronen A, Harju P, Loyttyniemi E, Pylkkanen L, Kleimola T, Perttunen K. 2000. Timing of food intake has a marked effect on the bioavailability of clodronate. Bone 27:293-296.
12. Ogura Y, Gonsho A, Cyong JC, Orimo H. 2004. Clinical trial of risedronate in Japanese volunteers: A study on the effect of timing of dosing on absorption. J Bone Miner Metab 22:120-126.
13. Shyu WC, Knupp CA, Pittman KA, Dunkle L, Barbhaiya RH. 1991. Food-induced reduction in bioavailability of didanosine. Clin Pharmacol Ther 50:503-507.
14. Yeh KC, Deutsch PJ, Haddix H, Hesnay M, Hoagland V, Ju WD, Justice SJ, Osborne B, Sterrett AT, Stone JA, Woolf E, Waldman S. 1998. Single-dose pharmacokinetics of indinavir and the effect of food. Antimicrob Agents Chemother 42:332-338.
15. Schuna A, Osman MA, Patel RB, Welling PG, Sundstorm WR. 1983. Influence of food on the bioavailability of penicillamine. J Rheumatol 10:95-97.
16. Neuvonen PJ, Kivisto KT, Lehto P. 1991. Interference of dairy products with the absorption of ciprofloxacin. Clin Pharmacol Ther 50:498-502.
17. Charman WN, Porter CJ, Mithani S, Dressman JB. 1997. Physiochemical and physiological mechanisms for the effects of food on drug absorption: The role of lipids and pH. J Pharm Sci 86:269-282.
18. Fujii Y, Takahashi M, Morita H, Kikuchi H, Aramaki H, Amidon GL. 2007. Characteristics of gastrointestinal absorption of DX-9065a, a new synthetic anticoagulant. Drug Metab Pharmacokinet 22:26-32.
19. Tanno FK, Sakuma S, Masaoka Y, Kataoka M, Kozaki T, Kamaguchi R, Ikeda Y, Kokubo H, Yamashita S. 2007. Site-specific drug delivery to the middle region of the small intestine by application of enteric coating with hypromellose acetate succinate (HPMCAS). J Pharm Sci (in press).
20. Nagai T, Obara S, Kokubo H, Hoshi N. 1997. Application of HPMC and HPMCAS to aqueous film coating of pharmaceutical dosage forms. In: McGinity JW, editor. Aqueous polymeric coatings for pharmaceutical dosage forms, 2nd edition. New York: Marcel Dekker. pp 177-225.
21. Ashford M. 2002. Biopharmaceutical principles of drug delivery. In: Aulton ME, editor. Pharmaceutics, 2nd edition. Edinbrugh: Churchill Livingstone. pp 211-305.
22. Evans DF, Pye G, Bramley R, Clark AG, Dyson TJ, Hardcastle JD. 1988. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut 29:1035-1041.
23. Monographs NF. 2007. National Formulary 25, Vol. 1. Rockville, MD: The United States Pharmacopoeia Convention. pp 1136-1138.
24. Physical Test. 2006. Disintegration. U.S. Pharmacopeia/National Formulary, 29/24. MD: The United States Pharmacopeia Convention. pp 2411-2412.
25. Physical Test. 2006. Drug release. U.S. Pharmacopoeia/National Formulary, 29/24. MD: The United States Pharmacopoeia Convention. pp 2417-2418.
26. Cao QR, Choi HG, Kim DC, Lee BJ. 2004. Release behavior and photo-image of nifedipine tablet coated with high viscosity grade hydroxypropylmethylcellulose: Effect of coating conditions. Int J Pharm 274:107-117.
27. Lehmann KOR. 1997. Chemistry and application properties of polymethacrylate coating systems. In: McGinity JW, editor. Aqueous polymeric coatings for pharmaceutical dosage forms, 2nd edition. New York: Marcel Dekker. pp 101-176.
28. Wu SHW, Wyatt DM, Adams MW. 1997. Chemistry and applications of cellulosic polymers for enteric coatings of solid dosage forms. In: McGinity JW, editor. Aqueous polymeric coatings for pharmaceutical dosage forms, 2nd edition. New York: Marcel Dekker. pp 385-418.
29. Davies B, Morris T. 1993. Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095.
30. Kararli TT. 1995. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos 16:351-380.
31. DeSesso JM, Jacobson CF. 2001. Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol 39:209-228.
32. Sutton SC. 2004. Companion animal physiology and dosage form performance. Adv Drug Deliv Rev 56:1383-1398.
33. Ward FW, Coates ME. 1987. Gastrointestinal pH measurement in rats: Influence of the microbial flora, diet and fasting. Lab Anim 21:216-222.
34. Ritschel WA. 1987. in vivo animal models for bioavailability assessment. STP Pharma Sci 3:125-141.
35. Yamada K, Furuya A, Akimoto M, Maki T, Suwa T, Ogata H. 1995. Evaluation of gastrointestinal transit controlled-beagle dog as a suitable animal model for bioavailability testing of sustained-release acetaminophen dosage form. Int J Pharm 119:1-10.
36. Chiou WL, Jeong HY, Chung SM, Wu TC. 2000. Evaluation of using dog as an animal model to study the fraction of oral dose absorbed of 43 drugs in humans. Pharm Res 17:135-140.
37. Dressman JB. 1986. Comparison of canine and human gastrointestinal physiology. Pharm Res 3:123-131.
38. Hossain M, Abramowitz W, Watrous BJ, Szpunar GJ, Ayres JW. 1990. Gastrointestinal transit of nondisintegrating, nonerodible oral dosage forms in pigs. Pharm Res 7:1163-1166.
39. Lentz KA, Quitko M, Morgan DG, Grace JE, Jr., Gleason C, Marathe PH. 2007. Development and validation of a preclinical food effect model. J Pharm Sci 96:459-472.
40. Li C, Fleisher D, Li L, Schwier JR, Sweetana SA, Vasudevan V, Zornes LL, Pao LH, Zhou SY, Stratford RE. 2001. Regional-dependent intestinal absorption and meal composition effects on systemic availability of LY303366, a lipopeptide antifungal agent, in dogs. J Pharm Sci 90:47-57.
41. Damle BD, Yan JH, Behr D, O'Mara E, Nichola P, Kaul S, Knupp C. 2002. Effect of food on the oral bioavailability of didanosine from encapsulated enteric-coated beads. J Clin Pharmacol 42:419-427.
42. López JC, Moreno S, Jiménez-Oñate Clotet FB, Rubio R, Hernández-Quero J. 2006. A cohort study of the food effect on virological failure and treatment discontinuation in patients on HAART containing didanosine enteric-coated capsules (FOODDle Study). HIV Clin Trials 7:155-162.
43. Lipinski CA, Lombardo F, Dominy BW, Feeney P. 2001. Experimental and computational approaches to estimate solubility and permeability in drug delivery and development setting. Adv Drug Deliv Rev 46:3-26.
44. Sakuma S, Matsumoto T, Yamashita S, Wang Y, Lu ZR. 2007. Conjugation of poorly absorptive drugs with mucoadhesive polymers for the improvement of oral absorption of drugs. J Control Release 123:195-202.
45. Davis SS, Hardy JG, Fara JW. 1986. Transit of pharmaceutical dosage forms through the small intestine. Gut 27:886-892.