Correlation between in vitro dissolution profiles from enteric-coated dosage forms and in vivo absorption in rats for high-solubility and high-permeability model drugs

Journal of Pharmaceutical Sciences

Volumn 98, Issue 11, 2009, Pages 4141-4152

  Sakuma, Shinji ^a   Ogura, Ryoko ^a   Masaoka, Yoshie ^a   Kataoka, Makoto ^a   Tanno, Fumié K ^b   Kokubo, Hiroyasu ^b   Yamashita, Shinji ^a  

^a SETSUNAN UNIVERSITY   (Japan)

^b SHIN ETSU CHEMICAL CO LTD   (Japan)

Author keywords

Enteric coated dosage form; Hypromellose acetate succinate; In vitro dissolution; In vitro in vivo correlation; In vivo absorption; IVIVC

Indexed keywords

PARACETAMOL; PHENAZONE; THEOPHYLLINE;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; ENTERIC COATED TABLET; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; INTESTINE FLUID; MALE; NONHUMAN; RAT;

EID: 70349643570     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.21716     Document Type: Article

References (32)

1. 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.
2. 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.
3. 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.
4. Ashford M. 2002. Biopharmaceutical principles of drug delivery. In: Aulton ME, editor. Pharmaceutics. 2nd edition. Edinburgh: Churchill Livingstone. pp 211-305.
5. 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. (Pubitemid 18199674)
6. Tanno FK, Sakuma S, Masaoka Y, Kataoka M, Kozaki T, Kamaguchi R, Ikeda Y, Kokubo H, Yamashita S. 2008. 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 97:2665-2679.
7. Tanno FK, Sakuma S, Masaoka Y, Kataoka M, Kozaki T, Kamaguchi R, Ikeda Y, Kokubo H, Yamashita S. 2008. 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. J Pharm Sci 97:5341-5353.
8. Physical Test. 2006. Drug release. U.S. Pharmacopeia/National Formulary, 29/24. MD: The United States Pharmacopeial Convention. pp 2417-2418.
9. Amidon GL, Lennernäs 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 12:413-420.
10. Löbenberg R, Amidon GL. 2000. Modern bioavailability, bioequivalence biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur J Pharm Biopharm 50:3-12. (Pubitemid 30326685)
11. Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernäs H, Hussain AS, Junginger HE, Stavchansky SA, Midha KK, Shah VP, Amidon GL. 2004. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol Pharm 1:85-96.
12. Polli JE, Yu LX, Cook JA, Amidon GL, Borchardt RT, Burnside BA, Burton PS, Chen ML, Conner DP, Faustino PJ, Hawi AA, Hussain AS, Joshi HN, Kwei G, Lee VH, Lesko LJ, Lipper RA, Loper AE, Nerurkar SG, Polli JW, Sanvordeker DR, Taneja R, Uppoor RS, Vattikonda CS, Wilding I, Zhang G. 2004. Summary workshop report: biopharmaceutics classification system - implementation challenges and extension opportunities. J Pharm Sci 93:1375-1381. (Pubitemid 38725012)
13. Vogelpoel H, Welink J, Amidon GL, Junginger HE, Midha KK, Möller H, Olling M, Shah VP, Barends DM. 2004. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: verapamil hydrochloride, propranolol hydrochloride, and atenolol. J Pharm Sci 93:1945-1956. (Pubitemid 39045477)
14. Takagi T, Ramachandran C, Bermejo M, Yamashita S, Yu LX, Amidon GL. 2006. A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol Pharm 3:631-643. (Pubitemid 46087480)
15. Kalantzi L, Reppas C, Dressman JB, Amidon GL, Junginger HE, Midha KK, Shah VP, Stavchansky SA, Barends DM. 2006. Biowaiver monographs for immediate release solid oral dosage forms: acetaminophen (paracetamol). J Pharm Sci 95:4-14.
16. Becker C, Dressman JB, Amidon GL, Junginger HE, Kopp S, Midha KK, Shah VP, Stavchansky SA, Barends DM. 2008. Biowaiver monographs for immediate release solid oral dosage forms: ethambutol dihydrochloride. J Pharm Sci 97:1350-1360.
17. Sankalia JM, Sankalia MG, Mashru RC. 2008. Drug release and swelling kinetics of directly compressed glipizide sustained-release matrices: establishment of level A IVIVC. J Control Release 129:49-58.
18. Mandal U, Ray KK, Gowda V, Ghosh A, Pal TK. 2007. In-vitro and in-vivo correlation for two gliclazide extended-release tablets. J Pharm Pharmcol 59:971-976. (Pubitemid 47051078)
19. Hu LD, Liu Y, Tang X, Zhang Q. 2006. Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets. Eur J Pharm Biopharm 64:185-192. (Pubitemid 44291990)
20. Dutta S, Qiu Y, Samara E, Cao G, Granneman GR. 2005. Once-a-day extended-release dosage form of divalproex sodium III: development and validation of a Level A in vitro-in vivo correlation (IVIVC). J Pharm Sci 94:1949-1956. (Pubitemid 41551479)
21. Royce A, Li S, Weaver M, Shah U. 2004. In vivo and in vitro evaluation of three controlled release principles of 6-N-cyclohexyl-20-O-methyladenosine. J Control Release 97:79-90.
22. Korhonen O, Kanerva H, Vidgren M, Urtti A, Ketolainen J. 2004. Evaluation of novel starch acetate-diltiazem controlled release tablets in healthy human volunteers. J Control Release 95:515-520. (Pubitemid 38340501)
23. Dalton JT, Straughn AB, Dickason DA, Grandolfi GP. 2001. Predictive ability of level A in vitro-in vivo correlation for ringcap controlled-release acetaminophen tablets. Pharm Res 18:1729-1734.
24. Sorasuchart W, Ayres JW. 2001. Preliminary bioequivalence testing of two nicardipine HCl sustained-release formulations with in vitro/in vivo correlations. Eur J Drug Metab Pharmacokinet 26:1-7. (Pubitemid 32802388)
25. Dressman JB, Amidon GL. 1984. Radiotelemetric methods for evaluating enteric coatings in vivo. J Pharm Sci 73:935-938.
26. Ebel JP, Jay M, Beihn RM. 1993. An in vitro/in vivo correlation for the disintegration and onset of drug release from enteric-coated pellets. Pharm Res 10:233-238. (Pubitemid 23041737)
27. Hayashi T, Ogura T, Takagishi Y. 1995. New evaluation method for in vitro/in vivo correlation of enteric-coated multiple unit dosage forms. Pharm Res 12:1333-1337.
28. Monographs NF. 2007. National Formulary 25, Vol.1. Rockville: The United States Pharmacopeial Convention. pp 1136-1138.
29. Physical Test. 2006. Disintegration. U.S. Pharmacopeia/ National Formulary, 29/24. MD: The United States Pharmacopeial Convention. pp 2411-2412.
30. Lipinski CA, Lombardo F, Dominy BW, Feeney P. 2001. Experimental and computational approaches to estimate solubility and permeability in drug delivery and development setting. AdvDrugDeliv Rev 46:3-26. (Pubitemid 33653411)
31. 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. (Pubitemid 350007820)
32. DeSesso JM, Jacobson CF. 2001. Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol 39:209-228.