Biowaiver monograph for immediate-release solid oral dosage forms: Acetylsalicylic acid

Journal of Pharmaceutical Sciences

Volumn 101, Issue 8, 2012, Pages 2653-2667

  Dressman, Jennifer B ^a   Nair, Anita ^a   Abrahamsson, Bertil ^b   Barends, Dirk M ^c   Groot, D W ^c   Kopp, Sabine ^d   Langguth, Peter ^e   Polli, James E ^f   Shah, Vinod P ^g   Zimmer, Markus ^h  

^a GOETHE UNIVERSITY   (Germany)

^b ASTRAZENECA R AND D   (Sweden)

^c NATIONAL INSTITUTE FOR PUBLIC HEALTH AND THE ENVIRONMENT   (Netherlands)

^d WORLD HEALTH ORGANIZATION   (Switzerland)

^e JOHANNES GUTENBERG UNIVERSITY   (Germany)

^f UNIVERSITY OF MARYLAND SCHOOL OF PHARMACY   (United States)

^g International Pharmaceutical Federation   (Netherlands)

^h YES Pharmaceutical Development Services GmbH   (Germany)

Author keywords

Absorption; Acetylsalicylic acid (ASA); Bioavailability; Bioequivalence; Biopharmaceutics Classification System; Permeability; Solubility; Stability

Indexed keywords

ACETYLSALICYLIC ACID; ACETYLSALICYLIC ACID CALCIUM; ALUMINUM GLYCINATE; ASCORBIC ACID; ASPIMAX; ASPIRINE RICHARD; ASS GAMMA; ASS RATIOPHARM; ASS STADA; ASTRIX 100; CALCIUM CARBONATE; CALCIUM PHOSPHATE DIBASIC; CARDIPRIN 100; CARTIA; CELLULOSE; CITRIC ACID; COTTON SEED OIL; CROSCARMELLOSE SODIUM; DISPERIN; EQUALIN ASPIRIN; EQUATE ASPIRIN; ETHYL CELLULOSE; EXCIPIENT; GELATIN; GLUCONATE CALCIUM; GLYCEROL PALMITOSTEARATE; GLYCINE; GUM ARABIC; HYDROXYPROPYLMETHYLCELLULOSE; LACTOSE; MACROGOL; MAGNECYL; MAGNESIUM HYDROXIDE; MAGNESIUM OXIDE; MAGNESIUM STEARATE; MANNITOL; MICROCRYSTALLINE CELLULOSE; PLATELIN; POLYVINYL ALCOHOL; POVIDONE; PROPYLENE GLYCOL; SALOSPIR; SHELLAC; SILICON DIOXIDE; TOGAL; TROMBYL; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ABDOMINAL PAIN; AMINOTRANSFERASE BLOOD LEVEL; ARTICLE; ASTHMA; BIOEQUIVALENCE; BLEEDING; CONTROLLED DRUG RELEASE; DISTRIBUTION VOLUME; DIZZINESS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSAGE FORM; DRUG ELIMINATION; DRUG EXCRETION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG PENETRATION; DRUG SOLUBILITY; DRUG STABILITY; DYSPEPSIA; EDEMA; ENTERIC COATED TABLET; EPISTAXIS; EUROPE; GASTROINTESTINAL MOTILITY; GASTROINTESTINAL SYMPTOM; HEMATOMA; HUMAN; HUMAN CELL; INTESTINE MUCOSA PERMEABILITY; NONHUMAN; PARTITION COEFFICIENT; RASH; RECOMMENDED DRUG DOSE; REYE SYNDROME; SIDE EFFECT; TINNITUS;

EID: 84862872852     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23212     Document Type: Note

References (42)

1. World Health Organization (WHO). Proposal to waive in vivo bioequivalence requirements for WHO model list of essential medicines immediate-release, solid oral dosage forms. Accessed August 10, 2010, 2006, at:
2. European Medical Agency. Committee for medicinal products for human use: Guideline on the Investigation of Bioequivalence. Accessed February 1, 2010, at:
3. US Department of Health and Human Services:Food and Drug Administration. Guidance for industry: Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biopharmaceutics Classification System. Accessed December 20, 2010, at:
4. Kees F, Jehnich D, Grobecker H. 1996. Simultaneous determination of acetylsalicylic acid and salicylic acid in human plasma by high-performance liquid chromatography. J Chromatogr B Biomed Appl 677(1):172-177.
5. th edt., London: Pharmaceutical Press. UK.
6. Lüllmann H, Mohr K, Hein L. 2006. Pharmakologie und toxicologie. 16th ed. Thieme, Sttutgart, Germany; pp 290-292.
7. Bayer Healthcare-Consumer Care. 2008. Acetylsalicylic acid for pain and fever. Company Core Data Sheet.
8. Drugbank. Acetylsalicylic acid. Accessed August 9, 2010, at:
9. Hohlfeld T, Kojda G. 2002. Kopfschmerz zur Resistenz. Bekanntes und Neues zu Aspirin. Accessed August 9, 2010, at:
10. Potthast H, Haufte S, Glaab V. 2003. Pharmazeutische Zeitung: Acetylsalicylsäure-Präparate im Vergleich. Accessed August 9, 2010, at:
11. Tawashi R. 1968. Aspirin: Dissolution rates of two polymorphic forms. Science 160(823):76.
12. Summers MP, Carless JE, Enever RP. 1970. The polymorphism of aspirin. J Pharm Pharmacol 22(8):615-616.
13. Watanabe A, Yamaoka Y, Takada K. 1982. Crystal habits and dissolution behavior of aspirin. Chem Pharma Bull 30(8):2958-2963.
14. Kasim NA, Whitehouse M, Ramachandran C, Bermejo M, Lennernas 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(1):85-96.
15. Connors K. 1986. Chemical stability of pharmaceuticals. 2nd ed. Wiley Interscience, New York, U S A.
16. European Pharmacopoeia. 2010. Acetylsalicylic Acid. 7th ed, pp 1317-1318.
17. United States Pharmacopoeia. The National Formulary, (USP33/NF28) ed, Rockville: Maryland, The United States Pharmacopoeial Inc., 2010.
18. ABDA Pharma-Daten-Service. 2002. Pharmazeutische Stoffliste: Acetylsalicylsäure. 13. Auflage ed.
19. Sigma-Aldrich. 2010 Acetylsalicylic Acid A5376. Accessed August 2, 2010, at:
20. World Health Organization. 2010. WHO Model List of Essential Medicines. Accessed 16 August 10, 2010, at:
21. Rote L. 2010 Aspirin Tabletten. Accessed August 10, 2010, at:
22. Benet LZ, Amidon GL, Barends DM, Lennernas H, Polli JE, Shah VP, Stavchansky SA, Yu LX 2008. The use of BDDCS in classifying the permeability of marketed drugs. Pharm Res 25(3):483-488.
23. Castillo-Garit JA Marrero-Ponce Y, Torrens F, Garcia-Domenech R. 2007. Estimation of ADME properties in drug discovery: Predicting Caco-2 cell permeability using atom-based stochastic and non-stochastic linear indices. 11th International Electronic Conference on Synthetic Organic Chemistry- ECSOC.
24. Artursson P, Karlsson J. 1991. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun 175(3):880-885.
25. Yee S. 1997. in vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man-Fact or myth. Pharm Res 14(6):763-766.
26. Insel PA. 1990. Analgesic-Antipyretics and Antiinflammatory agents;Drugs employed in treatment of Rhematoid Arthritis and Gout, In Goodman and Gilman'sThe Pharmacological basis of therapeutics; Gilman AG, Rall Tw, Nies AS, Taylor P, Eds. 8th ed. Elmsford, New York: Pergamon Press.
27. Rowland M, Riegelman S, Harris PA, Sholkoff SD. 1972. Absorption kinetics of aspirin in man following oral administration of an aqueous solution. J Pharm Sci 61(3):379-385.
28. Bergström C, Dressman J, Artursson P. 2011. Permeability determination of six essential medicines. FIP International Symposium on BA/BE of Oral Drug Products. Tokyo, Japan.
29. Bogentoft C, Carlsson I, Ekenved G, Magnusson A. 1978. Influence of food on the absorption of acetylsalicylic acid from enteric-coated dosage forms. Eur J Clin Pharmacol 14(5):351-355.
30. Hutt AJ, Caldwell J, Smith RL. 1982. The metabolism of [carboxyl-14C]aspirin in man. Xenobiotica 12(10):601-610.
31. Needs CJ, Brooks PM. 1985. Clinical pharmacokinetics of the salicylates. Clin Pharmacokinet 10(2):164-177.
32. Hutt AJ, Caldwell J, Smith RL. 1986. The metabolism of aspirin in man: A population study. Xenobiotica 16(3):239-249.
33. Ritschel W. 1992. Handbook of Basic Pharmacokinetics, 4th ed. Drug Intelligence Publications, Bethesda, U S A, pp 530-535.
34. Cooke AR, Hunt JN. 1970. Absorption of acetylsalicylic acid from unbuffered and buffered gastric contents. Am J Dig Dis 15(2):95-102.
35. George CF. 1981. Drug metabolism by the gastrointestinal mucosa. Clin Pharmacokinet 6(4):259-274.
36. Medscape AHFS. 2009 Monograph: Enteric coated aspirin oral. Accessed August 5, 2010, at:
37. Dubovska D, Piotrovskij VK, Gajdos M, Krivosikova Z, Spustova V, Trnovec T. 1995. Pharmacokinetics of acetylsalicylic acid and its metabolites at low doses: a compartmental modeling. Methods Find Exp Clin Pharmacol 17(1):67-77.
38. Levy G. 1961. Comparison of dissolution and absorption rates of different commercial aspirin tablets. J Pharm Sci 50:388-392.
39. Bochner F, Somogyi AA, Wilson KM. 1991. Bioinequivalence of four 100 mg oral aspirin formulations in healthy volunteers. Clin Pharmacokinet 21(5):394-399.
40. Brantmark B, Wahlin-Boll E, Melander A. 1982. Bioavailability of acetylsalicylic acid and salicylic acid from rapid-and slow-release formulations, and in combination with dipyridamol. Eur J Clin Pharmacol 22(4):309-314.
41. Ozturk SS, Palsson BO, Dressman JB. 1988. Dissolution of ionizable drugs in buffered and unbuffered solutions. Pharm Res 5(5):272-282.
42. Vertzoni M, Dressman J, Butler J, Hempenstall J, Reppas C. 2005. Simulation of fasting gastric conditions and its importance for the in vivo dissolution of lipophilic compounds. Eur J Pharm Biopharm 60(3):413-417.