Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen (Paracetamol)

Journal of Pharmaceutical Sciences

Volumn 95, Issue 1, 2006, Pages 4-14

  Kalantzi, L ^a   Reppas, C ^a   Dressman, J B ^b   Amidon, G L ^c   Junginger, H E ^d   Midha, K K ^e   Shah, V P ^f   Stavchansky, S A ^g   Barends, Dirk M ^h  

^a NATIONAL AND KAPODISTRIAN UNIVERSITY OF ATHENS   (Greece)

^b GOETHE UNIVERSITY   (Germany)

^c UNIVERSITY OF MICHIGAN   (United States)

^d LEIDEN UNIVERSITY   (Netherlands)

^e UNIVERSITY OF SASKATCHEWAN   (Canada)

^f CENTER FOR DRUG EVALUATION AND RESEARCH   (United States)

^g UNIVERSITY OF TEXAS AT AUSTIN   (United States)

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

Author keywords

Absorption; Acetaminophen; Biopharmaceutics Classification System (BCS); Paracetamol; Permeability; Solubility

Indexed keywords

ACETYLCYSTEINE; APOTEL UNI PHARMA; BICARBONATE; CAPTIN; CARNAUBA WAX; CELLULOSE; CROSCARMELLOSE SODIUM; CROSPOVIDONE; CYCLAMATE SODIUM; CYSTEINE; DEMOCYL; DODECYL SULFATE SODIUM; ETHYL PARABEN; EXCIPIENT; FENSUM; GELATIN; GLYCEROL PALMITOSTEARATE; HYDROXYPROPYLCELLULOSE; HYDROXYPROPYLMETHYLCELLULOSE; KINDERPARACETAMOL CF; LACTOSE; MACROGOL; MAGNESIUM STEARATE; MOMENTUM; MONO PRAECIMED; PAEDIALGON; PANADOL GLADDE; PANADOL ZAPP; PARA TABS; PARACEON; PARACETAMOL; PARACETAMOL 500 1 A PHARMA; PARACETAMOL 500 HEXAL; PARACETAMOL ALPHARMA; PARACETAMOL BETA; PARACETAMOL FLX; PARACETAMOL PAMOL; PARACETAMOL RATIOPHARM; PARACETAMOL SANDOZ; PARACETAMOL STADA; PARACETAMOL TABLETTEN LICHTENSTEIN; PARAMAX RAP; POTATO STARCH; POVIDONE; PROPYLENE GLYCOL; SILICON DIOXIDE; SORBATE POTASSIUM; STARCH; STARCH GLYCOLATE SODIUM; STEARIC ACID; TALC; TRIACETIN; UNCLASSIFIED DRUG; WAX; ANALGESIC AGENT;

ANALGESIC ACTIVITY; ANTIINFLAMMATORY ACTIVITY; ANTIPYRETIC ACTIVITY; AREA UNDER THE CURVE; BIOEQUIVALENCE; BIOWAIVER; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLASSIFICATION; DRUG CLEARANCE; DRUG DIFFUSION; DRUG DISTRIBUTION; DRUG GLUCURONIDATION; DRUG GRANULE; DRUG INDICATION; DRUG MARKETING; DRUG PROTEIN BINDING; DRUG RELEASE; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SULFATION; EFFERVESCENT TABLET; HUMAN; PARTITION COEFFICIENT; PERMEABILITY; PKA; REVIEW; SOLID; STOMACH EMPTYING; SYRUP; ARTICLE; BIOAVAILABILITY; CHEMISTRY; DRUG DOSAGE FORM; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; SOLUBILITY;

ACETAMINOPHEN; ADMINISTRATION, ORAL; ANALGESICS, NON-NARCOTIC; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DOSAGE FORMS; EXCIPIENTS; SOLUBILITY; THERAPEUTIC EQUIVALENCY;

EID: 33645215141     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.20477     Document Type: Note

References (94)

1. 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.
2. Verbeeck RK, Junginger HE, Midha KK, Shah VP, Barends DM. 2005. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: Chloroquine phosphate, chloroquine sulfate and chloroquine hydrochloride. J Pharm Sci 94:1389-1395.
3. Kortejärvi H, Yliperttula M, Dressman JB, Junginger HE, Midha KK, Shah VP, Barends DM. 2005. Biowaiver monographs for immediate release solid oral dosage forms: Ranitidine hydrochloride. J Pharm Sci 94:1617-1625.
4. Sweetman S, editor. 2004. Martindale: The complete drug reference. Electronic version. London UK: Pharmaceutical Press; Greenwood Village, Colorado: Thomson MICROMEDEX.
5. Prescott LF. 2000. Paracetamol: Past, present, and future. Am J Ther Mar 7:143-147.
6. Hardman JG, Limbird LE, editors. 2001. Goodman & Gilman's The Pharmacological Basis of Therapeutics, 10th edn. New York: McGraw-Hill.
7. Burger A. 1982. Zur Interpretation von Polymorphie-Untersuchungen. Acta Pharm Technol 28:1-20.
8. Di Martino P, Confiant P, Drache M, Huvenne JP, Guyot-Hermann AM. 1997. Preparation and physical characterization of forms II and III of paracetamol. J Therm Anal 48:447-458.
9. Beyer T, Graeme MD, Price SL. 2001. The prediction, morphology, and mechanichal properties of the polymorphs of paracetamol. J Am Chem Soc 123:5086-5094.
10. Rossi A, Savioli A, Bini M, Capsoni D, Massarotti V, Bettini R, Gazzaniga A, Sangalli ME, Giordano F. 2003. Solid state characterization of paracetamol metastable polymorphs formed in binary mixtures with hydroxypropylmethylcellulose. Therm Acta 406:55-67.
11. Peterson ML, Morissette SL, McNulty C, Coldsweig A, Shaw P, LeQuesne M, Monagle J, Encina N, Marchionna J, Johnson A, Gonzalez-Zugasti J, Lemmo AV, Ellis SJ, Cima MJ, Almarsson O. 2002. Iterative high-throughput polymorphism studies on acetaminophen and an experimentally derived structure for form III. J Am Chem Soc 124:10958-10959.
12. Szelagiewicz M, Marcolli C, Cianferani S, Hard AP, Vit A, Burkhard A, Von Raumer M, Hofmeier UC, Zilian A, Francotte E, Schenker R. 1999. In situ characterization of polymorphic forms. The potential of Raman techniques. J Therm Anal Cal 57:23-43.
13. Sohn YT. 1990. Study on the polymorphism of acetaminophen (abstract). J Kor Pharm Sci 20:97-104.
14. Nichols G, Frampton CS. 1998. Physicochemical characterization of the orthorhombic polymorph of paracetamol crystallized from solution. J Pharm Sci 87:684-693.
15. El Obeid HA, Al-Badr AA. 1985. Acetaminophen. In: Florey K, editor. Analytical profiles of drug substances, Vol 14. London: Academic Press, Inc. pp 551-596.
16. Reynolds JEF, editor. 1993. Martindale: The extra pharmacopeia, 30th edn. London: The Pharmaceutical Press.
17. Etman MA, Naggar VF. 1990. Thermodynamics of paracetamol solubility in sugar-water cosolvent systems. Int J Pharm 58:177-184.
18. Garekani HA, Sadeghi F, Ghazi A. 2003. Increasing the aqueous solubility of acetaminophen in the presence of polyvinylpyrrolidone and investigation of the mechanisms involved. Drug Dev Ind Pharm 29:173-179.
19. Poelma FGJ, Breäs R, Tukker JJ, Crommelin DJA. 1991. Intestinal absorption of drugs. The influence, of mixed micelles on the disappearance kinetics of drugs from the small intestine of the rats. J Pharm Pharmacol 43:317-324.
20. Hansch C, Leo A, Hoekman D. 1995. Exploring QSAR, hydrophobic, electronic and steric constants. ACS Publications, American Chemical Society.
21. 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.
22. Vozeh S, Schmidlin O, Taeschner W. 1988. Pharmacokinetic drug data. Clin Pharmacokinet 15:254-282.
23. WHO. 2003. WHO Model List of Essential Medicines, 13th edition. URL: www.who.int/medicines/organization/par/edl/expcom13/eml13_en.doc.
24. Bannwarth B, Pehourcq F. 2003. Pharmacologic basis for using paracetamol: Pharmacokinetic and pharmacodynamic issues (abstract). Drugs 63:5-13.
25. Rote Liste Service GmbH FMG. 2005. Arzneimittelverzeichnis fur Deutschland. In Vergal EG, Aulendorf, Germany, www.rote-liste.de/online.
26. Finnish National Agency for Medicines. 2005. www.nam.nl.
27. Dutch Medicines Evaluation Board. 2005. www. cbg-med.nl.
28. Greek National Formulatory. 2003. Ethniko Syntagologio ISBN 960-86876-2-4. Athens: National Drug Organisation.
29. Eandi M, Viano I, Ricci Camalero S. 1984. Absolute bioavailability of paracetamol after oral and rectal administration in healthy volunteers. Drug Res 34:903-907.
30. Ameer B, Divoll M, Abernethy DR, Greenblatt DJ, Shargel L. 1983. Absolute and relative bioavailability of oral acetaminophen preparations. J Pharm Sci 72:955-958.
31. Clements JA, Critchley JA, Prescott LF. 1984. The role of sulfate conjugation in the metabolism and disposition of oral and intravenous paracetamol in man. Br J Clin Pharmacol 18:481-485.
32. Perucca E, Richens A. 1979. Paracetamol disposition in normal subjects and in patients treated with antiepileptic drugs. Br J Clin Pharmacol 7:201-206.
33. Prescott LF. 1980. Kinetics and metabolism of paracetamol and phenacetin. Br J Clin Pharmacol 10:2918-2988.
34. Tukker JJ, Sitsen JM, Gusdorf CF. 1986. Bioavailability of paracetamol after oral administration to healthy volunteers. Influence of caffeine on rate and extent of absorption (abstract). Pharm Weekbl Sci 8:239-243.
35. Zapater P, Lasso De La Vega MC, Horga JF, Such J, Frances R, Esteban A, Palazon JM, Carnicer F, Pascual S, Perez-Mateo M. 2004. Pharmacokinetic variations of acetaminophen according to liver dysfunction and portal hypertension status. Aliment Pharmacol Ther 20:29-36.
36. 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.
37. Grattan T, Hickman R, Darby-Dowman A, Hayward M, Boyce M, Warrington S. 2000. A five way crossover human volunteer study to compare the pharmacokinetics of paracetamol following oral administration of two commercially available paracetamol tablets and three development tablets containing paracetamol in combination with sodium bicarbonate or calcium carbonate. Eur J Pharm Biopharm 49:225-229.
38. Clements JA, Heading RC, Nimmo WS, Prescott LF. 1978. Kinetics of acetaminophen absorption and gastric emptying in man. Clin Pharmacol Therap 24:420-431.
39. Prescott LF, Speirs GC, Critchley JA, Temple RM, Winney RJ. 1989. Paracetamol disposition and metabolite kinetics in patients with chronic renal failure. Eur J Clin Pharmacol 36:291-297.
40. Torrado G, Carrascosa C, Torrado-Santiago S. 2001. Correlation of in vitro and in vivo acetaminophen availability from albumin microaggregates oral modified release formulations. Int J Pharm 217:193-199.
41. American Hospital Formulary Service. 1994. Drug information. Bethesda: American Society of Hospital Pharmacists. 1328p.
42. Rayburn W, Shukla U, Stetson P, Piehl E. 1986. Acetaminophen pharmacokinetics: Comparison between pregnant and nonpregnant women (abstract). Am J Obstet Gynecol 155:1353-1356.
43. Borin MT, Ayres JW. 1989. Single dose bioavailaility of paracetamol following oral administration. Int J Pharm 54:199-209.
44. Rostami-Hodjegan A, Shiran MR, Ayesh R, Grattan TJ, Burnett I, Darby-Dowman A, Tucker GT. 2002. A new rapidly absorbed paracetamol tablet containing sodium bicarbonate. I. A four way crossover study to compare the concentration-time profile of paracetamol from the new paracetamol/sodium bicarbonate tablet and a conventional paracetamol tablet in fed and fasted volunteers. Drug Dev Ind Pharm 28:523-531.
45. Stillings M, Havlik I, Chetty M, Clinton C, Schall R, Moodley I, Muir N, Little S. 2000. Comparison of the pharmacokinetic profiles of soluble aspirin and solid paracetamol tablets in fed and fasted volunteers (abstract). Curr Med Res Opin 16:115-124.
46. Willems M, Quartero AO, Numans ME. 2001. How useful is paracetamol absorption as a marker of gastric emptying? Dig Dis Sci 46:2256-2262.
47. Stewart BH, Chan OH, Lu RH, Reyner EL, Schmid HL, Hamilton HW, Steinbaugh BA, Taylor MD. 1995. Comparison of intestinal permeabilities determined in multiple in vitro and in situ models: Relationship to absorption in humans. Pharm Res 12:693-699.
48. Lu HH, Thomas JD, Tukker JJ, Fleisher D. 1992. Intestinal water and solute absorption studies: Comparison of in situ perfusion with chronic isolated loops in rats. Pharm Res 9:894-900.
49. Amidon GL, Sinko PJ, Fleisher D. 1988. Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier mediated compounds. Pharm Res 5:651-654.
50. Watanabe E, Takahashi M, Hayashi M. 2004. A possibility to predict the absorbability of poorly water-soluble drugs in humans based on rat intestinal permeability assessed by an in vitro chamber method. Eur J Pharm Biopharm 58:659-665.
51. Lennernäs H. 1998. Human intestinal permeability. J Pharm Sci 87:403-410.
52. Clements JA, Prescott LF. 1976. Data point weighting in pharmacokinetic analysis: Intravenous paracetamol in man. J Pharm Pharmacol 28:707-709.
53. Divoll M, Abernethy DR, Ameer B, Greenblatt DJ. 1982. Acetaminophen kinetics in the elderly. Clin Pharmacol Ther 31:151-156.
54. Rumack BH. 2004. Acetaminophen misconceptions. Hepatology 40:10-15.
55. Abernethy DR, Greenblatt DJ, Divoll M, Ameer B, Shader RI. 1982. Differential effect of cimetidine on drug oxidation (antipyrine and lorazepam): prevention of acetaminophen toxicity by cimetidine. Am J Pharm Exp Therapeut 224:508-513.
56. Forrest JA, Clements JA, Prescott LF. 1982. Clinical pharmacokinetics of paracetamol (abstract). Clin Pharmacokinet 7:93-107.
57. Morris ME, Levy G. 1984. Renal clearance and serum protein binding of acetaminophen and its major conjugates in humans (abstract). J Pharm Sci 73:1038-1041.
58. Drug Evaluation Monographs. 1996. Paracetamol, Vol. 88. Greenwood Village, CO: Micromedex, Inc.
59. Arana A, Morton NS, Hansen TG. 2001. Treatment with paracetamol in infants. Acta Anaesthesiol Scand 45:20-29.
60. Bailey DN, Briggs JR. 2004. The binding of acetaminophen, lidocaine and valproic acid to human milk. Am J Clin Pathol 121:754-757.
61. Prescott LF. 1996. The metabolism of paracetamol. In: Prescott LF, editor. Paracetamol (Acetaminophen). A critical bibliographic review. London: Taylor and Francis. pp 67-102.
62. Slattery IT, Wilson IM, Kalhorn TF, Nelson SD. 1987. Dose dependent pharmacokinetics of acetaminophen: Evidence of glutathione depletion in humans. Clin Pharmac Ther 41:413-418.
63. Heading RC, Nimmo J, Prescott LF, Tothill P. 1973. The dependence of paracetamol absorption on the rate of gastric emptying. Br J Pharmacol 47:415-421.
64. Steventon GB, Mitchell SC, Waring RH. 1996. Human metabolism of paracetamol (acetaminophen) at different dose levels (abstract). Drug Metabol Drug Interact 13:111-117.
65. Seymour RA, Rawlins MD. 1981. Pharmacokinetics of parenteral paracetamol and its analgesic effects in post-operative dental pain. Eur J Clin Pharmacol 20:215-218.
66. Cummings AJ, King ML, Martin BK. 1967. A kinetic study of drug elimination: The excretion of paracetamol and its metabolites in man. Br J Pharmacol 29:150-157.
67. Ishikawa T, Koizumi N, Mukai B, Utocuchi N, Fujii M, Matsumoto M, Endo H, Shirotake S, Watanabe Y. 2001. Pharmacokinetics of acetaminophen from rapidly disintegrating compressed tablet prepared using microcrystalline cellulose (PH-M-06) and spherical sugar granules. Chem Pharm Bull 49:230-232.
68. Kalantzi L, Polentarutti B, Albery T, Laitmer D, Abrahamsson B, Dressman JB, Reppas C. 2005. The delayed dissolution of paracetamol products in the fed canine stomach can be predicted in vitro but it does not affect the onset of plasma levels. Int J Pharm 296:87-93.
69. Sotiropoulus JB, Deutsch T, Plakogiannis FM. 1981. Comparative bioavailability of three commercial acetaminophen tablets. J Pharm Sci 70:422-425.
70. Hekimoglu S, Ayanoglu-Dulger G, Hincal AA. 1987. Comparative bioavailability of three commercial acetaminophen tablets. Int J Clin Pharmacol Ther Toxicol 25:93-96.
71. Walter-Sack IE, De Vries JX, Nickel B, Stenzhorn G, Weber B. 1989. The influence of different formula diets and different pharmaceutical formulations on the systemic availability of paracetamol, gallbladder size, and plasma glucose. Int J Clin Pharmacol Ther Toxicol 27:544-550.
72. Hekimoglu S, Sahin S, Sumnu M, Hincal AA. 1991. Comparative bioavailability of three batches of four commercial acetaminophen tablets (abstract). Eur J Drug Metab Pharmacokinet Spec 3:228-232.
73. Retaco P, Gonzalez M, Pizzorno MT, Volonte MG. 1996. Bioavailability study of paracetamol tablets in saliva and urine. Eur J Drug Met Pharmacokinet 21:295-300.
74. Dominguez AR, Medina RL, Hurtado MP. 2000. Bioequivalence study of paracetamol tablets: In vitro-in vivo correlation. Drug Dev Ind Pharm 26:821-828.
75. Babalola CP, Oladimeji FA, Femi-Oyewo MN. 2001. Correlation between in vitro and in vivo parameters of commercial paracetamol tablets (abstract). Afr J Med Med Sci 30:275-280.
76. Sevilla-Tirado FJ, Gonzalez-Vallejo EB, Leary AC, Breedt HJ, Hyde VJ, Fernandez-Hernando N. 2003. Bioavailability of two new formulations of paracetamol, compared with three marketed formulations, in healthy volunteers. Methods Find Exp Clin Pharmacol 25:531-535.
77. Kelly K, O'Mahony B, Lindsay B, Jones T, Grattan T, Rostami-Hodjegan A, Stevens HNE, Wilson CG. 2003. Comparison of the rates of disintegration, gastric emptying, and drug absorption following administration of a new and a conventional paracetamol formulation, using gamma-scintigraphy. Pharm Res 20:1668-1673.
78. Rygnestad T, Zahlsen K, Samdal FA. 2000. Absorption of effervescent paracetamol tablets relative to ordinary paracetamol tablets in healthy volunteers. Eur J Clin Pharmacol 56:141-143.
79. Gleiter GH, Klotz U, Kuhlmann J, Blume H, Stanislaus F, Harder S, Paulus H, Poethko-Müller C, Holz-Slomczyk M. 1998. When are bioavailability studies required? A German Proposal. J Clin Pharmacol 38:904-911.
80. The Dutch Medicines Evaluation board. 2005. www.cbg-med.nl/nl/reghoudr/ index.htm.
81. Bundesinstitut für Arzneimittel und Medizinprodukte. 2003. BundesAnzeiger, March 25:5296.
82. USP 26-NF 21. 2003. The United States Pharmacopeia-The National Formulatory. Rockville, MD: The United States Pharmacopeial Convention, Inc.
83. Rostami-Hodjegan A, Shiran MR, Tucker GT, Conway BR, Irwin WJ, Shaw LR, Grattan TJ. 2002. A new rapidly absorbed paracetamol tablet containing sodium bicarbonate. II Dissolution studies and in vitro/in vivo correlation. Drug Dev Ind Pharm 28:533-543.
84. Galia E, Nicolaides E, Hörter D, Löbenberg R, Reppas C, Dressman JB. 1998. Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs. Pharm Res 15:698-705.
85. Macheras P, Koupparis M, Tsaprounis C. 1986. Drug dissolution studies in milk using the automated flow injection serial dynamic dialysis technique. Int J Pharm 33:125-136.
86. U.S. Department of Health and Human Services FDA, Center for Drug Evaluation and Research (CDER). 2000. Guidance for industry: Waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a biopharmaceutics classification system. URL: www.fda.gov/cder/guidance/3618fnl.htm.
87. Committee for Proprietary Medicinal Products (CPMP). 2001. Note for guidance on the investigation of bioavailability and bioequivalence. URL: www.emea.eu.int/pdfs/human/ewp/140198en.pdf.
88. Amidon GL, Lennernäs H, Shah VP, Crison JR. 1995. A theoretical basis for the biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 12:413-420.
89. Lindenberg M, Kopp S, Dressman JB. 2004. Classification of orally administered drugs on the World Health Organization model list of essential medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm 58:265-278.
90. Yu LX, Amidon GL, Polli JE, Zhao H, Mehta MU, Conner DP, Shah VP, Lesko LJ, Chen ML, Lee VHL, Hussain AS. 2002. Biopharmaceutics classification system: The scientific basis for biowaiver extensions. Pharm Res 19:921-925.
91. Blume HH, Schug BS. 1999. The biopharmaceutics classification system (BCS): Class III drugs-Better candidates for BA/BE waiver? Eur J Pharm Sci 9:117-121.
92. Dressman JB, Butler J, Hempenstall J, Reppas C. 2001. The BCS: Where do we go from here? Pharm Technol 7:68-76.
93. 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.
94. Of Health and Human Services FDA, Center for Drug Evaluation and Research (CDER). 2005. www.fda.gov/cder/iig/iigfaqWEB.htm.