Advertisement

Absolute and Relative Bioavailability

  • Khaled Abo-EL-Sooud
Living reference work entry

Latest version View entry history

Abstract

Attaining desired blood drug concentration and, consequently, augmenting the bioavailability of poorly absorbed drugs have always been an essential aspect for the pharmaceutical agency. The achievement of this target gives positive economic benefits as reducing drug dosage and medical impacts in decreasing toxicity and bacterial resistance in case of antimicrobials. Various factors may reduce the availability of drugs. There are numerous ways to estimate bioavailability. Various software’s models have been developed to simplify such analyses. The newly developed programs should provide a range of modules for pharmacokinetic and pharmacodynamic analysis with a more user-friendly interface.

Attaining desired blood drug concentration and, consequently, augmenting the bioavailability of poorly absorbed drug molecules have always been an essential aspect of development plans for the pharmaceutical agency. The achievement of this target gives positive economic benefits as reducing drug dosage and frequency and medical impacts in decreasing toxicity and bacterial resistance in case of antimicrobials. A drug may be well absorbed orally because of good lipid solubility and yet not has a good oral bioavailability because of extensive presystemic loss. Various physiological factors reduce the availability of drugs prior to their entry into the systemic circulation. There are numerous ways that are followed to estimate bioavailability. To simplify such analyses, various software’s models have been developed. The newly developed programs should provide a range of modules for pharmacokinetic and pharmacodynamic analysis with a more user-friendly interface. Factors that reduce the availability of drugs prior to their entry into the systemic circulation should be considered during prescription. Understanding the difference between absolute and relative bioavailability and be able to convert between these values is an essential issue. Relative bioavailability is one of the significant measures used to assess bioequivalence between several drug products.

References and Further Reading

  1. Abdallah HY, Ludden TM (1995) A spreadsheet program for simulation of bioequivalence and bioavailability studies. Comput Biol Med 25:349–354.  https://doi.org/10.1016/0010-4825(95)00015-VCrossRefPubMedGoogle Scholar
  2. Abo-El-Sooud K, Swielim GA, Wally YR, El-Gammal SM (2016) Comparative biliary and serum kinetics of doxycycline after oral and intramuscular routes with special reference to its unique entero-hepatic circulation in turkeys. Wulfenia 23:206–219Google Scholar
  3. Abo-EL-Sooud K, Mouneir SM, Fahmy MAF (2017) Curcumin ameliorates the absolute and relative bioavailabilities of marbofloxacin after oral administrations in broiler chickens. Wulfenia 24:284–297Google Scholar
  4. Baggot JD, McKellar QA (1994) The absorption, distribution and elimination of anthelmintic drugs: the role of pharmacokinetics. J Vet Pharmacol Ther 17:409–419CrossRefPubMedGoogle Scholar
  5. Brown AM (2006) A non-linear regression analysis program for describing electrophysiological data with multiple functions using Microsoft Excel. Comput Methods Prog Biomed 82:51–57.  https://doi.org/10.1016/j.cmpb.2006.01.007CrossRefGoogle Scholar
  6. Chaudhary A, Nagaich U, Gulati N et al (2012) Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: a recent review. J Adv Pharm Educ Res 2:32–67.  https://doi.org/10.1016/S0040-6031(02)00451-3CrossRefGoogle Scholar
  7. Chow S-C, Liu J-P (2009) Design and analysis of bioavailability and bioequivalence studies. J Chem Inf Model 53:758.  https://doi.org/10.1002/1521-3773(20010316)40:6<9823::AID-ANIE9823>3.3.CO;2-CCrossRefGoogle Scholar
  8. Chow S-C, Endrenyi L, Chi E et al (2011) Statistical issues in bioavailability/bioequivalence studies. J Bioequiv Availab S1:007.  https://doi.org/10.4172/jbb.S1-007
  9. Cuiné JF, Mcevoy CL, Charman WN et al (2008) Evaluation of the impact of surfactant digestion on the bioavailability of danazol after oral administration of lipidic self-emulsifying formulations to dogs. J Pharm Sci 97:995–1012.  https://doi.org/10.1002/jps.21246CrossRefPubMedGoogle Scholar
  10. Dansirikul C, Choi M, Duffull SB (2005) Estimation of pharmacokinetic parameters from non-compartmental variables using Microsoft Excel? Comput Biol Med 35:389–403.  https://doi.org/10.1016/j.compbiomed.2004.02.008CrossRefPubMedGoogle Scholar
  11. De Beule K, Van Gestel J (2001) Pharmacology of itraconazole. Drugs 61:27–37.  https://doi.org/10.1016/S1043-6618(02)00088-9CrossRefPubMedGoogle Scholar
  12. Endrenyi L, Yan W (1993) Variation of Cmax and Cmax/AUC in investigations of bioequivalence. Int J Clin Pharmacol Ther Toxicol 31:184–189PubMedGoogle Scholar
  13. Felmlee MA, Morris ME, Mager DE (2012) Mechanism-based pharmacodynamic modeling. Methods Mol Biol 929:583–600.  https://doi.org/10.1007/978-1-62703-050-2-21CrossRefPubMedPubMedCentralGoogle Scholar
  14. Foster DM (2007) Noncompartmental versus compartmental approaches to pharmacokinetic analysis. Princ Clin Pharmacol 8:102–130.  https://doi.org/10.1016/B978-0-12-369417-1.50048-1CrossRefGoogle Scholar
  15. Gabrielsson JL, Weiner DL (1999) Methodology for pharmacokinetic/pharmacodynamic data analysis. Pharm Sci Technol Today 2:244–252CrossRefPubMedGoogle Scholar
  16. Gray M, Jones DP (2004) The effect of different formulations of equivalent active ingredients on the performance of two topical wound treatment products. Ostomy Wound Manag 50:34–40Google Scholar
  17. Guerville M, Boudry G (2016) Gastrointestinal and hepatic mechanisms limiting entry and dissemination of lipopolysaccharide into the systemic circulation. Am J Physiol Gastrointest Liver Physiol 311:G1–G15.  https://doi.org/10.1152/ajpgi.00098.2016CrossRefPubMedGoogle Scholar
  18. Hasbach AE, Langlois DK, Rosser EJ, Papich MG (2017) Pharmacokinetics and relative bioavailability of orally administered innovator-formulated itraconazole capsules and solution in healthy dogs. J Vet Intern Med 31:1163–1169.  https://doi.org/10.1111/jvim.14779CrossRefPubMedPubMedCentralGoogle Scholar
  19. Howgate EM, Rowland Yeo K, Proctor NJ et al (2006) Prediction of in vivo drug clearance from in vitro data I: impact of inter-individual variability. Xenobiotica 36:473–497.  https://doi.org/10.1080/00498250600683197CrossRefPubMedGoogle Scholar
  20. Jaki T, Wolfsegger MJ (2012) Non-compartmental estimation of pharmacokinetic parameters for flexible sampling designs. Stat Med 31:1059–1073.  https://doi.org/10.1002/sim.4386CrossRefPubMedGoogle Scholar
  21. Khan AA, Mudassir J, Mohtar N, Darwis Y (2013) Advanced drug delivery to the lymphatic system: lipid-based nanoformulations. Int J Nanomedicine 8:2733–2744PubMedCentralGoogle Scholar
  22. Kota J, Machavaram KK, McLennan DN et al (2007) Lymphatic absorption of subcutaneously administered proteins: influence of different injection sites on the absorption of darbepoetin alfa using a sheep model. Drug Metab Dispos 35:2211–2217.  https://doi.org/10.1124/dmd.107.015669CrossRefPubMedGoogle Scholar
  23. Meineke I (2000) An add-in implementation of the RESAMPLING syntax under Microsoft EXCEL. Comput Methods Prog Biomed 63:99–104.  https://doi.org/10.1016/S0169-2607(00)00077-8CrossRefGoogle Scholar
  24. Morris CA, Duparc S, Borghini-Fuhrer I et al (2011) Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration. Malar J 10:263CrossRefPubMedPubMedCentralGoogle Scholar
  25. Musther H, Olivares-Morales A, Hatley OJD et al (2014) Animal versus human oral drug bioavailability: do they correlate? Eur J Pharm Sci 57:280–291.  https://doi.org/10.1016/j.ejps.2013.08.018CrossRefPubMedPubMedCentralGoogle Scholar
  26. Narang N, Sharma J (2011) Sublingual mucosa as a route for systemic drug delivery. Int J Pharm Pharm Sci 3:18–22Google Scholar
  27. Okusanya O, Forrest A, DiFrancesco R et al (2007) Compartmental pharmacokinetic analysis of oral amprenavir with secondary peaks. Antimicrob Agents Chemother 51:1822–1826.  https://doi.org/10.1128/AAC.00570-06CrossRefPubMedPubMedCentralGoogle Scholar
  28. Persky AM (2012) The impact of team-based learning on a foundational pharmacokinetics course. Am J Pharm Educ 76:1–10.  https://doi.org/10.5688/ajpe76231CrossRefGoogle Scholar
  29. Plusquellec Y, Efthymiopoulos C, Duthil P, Houin G (1999) A pharmacokinetic model for multiple sites discontinuous gastrointestinal absorption. Med Eng Phys 21:525–532CrossRefPubMedGoogle Scholar
  30. Roberts MS, Magnusson BM, Burczynski FJ, Weiss M (2002) Enterohepatic circulation: physiological, pharmacokinetic and clinical implications. Clin Pharmacokinet 41:751–790.  https://doi.org/10.2165/00003088-200241100-00005CrossRefPubMedGoogle Scholar
  31. Shargel L, Wu-Pong S, Yu A (2004) Applied biopharmaceutics and pharmacokinetics, 7th edn. McGraw-Hill education, New York, pp 471–475.  https://doi.org/10.7326/0003-4819-94-6-826_2
  32. Sim DSM (2015) Drug absorption and bioavailability. In: Chan YK, Ng KP, Sim DSM (eds) Pharmacological basis of acute care. Springer International Publishing, Switzerland, pp 17–26Google Scholar
  33. Tatiraju DV, Bagade VB, Karambelkar PJ et al (2013) Natural bioenhancers: an overview. J Pharmacogn Phytochem 2:55–60Google Scholar
  34. Toutain PL, Bousquet-Mélou A (2004) Bioavailability and its assessment. J Vet Pharmacol Ther 27(6):455–466CrossRefPubMedGoogle Scholar
  35. Watabe H, Ikoma Y, Kimura Y et al (2006) PET kinetic analysis – compartmental model. Ann Nucl Med 20:583–588.  https://doi.org/10.1007/BF02984655CrossRefPubMedGoogle Scholar
  36. Wolfsegger MJ, Jaki T (2009) Non-compartmental estimation of pharmacokinetic parameters in serial sampling designs. J Pharmacokinet Pharmacodyn 36:479–494.  https://doi.org/10.1007/s10928-009-9133-9CrossRefPubMedGoogle Scholar
  37. Zhang Y, Huo M, Zhou J, Xie S (2010) PKSolver: an add-in program for pharmacokinetic and pharmacodynamic data analysis in Microsoft Excel. Comput Methods Prog Biomed 99:306–314.  https://doi.org/10.1016/j.cmpb.2010.01.007CrossRefGoogle Scholar
  38. Zweig AS, Tress ML, Vanden Hoek TL (2007) Absorption of drugs transport of a drug from the GI tract factors affecting drug absorption related to patient. J Pharm Pharmacol 7:23–25Google Scholar

Copyright information

© Springer International Publishing AG, part of Springer Nature 2018

Authors and Affiliations

  1. 1.Pharmacology Department, Faculty of Veterinary MedicineCairo UniversityGizaEgypt

Personalised recommendations