Skip to main content

Transdermal Absorption: A Unique Opportunity for Drug Delivery

  • Chapter
Pharmacokinetics

Abstract

The amount of drug absorbed from the gastrointestinal (GI) tract into the systemic circulation with conventional tablet and capsule dosage forms is dependent on the quantity and type of food in the stomach, GI motility and GI microbial flora. Furthermore, for drugs with a high hepatic extraction ratio, the drug may be largely deactivated by first-pass metabolism before reaching the systemic circulation. Drug absorption from the GI tract can, therefore, result in variable and/or unpredictable plasma concentrations. Some of this variability can be minimized by administering controlled release tablet and capsule formulations. However, these dosage forms cannot eliminate the inherent variability associated with first-pass metabolism.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

eBook
USD 16.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 109.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. A.S. Michaels, S.K. Chandrasekaran and J.E. Shaw, Drug permeation through human skin. Theory andin vitro experimental measurement, Am. Inst. Chem. Eng. J. 21: 985–996 (1975).

    CAS  Google Scholar 

  2. R.J. Scheuplein, Mechanism of percutaneous absorption. I. Routes of penetration and the influence of solubility, J. Invest. Dermatol. 45: 334–346 (1965).

    PubMed  CAS  Google Scholar 

  3. R.J. Scheuplein, Mechanism of percutaneous absorption. II. Transient diffusion and the relative importance of various routes of skin penetration, J. Invest. Dermatol. 48: 79–88 (1967).

    PubMed  CAS  Google Scholar 

  4. R.J. Scheuplein and I.H. Blank, Permeability of the skin, Physiol. Rev. 51: 702–747 (1971).

    PubMed  CAS  Google Scholar 

  5. R.J. Scheuplein and I.H. Blank, Mechanism of percutaneous absorption. IV. Penetration of nonelectrolytes (alcohols) from aqueous solutions and from pure liquids, J. Invest. Dermatol. 60: 286–296 (1973).

    Article  CAS  Google Scholar 

  6. J.E. Wahlberg, Percutaneous absorption, Curr. Probl. Dermatol. 5: 1–36 (1973).

    PubMed  CAS  Google Scholar 

  7. H. Baker, The effects of dimethylsulfoxide, dimethylformamide and dimethylacetamide on the cutaneous barrier to water in human skin, J. Invest Dermatol. 50: 283–288 (1968).

    PubMed  CAS  Google Scholar 

  8. S.K. Chandrasekaran, P.S. Campbell and A.S. Michaels, Effect of dimethylsulfoxide on drug permeation through human skin, Am. Inst. Chem. Eng. J. 23: 810–816 (1977).

    CAS  Google Scholar 

  9. R.J. Feldmann and H.I. Maibach, Regional variation in percutaneous penetration of Cortisol- in man, J. Invest. Dermatol. 48: 181–183 (1967).

    PubMed  CAS  Google Scholar 

  10. H.I. Maibach, R.J. Feldmann, T.H. Milby and W.F. Serat, Regional variation in percutaneous penetration in man. Pesticides, Arch. Environ. Health 23: 208–211 (1971).

    CAS  Google Scholar 

  11. J.E. Shaw and S.K. Chandrasekaran, Controlled topical delivery of drugs for systemic action, in: “Drug Metabolism Reviews” (Vol. 8), F. DiCarlo, ed., Marcel Dekker, New York (1978), pp. 223–233.

    Google Scholar 

  12. C.F.H. Vickers, Stratum corneum reservoir for drugs, in: “Pharmacology and the Skin,” W. Montagna, R.B. Stoughton and E.J. Van Scott, eds., Appleton Century Crofts, New York (1972), pp. 177–189.

    Google Scholar 

  13. P.W. Armstrong, J.A. Armstrong and G.S. Marks, Blood levels after sublingual nitroglycerin, Circulation 59: 585–588 (1979).

    PubMed  CAS  Google Scholar 

  14. E.F. McNiff, A. Yacobi, F.M. Young-Chang, L.H. Golden, A. Goldfarb and H.-L. Fung, Nitroglycerin pharmacokinetics after intravenous infusion in normal subjects, J. Pharm. Sci. 70: 1054–1058 (1981).

    Article  PubMed  CAS  Google Scholar 

  15. J.A. Franciosa, R.C. Blank, J.N. Cohn and E. Mikulic, Hemodynamic effects of topical, oral and sublingual nitroglycerin in left ventricular failure, Curr. Ther. Res. 22: 231–245 (1977).

    Google Scholar 

  16. P.W. Armstrong, J.A. Armstrong, G.S. Marks, J. McKinven and S. Slaughter, Pharmacokinetic-hemodynamic studies of nitroglycerin ointment in congestive heart-failure, Am. J. Cardiol. 46: 670–676 (1980).

    Article  PubMed  CAS  Google Scholar 

  17. S. Sved, W.M. McLean and I.J. McGilveray, Influence of the method of application on pharmacokinetics of nitroglycerin from ointment in humans, J. Pharm. Sci. 70: 1368–1369 (1981).

    Article  PubMed  CAS  Google Scholar 

  18. C. Wu, T. Sokoloski, M.F. Blanford and A.M. Burkman, Absence of metabolite in the disappearance of nitroglycerin following incubation with red blood cells, Int. J. Pharm. 8: 323–329 (1981).

    Article  CAS  Google Scholar 

  19. J.A. Armstrong, S.E. Slaughter, G.S. Marks and P.W. Armstrong, Rapid disappearance of nitroglycerin following incubation with human blood, Can. J. Physiol. Pharm. 58: 459–462 (1980).

    Article  CAS  Google Scholar 

  20. Nitro-Bid® Ointment (2% nitroglycerin), “Physicians’ Desk Reference,” Med. Economics Co. (1980), p. 1093.

    Google Scholar 

  21. A. Kamiya and H.-L. Fung, First-pass uptake of nitroglycerin by rat blood vessels after intra-vessel injections, Abstract, American Pharmaceutical Association Meeting, April (1981).

    Google Scholar 

  22. H.-L. Fung and A. Kamiya, Disposition of nitroglycerin in rat plasma and selected blood vessels, Abstract #1087, Eighth International Congress of Pharmacology, Tokyo, July (1981), p. 552.

    Google Scholar 

  23. M.S. Hansen, S.L. Wood and R.E. Wills, Relative effectiveness of nitroglycerin ointment according to site of application, Heart Lung 8: 716–720 (1979).

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1984 Plenum Press, New York

About this chapter

Cite this chapter

Azarnoff, D.L., Karim, A., Lambert, H., Boylan, J., Schoenhardt, G. (1984). Transdermal Absorption: A Unique Opportunity for Drug Delivery. In: Benet, L.Z., Levy, G., Ferraiolo, B.L. (eds) Pharmacokinetics. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-2799-8_10

Download citation

  • DOI: https://doi.org/10.1007/978-1-4613-2799-8_10

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4612-9725-3

  • Online ISBN: 978-1-4613-2799-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics