Buccal Absorption of Drugs

  • Arnold H. Beckett
  • R. D. Hossie
Part of the Handbuch der experimentellen Pharmakologie/Handbook of Experimental Pharmacology book series (HEP, volume 28 / 1)


The buccal cavity is lined with a mucous membrane which, like the lining of the entire alimentary canal, behaves as a lipoidal barrier to the passage of drugs (Schanker, 1962). In general, drugs penetrate the mucous membrane by simple diffusion and are carried in the blood that richly supplies the salivary glands and their ducts into the general circulation via the jugular vein. Active transport, pinocytosis, and passage through aqueous pores usually play only insignificant roles in moving drugs across the oral mucosa.


Partition Coefficient Oral Mucosa Phenylacetic Acid Basic Drug Buccal Cavity 
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  1. Altman, G.E., Gasche, P.: Schweiz, med. Wschr. 72, 279 (1942).Google Scholar
  2. Altman, G.E., Gasche, P.: Schweiz, med. Wschr.,Riseman, J.E.F., Koretsky, S.: Sublingual erythrol tetranitrate treatment in angina pectoris. The effect of varying the doses and rate of administration. Amer. J. med. Sci. 240, 66–76 (1960).CrossRefGoogle Scholar
  3. Anderson, E., Kinsell, L., Daniels, T.C., Henderson, E.: Letter to the Editor: The intraoral administration of desoxycorticosterone acetate tablets in the treatment of Addison’s Disease. J. clin. Endocr. 8, 884–886 (1948).PubMedGoogle Scholar
  4. Beckett, A.H., Boyes, R.N., Triggs, E. J.: Kinetics of buccal absorption of amphetamines. J. Pharm. Pharmacol. 20, 92–97 (1968).CrossRefGoogle Scholar
  5. Beckett, A.H., Boyes, R.N., Triggs, E. J., Jenner, P.G., Gorrod, J.W.: To be published.Google Scholar
  6. Beckett, A.H., Boyes, R.N., Triggs, E. J.— Moffat, A. C.: The influence of alkyl substitution in acids on their performance in the buccal absorption test. J. Pharm. Pharmacol. 20, Suppl. 239S+ (1968).PubMedGoogle Scholar
  7. Beckett, A.H., Boyes, R.N., Triggs, E. J.: The influence of substitution in phenylacetic acids on their performance in the buccal absorption test. J. Pharm. Pharmacol. 21, 139–143S (1969 a).Google Scholar
  8. Beckett, A.H., Boyes, R.N., Triggs, E. J.: Correlation of partition coefficients in n-heptane-aqueous systems with buccal absorption data for a series of amines and acids. J. Pharm. Pharmacol. 21, 144S–150S (1969b).PubMedCrossRefGoogle Scholar
  9. Beckett, A.H., Boyes, R.N., Triggs, E. J.: Kinetics of buccal absorption of some carboxylic acids and the correlation of the rate constants and n-heptane:aqueous phase partition coefficients. J. Pharm. Pharmacol. 22, 15–19 (1970a).PubMedCrossRefGoogle Scholar
  10. Beckett, A.H., Boyes, R.N., Triggs, E. J.: J. Pharm. Pharmacol. 22, in the press (1970b).Google Scholar
  11. Beckett, A.H., Boyes, R.N., Triggs, E. J.: The buccal absorption of some barbiturates. J. Pharm. Pharmacol. 22, in the press (1970).Google Scholar
  12. Beckett, A.H., Boyes, R.N., Triggs, E. J., Salmon, J. A., Mitchard, M.: The relation between blood levels and urinary excretion of amphetamine under controlled acidic and under fluctuating urinary pH values using [14C] amphetamine. J. Pharm. Pharmacol. 21, 251–258 (1969).PubMedCrossRefGoogle Scholar
  13. Beckett, A.H., Boyes, R.N., Triggs, E. J.: Triggs, E.J.: Buccal absorption of basic drugs and its applications as an in vivo model of passive drug transfer through lipid membranes. J. Pharm. Pharmacol. 19, 31S–41S (1967).PubMedGoogle Scholar
  14. Beckett, A.H., Boyes, R.N., Triggs, E. J., Tucker, G.T.: Montpellier Symposium. J. mond. Pharm. (La Haye) 3, 181 (1967).Google Scholar
  15. Problems in the in vivo evaluation of drug preparations and the interpretation of in vivodata. J. mond. Pharm. (La Haye), 3, 181–202 (1967)Google Scholar
  16. Bickel, M.H., Weder, H.J.: Buccal absorption and other properties of pharmacokinetic importance of imipramine and its metabolites. J. Pharm. Pharmacol. 21, 160–168 (1969).PubMedCrossRefGoogle Scholar
  17. Brodie, B.B.: Physico-chemical factors in drug absorption. T.B. Binns, ed. pp. 16-48. Baltimor: Williams and Wilkins Co. 1964.Google Scholar
  18. Brown, A., Kennedy, A.C.: Sublingual heparin. Lancet 263, 936 (1952).CrossRefGoogle Scholar
  19. Brunton, R. L.: The Gaulstonian Lectures Delivered before the Royal College of Surgeons. London: McMillan and Co. 1877.Google Scholar
  20. De Re Medica: Ed. 3. Indianapolis: Eli Lilly & Co. 1951.Google Scholar
  21. Escamilla, R. F.: Treatment of preadolescent eunuchoidism with testosterone linguets. Amer. Practit. 3, 425–427 (1949).Google Scholar
  22. Evans, E., Hoyle, C.: The prevention and treatment of individual attacks of angina pectoris (angina of effort). Quart. J. Med. 3, 105–135 (1934).Google Scholar
  23. Fantus, B.: The technique of medication. J. Amer. med. Ass. 86, 687–689 (1926).Google Scholar
  24. Fuller, H.L.: Sublingual heparin in Hyperlipemia. Angiology 9, 311–313 (1958).PubMedCrossRefGoogle Scholar
  25. Fuller, H.L.: Effect of sublingual heparin on lipemia clearing and on recurrence of myocardial infarction. Angiology 11, 200–206 (1960).PubMedCrossRefGoogle Scholar
  26. Grossman, M., Sandor, J.: Zur Klinischen Pharmakologie des Nitroglycerins. Klin. Wschr. 2, 1833–1835 (1923).CrossRefGoogle Scholar
  27. Heni, F., Nieth, H.: Vergleich der Hyderginwirkung bei enteraler und sublingualer Zufuhr. Klin. Wschr. 30, 354–357 (1952).PubMedCrossRefGoogle Scholar
  28. Jacobs, M.H.: Some aspects of cell permeability to weak electrolytes. Cold Spr. Harb. Symp. quant. Biol. 8, 30–39 (1960).Google Scholar
  29. Litwins, J., Vorzimer, J.J., Sussman, L.N., Applezweig, N., Etess, A.D.: Sublingual administration of heparin. Proc. Soc. exp. Biol. (N.Y.) 77, 325–326 (1951).PubMedGoogle Scholar
  30. McCullagh, E.P., Lewis, L.A.: Comparison of effectiveness of various methods of administration of insulin. J. clin. Endocr. 2, 435–437 (1942).CrossRefGoogle Scholar
  31. MCDevttt, E., Huebner, R., Wright, I.S.: Ineffectiveness of heparin by sublingual administration. J. Amer. med. Ass. 148, 1123–1124 (1952).Google Scholar
  32. Miescher, K., Gasche, P.: Zur lingualen Applikation von männlichem Sexualhormon. Beitrag zur Therapie mit Perandren-Linguetten. Schweiz, med. Wschr. 72, 279–281 (1942).Google Scholar
  33. Miller, J.M., Papastrat, C.J., Ginsberg, M.: Antibiot. Med. 5, 720 (1958).PubMedGoogle Scholar
  34. Miller, J.M., Papastrat, C.J., Ginsberg, M.Gibaldi, M., Kanig, J.L.: Absorption of drugs through the oral mucosa. J. Oral. ther. Pharm. 1, 440–450.Google Scholar
  35. Moffat, A.C.: Partition characteristics of acids and bases in relation to biological membranes. Ph.D. Thesis, University of London, London, pp. 1–276 (1968).Google Scholar
  36. Neubauer, R., Esposito, J., Sindoni, A.: Use of buccal trypsin in two diabetics with the nephrotic syndrome. A preliminary report. Amer. J. med. Sci. 237, 559–565 (1959).CrossRefGoogle Scholar
  37. Perloff, W. H.: Estradiol buccal tablets in the treatment of the menopause. Amer. J. Obstet. Gynec. 59, 223–225 (1950).PubMedGoogle Scholar
  38. Sacks, D. R.: Regulation of blood sugar in diabetes by sublingual administration of insulin. Tex. St. J. Med. 37, 39–41 (1941).Google Scholar
  39. Schachter, M.: Med. espan. 8, 31 (1942).Google Scholar
  40. Schachter, M.A.: A studio sobra o hormonaterapia peroral o perlingual. Med. espan. 8, 31–38 (1942).Google Scholar
  41. Schanker, L.S.: Passage of drugs across body membranes. Pharmacol. Rev. 14, 501–530 (1962).PubMedGoogle Scholar
  42. Schanker, L.S.:Advances in Drug Research. Harper, N.J. and Simmonds, A.B., ed. pp. 71–100. London and New York: Academic Press 1964.Google Scholar
  43. Spence, A.W.: Sublingual administration of methyl testosterone. Brit. med. J. 1, 668 (1942).PubMedCrossRefGoogle Scholar
  44. Turnoff, D., Rountree, L.G.: Successful sublingual therapy in Addison’s Disease. J. Amer. med. Ass. 116, 2016–2018 (1941).Google Scholar
  45. Walton, R.P.: Absorption of drugs through the oral mucosa. III. Fat-water solubility coefficient of alkaloids. Proc. Soc. exp. Biol. (N.Y.) 32, 1488–1492 (1935).Google Scholar
  46. Walton, R.P.: Further studies dealing with the sublingual absorption of drugs. J. Pharmacol, exp. Ther. 57, 148 (1936).Google Scholar
  47. Walton, R.P.: Sublingual administration of drugs. J. Amer. med. Ass. 124, 138–143 (1944).Google Scholar
  48. Walton, R.P.: Basset, E.F.: The enteral absorption of insulin as modified by various drugs. Arch. int. Pharmacodyn. 48, 322–327 (1934).Google Scholar
  49. Walton, R.P., Lacey, C.F.: Absorption of drugs through the oral mucosa. J. Pharmacol, exp. Ther. 54, 61–76 (1935).Google Scholar
  50. Wilbrant, R.: Kurze Mitteilung über die Wirkung von Hydergin-Sublingualtabletten bei Hypertonie. Praxis 41, 384–385 (1952).Google Scholar

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© Springer-Verlag Berlin · Heidelberg 1971

Authors and Affiliations

  • Arnold H. Beckett
  • R. D. Hossie

There are no affiliations available

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