Drug Delivery of Peptides: The Buccal Route

  • Hans P. Merkle
  • Reinhold Anders
  • Jürgen Sandow
  • Werner Schurr
Part of the NATO ASI Series book series (NSSA, volume 125)

Abstract

Peptides and proteins are currently emerging as a major class of future drugs. So far the research in this field is mainly focused on basic research covering isolation, synthesis, analysis, and biological and clinical effects. However, increasing attention is now also given to considerations regarding suitable dosage forms and routes of absorption. It is widely accepted that the most common dosage forms and routes, i.e. solid dosage forms for peroral application and sterile preparations for parenteral application, will not provide a realistic basis for a widespread use of these drugs in the future. This is because (i) most oligopeptides and proteins are not readily absorbed in the gastrointestinal tract, e.g. due to the presence of proteolytic enzymes and the low permeability of the gut membranes to such often hydrophilic compounds. And also (ii) parenteral application, certainly, is of limited suitability to long term treatments and frequent use of drugs.

Keywords

Drug Release Dosage Form Buccal Mucosa Pharmacodynamic Response Absorption Enhancer 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Anders, R., Merkle, H.P., Schurr, W., Ziegler, R., 1983, Buccal Absorption of protirelin: an effective way to stimulate thyrotropin and prolactin, J. Pharm. Sci., 72: 1481.PubMedCrossRefGoogle Scholar
  2. Anders, R., 1984, Ph.D. Thesis: Selbsthaftende Polymerfilme zur bukkalen Applikation von Peptiden, Universität Bonn, Bonn.Google Scholar
  3. Anders, R., and Merkle. H.P., 1986, Arzneiformung selbsthaftender Polymerfilme zur bukkalen Applikation, manuscript in preparation.Google Scholar
  4. Bergjoe, P., and Jenssen, H., 1969, Nasal and buccal oxytocin for the introduction of labour: a clinical trial, J. Obstet. Gynaec. Brit. Cwlth., 76: 131.CrossRefGoogle Scholar
  5. Chien, Y.W., ed., 1985, Transnasal Systemic Medications, Elsevier, Amsterdam.Google Scholar
  6. Chien, Y.W., and Chang, S.F., 1985, Historic development of transnasal systemic medications, in: “Transnasal systemic medications”, Y.W. Chien, ed., Elsevier, Amsterdam, 1.Google Scholar
  7. Ch’ng, H.S., Park, H., Kelly, P., and Robinson, J.R., 1985, Bioadhesive polymers as platforms for oral controlled drug delivery II: synthesis and evaluation of some swelling, water-insoluble bioadhesive polymers, J. Pharm. Sci., 74: 399.CrossRefGoogle Scholar
  8. Davis, S.S., Daly, P.B., Kennerley, J.W., Frier, M., Hardy, J.G., and Wilson, C.G., 1982, Design and evaluation of sustained release formulations for oral and buccal administration, in: “Controlled release nitroglycerin in buccal and oral form”, W.-D. Bussmann, R.-D. Dries, and W. Wagner, eds., Advances in Pharmacotherapy, Vol. 1, Karger, Basel, 17.Google Scholar
  9. Davis, S.S., 1985, personal communication.Google Scholar
  10. Ishida, M., Machida, Y., Nambu, N., and Nagai, T., 1981, New mucosal dosage form of insulin, Chem. Pharm. Bull., 29: 810.PubMedCrossRefGoogle Scholar
  11. Ishida, M., Nambu, N., Nagai, T., 1982, Mucosal dosage form of lidocain for toothache using hydroxypropyl cellulose and carbopol, Chem. Pharm. Bull., 30: 980.PubMedCrossRefGoogle Scholar
  12. Hussain, A.A., Bawarshi-Nassar, R., Huang, C.H., 1985, Physicochemical considerations in intranasal drug administration, in: “Transnasal systemic medications”, Y.W. Chien, ed., Elsevier, Amsterdam, 121.Google Scholar
  13. Lee, P., 1986, Kinetics of drug release from hydrogel matrices, in: “Advances in drug delivery systems”, J.M. Anderson and S.W. Kim, eds., Elsevier, Amsterdam, 277.Google Scholar
  14. Merkle, H.P., Anders, R., Sandow, J., Schurr, W., 1985, Self-adhesive patches for buccal delivery of peptides, Proceed. Intern. Symp. Control. Rel. Bioact. Mater., 12: 85.Google Scholar
  15. Merkle, H.P., Anders, R., and Sandow, J., 1986, Abstract: Buccal Absorption of peptides in rats, Proceed. 32th annual congress of APV, Mainz, 57.Google Scholar
  16. Nagai, T., 1986, Adhesive topical drug delivery systems, in: “Advances in drug delivery systems”, J.M. Anderson, S.W. Kim, eds., Elsevier, Amsterdam, 121.Google Scholar
  17. Nishi, N., Arimura, A., Coy, D.H., Vilches-Martinez, J.A., Schally, A.V., 1975, The effect of oral and vaginal administration of synthetic LHRH and (D-Ala(6)-DesGly(10)-NH)-LHRH ethylamid on serum LH-levels on ovariectomized, steroid blocked rats, Proc. Soc. Exp. Biol. Med., 148: 1009.PubMedGoogle Scholar
  18. Nishihata, T., Rytting, J.H., Higuchi, T., Caldwell, L., 1981, Enhanced rectal absorption of insulin and heparin in rats in the presence of non-surfactant adjuvants, J. Pharm. Sci., 33: 334.Google Scholar
  19. Okada, H., Yamazaki, I., Ogawa, Y., Hirai, S., Yashiki, T., Mima, H., 1982, Vaginal absorption of a potent luteinizing hormone-releasing analogue (Leuprolide) in rats I: absorption by various routes and absorption enhancement, J. Pharm. Sci., 71: 1367.PubMedCrossRefGoogle Scholar
  20. Okada, H., Yamazaki, I., Yashiki, T., Mima, H., 1983, Vaginal absorption of a potent luteinizing hormone-releasing analogue (Leuprolide) in rats II: mechanism of absorption enhancement, J. Pharm. Sci., 72: 75.PubMedCrossRefGoogle Scholar
  21. Park, H., and Robinson, J.R., 1986, Physico-chemical properties of water insoluble polymers important to mucin/epithelial adhesion, in: “Advances in drug delivery systems”, J.M. Anderson, and S.W. Kim, eds., Elsevier, Amsterdam, 47.Google Scholar
  22. Peppas, N.A., and Buri, P.A., 1986, Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues, in: “Advances in drug delivery systems”, J.M. Anderson, and S.W. Kim, eds., Elsevier, Amsterdam, 257.Google Scholar
  23. Sandow, J., and Petri, W., 1985, Intranasal administration of peptides biological activity and therapeutic efficacy, in: “Transnasal Systemic Medications”, Y.W. Chien, ed., Elsevier, Amsterdam, 183.Google Scholar
  24. Schurr, W., Knoll, B., Ziegler, R., Anders, R., and Merkle, H.P., 1985, Comparative study of intravenous, nasal, oral and buccal TRH administration among healthy subjects, J. Endocrin. Invest., 8: 41.Google Scholar
  25. Stratford, R.E., and Lee, V.H.L., 1985, Aminopeptidase activity in albino rabbit extraocular tissues relative to the small intestine, J. Pharm. Sci, 74: 731.PubMedCrossRefGoogle Scholar
  26. Su, K.S.E., 1986, Intranasal delivery of peptides and proteins, Pharm. Int., 7: 8.Google Scholar
  27. Su, K.S.E., and Campanale, K.M., 1985, Nasal drug delivery systems requirements, development and evaluations, in: “Transnasal Systemic medications”, Y.W. Chien, ed., Elsevier, Amsterdam, 139.Google Scholar
  28. Van de Donk, H.J.M., Van den Heuvel, A.G.M., Zuidema, J., and Merkus, F.W. H.M., 1982, The effects of nasal drops and their additives on human, nasal mucociliary clearance, Rhinology, 20: 127.PubMedGoogle Scholar
  29. Wespi, H.J., and Rehsteiner, H.P., 1966, Erfahrungen mit Syntocinon-und ODA-Buccaltabletten, Gynaecologia, 162: 414.PubMedGoogle Scholar
  30. Yoshioka, S., Caldwell, L., and Higuchi, T., 1982, Enhanced rectal bioavailability of polypeptides using sodium 5-methoxysalicylate as an absorption promotor, J. Pharm. Sci., 71: 593.PubMedCrossRefGoogle Scholar

Copyright information

© Springer Science+Business Media New York 1986

Authors and Affiliations

  • Hans P. Merkle
    • 1
  • Reinhold Anders
    • 1
    • 2
  • Jürgen Sandow
    • 2
  • Werner Schurr
    • 3
  1. 1.Pharmazeutische TechnologiePharmazeutisches Institut der UniversitätBonn 1Germany
  2. 2.Hoechst AGFrankfurt aM 80Germany
  3. 3.Abteilung Innere Medizin VIUniversitätspoliklinikHeidelbergGermany

Personalised recommendations