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Biopharmaceutics of rectal administration of drugs in man

Absorption rate and bioavailability of acetylsalicylic acid and its calcium salt after oral and rectal administration

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Abstract

Rectal absorption of acetylsalicylic acid and its calcium salt was studied in man and compared with oral absorption.

Plasma concentrations of acetylsalicylic acid and salicylic acid were measured by means ofHplc analysis, after a single dose of acetylsalicylic acid (500 mg) and after single rectal doses of acetylsalicylic acid (500 mg) and calcium acetylsalicylate (640 mg) in a cross-over study in 8 volunteers. The rectal dosage forms included fatty suppositories and aqueous solutions.

Compared with oral administration rectal absorption of acetylsalicylic acid can be equally rapid, if the volume and the pH of the aqueous micro-enema was optimized (20 ml, pH 4.0). Rectal absorption of calcium acetylsalicylate occurred very slowly. If fatty suppositories were used smaller particles favoured the rate of acetylsalicylic acid absorption. Compared with oral administration absorption from the optimized suppository dosage form proceeded significantly (P < 0.05) slower. For all rectal dosage forms, the extent to which acetylsalicylic acid reached the general circulation intact, was smaller than after oral administration.

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References

  • Bywaters, E. G. L. (1963) Clinical implications of the antiinflammatory effects of salicylate. InSalicylates, an international symposium (A. St. J. Dixon, B. K. Martin, M. J. H. Smith andP. H. W. Wood, eds.), 154–160. Little Brown, Boston.

    Google Scholar 

  • Cacchillo, A. F., andW. H. Hassler (1954) The influence of suppository bases upon the rectal absorption of acetylsalicylic acid.J. Am. Pharm. Assoc. 43, 683–685.

    Article  CAS  Google Scholar 

  • Cid, E. (1974) Absorption rectale de médicaments. Influence de la taille des cristaux d'acide acetylsalicylique.Ann. Pharm. Franc. 32, 273–281.

    CAS  PubMed  Google Scholar 

  • Coldwell, B. B., G. Solomonray, E. M. Boyd, J. Jantz andA. B. Morrison (1969) The effect of dosage form and route of administration on the absorption and excretion of acetylsalicylic acid in man.Clin. Toxicol. 2, 111–127.

    Article  Google Scholar 

  • Duthie, J. J. R. (1963) InSalicylates, an international symposium (A. St. J. Dixon, M. J. H. Smith, B. K. Martin andP. H. W. Wood, eds.), 288–292, Little Brown, Boston.

    Google Scholar 

  • Gibaldi, M., andB. Grundhofer (1975) Bioavailability of aspirin from commercial suppositories.J. Pharm. Sci. 64, 1064–1066.

    Article  CAS  PubMed  Google Scholar 

  • Ginneken, C. A. M. Van (1976)Pharmacokinetics of antipyretic and anti-inflammatory analgesics. Thesis, Nijmegen.

  • Houde, R. W., S. L. Wallenstein andW. T. Beaver (1965) Clinical measurement of pain. InAnalgetics (G. De Stevens, ed.), 76–122. Academic Press, New York.

    Google Scholar 

  • Lasagna, L. (1961) Progress of medical science: Analgesic drugs.Am. J. Med. Sci. (R. A. Kern, T. M. Durant andK. M. Schreck, eds.), Vol. 242, 620–627. Lea & Febiger, Philadelphia.

    Google Scholar 

  • Lester, D., G. Lolli andL. A. Greenberg (1946) The fate of acetylsalicylic acid.J. Pharmacol. Exp. Ther. 87, 329–342.

    CAS  PubMed  Google Scholar 

  • Levy, G., andL. P. Amsel (1966) Kinetics of competitive inhibition of salicylic acid conjugation with glycine in man.Bioch. Pharmacol. 15, 1033–1038.

    Article  CAS  Google Scholar 

  • Lim, R. K. S., D. G. Miller, F. Guzman, D. W. Rodgers, S. K. Wang, P. Y. Chao andT. Y. Shih (1967) Pain and analgesia evaluated by the intraperitoneal bradykininevoked pain method in man.Clin. Pharmacol. Therap. 8, 521–542.

    Article  CAS  Google Scholar 

  • Lowenthal, W., J. F. Borzelleca andC. D. Corder (1970) Drug absorption from the rectum III: Aspirin and some aspirin derivates,J. Pharm. Sci. 59, 1353–1355.

    Article  CAS  PubMed  Google Scholar 

  • Margolin, S. (1960) Pharmacologic demonstration in man of increased thresholds to tooth pain following carisoprodal and other analgesics.Proc. Soc. Exp. Biol. Med. 105, 531–533.

    Article  CAS  PubMed  Google Scholar 

  • Moolenaar, F., A. G. G. Stuurman-Bieze, J. Visser andT. Huizinga (1978) Biopharmaceutics of rectal administration of drugs in man, part 1: Introduction of benzoic acid as a test drug.Int. Journ. Pharm. 1, 323–336.

    Article  CAS  Google Scholar 

  • Moolenaar, F., B. Koning and T.Huizinga (1979a), part 7: Absorption rate and bioavailability of phenobarbital and its sodium salt from rectal dosage forms.Int. Journ. Pharm., accepted.

  • Moolenaar, F., W. J. Greving and T.Huizinga (1979b) part 8: Absorption rate and bioavailability of valproic acid and its sodium salt from different rectal dosage forms.Europ. Journ. Clin. Pharmacol., submitted.

  • Moolenaar, F., L. Olthof andT. Huizinga (1979c) part 3: Absorption rate and bioavailability of paracetamol from rectal aqueous suspensions,Pharm. Weekblad Sci. Ed. 1, 25–30.

    Google Scholar 

  • Moolenaar, F., A. J. M. Schoonen, A. Everts andT. Huizinga (1979d) part 4: Absorption rate and bioavailability of paracetamol from fatty suppositories,Pharm. Weekblad Sci. Ed. 1, 89–94.

    CAS  Google Scholar 

  • Neuwald, F., andF. Kunze (1964) Vergleichende Untersuchungen über die Abgabe von Salicylaten aus Suppositorien-fettgrundmassen in vitro und in vivo.Arzneimittel-Forsch. 14, 1162–1167.

    CAS  Google Scholar 

  • Parrot, E. L. (1971) Salicylate absorption from rectal suppositories,J. Pharm. Sci. 60, 867–872.

    Article  Google Scholar 

  • Parrot, E. L. (1975) Influence of particle size on rectal absorption of aspirin.J. Pharm. Sci. 64, 878–880.

    Article  Google Scholar 

  • Rowland, M., andS. Riegelman (1968) Pharmacokinetics of acetylsalicylic acid and salicylic acid after intravenous administration in man.J. Pharm. Sci. 57, 1313–1319.

    Article  CAS  Google Scholar 

  • Rowland, M., S. Riegelman, P. A. Harris andS. D. Sholkoff (1972) Absorption kinetics of aspirin in man following oral administration of an aqueous solution.J. Pharm. Sci. 61, 379–385.

    Article  CAS  PubMed  Google Scholar 

  • Rowland, M., S. Riegelman, P. A. Harris, S. D. Sholkoff andE. J. Eyring (1967) Kinetics of acetylsalicylic acid disposition in man.Nature 215, 413–414.

    Article  CAS  PubMed  Google Scholar 

  • Samelius, U., andA. äström (1958) The absorption of an N-methylated barbiturate and acetylsalicylic acid from different suppository masses.Acta Pharmacol. Toxicol. 14, 240–250.

    Article  CAS  Google Scholar 

  • Schoonen, A. J. M., F. Moolenaar, C. Haverschmidt andT. Huizinga (1976) The interphase transport of drugs from fatty suppository bases.Pharm. Weekblad 111, 585–590.

    CAS  Google Scholar 

  • Schoonen, A. J. M., F. Moolenaar and T.Huizinga (1979) Release of drugs from fatty suppository bases in vitro and in vivo.Int. Journ. Pharm., accepted.

  • Seed, J. C. (1965) A clinical comparison of the antipyretic potency of aspirin and sodium salicylate.Clin. Pharmacol. Ther. 6, 354–358.

    Article  CAS  PubMed  Google Scholar 

  • Senior, N. (1974)Advances in pharmaceutical sciences. Academic Press, London.

    Google Scholar 

  • Smith, M. J. H., andP. K. Smith (1966)The salicylates. Interscience, New York.

    Google Scholar 

  • Superstine, S. Y., E. Superstine andS. Penchas (1978) Comparison of the bioavailability of aspirin tablets and suppositories.Israel. J. Med. Sci. 14, 292–294.

    CAS  PubMed  Google Scholar 

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Authors and Affiliations

  1. Laboratorium voor Farmacologie en Farmacotherapie, Ant. Deusinglaan 2, 9713, AW Groningen, The Netherlands

    F. Moolenaar, N. J. J. Oldenhof, W. Groenewoud & T. Huizinga

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  1. F. Moolenaar
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  2. N. J. J. Oldenhof
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  3. W. Groenewoud
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  4. T. Huizinga
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In honour of ProfessorPolderman on the occasion of his retirement.

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Moolenaar, F., Oldenhof, N.J.J., Groenewoud, W. et al. Biopharmaceutics of rectal administration of drugs in man. Pharmaceutisch Weekblad Scientific Edition 1, 1459–1469 (1979). https://doi.org/10.1007/BF02293485

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  • DOI: https://doi.org/10.1007/BF02293485

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