Pharmacy World and Science

, Volume 18, Issue 3, pp 109–113 | Cite as

Pharmacokinetics of propylene glycol after rectal administration

  • W. J. Kollöffel
  • L. E. A. Weekers
  • P. B. Goldhoorn


Propylene glycol is an excipient of various pharmaceutical preparations. The pharmacokinetics after rectal administration are studied, followed by a consideration on local and systemic side-effects for a solution of paracetamol in a mixture of propylene glycol and water. After administration of 8.64 g propylene glycol to 10 adults and 173 mg/kg body weight to 4 children, peak concentrations (Cmax) of 119 mg/l and 171 mg/l respectively were reached (tmax) after 1.5 hr and 1.0 hr. The average terminal half-lives (t1/2) in adults and children were respectively 2.8 hr and 2.6 hr, total body clearance (Cl/F) 0.20 l/hr* kg and 0.21 l/hr*kg and apparent volume of distribution (VD/F) 0.79 l/kg and 0.77 l/kg.


Administration, rectal Pharmacokinetics Propanediols Propylene glycol Solution, rectal Solvents 


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  1. 1.
    Reynolds JEF, ed. Martindale, the extra pharmacopoeia. London: The Pharmaceutical Press 1993, 1406–7.Google Scholar
  2. 2.
    American Pharmaceutical Association & The Pharmaceutical Society of Great Britain. Handbook of pharmaceutical excipients. Londen: The Pharmaceutical Press 1986, 241–2.Google Scholar
  3. 3.
    17th report of the FAO/WHO Expert Committee on Food Additives. WHO Tech Rep Ser no 539, 1974.Google Scholar
  4. 4.
    Van derLaan JW, DeWaal EJ, Peters-Volleberg GWM. Toxicologische evaluatie van propyleenglycol als oplosmiddel in hoestmiddelen [Toxicological evaluation of propylene glycol as solvent in cough medicines]. Pharm Weekbl 1994;129(27):687–8.Google Scholar
  5. 5.
    Laan JWvan der, Nijenhuis Aten. Gebruiksduur propyleenglycol [Duration of use of propylene glycol]. Pharm Weekbl 1995;130(14):345.Google Scholar
  6. 6.
    Moolenaar F, Huizinga T. Rectale irritatie van vehicula geschikt voor diazepam micro-klysma's [Rectal irritation of vehiculae suitable for diazepam micro-enemas]. Pharm Weekbl 1981;116:33–4.Google Scholar
  7. 7.
    Kollöffel WJ, Driessen FGWHM, Goldhoorn PB. Rectal administration of paracetamol: a comparison of a solution and suppositories in adult volunteers. Pharm World Sci 1996;18:26–9.Google Scholar
  8. 8.
    Speth PAJ, Vree TB, Neilen NFM, DeMulder PHM, Newell DR, Gore ME et al. Propylene glycol pharmacokinetics and effects after intravenous infusions in humans. Ther Drug Monit 1987;9:255–8.Google Scholar
  9. 9.
    Yu DK, Elmquist WF, Sawchuk RJ. Pharmacokinetics of propylene glycol in humans during multiple dosing regimens. J Pharm Sci 1985;74(8):876–9.Google Scholar
  10. 10.
    Kollöffel WJ, Driessen FGWHM, Goldhoorn PB. Plasma-concentration profiles after pre-operative rectal administration of a solution of paracetamol in children. Pharm World Sci, 1996;18(3):105–8.Google Scholar
  11. 11.
    Yu DK, Sawchuk RJ. Gas-liquid chromatographic determination of propylene glycol in plasma and urine. Clin Chem 1983;29(12):2088–90.Google Scholar
  12. 12.
    Proost JH, Meijer DKF. MW/PHARM, an integrated software package for drug dosage regimen calculation and therapeutic drug monitoring. Comput Biol Med 1992;22:155–63.Google Scholar
  13. 13.
    Wagner JG, ed. Fundamentals of clinical pharmacokinetics. Hamilton, Illinois: Drug Intelligence Publications, 1975.Google Scholar
  14. 14.
    Demey HE, Daelemans RA, Verpooten GA, DeBroe ME, VanCampenhout CM, Lakiere FV, et al. Propylene glycol-induced side effects during intravenous nitroglycerin therapy. Intensive Care Med 1988;14(3):221–6.Google Scholar
  15. 15.
    Fligner CL, Jack R, Twiggs GA, Raisys VA. Hyperosmolality induced by propylene glycol. A complication of silver sulfadiazine therapy. JAMA 1985;253(11):1606–9.Google Scholar
  16. 16.
    Kelner MJ, Bailey DN. Propylene glycol as a cause of lactic acidosis. J Anal Toxicol 1985;9(1):40–2.Google Scholar
  17. 17.
    Kulick MI, Wong R, Okarma TB, Falces E, Berkowitz RL. Prospective study of side effects associated with the use of silver sulfadiazine in severely burned patients. Ann Plast Surg 1985;14(5):407–19.Google Scholar
  18. 18.
    Lolin Y, Francis DA, Flanagan RJ, Little P, Lascelles PT. Cerebral depression due to propylene glycol in a patient with chronic epilepsy — the value of the osmolal gap in diagnosis. Postgrad Med J 1988;64(754):610–3.Google Scholar
  19. 19.
    Huggon I, James I, Macrae D. Hyperosmolality related to propylene glycol in an infant treated with enoximone infusion. Br Med J 1990;301(6742):19–20.Google Scholar
  20. 20.
    Bedichek E, Kirschbaum B. A case of propylene glycol toxic reaction associated with etomidate infusion. Arch Intern Med 1991;151(11):2297–8.Google Scholar
  21. 21.
    Cate JC, Hedrick R. Propylene glycol intoxication and lactic acidosis. N Engl J Med 1980;303:1237.Google Scholar
  22. 22.
    Bekeris L, Baker C, Fenton J, Kimball D, Bermes E. Propylene glycol as a cause of an elevated serum osmolality. Am J Clin Pathol 1979;72:633–6.Google Scholar
  23. 23.
    Glasgow AM, Boeckx RL, Miller MK, MacDonald MG, August GP. Hyperosmolality in small infants due to propylene glycol. Pediatrics 1983;72(3):353–5.Google Scholar
  24. 24.
    Kulick MI, Lewis NS, Bansal V, Warpeha R. Hyperosmolality in the burn patient: analysis of an osmolal discrepancy. J Trauma 1980;20(3):223–8.Google Scholar
  25. 25.
    Snawder JE, Benson RW, Leakey JE, Roberts DW. The effect of propylene glycol on the P450-dependent metabolism of acetaminophen and other chemicals in subcellular fractions of mouse liver. Life Sci 1993;52(2):183–9.Google Scholar

Copyright information

© Kluwer Academic Publishers 1996

Authors and Affiliations

  • W. J. Kollöffel
    • 1
  • L. E. A. Weekers
    • 2
  • P. B. Goldhoorn
    • 2
  1. 1.Department of Clinical PharmacyTwenteborg Hospitalthe Netherlands
  2. 2.Department of Clinical PharmacyTwenteborg Hospitalthe Netherlands

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