Is bisacodyl absorbed at all from suppositories in man?

Int J Pharm. 2000 Feb 25;196(1):11-20. doi: 10.1016/s0378-5173(99)00385-3.


A HPLC procedure was developed to determine free BHPM in human plasma and urine after prior deconjugation of its glucuronides with glucuronidase. A single dose administration of a 10 mg bisacodyl suppository from Glaxo Wellcome, Poznań (Poland) to 16 volunteers each resulted in its low active metabolite (BHPM) plasma levels (10-55 microgram l(-1)) according to general assumptions. Its prompt laxative effect appeared within 56.6+/-10.8 min. The calculated serum half-life time of BHPM glucuronide excretion in urine was approximately 7.32+/-0.99 h. BHPM was excreted in urine in only 3. 36+/-0.52% if compared with the above bisacodyl rectal dose administered. Any relationship between BHPM plasma and/or urine levels and its laxative action does not occur. These results confirm the thesis that the laxative action of bisacodyl suppositories is initiated through a direct interaction of the drug in the rectum.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Bisacodyl / administration & dosage
  • Bisacodyl / blood
  • Bisacodyl / pharmacokinetics*
  • Bisacodyl / urine
  • Cathartics / administration & dosage
  • Cathartics / pharmacokinetics*
  • Chromatography, High Pressure Liquid
  • Defecation / drug effects
  • Female
  • Humans
  • Intestinal Absorption
  • Male
  • Randomized Controlled Trials as Topic
  • Rectum / drug effects
  • Rectum / metabolism*
  • Suppositories


  • Cathartics
  • Suppositories
  • Bisacodyl