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Is bisacodyl absorbed at all from suppositories in man?
1Department of Physical Chemistry, K. Marcinkowski University of Medical Sciences, 6 Swiecickiego Street, 60 781, Poznań, Poland.
International Journal of Pharmaceutics
|February 17, 2000
Summary
Bisacodyl suppositories
Area of Science:
- Pharmacokinetics
- Drug Metabolism
Background:
- Bisacodyl is a widely used stimulant laxative.
- Its active metabolite, bis-(p-hydroxyphenyl)-pyridyl-2-methane (BHPM), is responsible for the laxative effect.
- Understanding the pharmacokinetics of BHPM is crucial for optimizing bisacodyl therapy.
Purpose of the Study:
- To develop and validate a HPLC method for quantifying free BHPM in human plasma and urine.
- To investigate the pharmacokinetics of BHPM after rectal administration of bisacodyl.
- To explore the relationship between BHPM levels and laxative effect.
Main Methods:
- High-performance liquid chromatography (HPLC) was employed for BHPM determination.
- Samples were pre-treated with glucuronidase for deconjugation of BHPM glucuronides.
- 16 healthy volunteers received a single 10 mg bisacodyl suppository.
Main Results:
- Low plasma concentrations of BHPM were observed (10-55 µg/L).
- Laxative effect onset was within 56.6 ± 10.8 minutes.
- Urinary excretion of BHPM was low (3.36 ± 0.52%), with a half-life of approximately 7.32 hours.
- No correlation was found between BHPM levels and laxative efficacy.
Conclusions:
- The study confirms that the laxative action of bisacodyl suppositories is mediated by direct rectal interaction.
- BHPM plasma and urine levels do not correlate with the observed laxative effect.
- The developed HPLC method is suitable for BHPM pharmacokinetic studies.
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