The use of phenothiazines to enhance the rectal absorption of water-soluble compounds

J Pharm Pharmacol. 1984 Apr;36(4):286-8. doi: 10.1111/j.2042-7158.1984.tb04375.x.

Abstract

The ability of phenothiazines to enhance the rectal absorption of sodium cefoxitin and gentamicin sulphate from aqueous formulations was examined in rats. In the absence of absorption-promoting adjuvants, sodium cefoxitin and gentamicin sulphate bioavailabilities from the rectal compartment were less than 5% of the corresponding intravenous administration. In aqueous microenemas containing 20 mg ml-1 phenothiazine, sodium cefoxitin bioavailability increased to 16-62%, while gentamicin sulphate bioavailability increased to 74-146%. The absorption-promoting potential of chlorpromazine and perphenazine was concentration-dependent, with significant increases in gentamicin sulphate absorption occurring with 1 mg ml-1 chlorpromazine or 2.5 mg ml-1 perphenazine. Maximal gentamicin sulphate bioavailability and serum concentrations were achieved with 10 mg ml-1 chlorpromazine or 20 mg ml-1 perphenazine. The findings indicate that the phenothiazines, which are well absorbed rectally, also significantly enhance the rectal absorption of water-soluble, poorly absorbed compounds.

MeSH terms

  • Animals
  • Cefoxitin / metabolism
  • Gentamicins / metabolism
  • Intestinal Absorption / drug effects*
  • Male
  • Phenothiazines / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Rectum / metabolism
  • Stimulation, Chemical

Substances

  • Gentamicins
  • Phenothiazines
  • Cefoxitin