Improvement of bioavailability of poorly absorbed drugs. IV. Mechanism of the promoting effect of medium chain glyceride on the rectal absorption of water soluble drugs

J Pharmacobiodyn. 1985 Aug;8(8):645-52. doi: 10.1248/bpb1978.8.645.

Abstract

The mechanisms of the promoting effect of medium chain glyceride (MCG) containing glyceryl mono-, di- and tri-caprylate on rectal absorption of water soluble drugs were investigated. It was found that the solubility behavior of the drugs in mucosal fluids on the surface of the membrane are critical factor for the enhanced rectal absorption. Moreover, the drugs to be readily absorbed from MCG base may be ones of low partition coefficients to MCG phase as well as high solubility in water. And it was found that MCG can't be absorbed from the rectum, different from oral administration, suggesting an interaction of MCG with absorption membrane, rather than the carrier effect of MCG itself. Furthermore, from the results in the pretreatment experiments and additional administration of MCG alone, it was suggested that the interactions of MCG with the membrane components, as well as the induction of biological or physiological changes, may be at least partly responsible for the promoting effect of MCG.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / metabolism
  • Biological Availability
  • Blood Glucose / metabolism
  • Cattle
  • Coloring Agents
  • Excipients
  • Fatty Acids, Nonesterified / blood
  • Glycerides / blood
  • Glycerides / pharmacology*
  • Insulin / metabolism
  • Intestinal Absorption / drug effects*
  • Lactams
  • Male
  • Rats
  • Rats, Inbred Strains
  • Rectum / metabolism
  • Solubility
  • Stimulation, Chemical

Substances

  • Anti-Bacterial Agents
  • Blood Glucose
  • Coloring Agents
  • Excipients
  • Fatty Acids, Nonesterified
  • Glycerides
  • Insulin
  • Lactams