Enhanced rectal absorption of [Asu1,7]-eel calcitonin in rats using polyacrylic acid aqueous gel base

J Pharm Sci. 1984 Oct;73(10):1366-8. doi: 10.1002/jps.2600731010.

Abstract

The effects of polyacrylic acid aqueous gel on the absorption of rectally administered [Asu1,7]-eel calcitonin, a calcitonin analogue, were investigated in rats. The [Asu1,7]-eel calcitonin (1 U/kg) was given into the rectal loop in gel bases at various pH (5.5-8.5) and polyacrylic acid concentrations (0.01-1.0% w/v). The maximum hypocalcemic effect was obtained in approximately 30 min after administration of the analogue in a 0.1% w/v polyacrylic acid gel base at pH 5.5. The plasma calcium level decreased by approximately 18% from the initial level. Rectal administration in vehicles such as polyethylene glycol 1000, triglyceride fatty acid mixture base, or saline solution had little or no hypocalcemic effect at a dose of 5 U/kg. The results indicated that a polyacrylic acid aqueous gel base significantly improved the absorption of this analogue. Furthermore, rectal administration in a polyacrylic acid gel base (0.1% w/v; pH 5.5) required a dose 35 times greater than an intravenously administered dose to achieve an equivalent hypocalcemic effect.

MeSH terms

  • Acrylic Resins
  • Animals
  • Biological Availability
  • Calcitonin / analogs & derivatives*
  • Calcitonin / metabolism
  • Calcium / metabolism
  • Gels
  • Intestinal Absorption
  • Intestinal Mucosa / metabolism
  • Kinetics
  • Male
  • Proteins / metabolism
  • Rats
  • Rats, Inbred Strains
  • Rectum / metabolism*
  • Suppositories

Substances

  • Acrylic Resins
  • Gels
  • Proteins
  • Suppositories
  • carbopol 940
  • Calcitonin
  • Calcium
  • elcatonin