RELATIVE BIOAVAILABILITY OF RISEDRONATE SODIUM ADMINISTERED IN SUPERABSORBENT COPOLYMER PARTICLES VERSUS ORAL SOLUTION TO NORMAL HEALTHY RABBITS

Acta Pol Pharm. 2016 Sep;73(5):1267-1274.

Abstract

In this study, sustained release superabsorbent copolymer particles have been prepared and analyzed to increase bioavailability of orally administered risedronate sodium. Formulations were prepared by free radical polymerization of combination of 2-hydroxyethyl methacrylate (HEMA), itaconic acid (IA), polyvinyl pyrrolidone (PVP) / chitosan (CTS) by using ethylene glycol dimethacrylate (EGDMA) as crosslinker, potassium persulfate as initiator, and N,N,N,N-tetramethylethylene diamine as activator. Formulations were successfully loaded with risedronate sodium. Formulations as gel particles encapsulated in hard gelatin were analyzed to estimate drug content. The maximum plasma drug concentration (C.) and its corresponding time (Tmax.), area under the curve and relative bioavailability (with reference to oral solution of drug administered) were calculated. It was found a marked increase in Tmax. with lower Cmax. that confirmed the multiparticulte system to deliver drug at controlled rate. The results of relative bioavailability after oral administration of these formulations indicated a remarkable increase in the bioavailability.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Chitosan / chemistry
  • Drug Compounding
  • Methacrylates / chemistry
  • Povidone / chemistry
  • Rabbits
  • Risedronic Acid / administration & dosage
  • Risedronic Acid / pharmacokinetics*
  • Solutions
  • Succinates / chemistry

Substances

  • Methacrylates
  • Solutions
  • Succinates
  • hydroxyethyl methacrylate
  • Chitosan
  • Povidone
  • Risedronic Acid
  • itaconic acid