In vitro release of new designs of modified-release tramadol hydrochloride included in a polymer matrix

Pak J Pharm Sci. 2021 Sep;34(5):1783-1790.

Abstract

Tramadol reaches therapeutic plasma concentrations in a time interval of 0.5 to 1.7 hours, so it is necessary to dose 4 times/day, which reduces compliance with the dose and the effectiveness of the treatment. Design formulations of tramadol that allow the release time to be prolonged, surpassing those obtained with the commercial product and tramadol without excipients. Several formulations of 5% tramadol hydrochloride were designed in a matrix system based on poloxamer 407 at different concentrations (10%, 14%, 17%, and 20%). In vitro release studies were performed, using a spectrophotometer at a wavelength of 273.15 nm; were compared the results with tramadol without polymeric supplements and with the commercial formulation samples were taken in a period of time from 0.25 to 72 hours, and also compared the use or absence of dialysis membrane with a porosity of 50 kilodaltons was. With the use of the membrane, the designed formulations had a release of 98%, 50%, 23%, 16% at 72 hours, respectively, different from the commercial product and the tramadol formulation without excipients released the 24 hours. Without using dialysis membranes, a 90-100% release was achieved in the 10% and 14% formulation at 36 hours. The 17% and 20% formulation at 48 hours and the commercial formulation and tramadol without excipient were released within 2 hours. Modified release formulations were obtained, which retain and prolong the release of tramadol compared to the commercial product. Therefore, we propose to conduct further in vivo model experiments to confirm our conclusion.

MeSH terms

  • Delayed-Action Preparations
  • Drug Compounding*
  • Drug Liberation*
  • Polymers / chemistry*
  • Rheology
  • Tramadol / chemistry*
  • Tramadol / pharmacokinetics

Substances

  • Delayed-Action Preparations
  • Polymers
  • Tramadol