Improved therapeutic potential of tapentadol employing cationic exchange resins as carriers in neuropathic pain: evidence from pharmacokinetic and pharmacodynamics study

Abstract

Current investigation was endeavoured to overcome problem of poor palatability and bioavailability of centrally acting analgesic, tapentadol (TAP) by formulating controlled release drug-resin complexes (DRCs). The technology encompassed in preparation of DRCs involved chemisorption of TAP to weak cationic resins (KyronT-134 and Tulsion335) by batch method. Various formulation variables like drug-resin ratio, pH, resin activation and swelling time were optimized to achieve maximum drug loading in DRCs. FT-IR, DSC, pXRD, in vitro release study under bio-relevant condition of mouth and in vivo sensory taste evaluation established formation of taste masked DRC whereas dissolution study assured prolonged drug release behaviour of optimized DRC. Among DRCs, TAP-KyronT-134 complex exhibited higher drug loading (80.89 ± 4.56%), stability and prolonged release profile (10 h) without any detectable amount of drug release under salivary conditions. Pharmacokinetic studies in wistar rats revealed increased Tmax (2.67-fold), MRT (1.94-fold), elimination half-life (2.79-fold) and relative oral bioavailability (2.62-fold) of TAP on oral administration of optimized formulation compared to TAP solution. Furthermore, pharmacodynamics study confessed higher potential of DRC in attenuating chronic injury induced tactile allodynia for prolonged duration. In conclusion, the method developed is easily scalable and holds potential for commercialization with an evidence of obtaining more efficacious neuropathic pain management therapy.

Fexofenadine Hydrochloride Dispersible Tablets: A Taste Masking Strategy using Ion Exchange Resin

“…9 Sharma and Soni et al, worked on overcoming the poor palatability of tapantadol with the help of Kyron T-134 ® and Tulsion 355 ® . 10 Sivaneswari and coworkers used Duolite AP 143® to prepare a taste-masked pediatric suspension of levetiracetam. 11 Indion 204 ® was used to mask the taste of etoricoxib by Patra et al, 12 Panraksa et al, used Dowex-50® cation exchange resin to mask the taste of nizatidine.…”

Efectividad del tapentadol en el paciente oncológico con dolor neuropático

“…Existen múltiples estudios y autores que han encontrado que es un fármaco efectivo para el tratamiento del DN, con una adecuada tolerabilidad y que mejora la calidad de vida de los pacientes posterior a su uso, sobre todo en pacientes con resistencia a los opioides [11][12][13] .…”

Effectiveness of Tapentadol in cancer patients with neuropathic pain

“…There are multiple studies and authors that have found that it is an effective drug for the treatment of NP, with adequate tolerability, and that it improves the quality of life of patients after its use, especially in patients with opioid resistance [11][12][13] .…”