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Development and in vitro-in vivo relationship of controlled-release microparticles loaded with tramadol hydrochloride
journal contributionposted on 2023-06-08, 19:21 authored by Muhammad Naeem Aamir, Mahmood Ahmad, Naveed Akhtar, Ghulam Murtaza, Shujat Ali Khan, Shahiq-uz-Zaman, Ali Nokhodchi
In conclusion, the controlled-release microparticles of TmH can be developed via phase separation method. The development and optimization of controlled-release microparticles of tramadol hydrochloride (TmH) for the oral delivery and their in vitro and in vivo correlation was prime objective of the present study. Four formulations of controlled-released microparticles were developed and optimized in terms of encapsulation efficiency, dissolution study and release kinetics. Among all formulated microparticles F-3 (ratio of TmH:EC 1:2) and F-4 (ratio of TmH:EC 1:3) presented the better characteristics in reference to entrapment efficiency, release kinetics and dissolution profile compared to other formulations (F-1, F-2). For in vivo analysis a new HPLC analytical method was developed and validated. The optimized formulations were subjected to in vivo studies to calculate various pharmacokinetic parameters, i.e., Cmax, tmax, AUC0–8 and MRT. The in vitro dissolution and in vivo absorption data was correlated with the help of Wagner–Nelson method. F-3 showed a good in vitro–in vivo correlation with a correlation determination of 0.9957. Moreover, lower Tmax, t1/2 and MRT, and higher values of Cmax and Ke were observed for F-3. The control formulation (immediate-release) presented lowest values of t1/2, MRT and Tmax but the highest values of Cmax and Ke. The controlled-release microparticles (F-3 and F-4) could sustain the drug release within therapeutic level up to 24 h and good IVIVC is expected from them.
JournalInternational Journal of Pharmaceutics
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- Chemistry Publications
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