TY - JOUR AU - Chandra, Amrish PY - 2022/06/15 Y2 - 2024/03/29 TI - Identification of biorelevant dissolution media to assess biopharmaceutical performance of erlotinib formulation with enhanced bioavailability using physiologybased pharmacokinetic modeling JF - Asian Journal of Pharmaceutics (AJP) JA - AJP VL - 16 IS - 2 SE - ORIGINAL ARTICLES DO - 10.22377/ajp.v16i2.4389 UR - https://asiapharmaceutics.info/index.php/ajp/article/view/4389 SP - AB - <p>Aim: The aim of the present work was to predict the bioavailability (BA) of poorly soluble drug. In vitro dissolution<br>of selected BCS Class II drug was conducted in different dissolution media to identify the discriminatory behaviors<br>of the dissolution media. Further, the development of physiology-based pharmacokinetic modeling performed<br>using GastroPlus® for BA predictions of formulation showing enhanced dissolution. Study Design: Using<br>GastroPlus® software (Simulations Plus, Lancaster, CA), a physiology-based pharmacokinetic model for<br>erlotinib was developed. Erlotinib absorption was described using the advanced compartmental absorption<br>and transit model. The input parameters for the simulation were either determined experimentally or gathered<br>from the literature. Place and Duration of Study: Amity Institute of Pharmacy, Noida. Methodology: In vitro<br>dissolution studies were conducted and data were analyze to find the biorelevent dissolution media. GastroPlus®<br>model was built to predict the Cmax and AUC and also was validated for the prediction error &lt;10%. Validated<br>model was used to predict the BA parameters of optimized formulation using the dissolution profile. Results:<br>Based on predicted T/R ratio, it is observed that optimized formulation shows approximately ~ 25% higher<br>rate of absorption and bioavailability. Conclusion: Erlotinib tablet formulation was prepared using micronized<br>drug substance, optimized formulation was subjected to various dissolution tests and biorelevent media was<br>identified based on best fit/correlation with the deconvulated profile, which was further used for simulation<br>modeling and BA prediction. Micronization can be used as a technique to enhance the drug dissolution of BCS<br>Class II drugs and corresponding BA. IVIVR GastroPlus modeling and simulations can be useful tool to assess<br>the biopharmaceutical performance for initial screening and further taking up the optimized formulation for<br>clinical studies.</p> ER -