CNS Update: Prediction of PK parameters and dose of pregabalin GR formulation in healthy adults


eMediNexus    22 January 2023

To forecast pregabalins individualized doses in healthy adults, paediatrics and renal impaired geriatric patients a study was conducted. It employed a physiological based pharmacokinetic (PBPK) model for gastroretentive (GR) formulation producing identical pharmacokinetics to that of the immediate-release (IR) formulation to acquire doses depending on an individuals physiological needs.


The PBPK model of pregabalin was designed for various population subsets considering various OD doses of the IR and GR formulations to forecast pharmacokinetics (PK) parameters in fasting as well as fed conditions after administering pregabalin 300 mg of IR and 330 mg of sustained-release (SR) formulations. The doses in the renal impaired geriatrics and healthy pediatric population were calculated using a dose decremental method and were determined at which the identical PK like that of the reported values in healthy adults were acquired.


Healthy adults acquired comparable PK parameters after receiving pregabalin 300 mg of IR and 330 mg of SR formulation in fasting as well as fed state, without any effect of food on the bioavailability of pregabalin. Neonates to infants and toddlers acquired AUC0-48 similar to the adults after a 40–82 mg dose of GR formulation of pregabalin. Pre-schooled and schooled virtual populations acquired AUC0-48 similar to the adults after a dose of 40–170 mg and adolescents acquired it after a dose of 40–330 mg. Renal impaired geriatric with CLcr, 60, 30, and 15 ml/min had to receive 220–330, 110 to 220 and 55–85 mg, respectively to acquire the same level of PK parameters as an elder individual with normal CLcr (90 ml/min) after administration of 330 mg of gastroretentive formulation.


This PBPK model is useful and effective in predicting the dose for the modified GR pregabalin formulations in special populations.


Source: Journal of Drug Delivery Science and Technology,2021;63. https://doi.org/10.1016/j.jddst.2021.102548

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