Optimizing Drug Partition Coefficient: A BCS Class III Molecule Approach with Complexation in Tablet Preparation

Abstract

Opioid-induced constipation (OIC) is one of the most common, under-recognized, and under-treated side effects of opioid analgesics. Being classified as a BCS Class III drug X compound use as a OIC treatment, Drug X has high water solubility and low partition coefficient. To overcome this challenge, we employed various formulation techniques like spray drying, top spray granulation, and RMG intra-extrusion granulation, along with different surfactant combinations. Notably, docusate sodium replaced SLS to achieve the desired partition coefficient range and match the dissolution profile of the innovator drug. Additionally, we conducted thorough tablet characterization and stability evaluations after formulation to ensure that the tablets were as effective and stable as the innovator tablet.