Biorelevant Drug Release of Metformin Dosage Forms Using Complementary in Vitro Tools

Forest Row, Scientific R&D, Yair Technologies Ltd, United , United Kingdom

Experimental Experiments were carried out at 37oC using 500 mg Metformin HCl IR (Glucophage®, BMS) and ER (Glucophage SR®, Merck Serono) tablets. 0.1 M HCl + 2 g/L NaCl, pH 1.2 and phosphate buffer, pH6.8 were used as dissolution media. FloVitro™ is a transfer system consisting of three cells representing gastric, intestinal and systemic absorption compartments (Figure 1). FloVitro™ dissolution was studied using flow rates of 1 and 2 mL/min for HCl and phosphate buffer, respectively. Metformin drug concentration was measured over 16 or 24 hours using inline spectrophotometry (247 nm) for the IR and ER tablets, respectively.

---

Short Biography of Presenting Author

Purpose A key challenge in formulation development is correlating data from traditional dissolution tests with in vivo outcomes. In this study, two proprietary dissolution technologies were utilized to investigate the effect of formulation differences on drug release for immediate (IR) and extended (ER) release Metformin tablets. The Dow Chemical Company’s FloVitro™ biorelevant dissolution instrument was implemented to achieve IVIVR for the IR dosage form and for in vitro comparison of IR and ER tablets. Mechanistic differences accounting for drug release were investigated by real-time UV/vis imaging using the Sirius SDi2 (surface dissolution imaging) platform.