Jamie Clayton, Phil Bone and Kyu Mok Hwang discuss the value of analyses such as mercury porosimetry and powder rheology in characterising excipients for gastroretentive tablet formulation, and go on to detail a case study investigating polymer excipients for a novel bilayer floating tablet.
For certain drugs, formulation into a gastroretentive (GR) oral solid dosage (OSD) form can be a successful strategy for improving bioavailability and therapeutic efficacy. Such drugs include those in Biopharmaceutics Classification System (BCS) Class IV, which covers actives with low solubility and low permeability, and as such present some of the toughest formulation challenges. Prime targets for GR OSD forms are drugs for local action in the stomach, with a narrow absorption window (NAW) or with poor solubility or stability under alkaline conditions. Improving the gastroretention of such drugs can boost efficacy, and at the same time enable a streamlined dosing regime via sustained or controlled release. Expandable, swelling, floating, muco-adhesive and high-density systems are all routinely deployed depending on the properties of the drug and the required delivery profile.
This article considers the specific challenge of developing floating GR OSD forms and the analytical techniques that can be deployed to support their formulation. Experimental work by researchers at the School of Pharmacy, Sungkyunkwan University highlights the value and relevance of porosity and powder flowability measurements in the development of novel, bilayer GR tablets.
Read the full article “Analytical Techniques for the Formulation of Gastroretentive Tablets” in OnDrugDelivery.