New Approach for the Application of USP Apparatus 3 in Dissolution Tests: Case Studies of Three Antihypertensive Immediate-Release Tablets

Abstract

The USP Apparatus 3 is a compendial dissolution Apparatus that has been mainly used to assess the performance of modified-release drug products. However, this Apparatus can be applied to dissolution testing of immediate-release tablets as well, with several advantages such as lower consumption of dissolution media, reduced setup time in quality control routine, and minimized hydrodynamic issues. In this work, three immediate-release (IR) tablets containing antihypertensive drugs of different Biopharmaceutic Classification System (BCS) classes were evaluated in order to assess the possible interchangeability between the official dissolution method using typical USP Apparatus 1 or 2 and the proposed methods using USP Apparatus 3. Depending on the selection of the appropriate operational conditions, such as dip rate and sieve mesh size, it was observed that USP Apparatus 3 could provide similar dissolution profiles compared to USP Apparatus 1 or 2 to the drug products tested. In addition, USP Apparatus 3 avoided conning issues related to USP Apparatus 2. The successful application of USP Apparatus 3 in dissolution tests for IR drug products depends on the definition of specific test conditions for each product, considering all the equipment variables, as well as drug and formulation characteristics.

Advancements in Dissolution Testing of Oral and Non-oral Formulations

“…The research paper "New Approach for the Application of USP Apparatus 3 in Dissolution Tests: Case Studies of Three Antihypertensive Immediate-Release Tablets" describes a method where the reciprocating cylinder apparatus (USP apparatus 3), an apparatus that was mainly established for in vitro drug release experiments for ER formulations, was successfully applied in designing dissolution methods for oral tablet formulations of three antihypertensive drugs with different solubilities. For the dosage forms screened in this study USP apparatus 3based methods presented with a higher robustness than a standard paddle (USP apparatus 2) method (17). This case example shows that even though there is currently a huge interest for developing bio-predictive methods, the development of QC methods based on compendial dissolution equipment is also still a challenge.…”

The Importance of Dissolution Tests to Evaluate Quality of Dietary Supplements: Case Study of Controlled Release Caffeine Capsules

“…API absorption depends on its dissolution and solubilization under physiological conditions, and the permeability across the gastrointestinal (GI) tract. Because of the critical nature of the first steps, in vitro dissolution is an important and necessary tool to predict the human biological response (8). For this reason, dissolution testing is required for quality control of solid dosage forms containing APIs (medicines), but it is not mandatory for dietary supplements.…”

“…Dissolution testing is an important instrument for characterizing the performance of oral solid dosage forms. Its significance is founded on the point that for an API to be effective, it must first be released from the product and dissolve in the GI fluids previously absorption (8).…”