A century of dissolution research: From Noyes and Whitney to the Biopharmaceutics Classification System

Abstract

Dissolution research started to develop about 100 years ago as a field of physical chemistry and since then important progress has been made. However, explicit interest in drug related dissolution has grown only since the realisation that dissolution is an important factor of drug bioavailability in the 1950s. This review attempts to account the most important developments in the field, from a historical point of view. It is structured in a chronological order, from the theoretical foundations of dissolution, developed in the first half of the 20th century, and the development of a relationship between dissolution and bioavailability in the 1950s, going to the more recent developments in the framework of the Biopharmaceutics Classification System (BCS). Research on relevant fields of pharmaceutical technology, like sustained release formulations, where drug dissolution plays an important role, is reviewed. The review concludes with the modern trends on drug dissolution research and their regulatory implications.

Groundnut oil based emulsion gels for passive and iontophoretic delivery of therapeutics

“…Korsmeyer-Peppas model was used to examine the release pattern of the drugs from the developed formulations. [32] The diffusion parameters (release rate constant: K; and release exponent: n) of the drugs were estimated using Korsmeyer-Peppas model (Equation 4). Among the metronidazole containing formulations, the release rate constant was highest in Metrogyl ® followed by OG5-80M and OG7-45M, respectively (Table 2).…”

Design and Statistical Evaluation of a Multiunit Delivery System Containing Nisoldipine-Soluplus® Solid Dispersion for Hypertension Chronotherapy

“…In the case of multiple response variables, an overall desirability function is used [14] to ascertain the optimum levels of the factors studied to provide the desired outcome (maximize %DE and minimize T90). Taking into consideration the effect of the independent variables on the studied parameters, the levels of these factors were determined using the generalized desirability function to maximize all the The magnitude of effect among the factors can be studied by comparing the coefficients.…”

Applications of USP apparatus 3 in assessing the in vitro release of solid oral dosage forms

“…As a result of the greater exposure time, the performance of extended-release products is more susceptible to the mechanical forces and physicochemical conditions of the luminal environment (Dokoumetzidis, Macheras, 2006). Since the reciprocating cylinder method enables these conditions to be simulated, it is reasonable to suppose that this apparatus is more efficient than the basket and paddle methods in predicting the in vivo performance of extended-release dosage forms (Krämer, Grady, Gajendran, 2005;Pezzini, Ferraz, 2009).…”

“…Where the absorption process is rapid, dissolution may be the stage that controls the introduction of the drug into the bloodstream (Amidon et al, 1995;Emami, 2006). This, in turn, led to universal recognition that the dissolution test is indispensable in the development, quality assurance and post-marketing authorization modifications of solid oral dosage forms (Dokoumetzidis, Macheras, 2006;Azarmi, Roa, Löbenberg, 2007).…”

“…With regards to the apparatuses used in the dissolution test, the basket apparatus (USP apparatus 1) was the first to be adopted by the U.S. Pharmacopeia in 1970, while the paddle apparatus (USP apparatus 2) was recognized in 1978, as the result of ongoing developments 266 in the area and a growing interest in matters related to dissolution (Dokoumetzidis, Macheras, 2006).…”