The " dissolution" method: a low volume, in vitro apparatus for assessing the dissolution/precipitation behaviour of an active pharmaceutical ingredient under biorelevant conditions.

This paper describes a low volume, in vitro apparatus for investigating the dissolution and precipitation behaviour of active pharmaceutical ingredients (APIs) under a wide range of experimental conditions and dissolution media. The apparatus has automated and dynamic pH control, allowing the simulated passage of drugs through the gastrointestinal tract (GIT). Experiments can be performed in the presence of biorelevant media and excipients, providing information related to the predicted behaviour of APIs under physiological conditions. The technique is described in detail and results are presented for a number of neutral, basic, acidic and ampholytic drug compounds.

[1]  Karl Box,et al.  New Ideas about the Solubility of Drugs , 2009, Chemistry & biodiversity.

[2]  T. Viegas,et al.  Measurement of Intrinsic Drug Dissolution Rates Using Two Types of Apparatus , 2001 .

[3]  Lawrence X. Yu,et al.  Feasibility studies of utilizing disk intrinsic dissolution rate to classify drugs. , 2004, International journal of pharmaceutics.

[4]  R. Löbenberg,et al.  Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. , 2000, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[5]  J. E. Carter,et al.  In Vitro and in Vivo Testing and Correlation for Oral Controlled/Modified-Release Dosage Forms , 2004, Pharmaceutical Research.

[6]  Alex Avdeef,et al.  Miniaturized Rotating Disk Intrinsic Dissolution Rate Measurement: Effects of Buffer Capacity in Comparisons to Traditional Wood’s Apparatus , 2008, Pharmaceutical Research.

[7]  S. Mcclintock,et al.  Developing a Discriminating Dissolution Procedure for a Dual Active Pharmaceutical Product with Unique Solubility Characteristics , 2004 .

[8]  Margareth R. C. Marques.  Dissolution Media Simulating Fasted and Fed States , 2004 .

[9]  Leon Shargel,et al.  Description of the Upcoming Change in Data Analysis for USP Dissolution Performance Verification Tests , 2009 .

[10]  J. Comer,et al.  Study of pH-dependent solubility of organic bases. Revisit of Henderson-Hasselbalch relationship. , 2010, Analytica chimica acta.

[11]  V. Shah,et al.  Dissolution: a Continuing Perspective , 2004 .

[12]  R. Brockson,et al.  Intrinsic Dissolution Performance Testing of the USP Dissolution Apparatus 2 (Rotating Paddle) Using Modified Salicylic Acid Calibrator Tablets: Proof of Principle , 2003 .

[13]  M A Mintun,et al.  Dissolution kinetics of carboxylic acids I: effect of pH under unbuffered conditions. , 1981, Journal of pharmaceutical sciences.

[14]  Jerome P. Skelly,et al.  In vitro/in vivo correlations in biopharmaceutics: scientific and regulatory implications , 2011, European Journal of Drug Metabolism and Pharmacokinetics.