Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds in Biorelevant Dissolution Media

Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media.

A series of poorly soluble BCS class II compounds with "grease ball" characteristics were assessed for solubility and dissolution rate in biorelevant dissolution media (BDM) with the purpose of investigating which molecular structures gain most in solubility when dissolved under physiologically relevant conditions. The compounds were studied in four media (simulated intestinal fluid in fasted (...

Simplified Biorelevant Media for Screening Dissolution Performance of Poorly Soluble Drugs

8 INTRODUCTION Simulation of gastrointestinal conditions is essential to adequately predict the in vivo behavior of poorly soluble drugs. Simulating small intestinal conditions with biorelevant media such as fasted state simulated intestinal fluid (FaSSIF) and fed state simulated intestinal fluid (FeSSIF) has become standard practice in many dissolution laboratories (1–6). However, due to their...

Impact of physiologically relevant viscosity on intrinsic dissolution rate of poorly soluble compounds in simulated gastric media

In order to simulate the in vivo dissolution of drugs, biorelevant dissolution media (BDM), simulating the gastric or intestinal juices are often employed. For gastric BDM, pH, surface tension and osmolality is simulated, however, viscosity has, to our knowledge not been taken into account. The dissolution rate of a drug compound is influenced by the viscosity of the dissolution medium. In the ...

Acceptable Analytical Practices for Dissolution Testing of Poorly Soluble Compounds

56 Pharmaceutical Technology DECEMBER 2004 Cynthia K. Brown is the head of analytical development in pharmaceutical product research and development at Eli Lilly and Company. Hitesh P. Chokshi, PhD, is a research director in pharmaceutical and analytical R&D at Hoffmann-La Roche Inc. Beverly Nickerson, PhD, is an associate research fellow in analytical research and development at Pfizer Inc., E...

soluplus®; a novel excipient to improve dissolution rate of poorly water soluble drug, celecoxib