Kin-Kai Hwang

Learn More
Artificial membrane permeability measurement is a potentially high throughput and low cost alternative for in vitro assessment of drug absorption potential. It will be an ideal screening/profiling tool in the lead generation program of drug discovery research if it is proven to be generally applicable for classifying drug absorption potential and is(More)
This paper describes a graphical model for simplifying in vitro absorption, metabolism, distribution, and elimination (ADME) data analysis through the estimation of oral bioavailability (%F) of drugs in humans and other species. This model integrates existing in vitro ADME data, such as Caco-2 permeability (P(app)) and metabolic stability (percent remaining(More)
The purpose of this study is to explore the use of classification regression trees (CART) in predicting, in the dose-independent range, the fraction dose absorbed in humans. Since the results from clinical formulations in humans were used for training the model, a hypothetical state of drug molecules already dissolved in the intestinal fluid was adopted.(More)
A fully automated HPLC assay for hydrochlorothiazide in plasma has been developed using a column-switching technique. The method involves direct injection of plasma to the extraction column for sample cleanup followed by switching onto the analytical column. Good precision, accuracy, and linearity were obtained over a range of 25 to 2000 ng/ml in rat, dog,(More)
PURPOSE Kansy et al first introduced the Parallel artificial membrane permeation assay (PAMPA) in 1998. In this system, the permeability through a membrane formed by a mixture of lecithin and an inert organic solvent on a filter support is assessed. PAMPA shows definite trends in the ability of molecules to permeate membranes by transcellular passive(More)
INTRODUCTION M100240--an acetate thioester of MDL 100,173--a dual angiotensin-converting enzyme (ACE)/neutral endopeptidase (NEP) inhibitor is in Phase II development for cardiovascular conditions. The absorption characteristics of M100240 and MDL 100,173 were evaluated in specific regions of the rat gastrointestinal (GI) tract. METHODS Solutions of(More)
A fully automated column-switching HPLC procedure has been developed and validated for quantitation of ML-1035 and its five metabolites in plasma employing direct injection. Plasma samples were injected onto a CN extraction column (4 × 4.6 mm, 5 µm) for micellar cleanup with 0.5% sodium dodecyl sulfate (SDS) in 50 mM phosphate. The proteinaceous components(More)
  • 1