Parallel artificial membrane

Kansy, M., Senner, F., Gubemator, K. Physicochemical high throughput screening parallel artificial membrane permeation assay in the description of passive absorption processes. /. Med. Chem. 1998, 43, 1007-1010. [Pg.49]

PAMPA parallel artificial membrane permeation assay... [Pg.55]

The evaluation of the apparent ionization constants (i) can indicate in partition experiments the extent to which a charged form of the drug partitions into the octanol or liposome bilayer domains, (ii) can indicate in solubility measurements, the presence of aggregates in saturated solutions and whether the aggregates are ionized or neutral and the extent to which salts of dmgs form, and (iii) can indicate in permeability measurements, whether the aqueous boundary layer adjacent to the membrane barrier, Umits the transport of drugs across artificial phospholipid membranes [parallel artificial membrane permeation assay (PAMPA)] or across monolayers of cultured cells [Caco-2, Madin-Darby canine kidney (MDCK), etc.]. [Pg.57]

Typical early in vitro permeability assessments measure the rate of flux of a compound from one side of a barrier to another [54, 55]. The barrier has historically been derived from a cell line, most commonly Caco-2 or Madin-Darby canine kidney (MDCK) cells. In the last several years, there has been substantial work and significant progress in the development of parallel artificial membrane permeability... [Pg.159]

BBB PAMPA Blood brain barrier parallel artificial membrane permeability assay... [Pg.176]

PARALLEL ARTIFICIAL-MEMBRANE PERMEABILITY ASSAY (PAMPA)... [Pg.128]

Zhu, C. Chen, T.-M. Hwang, K., A comparative study of parallel artificial membrane permeability assay for passive absorption screening, in CPS A2000 The Symposium on Chemical and Pharmaceutical Structure Analysis. Milestone Development Services. Princeton, NJ, Sept. 26-28, 2000. [Pg.281]

Sugano, K. Hamada, H. Machida, M. Ushio, H., High throughput prediction of oral absorption Improvement of the composition of the lipid solution used in parallel artificial membrane permeability assay, J. Biomolec. Screen. 6, 189-196 (2001). [Pg.281]

This book is written for the practicing pharmaceutical scientist involved in absorption-distribution-metabolism-excretion (ADME) measurements who needs to communicate with medicinal chemists persuasively, so that newly synthesized molecules will be more drug-like. ADME is all about a day in the life of a drug molecule (absorption, distribution, metabolism, and excretion). Specifically, this book attempts to describe the state of the art in measurement of ionization constants (p Ka), oil-water partition coefficients (log PI log D), solubility, and permeability (artificial phospholipid membrane barriers). Permeability is covered in considerable detail, based on a newly developed methodology known as parallel artificial membrane permeability assay (PAMPA). [Pg.299]

There are several approaches to estimating absorption using in vitro methods, notably Caco-2 and MDCK cell-based methods or using methods that assess passive permeability, for example the parallel artificial membrane permeation assay (PAMPA) method. These are reviewed elsewhere in this book. The assays are very useful, and usually have an important role in the screening cascades for drug discovery projects. However, as discussed below, the cell-based assays are not without their drawbacks, and it is often appropriate to use ex vivo and/or in vivo absorption assays. [Pg.140]

The use of artificial membranes to investigate passive permeation processes has a long history, going back more than 40 years [68], The parallel artificial membrane permeation assay (PAMPA) is an application of the filter-supported lipid membrane system [149] and was first introduced by Kansy and... [Pg.187]

Batzl-Hartmann C, Hurst L, Maas R (2002) Method for the improvement of parallel artificial membrane permeation assay (PAMPA) by using an additional hydrophilic membrane. German Patent Application 4. [Pg.207]

Kerns EH, Di L, Petusky S, Farris M, Ley R, Jupp P (2004) Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J Pharm Sci 93 1440-1453. [Pg.209]

Table 18.3 Parallel artificial membrane permeability assay (PAMPA) permeability and human absorption for 19 drug compounds.

Solubility and permeability were measured by a high throughput solubility assay and parallel artificial membrane permeation assay (PAMPA), respectively [56], The assays categorized 14 out of 18 drugs based on the BCS consistent with their known solubility and permeability characteristics [56],... [Pg.675]