Millipore Technical Publications |
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MultiScreen Filter Plates for PAMPA and Permeability AssaysData review and optimization of PAMPA and Permeability Assays | ||
| Lit No: | AN1729EN00 | |
| Year: | 2003 | |
| The bioavailability of a drug is affected by a number of factors including its ability to be absorbed into the blood stream through the cells lining the intestines. There are a number of different in vitro assay options available to predict the gastrointestinal absorption property of drugs including a permeability assay1 that uses a hexadecane-filled membrane as a lipophilic barrier, and a method known as PAMPA2 (Parallel Artificial Membrane Permeability Assay), which uses a lipid filled membrane to simulate the lipid bilayer of various cell types, including intestinal epithelium. These non-cell based permeability assays are automation compatible, relatively fast (4–24 hours), inexpensive, and straightforward. They are being used with increasing frequency to determine the passive, transcellular permeability properties of potential drug compounds. The majority of drugs (>80%) enter the blood stream by passive diffusion through the intestinal epithelium3. Consequently, permeability assays that measure passive transport through lipophilic barriers correlate with human drug absorption values from published methods. Click the PDF above for the full document. 1 Wohnsland, F.; Faller, B. High-throughput Permeability pH Profile and High-throughput Alkane/Water Log P With Artificial Membranes, J. Med. Chem., 2001; 44, p. 923–930. 2 Kansy, M.; Senner, F.; Gubernator, K. Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes, J. Med. Chem., 1998; 41, p. 1007–1010.. 3 Brennan, M.B., Drug Discovery (Filtering out Failures Early in the Game), Chem. & Eng. News, 2000; 78, 63. | |
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