An in vitro methodology for forecasting luminal concentrations and precipitation of highly permeable lipophilic weak bases in the fasted upper small intestine.

作者: Dimitrios Psachoulias , Maria Vertzoni , James Butler , David Busby , Moira Symillides

DOI: 10.1007/S11095-012-0844-Z

关键词: Small intestinePharmacology toxicologySolubilityIn vitroChemistryUrea metabolismChromatographyIntestinal absorption

摘要: Purpose To develop an in vitro methodology for prediction of concentrations and potential precipitation highly permeable, lipophilic weak bases fasted upper small intestine based on ketoconazole dipyridamole luminal data. Evaluate usefulness predicting AZD0865 SB705498 plasma

参考文章(24)
Mei‐Ling Chen, An alternative approach for assessment of rate of absorption in bioequivalence studies. Pharmaceutical Research. ,vol. 9, pp. 1380- 1385 ,(1992) , 10.1023/A:1015842425553
Jeroen Walravens, Joachim Brouwers, Isabel Spriet, Jan Tack, Pieter Annaert, Patrick Augustijns, Effect of pH and comedication on gastrointestinal absorption of posaconazole: monitoring of intraluminal and plasma drug concentrations. Clinical Pharmacokinectics. ,vol. 50, pp. 725- 734 ,(2011) , 10.2165/11592630-000000000-00000
Panos Macheras, Mira Symillides, Christos Reppas, The cutoff time point of the partial area method for assessment of rate of absorption in bioequivalence studies. Pharmaceutical Research. ,vol. 11, pp. 831- 834 ,(1994) , 10.1023/A:1018921622981
Kilian Kelly, Bridget O'Mahony, Blythe Lindsay, Tamara Jones, Tim J. Grattan, Amin Rostami‐Hodjegan, Howard N. E. Stevens, Clive G. Wilson, Comparison of rates of disintegration, gastric emptying, and drug absorption following administration of a new and a conventional paracetamol formulation, using γ scintigraphy Pharmaceutical Research. ,vol. 20, pp. 1668- 1673 ,(2003) , 10.1023/A:1026155822121
Rebecca L. Oberle, Tzyy-Show Chen, Charles Lloyd, Jeffrey L. Barnett, Chung Owyang, James Meyer, Gordon L. Amidon, The influence of the interdigestive migrating myoelectric complex on the gastric emptying of liquids Gastroenterology. ,vol. 99, pp. 1275- 1282 ,(1990) , 10.1016/0016-5085(90)91150-5
Edmund S. Kostewicz, Martin Wunderlich, Ulrich Brauns, Robert Becker, Thomas Bock, Jennifer B. Dressman, Predicting the precipitation of poorly soluble weak bases upon entry in the small intestine Journal of Pharmacy and Pharmacology. ,vol. 56, pp. 43- 51 ,(2010) , 10.1211/0022357022511
Sara Carlert, Anna Pålsson, Gunilla Hanisch, Christian von Corswant, Catarina Nilsson, Lennart Lindfors, Hans Lennernäs, Bertil Abrahamsson, Predicting Intestinal Precipitation—A Case Example for a Basic BCS Class II Drug Pharmaceutical Research. ,vol. 27, pp. 2119- 2130 ,(2010) , 10.1007/S11095-010-0213-8
G. Steffen Paulekuhn, Jennifer B. Dressman, Christoph Saal, Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange Book database. Journal of Medicinal Chemistry. ,vol. 50, pp. 6665- 6672 ,(2007) , 10.1021/JM701032Y
Chong‐Hui Gu, Deepa Rao, Rajesh B. Gandhi, J.o.n. Hilden, Krishnaswamy Raghavan, Using a novel multicompartment dissolution system to predict the effect of gastric pH on the oral absorption of weak bases with poor intrinsic solubility. Journal of Pharmaceutical Sciences. ,vol. 94, pp. 199- 208 ,(2005) , 10.1002/JPS.20242
Y C Huang, J L Colaizzi, R H Bierman, R Woestenborghs, J Heykants, Pharmacokinetics and dose proportionality of ketoconazole in normal volunteers. Antimicrobial Agents and Chemotherapy. ,vol. 30, pp. 206- 210 ,(1986) , 10.1128/AAC.30.2.206