Design of Lipid-Based Formulations for Oral Administration of Poorly Water-Soluble Drug Fenofibrate: Effects of Digestion

作者: Kazi Mohsin

DOI: 10.1208/S12249-012-9787-2

关键词:

摘要: Lipid-based drug carriers are likely to have influence on bioavailability through enhanced solubilization of the in gastrointestinal tract. The study was designed investigate lipid formulation digestibility simulated gastro intestinal media. Fenofibrate formulated representative Type II, IIIA, IIIB and IV self-emulsifying/microemulsifying delivery systems (SEDDS SMEDDS for oral administration) using various medium-chain glyceride components, non-ionic surfactants cosolvents as excipients. Soybean oil used only an example long-chain triglycerides compare effects with their counterparts. formulations were subjected vitro digestion specifically predict fate tract after exposure pancreatic enzymes bile. In experiments carried out a pH-stat maintained at pH 7.5 30 min fluids simulating fed fasted states. rate faster almost completed II IIIA systems. Most studies digestible. However, high concentration surfactant and/or cosolvent or lowered digestion. than triglycerides, but kept comparatively less post products. Medium-chain mixed glycerides good solvents fenofibrate rapidly digested improve products use suggested further investigations.

参考文章(31)
Panayiotis P. Constantinides, Jean‐Paul Scalart, Cindy Lancaster, Joseph Marcello, Gary Marks, Harma Ellens, Philip L. Smith, Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharmaceutical Research. ,vol. 11, pp. 1385- 1390 ,(1994) , 10.1023/A:1018927402875
Panayiotis P. Constantinides, Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects Pharmaceutical Research. ,vol. 12, pp. 1561- 1572 ,(1995) , 10.1023/A:1016268311867
W. H. Lim, M. J. Lawrence, Aggregation behaviour of mixtures of phosphatidylcholine and polyoxyethylene sorbitan monoesters in aqueous solution Physical Chemistry Chemical Physics. ,vol. 6, pp. 1380- 1387 ,(2004) , 10.1039/B314610N
Leab Sek, Christopher J. H. Porter, Ann Marie Kaukonen, William N. Charman, Evaluation of the in-vitro digestion profiles of long and medium chain glycerides and the phase behaviour of their lipolytic products. Journal of Pharmacy and Pharmacology. ,vol. 54, pp. 29- 41 ,(2010) , 10.1211/0022357021771896
M. Kuentz, Oral self-emulsifying drug delivery systems, from biopharmaceutical to technical formulation aspects Journal of Drug Delivery Science and Technology. ,vol. 21, pp. 17- 26 ,(2011) , 10.1016/S1773-2247(11)50002-4
Janne Ørskov Christensen, Kirsten Schultz, Birgitte Mollgaard, Henning Gjelstrup Kristensen, Anette Mullertz, Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols. European Journal of Pharmaceutical Sciences. ,vol. 23, pp. 287- 296 ,(2004) , 10.1016/J.EJPS.2004.08.003
Colin W. Pouton, Formulation of self-emulsifying drug delivery systems Advanced Drug Delivery Reviews. ,vol. 25, pp. 47- 58 ,(1997) , 10.1016/S0169-409X(96)00490-5