Self nano-emulsifying simvastatin based tablets: design and in vitro/in vivo evaluation

作者: Ghada Abdelbary , Maha Amin , Salwa Salah

DOI: 10.3109/10837450.2012.672989

关键词: BioavailabilityNano-SimvastatinFlow propertiesZeta potentialMaterials scienceChromatographyIn vitro in vivoPharmacokineticsWater soluble drug

摘要: The aim of this work is to improve the oral bioavailability poorly water soluble drug, simvastatin (SV) through combining advantages self-nanoemulsifying systems (SNEs) and tablets. Ternary phase diagram was constructed using Labrafil, Tween 80 Transcutol, in order evaluate self-nanoemulsification domain. particle size distribution zeta potential prepared were evaluated Malvern Zetasizer. Liquisolid powders Aeroperl® as a coating material Avicel® or Starch 1500 carrier materials, powder flow properties then evaluated. Compressed SV SNE based tablets regarding their physical characteristics, in-vitro release well in-vivo pharmacokinetic evaluation six healthy human volunteers validated LC/MS/MS method. results revealed that developed improved significantly, compared commercially available (Zocor®). optimal...

参考文章(41)
Susan A. Charman, William N. Charman, Mark C. Rogge, Terry D. Wilson, Frank J. Dutko, Colin W. Pouton, Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharmaceutical Research. ,vol. 9, pp. 87- 93 ,(1992) , 10.1023/A:1018987928936
Haiyung Cheng, Steven C. Sutton, James D. Pipkin, Gaylen M. Zentner, J. Douglas Rogers, Jules I. Schwartz, Yale B. Mitchel, Kenneth Grasing, Michael S. Schwartz, Raju D. Amin, Lida Liu, David L. Ebel, Amy Coulter, Karen Engle, Gregory A. McClelland, Chung Y. Lui, Gerald S. Rork, Evaluation of Sustained/Controlled-Release Dosage Forms of 3-Hydroxy-3-methylglutaryl–Coenzyme A (HMG-CoA) Reductase Inhibitors in Dogs and Humans Pharmaceutical Research. ,vol. 10, pp. 1683- 1687 ,(1993) , 10.1023/A:1018997308946
Tugrul T. Kararli, Thomas E. Needham, Marty Griffin, Grant Schoenhard, Leonard J. Ferro, Lisa Alcorn, Oral delivery of a renin inhibitor compound using emulsion formulations. Pharmaceutical Research. ,vol. 9, pp. 888- 893 ,(1992) , 10.1023/A:1015896731545
Gregory A. McClelland, R. John Stubbs, Joseph A. Fix, Stefano A. Pogany, Gaylen M. Zentner, Enhancement of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor efficacy through administration of a controlled-porosity osmotic pump dosage form. Pharmaceutical Research. ,vol. 8, pp. 873- 876 ,(1991) , 10.1023/A:1015899328105
Analytical methods validation: bioavailability, bioequivalence and pharmacokinetic studies. Conference report. European Journal of Drug Metabolism and Pharmacokinetics. ,vol. 16, pp. 249- ,(1991) , 10.1007/BF03189968
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
Herbert A. Lieberman, Martin M. Rieger, Gilbert S. Banker, Pharmaceutical Dosage Forms: Disperse Systems ,(1988)
Prabagar Balakrishnan, Beom-Jin Lee, Dong Hoon Oh, Jong Oh Kim, Myung Ja Hong, Jun-Pil Jee, Jung Ae Kim, Bong Kyu Yoo, Jong Soo Woo, Chul Soon Yong, Han-Gon Choi, Enhanced oral bioavailability of dexibuprofen by a novel solid Self-emulsifying drug delivery system (SEDDS) European Journal of Pharmaceutics and Biopharmaceutics. ,vol. 72, pp. 539- 545 ,(2009) , 10.1016/J.EJPB.2009.03.001
Marie-Elise Chateau, Laurence Galet, Yannick Soudais, Jacques Fages, Processing a detergent powder formulation: Direct compression, and high shear wet granulation followed by compression Powder Technology. ,vol. 157, pp. 191- 198 ,(2005) , 10.1016/J.POWTEC.2005.05.026