Abstract
One approach for delivery of narrow absorption window drugs is to formulate gastroretentive drug delivery systems. This study was undertaken to provide insight into in vivo performances of two gastroretentive systems (PXLNET and IPB matrices) in comparison to Madopar® HBS capsules. The pig model was used to assess gastric residence time and pharmacokinetic parameters using blood, cerebrospinal fluid (CSF), and urine samples. Histopathology and cytotoxicity testing were also undertaken. The pharmacokinetic parameters indicated that levodopa was liberated from the drug delivery systems, absorbed, widely distributed, metabolized, and excreted. Cmax were 372.37, 257.02, and 461.28 ng/mL and MRT were 15.36, 14.98, and 13.30 for Madopar HBS capsules, PXLNET, and IPB, respectively. In addition, X-ray imaging indicated that the gastroretentive systems have the potential to reside in the stomach for 7 hours. There was strong in vitro-in vivo correlation for all formulations with r(2) values of 0.906, 0.935, and 0.945 for Madopar HBS capsules, PXLNET, and IPB, respectively. Consequently, PXLNET and IPB matrices have pertinent potential as gastroretentive systems for narrow absorption window drugs (e.g., L-dopa) and, in this application s...Continue Reading
References
Oct 1, 1992·Naunyn-Schmiedeberg's Archives of Pharmacology·B Mühlbauer, H Osswald
Jan 1, 1992·European Journal of Clinical Pharmacology·D R RobertsonJ S Fleming
Jun 1, 1992·The American Journal of Physiology·E GrossmanM Epstein
May 1, 1991·Annals of Neurology·C W OlanowJ M Cedarbaum
Nov 11, 1991·Hypertension·J R GillD S Goldstein
Jan 1, 1990·British Journal of Clinical Pharmacology·D R RobertsonC F George
Jun 1, 1987·Annals of Neurology·J G NuttD Merrick
Jan 1, 1984·European Journal of Applied Physiology and Occupational Physiology·W Fibiger, G Singer
May 1, 1997·Movement Disorders : Official Journal of the Movement Disorder Society·J G NuttW R Woodward
Mar 4, 1999·European Journal of Neurology : the Official Journal of the European Federation of Neurological Societies·K M JorgaB Moe
Oct 16, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·E Lipka, G L Amidon
Jul 11, 2000·Japanese Journal of Pharmacology·M ItoM Ishihara
Oct 18, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·J B Dressman, C Reppas
Feb 24, 2001·The Journal of Pharmacy and Pharmacology·S S DavisM Hinchcliffe
Jul 2, 2003·The Journal of Pharmacy and Pharmacology·K D RainsfordS Debski
Jul 16, 2003·Eye & Contact Lens·Joseph G VehigeNancy Brady
Jun 29, 2004·NeuroImage·Pedro Rosa-NetoPaul Cumming
Jan 25, 2005·Eye & Contact Lens·Ling C HuangAlison M McDermott
Dec 31, 2005·Synapse·Luciano MinuzziPaul Cumming
Apr 1, 2006·The Journal of Experimental Biology·Jacob JelsingBente Pakkenberg
Apr 15, 2006·Clinical Neuropharmacology·Thomas MüllerOliver Goetze
Mar 29, 2007·Investigative Ophthalmology & Visual Science·Qian GarrettMark Willcox
Apr 21, 2007·Neuroscience and Biobehavioral Reviews·Nanna Marie LindAxel K Hansen
Aug 12, 2008·Current Clinical Pharmacology·Soo-Peang Khor, Ann Hsu
Oct 22, 2009·Molecular and Cellular Biochemistry·Fariba KhodagholiParisa Fathi Rezaei
Feb 24, 2010·Computer Methods and Programs in Biomedicine·Yong ZhangShaofei Xie
Feb 24, 2011·International Journal of Dermatology·Mirela SusanRodica Cosgarea
Oct 22, 2011·International Journal of Molecular Sciences·Ndidi C NgwulukaRiaz A Khan
Mar 16, 2013·AAPS PharmSciTech·Ndidi C NgwulukaViness Pillay