title: Preparation and evaluation of enteric coated tablets of hot-melt extruded lansoprazole.
abstract: The objective of this work was to use hot-melt extrusion (HME) technology to improve the physiochemical properties of lansoprazole (LNS) to prepare stable enteric coated LNS tablets. For the extrusion process, we chose Kollidon®12 PF (K12) polymeric matrix. Lutrol®F 68 was selected as the plasticizer and magnesium oxide (MgO) as the alkalizer. With or without the alkalizer, LNS at 10% drug load was extruded with K12 and F68. LNS changed to the amorphous phase and showed better release compared to that of the pure crystalline drug. Inclusion of MgO improved LNS extrudability and release and resulted in over 80% drug release in the buffer stage. Hot-melt extruded LNS was physically and chemically stable after 12 months of storage. Both formulations were studied for compatibility with Eudragit®L100-55. The optimized formulation was compressed into a tablet followed by coating process utilizing a pan coater using L100-55 as an enteric coating polymer. In a two-step dissolution study, the release profile of the enteric coated LNS tablets in the acidic stage was less than 10% of the LNS, while that in the buffer stage was more than 80%. Drug content analysis revealed the LNS content to be 97%, indicating the chemical stability of the enteric coated tablet after storage for six months. HME, which has not been previously used for LNS, is a valuable technique to reduce processing time in the manufacture of enteric coated formulations of an acid-sensitive active pharmaceutical ingredient as compared to the existing methods.
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.|b Department of Pharmaceutics, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia.
authors.forename: Bader B
authors.initials: BB
authors.lastname: Alsulays
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Vijay
authors.initials: V
authors.lastname: Kulkarni
authors.affiliation: c Department of Pharmaceutics, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia.
authors.forename: Sultan M
authors.initials: SM
authors.lastname: Alshehri
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Bjad K
authors.initials: BK
authors.lastname: Almutairy
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Eman A
authors.initials: EA
authors.lastname: Ashour
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Joseph T
authors.initials: JT
authors.lastname: Morott
authors.affiliation: b Department of Pharmaceutics, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia.
authors.forename: Abdullah S
authors.initials: AS
authors.lastname: Alshetaili
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Jun-Bom
authors.initials: JB
authors.lastname: Park
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Roshan V
authors.initials: RV
authors.lastname: Tiwari
authors.affiliation: a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.|d Pii Center for Pharmaceutical Technology, School of Pharmacy , The University of Mississippi , Oxford , MS , USA.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Repka
mesh_terms: D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D064747:Lansoprazole / Q000737:chemistry*; D010968:Plasticizers / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012995:Solubility / Q000187:drug effects; D013608:Tablets, Enteric-Coated / Q000737:chemistry*; D013678:Technology, Pharmaceutical
chemical_list: D005079:Excipients; C506200:Lutrol; D010968:Plasticizers; D011108:Polymers; D013608:Tablets, Enteric-Coated; D064747:Lansoprazole; D011092:Polyethylene Glycols; D011205:Povidone
keywords: Lansoprazole; enteric coating; hot-melt extrusion; release; stability