title: Formulation and Coating of Alginate and Alginate-Hydroxypropylcellulose Pellets Containing Ranolazine.
abstract: The formulation and the coating composition of biopolymeric pellets containing ranolazine were studied to improve their technological and biopharmaceutical properties. Eudragit L100 (EU L100) and Eudragit L30 D-55-coated alginate and alginate-hydroxypropylcellulose (HPC) pellets were prepared by ionotropic gelation using 3 concentrations of HPC (0.50%, 0.65%, and 1.00% wt/wt) and applying different percentages (5%, 10%, 20%, and 30% wt/wt) of coating material. The uncoated pellets were regular in shape and had mean diameter between 1490 and 1570 μm. The rate and the entity of the swelling process were affected by the polymeric composition: increasing the HPC concentration, the structure of the pellets became more compact and slowed down the penetration of fluids. Coated alginate-HPC formulations were able to control the drug release at neutral pH: a higher quantity of HPC in the system determined a slower release of the drug. The nature of the coating polymer and the coating level applied affected the drug release in acidic environment: EU L100 gave better performance than Eudragit L30 D-55 and the best coating level was 20%. The pellets containing 0.65% of HPC and coated with 20% EU L100 represented the best formulation, able to limit the drug release in acidic environment and to control it at pH 6.8.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Novara 28100, Italy. Electronic address: lorena.segale@uniupo.it.
authors.forename: Lorena
authors.initials: L
authors.lastname: Segale
authors.affiliation: Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Novara 28100, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Mannina
authors.affiliation: Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Novara 28100, Italy.
authors.forename: Lorella
authors.initials: L
authors.lastname: Giovannelli
authors.affiliation: College of Pharmacy, Univ. Lille Nord de France, Lille 59006, France; INSERM U 1008, Lille 59006, France.
authors.forename: Susanne
authors.initials: S
authors.lastname: Muschert
authors.affiliation: Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Novara 28100, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Pattarino
mesh_terms: D000464:Alginates / Q000737:chemistry* / Q000493:pharmacokinetics; D002317:Cardiovascular Agents / Q000737:chemistry / Q000493:pharmacokinetics; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding; D004343:Drug Implants / Q000737:chemistry* / Q000493:pharmacokinetics; D065546:Drug Liberation; D020723:Glucuronic Acid / Q000737:chemistry / Q000493:pharmacokinetics; D006603:Hexuronic Acids / Q000737:chemistry / Q000493:pharmacokinetics; D008689:Methacrylates / Q000737:chemistry / Q000493:pharmacokinetics; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics; D011109:Polymethacrylic Acids / Q000737:chemistry / Q000493:pharmacokinetics; D000069458:Ranolazine / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D000464:Alginates; D002317:Cardiovascular Agents; D004337:Drug Carriers; D004343:Drug Implants; C477852:Eudragit L 30 D-55; D006603:Hexuronic Acids; D008689:Methacrylates; D011108:Polymers; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D020723:Glucuronic Acid; D002482:Cellulose; C008079:hydroxypropylcellulose; D000069458:Ranolazine
keywords: alginate; enteric coating; hydroxypropylcellulose; polymeric pellets; ranolazine