title: Evaluation of hot-melt extrusion and injection molding for continuous manufacturing of immediate-release tablets.
abstract: The exploitation of hot-melt extrusion and injection molding for the manufacturing of immediate-release (IR) tablets was preliminarily investigated in view of their special suitability for continuous manufacturing, which represents a current goal of pharmaceutical production because of its possible advantages in terms of improved sustainability. Tablet-forming agents were initially screened based on processability by single-screw extruder and micromolding machine as well as disintegration/dissolution behavior of extruded/molded prototypes. Various polymers, such as low-viscosity hydroxypropylcellulose, polyvinyl alcohol, polyvinyl alcohol-polyethylene glycol graft copolymer, various sodium starch glycolate grades (e.g., Explotab(®) CLV) that could be processed with no need for technological aids, except for a plasticizer, were identified. Furthermore, the feasibility of both extruded and molded IR tablets from low-viscosity hydroxypropylcellulose or Explotab(®) CLV was assessed. Explotab(®) CLV, in particular, showed thermoplastic properties and a very good aptitude as a tablet-forming agent, starting from which disintegrating tablets were successfully obtained by either techniques. Prototypes containing a poorly soluble model drug (furosemide), based on both a simple formulation (Explotab(®) CLV and water/glycerol as plasticizers) and formulations including dissolution/disintegration adjuvants (soluble and effervescent excipients) were shown to fulfill the USP 37 dissolution requirements for furosemide tablets.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy.
authors.forename: Alice
authors.initials: A
authors.lastname: Melocchi
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy.
authors.forename: Giulia
authors.initials: G
authors.lastname: Loreti
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy.
authors.forename: Maria Dorly
authors.initials: MD
authors.lastname: Del Curto
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Maroni
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Gazzaniga
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Sezione di Tecnologia e Legislazione Farmaceutiche "M.E. Sangalli", Università degli Studi di Milano, Milan 20133, Italy. Electronic address: lucia.zema@unimi.it.
authors.forename: Lucia
authors.initials: L
authors.lastname: Zema
mesh_terms: D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004232:Diuretics / Q000008:administration & dosage*; D004339:Drug Compounding / Q000379:methods; D005079:Excipients / Q000737:chemistry*; D005665:Furosemide / Q000008:administration & dosage*; D005990:Glycerol / Q000737:chemistry; D010968:Plasticizers / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D014783:Viscosity
chemical_list: D004232:Diuretics; D005079:Excipients; D010968:Plasticizers; D011108:Polymers; D013607:Tablets; D005665:Furosemide; D002482:Cellulose; C008079:hydroxypropylcellulose; D005990:Glycerol
keywords: Explotab®CLV; Nisso HPCSSL; continuous manufacturing; extrusion; formulation; injection molding; oral drug delivery; polymers; solid dosage form; tablet