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: Alice Melocchi, Giulia Loreti, Maria Dorly Del Curto, Alessandra Maroni, Andrea Gazzaniga, Lucia Zema
• Journal: Journal of pharmaceutical sciences (J Pharm Sci) Vol. 104 Issue 6 Pg. 1971-1980 (Jun 2015) ISSN: 1520-6017 [Electronic] United States
• PMID: 25761921 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

Chemical References

• Diuretics
• Excipients
• Plasticizers
• Polymers
• Tablets
• Furosemide
• Cellulose
• hydroxypropylcellulose
• Glycerol

Topics

• Cellulose (analogs & derivatives, chemistry)
• Chemistry, Pharmaceutical (methods)
• Diuretics (administration & dosage)
• Drug Compounding (methods)
• Excipients (chemistry)
• Furosemide (administration & dosage)
• Glycerol (chemistry)
• Plasticizers (chemistry)
• Polymers (chemistry)
• Solubility
• Tablets (chemistry)
• Viscosity