title: Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs.
abstract: Traditionally, the melt granulation for pharmaceutical products was performed at low temperature (<90°C) with high-shear granulators using low-melting waxy binders, and tablets produced using such granules were not amenable to large-scale manufacturing. The situation has changed in recent years by the use of twin screw extruder where the processing temperature could be increased to as high as 180°C and polymers with high Tgcould be used as binders. In this study, different polymeric binders were screened for their suitability in improving compactibility of 2 drugs, metformin hydrochloride and acetaminophen, by twin screw melt granulation. Processing temperatures for the 2 drugs were set at 180°C and 130°C, respectively. Screw configuration, screw speed, and feed rate were optimized such that all polymeric binders used produced granules. Several hydroxypropyl cellulose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, and methacrylate-based polymers, including Klucel®EXF, Eudragit®EPO, and Soluplus®, demonstrated good tablet tensile strength (>2 MPa) when granules were produced using only 10% wt/wt polymer concentration. Certain polymers provided acceptable compactibility even at 5% wt/wt. Thus, twin screw melt granulation process may be used with different polymers at a wide range of temperature. Due to low excipient concentration, this granulation method is especially suitable for high-dose tablets.
authors: Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York 11439.
authors: Amol
authors: A
authors: Batra
authors: Kashiv Pharma LLC, Bridgewater, New Jersey 08807.
authors: Dipen
authors: D
authors: Desai
authors: Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York 11439. Electronic address: serajuda@stjohns.edu.
authors: Abu T M
authors: ATM
authors: Serajuddin
mesh_terms: D000082:Acetaminophen / Q000008:administration & dosage* / Q000737:chemistry; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000737:chemistry; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods; D005079:Excipients / Q000737:chemistry*; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry; D065347:Hypromellose Derivatives / Q000737:chemistry; D008687:Metformin / Q000008:administration & dosage* / Q000737:chemistry; D008689:Methacrylates / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D013607:Tablets; D013718:Tensile Strength
chemical_list: D018712:Analgesics, Non-Narcotic; D005079:Excipients; D007004:Hypoglycemic Agents; D008689:Methacrylates; D011108:Polymers; D011109:Polymethacrylic Acids; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D000082:Acetaminophen; D065347:Hypromellose Derivatives; D002482:Cellulose; D008687:Metformin; C008079:hydroxypropylcellulose; D011205:Povidone
keywords: compaction; granulation; polymers; powder technology; processing; tablet