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Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs.
J Pharm Sci. 2017 01; 106(1):140-150.JP

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 Tg could 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+Show Affiliations

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York 11439.Kashiv Pharma LLC, Bridgewater, New Jersey 08807.Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, New York 11439. Electronic address: serajuda@stjohns.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27578544

Citation

Batra, Amol, et al. "Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs." Journal of Pharmaceutical Sciences, vol. 106, no. 1, 2017, pp. 140-150.
Batra A, Desai D, Serajuddin ATM. Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs. J Pharm Sci. 2017;106(1):140-150.
Batra, A., Desai, D., & Serajuddin, A. T. M. (2017). Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs. Journal of Pharmaceutical Sciences, 106(1), 140-150. https://doi.org/10.1016/j.xphs.2016.07.014
Batra A, Desai D, Serajuddin ATM. Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs. J Pharm Sci. 2017;106(1):140-150. PubMed PMID: 27578544.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Investigating the Use of Polymeric Binders in Twin Screw Melt Granulation Process for Improving Compactibility of Drugs. AU - Batra,Amol, AU - Desai,Dipen, AU - Serajuddin,Abu T M, Y1 - 2016/08/28/ PY - 2016/03/30/received PY - 2016/06/26/revised PY - 2016/07/12/accepted PY - 2016/9/1/pubmed PY - 2017/12/13/medline PY - 2016/9/1/entrez KW - compaction KW - granulation KW - polymers KW - powder technology KW - processing KW - tablet SP - 140 EP - 150 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 106 IS - 1 N2 - 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 Tg could 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. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/27578544/Investigating_the_Use_of_Polymeric_Binders_in_Twin_Screw_Melt_Granulation_Process_for_Improving_Compactibility_of_Drugs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(16)41601-1 DB - PRIME DP - Unbound Medicine ER -