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The Effect of Process Variables and Binder Concentration on Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced by Twin Screw Melt Granulation with Different Polymeric Binders.
AAPS PharmSciTech. 2021 May 13; 22(4):154.AP

Abstract

In twin screw melt granulation, granules are produced by passing mixtures of drug substances and polymeric binders through twin screw extruder such that temperatures are maintained below melting point of drugs but above glass transition of polymers used, whereby the polymers coat surfaces of drug particles and cause their agglomeration into granules. Since various formulation factors, such as binder type and concentration, and processing variables like extrusion temperature, screw configuration, and screw speed, can influence the granulation process, the present investigation was undertaken to study their effects on tabletability of granules produced. Three different types of polymeric binders, Klucel® EXF (hydroxypropyl cellulose), Eudragit® EPO (polyacrylate binder), and Soluplus® (polyvinyl caprolactam-co-vinyl acetate-ethylene glycol graft polymer), were used at 2, 5, and 10% concentrations. Metformin hydrochloride (HCl) (mp: 222°C) and acetaminophen (mp: 169°C) were used as model drugs, and drug-polymer mixtures with metformin HCl were extruded at 180, 160, and 130°C, while those with acetaminophen were extruded at 130 and 110°C. Other process variables included screw configurations: low, medium, and high shear for metformin HCl, and low and medium shear for acetaminophen; feed rates: 20 and 60 g/min; and screw speed of 100 and 300 RPM. Formulation and process variables had significant impact on tabletability. The target tensile strength of ≥2 MPa could be obtained with all polymers and at all processing temperatures when metformin HCl was granulated at 180°C and acetaminophen at 130°C. At other temperatures, the target tensile strength could be achieved at certain specific sets of processing conditions.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, New York, 11439, USA. , Ashland Specialty Ingredients, 500 Hercules Rd, Wilmington, USA.Kashiv Biosciences, 995 US 202/206, Bridgewater, New Jersey, 08807, USA.Kashiv Biosciences, 995 US 202/206, Bridgewater, New Jersey, 08807, USA.Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, New York, 11439, USA. serajuda@stjohns.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

33983536

Citation

Batra, Amol, et al. "The Effect of Process Variables and Binder Concentration On Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced By Twin Screw Melt Granulation With Different Polymeric Binders." AAPS PharmSciTech, vol. 22, no. 4, 2021, p. 154.
Batra A, Thongsukmak A, Desai D, et al. The Effect of Process Variables and Binder Concentration on Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced by Twin Screw Melt Granulation with Different Polymeric Binders. AAPS PharmSciTech. 2021;22(4):154.
Batra, A., Thongsukmak, A., Desai, D., & Serajuddin, A. T. M. (2021). The Effect of Process Variables and Binder Concentration on Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced by Twin Screw Melt Granulation with Different Polymeric Binders. AAPS PharmSciTech, 22(4), 154. https://doi.org/10.1208/s12249-021-02018-6
Batra A, et al. The Effect of Process Variables and Binder Concentration On Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced By Twin Screw Melt Granulation With Different Polymeric Binders. AAPS PharmSciTech. 2021 May 13;22(4):154. PubMed PMID: 33983536.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The Effect of Process Variables and Binder Concentration on Tabletability of Metformin Hydrochloride and Acetaminophen Granules Produced by Twin Screw Melt Granulation with Different Polymeric Binders. AU - Batra,Amol, AU - Thongsukmak,Atsawin, AU - Desai,Dipen, AU - Serajuddin,Abu T M, Y1 - 2021/05/13/ PY - 2020/12/15/received PY - 2021/04/14/accepted PY - 2021/5/13/entrez PY - 2021/5/14/pubmed PY - 2021/5/25/medline KW - Eudragit® EPO KW - Klucel® EXF KW - Soluplus® KW - acetaminophen KW - binder KW - melt granulation KW - metformin HCl KW - tablet KW - tabletability KW - twin screw extruder SP - 154 EP - 154 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 22 IS - 4 N2 - In twin screw melt granulation, granules are produced by passing mixtures of drug substances and polymeric binders through twin screw extruder such that temperatures are maintained below melting point of drugs but above glass transition of polymers used, whereby the polymers coat surfaces of drug particles and cause their agglomeration into granules. Since various formulation factors, such as binder type and concentration, and processing variables like extrusion temperature, screw configuration, and screw speed, can influence the granulation process, the present investigation was undertaken to study their effects on tabletability of granules produced. Three different types of polymeric binders, Klucel® EXF (hydroxypropyl cellulose), Eudragit® EPO (polyacrylate binder), and Soluplus® (polyvinyl caprolactam-co-vinyl acetate-ethylene glycol graft polymer), were used at 2, 5, and 10% concentrations. Metformin hydrochloride (HCl) (mp: 222°C) and acetaminophen (mp: 169°C) were used as model drugs, and drug-polymer mixtures with metformin HCl were extruded at 180, 160, and 130°C, while those with acetaminophen were extruded at 130 and 110°C. Other process variables included screw configurations: low, medium, and high shear for metformin HCl, and low and medium shear for acetaminophen; feed rates: 20 and 60 g/min; and screw speed of 100 and 300 RPM. Formulation and process variables had significant impact on tabletability. The target tensile strength of ≥2 MPa could be obtained with all polymers and at all processing temperatures when metformin HCl was granulated at 180°C and acetaminophen at 130°C. At other temperatures, the target tensile strength could be achieved at certain specific sets of processing conditions. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/33983536/The_Effect_of_Process_Variables_and_Binder_Concentration_on_Tabletability_of_Metformin_Hydrochloride_and_Acetaminophen_Granules_Produced_by_Twin_Screw_Melt_Granulation_with_Different_Polymeric_Binders_ DB - PRIME DP - Unbound Medicine ER -