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Optimization of hot melt extrusion parameters for sphericity and hardness of polymeric face-cut pellets.
Drug Dev Ind Pharm. 2016 Nov; 42(11):1833-41.DD

Abstract

The aim of this study was to formulate face-cut, melt-extruded pellets, and to optimize hot melt process parameters to obtain maximized sphericity and hardness by utilizing Soluplus(®) as a polymeric carrier and carbamazepine (CBZ) as a model drug. Thermal gravimetric analysis (TGA) was used to detect thermal stability of CBZ. The Box-Behnken design for response surface methodology was developed using three factors, processing temperature (°C), feeding rate (%), and screw speed (rpm), which resulted in 17 experimental runs. The influence of these factors on pellet sphericity and mechanical characteristics was assessed and evaluated for each experimental run. Pellets with optimal sphericity and mechanical properties were chosen for further characterization. This included differential scanning calorimetry, drug release, hardness friability index (HFI), flowability, bulk density, tapped density, Carr's index, and fourier transform infrared radiation (FTIR) spectroscopy. TGA data showed no drug degradation upon heating to 190 °C. Hot melt extrusion processing conditions were found to have a significant effect on the pellet shape and hardness profile. Pellets with maximum sphericity and hardness exhibited no crystalline peak after extrusion. The rate of drug release was affected mainly by pellet size, where smaller pellets released the drug faster. All optimized formulations were found to be of superior hardness and not friable. The flow properties of optimized pellets were excellent with high bulk and tapped density.

Authors+Show Affiliations

a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ; b Department of Pharmaceutics, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ;b Department of Pharmaceutics, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ;c Department of Pharmaceutics, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ;b Department of Pharmaceutics, College of Pharmacy , Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ;d BASF Corporation , Tarrytown , NY , USA ;e R&D Project, Management Excipients, BASF SE , Ludwigshafen , Germany ;f Global Development and Technical Marketing, BASF SE , Ludwigshafen , Germany ;g Thermo Fisher Scientific , Tewksbury , MA , USA ;a Department of Pharmaceutics and Drug Delivery, School of Pharmacy , The University of Mississippi, University , MS , USA ; h Pii Center for Pharmaceutical Technology, The University of Mississippi, University , MS , USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27080252

Citation

Alshetaili, Abdullah S., et al. "Optimization of Hot Melt Extrusion Parameters for Sphericity and Hardness of Polymeric Face-cut Pellets." Drug Development and Industrial Pharmacy, vol. 42, no. 11, 2016, pp. 1833-41.
Alshetaili AS, Almutairy BK, Alshahrani SM, et al. Optimization of hot melt extrusion parameters for sphericity and hardness of polymeric face-cut pellets. Drug Dev Ind Pharm. 2016;42(11):1833-41.
Alshetaili, A. S., Almutairy, B. K., Alshahrani, S. M., Ashour, E. A., Tiwari, R. V., Alshehri, S. M., Feng, X., Alsulays, B. B., Majumdar, S., Langley, N., Kolter, K., Gryczke, A., Martin, S. T., & Repka, M. A. (2016). Optimization of hot melt extrusion parameters for sphericity and hardness of polymeric face-cut pellets. Drug Development and Industrial Pharmacy, 42(11), 1833-41. https://doi.org/10.1080/03639045.2016.1178769
Alshetaili AS, et al. Optimization of Hot Melt Extrusion Parameters for Sphericity and Hardness of Polymeric Face-cut Pellets. Drug Dev Ind Pharm. 2016;42(11):1833-41. PubMed PMID: 27080252.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Optimization of hot melt extrusion parameters for sphericity and hardness of polymeric face-cut pellets. AU - Alshetaili,Abdullah S, AU - Almutairy,Bjad K, AU - Alshahrani,Saad M, AU - Ashour,Eman A, AU - Tiwari,Roshan V, AU - Alshehri,Sultan M, AU - Feng,Xin, AU - Alsulays,Bader B, AU - Majumdar,Soumyajit, AU - Langley,Nigel, AU - Kolter,Karl, AU - Gryczke,Andreas, AU - Martin,Scott T, AU - Repka,Michael A, Y1 - 2016/05/04/ PY - 2016/4/16/entrez PY - 2016/4/16/pubmed PY - 2017/3/25/medline KW - Box–Behnken design KW - Soluplus® KW - carbamazepine KW - design of experiment KW - face-cut pellets KW - hardness KW - hot melt extrusion KW - sphericity SP - 1833 EP - 41 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 42 IS - 11 N2 - The aim of this study was to formulate face-cut, melt-extruded pellets, and to optimize hot melt process parameters to obtain maximized sphericity and hardness by utilizing Soluplus(®) as a polymeric carrier and carbamazepine (CBZ) as a model drug. Thermal gravimetric analysis (TGA) was used to detect thermal stability of CBZ. The Box-Behnken design for response surface methodology was developed using three factors, processing temperature (°C), feeding rate (%), and screw speed (rpm), which resulted in 17 experimental runs. The influence of these factors on pellet sphericity and mechanical characteristics was assessed and evaluated for each experimental run. Pellets with optimal sphericity and mechanical properties were chosen for further characterization. This included differential scanning calorimetry, drug release, hardness friability index (HFI), flowability, bulk density, tapped density, Carr's index, and fourier transform infrared radiation (FTIR) spectroscopy. TGA data showed no drug degradation upon heating to 190 °C. Hot melt extrusion processing conditions were found to have a significant effect on the pellet shape and hardness profile. Pellets with maximum sphericity and hardness exhibited no crystalline peak after extrusion. The rate of drug release was affected mainly by pellet size, where smaller pellets released the drug faster. All optimized formulations were found to be of superior hardness and not friable. The flow properties of optimized pellets were excellent with high bulk and tapped density. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/27080252/Optimization_of_hot_melt_extrusion_parameters_for_sphericity_and_hardness_of_polymeric_face_cut_pellets_ L2 - https://www.tandfonline.com/doi/full/10.1080/03639045.2016.1178769 DB - PRIME DP - Unbound Medicine ER -