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Effect of Tablet Structure on Controlled Release from Supersaturating Solid Dispersions Containing Glyceryl Behenate

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The University of Texas at Austin, 1 University Station, Austin, Texas 78712, United States
DisperSol Technologies, 111 West Cooperative Way, Suite 200, Georgetown, Texas 78626, United States
§ GATTEFOSSE SAS, 36, Chemin de GENGAS, Sain-Priest 69804, France
*Address: The University of Texas at Austin, Division of Pharmaceutics, 1 University Station A1920, Austin, Texas 78712, United States. Phone: 512-471-6834. Fax: 512-471-7474. E-mail: [email protected]
Cite this: Mol. Pharmaceutics 2015, 12, 1, 120–126
Publication Date (Web):October 27, 2014
https://doi.org/10.1021/mp500480y
Copyright © 2014 American Chemical Society
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Abstract

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The objective of this study was to evaluate the use of glyceryl behenate as a plasticizer and release modifier in solid dispersion systems containing itraconazole and carbamazepine. Amorphous solid dispersions of high molecular weight polyvinylpyrrolidone were prepared by hot-melt extrusion, the processing of which was improved by the inclusion of glyceryl behenate. Dispersions were milled and subsequently compressed into tablets. Solid dispersions were also prepared by KinetiSol Dispersing, which allowed for the manufacture of monolithic tablets of the same composition and shape as compressed tablets. Tablets without glyceryl behenate and all compressed tablets were observed to have an incomplete release profile likely due to drug crystallization within the tablet as this occurred at conditions in which dissolution concentrations were below saturation. Monolithic tablets formulated to be more hydrophobic, by including glyceryl behenate, allowed for sustained release below and above saturation conditions.

Cited By


This article is cited by 10 publications.

  1. Abdullah Alshetaili, Bjad K. Almutairy, Sultan M. Alshehri, Michael A. Repka. Development and Characterization of Sustained-Released Donepezil Hydrochloride Solid Dispersions Using Hot Melt Extrusion Technology. Pharmaceutics 2021, 13 (2) , 213. https://doi.org/10.3390/pharmaceutics13020213
  2. Gautam Chauhan, Abdul A. Shaik, Nishant S. Kulkarni, Vivek Gupta. The preparation of lipid-based drug delivery system using melt extrusion. Drug Discovery Today 2020, 25 (11) , 1930-1943. https://doi.org/10.1016/j.drudis.2020.07.025
  3. Xin Feng, Feng Zhang. Twin-screw extrusion of sustained-release oral dosage forms and medical implants. Drug Delivery and Translational Research 2018, 8 (6) , 1694-1713. https://doi.org/10.1007/s13346-017-0461-9
  4. Julien Maincent, Robert O. Williams. Sustained-release amorphous solid dispersions. Drug Delivery and Translational Research 2018, 8 (6) , 1714-1725. https://doi.org/10.1007/s13346-018-0494-8
  5. Daniel J. Ellenberger, Dave A. Miller, Robert O. Williams. Expanding the Application and Formulation Space of Amorphous Solid Dispersions with KinetiSol®: a Review. AAPS PharmSciTech 2018, 19 (5) , 1933-1956. https://doi.org/10.1208/s12249-018-1007-2
  6. Toshiro Sakai, Daiki Hirai, Shin-ichiro Kimura, Yasunori Iwao, Shigeru Itai. Effects of tablet formulation and subsequent film coating on the supersaturated dissolution behavior of amorphous solid dispersions. International Journal of Pharmaceutics 2018, 540 (1-2) , 171-177. https://doi.org/10.1016/j.ijpharm.2018.02.013
  7. Jiannan Lu, Sakae Obara, Fei Liu, Wanyi Fu, Wen Zhang, Shingo Kikuchi. Melt Extrusion for a High Melting Point Compound with Improved Solubility and Sustained Release. AAPS PharmSciTech 2018, 19 (1) , 358-370. https://doi.org/10.1208/s12249-017-0846-6
  8. Julien Maincent, Feng Zhang. Recent advances in abuse-deterrent technologies for the delivery of opioids. International Journal of Pharmaceutics 2016, 510 (1) , 57-72. https://doi.org/10.1016/j.ijpharm.2016.06.012
  9. Leena Kumari Prasad, Justin R. Hughey, James W. McGinity, Dave A. Miller, Robert O. Williams. Emerging Technologies to Increase the Bioavailability of Poorly Water-Soluble Drugs. 2016,,, 691-740. https://doi.org/10.1007/978-3-319-42609-9_13
  10. Karin Becker, Sharareh Salar-Behzadi, Andreas Zimmer. Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations. Pharmaceutical Research 2015, 32 (5) , 1519-1545. https://doi.org/10.1007/s11095-015-1661-y

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