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Particle Engineering Via Surface Modification During Micronization for Pharmaceutical Applications

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Particle Engineering Via Surface Modification During Micronization for Pharmaceutical Applications New Jersey Institute of Technology Digital Commons @ NJIT Dissertations Electronic Theses and Dissertations Fall 1-31-2013 Particle engineering via surface modification during micronization for pharmaceutical applications Xi Han New Jersey Institute of Technology Follow this and additional works at: https://digitalcommons.njit.edu/dissertations Part of the Chemical Engineering Commons Recommended Citation Han, Xi, "Particle engineering via surface modification during micronization for pharmaceutical applications" (2013). Dissertations. 349. https://digitalcommons.njit.edu/dissertations/349 This Dissertation is brought to you for free and open access by the Electronic Theses and Dissertations at Digital Commons @ NJIT. It has been accepted for inclusion in Dissertations by an authorized administrator of Digital Commons @ NJIT. For more information, please contact [email protected]. Copyright Warning & Restrictions The copyright law of the United States (Title 17, United States Code) governs the making of photocopies or other reproductions of copyrighted material. Under certain conditions specified in the law, libraries and archives are authorized to furnish a photocopy or other reproduction. One of these specified conditions is that the photocopy or reproduction is not to be “used for any purpose other than private study, scholarship, or research.” If a, user makes a request for, or later uses, a photocopy or reproduction for purposes in excess of “fair use” that user may be liable for copyright infringement, This institution reserves the right to refuse to accept a copying order if, in its judgment, fulfillment of the order would involve violation of copyright law. Please Note: The author retains the copyright while the New Jersey Institute of Technology reserves the right to distribute this thesis or dissertation Printing note: If you do not wish to print this page, then select “Pages from: first page # to: last page #” on the print dialog screen The Van Houten library has removed some of the personal information and all signatures from the approval page and biographical sketches of theses and dissertations in order to protect the identity of NJIT graduates and faculty. ABSTRACT PARTICLE ENGINEERING VIA SURFACE MODIFICATION DURING MICRONIZATION FOR PHARMACEUTICAL APPLICATIONS by Xi Han Improving the dissolution rate of Biopharmaceutics Classification System (BCS) class II drugs is an important research area. Micronization which can increase the specific surface area is a promising method to improve the dissolution rate. Micronization alone, however, can lead to downstream processing problems related to poor flow and dispersion properties. The importance of the flowability of pharmaceutical powders is well-documented in the literature. It is, therefore, important to develop a method that can simultaneously overcome these processing issues and allow for micronizing the API. In this work, dry particle coating technique is investigated in the context of micronizing API powders and overcoming problems associated with the micronized fine powders due to their strong cohesive forces. Consequently, the main objective of this dissertation is to investigate if simultaneous micronization and dry coating process (SM-DC) is beneficial for pharmaceutical applications. The work addresses and answers several important issues as discussed next. First, using ibuprofen as a test-case, it is shown that flow properties and dissolution rate were significantly improved when micronization was performed along with dry coating (SM-DC process). Additionally, co-grinding with water-soluble polymer during micronization was considered and led to further dissolution rate improvement and increased bulk density. The surface modified, micronized powders also showed improved dispersion, significantly higher bulk densities, reduced electrostatic charging, and higher flowability compared to the pure micronized sample. Next, these dry coated fine API powders were formulated into blends with different API loadings. The results showed that the blends containing dry coated API powders had excellent flowability and high bulk density. In contrast, blends containing uncoated APIs had poor flow and lower bulk densities. As the API loading increased, the difference between dry coated and uncoated blends was more pronounced. Tablets prepared from dry coated API blends exhibited superior compactibility and dissolution profiles, particularly for higher drug loadings. This illustrated the advantages of the dry coating during API micronization, without any adverse impact on tabletting operations and tablet properties. Next, an in-depth understanding of the effect of milling and dry coating on the surface properties of milled ibuprofen powders was investigated. Inverse Gas Chromatography technique was used and the dispersive surface energy of pure milled powders was heterogeneous in nature. In contrast, dry coating with nano-particles was found to quench the high energy sites and make the surface energy of the powders comparatively uniform and the average values similar to that of the nano-particle used for the dry coating. Last, a simple shear test based method was developed to estimate the granular Bond number to evaluate the performance of dry coating. This technique eliminates the usual need of detailed, time consuming particle scale characterization via atomic force microscopy. Estimated Bond numbers were compared and verified with those calculated from IGC method. Further, estimated Bond number was correlated with the bulk flow properties. The overall effect of dry coating (changing both the surface energy and nano-scale asperities) can be well demonstrated using the estimated Bond numbers. By addressing these four issues, the main hypothesis of the thesis, dry coating applied to the micronization process is beneficial to the pharmaceutical application, is proven. ii PARTICLE ENGINEERING VIA SURFACE MODIFICATION DURING MICRONIZATION FOR PHARMACEUTICAL APPLICATIONS by Xi Han A Dissertation Submitted to the Faculty of New Jersey Institute of Technology in Partial Fulfillment of the Requirements for the Degree of Doctor of Philosophy in Chemical Engineering Otto H. York Department of Chemical, Biological and Pharmaceutical Engineering January 2013 Copyright © 2013 by Xi Han ALL RIGHTS RESERVED . iv APPROVAL PAGE PARTICLE ENGINEERING VIA SURFACE MODIFICATION DURING MICRONIZATION FOR PHARMACEUTICAL APPLICATIONS Xi Han Dr. Rajesh Davé, Dissertation Advisor Date Distinguished Professor of Chemical, Biological and Pharmaceutical Engineering, NJIT Dr. Ecevit Bilgili, Committee Member Date Assistant Professor of Chemical, Biological and Pharmaceutical Engineering, NJIT Dr. Norman Loney, Committee Member Date Professor of Chemical, Biological and Pharmaceutical Engineering, NJIT Dr. Edward Dreyzin, Committee Member Date Professor of Chemical, Biological and Pharmaceutical Engineering, NJIT Dr. Zafar Iqbal, Committee Member Date Research Professor of Chemistry and Environmental Science, NJIT BIOGRAPHICAL SKETCH Author: Xi Han Degree: Doctor of Philosophy Date: January 2013 Undergraduate and Graduate Education: • Doctor of Philosophy in Chemical Engineering, New Jersey Institute of Technology, Newark, NJ, 2013 • Bachelor of Science in Chemical Engineering and Technology, Tianjin University, Tianjin, P. R. China, 2007 Major: Chemical Engineering Presentations and Publications: Journals: Han, X., et al., Simultaneous micronization and surface modification for improvement of flow and dissolution of drug particles. International Journal of Pharmaceutics, 2011. 415(1-2): p. 185-195. Han, X., C. Ghoroi, and R. Davé, Dry coating of micronized API powders for improved dissolution of directly compacted tablets with high drug loading. International Journal of Pharmaceutics, 2012. In press. Ghoroi, C., et al., Dispersion of fine and ultrafine powders through surface modification and rapid expansion. Chemical Engineering Science, 2012. In press. Han, X., et al., Passivation of High Surface Energy Sites of Milled Pharmaceutical Crystals via Dry Coating. Journal of Pharmaceitcal Sciences, 2012. In review. He, X., et al., Assessing powder segregation potential by near infrared (NIR) spectroscopy and correlating segregation tendency to tabletting performance . Powder Technology, 2012. In press. Han, X., et al., A simple method to estimate the granular Bond number , Granular Matter, 2012. In preparation. iv Proceedings: Han, X., et al., Engineered Particles By Using Fluid Energy Mill for Pharmaceutical Application, AICHE Annual meeting, Conference Proceedings, 2009. Han, X., et al., Simultaneous Micronization and Surface Modification as a Tool to Improve Flow and Dissolution of Pharmaceutical Powders, AICHE Annual meeting, Conference Proceedings, 2010. Han, X., et al., Particle Engineering Via Dry Coating of Micronized API Powders for Improved Dissolution of Directly Compacted Tablets with High Drug Loading, AICHE Annual meeting, Conference Proceedings, 2012. Han, X., et al., Using Inverse Gas Chromatography to Assess Passivation of High Surface Energy Sites of Milled Pharmaceutical Crystals Via Dry Coating of Nano-Silica, AICHE Annual meeting, Conference Proceedings, 2012. He, X., et al., Assessing Powder Segregation Potential by near Infrared (NIR) Spectroscopy and Correlating Bench Scale Segregation Tendency to Tabletting Performance, Annual meeting, Conference Proceedings, 2012. v 献给我的父母： 韩庆发， 李群； 姥姥姥爷：李麒祥，谷洪范; 男友: 杜伍耀 To my parents，my grandparents and my boyfriend vi ACKNOWLEDGMENT
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