Isothermal Microcalorimetry as a Quality by Design Tool to Determine Optimal Blending Sequences
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- 作者：M. H. D. Kamal Al-Hallak (1) (2)
Shirzad Azarmi (1) (3)
Zhenghe Xu (4)
Yadollah Maham (4)
Raimar L?benberg (1) - 关键词：isothermal microcalorimetry ; powders blending ; quality by design ; tablets
- 刊名：The AAPS Journal
- 出版年：2010
- 出版时间：September 2010
- 年：2010
- 卷：12
- 期：3
- 页码：417-423
- 全文大小：471KB
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Shirzad Azarmi (1) (3)
Zhenghe Xu (4)
Yadollah Maham (4)
Raimar L?benberg (1)
1. Faculty of Pharmacy and Pharmaceutical Sciences, 3126 Dentistry/Pharmacy Centre, University of Alberta, Edmonton, Alberta, Canada, T6G 2N8
2. Faculty of Pharmacy and Pharmaceutical Sciences, Damascus University, Damascus, Syria
3. Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
4. Department of Chemical and Materials Engineering, Faculty of Engineering, University of Alberta, Edmonton, Alberta, Canada - ISSN：1550-7416
文摘
This study was designed to assess the value of isothermal microcalorimetry (ITMC) as a quality by design (QbD) tool to optimize blending conditions during tablet preparation. Powder mixtures that contain microcrystalline cellulose (MCC), dibasic calcium phosphate dihydrate (DCPD), and prednisone were prepared as 1:1:1 ratios using different blending sequences. ITMC was used to monitor the thermal activity of the powder mixtures before and after each blending process. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) were performed on all final powder mixtures. Final powder mixtures were used to prepare tablets with 10?mg prednisone content, and dissolution tests were performed on all tablet formulations. Using ITMC, it was observed that the powder mixtures had different thermal activity depending on the blending sequences of the ingredients. All mixtures prepared by mixing prednisone with DCPD in the first stage were associated with relatively fast and significant heat exchange. In contrast, mixing prednisone with MCC in the first step resulted in slower heat exchange. Powder mixture with high thermal activity showed extra DSC peaks, and their dissolution was generally slower compared to the other tablets. Blending is considered as a critical parameter in tablet preparation. This study showed that ITMC is a simple and efficient tool to monitor solid-state reactions between excipients and prednisone depending on blending sequences. ITMC has the potential to be used in QbD approaches to optimize blending parameters for prednisone tablets.