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Preparation of Sustained Release Tablet with Minimized Usage of Glyceryl Behenate Using Post-Heating Method

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Abstract

The purpose of this study was to prepare sustained release (SR) matrix tablets using a direct compression incorporated with a post-heating process. Allopurinol was selected due to the water-soluble property and Compritol 888 ATO® (also known as glyceryl behenate) was used as an SR matrix-forming agent. The API, SR material, microcrystalline cellulose, and magnesium stearate (lubricant) were mixed and prepared into a tablet by a direct compression method. The compressed tablets were stored in a dry oven at four temperatures (60, 70, 80, and 90°C) and for three time periods (15, 30, 45 min). The DSC and PXRD data indicated that the crystallinity of the API was not altered by the post-heating method. However, SEM images demonstrated that Compritol 888 ATO® was melted by the post-heating method, and that the melted Compritol 888 ATO® could form a strong matrix. This strong matrix led to the significant sustained release behavior of hydrophilic APIs. As little as 3 mg of Compritol 888 ATO® (0.65% of total tablet weight), when heated at 80°C for 15 min, showed sustained release over 10 h. The post-heating method exerted a significant influence on lipid-based matrix tablets and allowed a reduction in the amount of material required for a water-soluble drug. This will also provide a valuable insight into lipid-based SR tablets and will allow their application to higher quality products and easier processing procedures.

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Acknowledgments

This work was supported by the Sahmyook University Research Fund in 2016 (no. RI22016007).

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Authors and Affiliations

  1. College of Pharmacy, Sahmyook University, Seoul, 01795, Republic of Korea

    Changmin Kang, Ju-Hyun Lee & Jun-Bom Park

  2. Department of Pharmaceutical Engineering, Cheongju University, Cheongju, 363-763, Republic of Korea

    Dong-Wook Kim

  3. College of Pharmacy, Ajou University, Suwon, 16499, Republic of Korea

    Beom-Jin Lee

  4. Bioavailability Control Lab, Sahmyook University, Seoul, 01795, Republic of Korea

    Jun-Bom Park

Authors
  1. Changmin Kang
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  2. Ju-Hyun Lee
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Correspondence to Jun-Bom Park.

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The authors declare that there is no conflict of interests regarding the publication of this paper.

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Kang, C., Lee, JH., Kim, DW. et al. Preparation of Sustained Release Tablet with Minimized Usage of Glyceryl Behenate Using Post-Heating Method. AAPS PharmSciTech 19, 3067–3075 (2018). https://doi.org/10.1208/s12249-018-1128-7

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  • DOI: https://doi.org/10.1208/s12249-018-1128-7

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