Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders

The introduction of the high-speed tableting machines and the lack of excipients with good flow and compaction properties required for direct compression process have increased research interest in the development of co-processed excipients. Melt granulation, as an environmentally friendly and cost-effective method, has recently been recognized as a promising co-processing technique. The aim of the present study was to prepare lipid-based co-processed excipients by in situ fluidized bed melt granulation and to investigated their suitability for direct compression process. Lactose monohydrate was co-processed with glyceryl dibehenate (Compritol® 888 ATO) or glyceryl palmitostearate (Precirol® ATO 5), as lipophilic meltable binders.

Highlights

• Fluidized bed melt granulation is used to co-process lactose with lipid excipients.

• Novel co-processed lactose is directly compressible and has high tabletability.

• High amounts of poorly compressible paracetamol can be formulated.

• Net work of compression is more efficiently converted into tablets tensile strength.

• No additional lubricants are required with small detachment and ejection stresses.

Besides the flowability testing, dynamic compaction analysis was applied for thorough investigation into the tableting properties of developed co-processed excipients. Solid state characterization, performed by means of XRPD and DRIFT, confirmed the absence of chemical changes of the single components of co-processed excipients. Co-processed excipients showed improved flowability in comparison with single ingredients and corresponding physical mixtures. Novel co-processed excipients were found to have better tabletability profiles than physical mixtures of the ingredients, and were able to retain acceptable tensile strength values at high content of paracetamol in tableting mixture. Tablets with high tensile strength could be obtained with less work of compression needed in comparison with the commercial lactose-based excipients. Furthermore, novel lipid-based co-processed excipients were found to be highly superior regarding the antiadhesive and lubricating properties, with no additional lubricants required.

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Slobodanka Ćirin-Varađan, Jelena Đuriš, Miljana Mirković, Marija Ivanović, Jelena Parojčić, Ivana Aleksić,
Comparative evaluation of mechanical properties of lactose-based excipients co-processed with lipophilic glycerides as meltable binders, Journal of Drug Delivery Science and Technology, 2021, 102981, ISSN 1773-2247,
https://doi.org/10.1016/j.jddst.2021.102981.