Co-Processed Excipients for Dispersible Tablets–Part 1: Manufacturability

Co-processed excipients may enhance functionality and reduce drawbacks of traditional excipients for the manufacture of tablets on a commercial scale. The following study aimed to characterise a range of co-processed excipients that may prove suitable for dispersible tablet formulations prepared by direct compression. Co-processed excipients were lubricated and compressed into 10.5-mm convex tablets using a Phoenix compaction simulator.

Compression profiles were generated by varying the compression force applied to the formulation and the prepared tablets were characterised for hardness, friability, disintegration and fineness of dispersion. Our data indicates that CombiLac, F-Melt type C and SmartEx QD100 were the top 3 most suitable out of 16 co-processed excipients under the conditions evaluated. They exhibited good flow properties (Carr’s index 20), excellent tabletability (tensile strength > 3.0 MPa at 0.85 solid fraction), very low friability (< 1% after 15 min), rapid disintegration times (27–49 s) and produced dispersions of ideal fineness (< 250 μm).

Other co-processed excipients (including F-Melt type M, Ludiflash, MicroceLac, Pharmaburst 500 and Avicel HFE-102) may be appropriate for dispersible tablets produced by direct compression providing the identified disintegration and dispersion risks were mitigated prior to commercialisation. This indicates that robust dispersible tablets which disintegrate rapidly could be manufactured from a range of co-processed excipients.

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Article information: Ben J. Bowles, Karolina Dziemidowicz, Felipe L. Lopez, Mine Orlu, Catherine Tuleu,
Andrew J. Edwards, and Terry B. Ernest. AAPS PharmSciTech. DOI: 10.1208/s12249-018-1090-4

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Materials: The excipients investigated in this study were Avicel® HFE-102 (FMC biopolymers, Philadelphia, PA, USA); Compressol® SM and Pharmaburst® 500 (SPI Pharma, Septemes Les Vallons, France); CombiLac® and MicroceLac® (Meggle Pharma, Wasserburg, Germany); Di- Pac (Domino Specialty Ingredients, Decatur, IL, USA); Ludiflash® and Ludipress® (BASF, Lampertheim, Germany); Emdex® and ProSolv® ODT (JRS Pharma, Cedar Rapids, IA, USA); F-Melt® type C and F-Melt® type M (Fuji Health Science, Toyama, Japan); Pearlitol® Flash (Roquette, Corby, Northamptonshire, UK); SmartEx® QD50 and SmartEx® QD100 (ShinEtsu, Tokyo, Japan); and StarCap 1500 (Colorcon, Indianapolis, IN, USA). Avicel® PH-102 (FMC Biopolymers) was tested as a comparator against the co-processed excipients since it is a highly compressible non-co-processed excipient. Sodium starch fumarate (SSF) was used as lubricant (Pruv®, JRS Pharma, Cedar Rapids, IA, USA). Croscarmellose sodium (Ac-Di- Sol®, FMC Biopolymers), crospovidone (Kollidon® CL-SF, BASF) and low-substituted hydroxypropyl cellulose (L-HPC, NBD-22®, ShinEtsu) were employed as disintegrants. All samples were kindly provided by the manufacturers. The individual constituents of the co-processed excipients are presented in Table I.