Poster: Granfiller-D® & Hisorad® As New Co-processed Excipients For Orally Disintegrating Tablets Produced by Direct Compression

Introduction: Tablets are still the most widely used dosage form for oral application due to their simple administration and relatively low manufacturing costs. One main disadvantage of tablets is the difficulty in swallowing or chewing. This is especially relevant for special patient groups, e.g. pediatric and geriatric patients [1]. To avoid this problem and still enable oral tablet drug therapy, orodispersible tablets (ODTs) can be used. Orodispersible tablets rapidly disintegrate after their administration to the mouth without chewing or intake of water. With the help of ODTs easy application of liquid dosage forms can be combined with the high physical and chemical stability of solid drug dosage forms [2]. Our investigations focused on the direct compression of co-processed excipients (CPE) together with enalapril maleate, ibuprofen and paracetamol as model APIs. Ideally, the co-processing leads to multifunctional excipients, which offer a better balance between sufficient strength and required disintegration time[3]. The aim of this study was the comparison of two new co-processed excipients with already commercially available ones. For this purpose, the dependence of disintegration time on achieved tablet strength was analyzed for seven CPEs including each of the three APIs.

Materials and methods: The CPEs investigated in this study were Granfiller-D®211 (Daicel, Japan), Hisorad® (Daicel, Japan), SmartEx®QD-50 (Shin-Etsu, Japan), Ludiflash® (BASF, Germany), Prosolv® ODT (JRS Pharma, Germany), Pearlitol® Flash (Roquette, France) and Parteck® ODT (Merck, Germany). Each of the CPEs to be tested was blended with 3 model APIs separately for 15 minutes. In a second mixing step 1% magnesium stearate was added as lubricant and mixed for 3 more minutes. Each batch of the powder blends containing paracetamol and ibuprofen (both 50%) as model APIs was directly compressed on the compaction simulator Styl´One Evolution (Medel´Pharm, France). To thoroughly evaluate in how far the CPEs can impact content uniformity (not shown) for low dosed formulations, the blends containing enalapril maleate (4%) were directly compressed on a rotary tablet press Korsch XM12 (Korsch, Germany). Six different compression pressures were applied (50-250 MPa). Flat faced, facetted punches with a diameter of 9mm were used. Tablet properties were measured by Smart Test ST50 (Sotax, Switzerland). The tensile strength was calculated according to Fell and Newton [4]. Disintegration studies were performed in a disintegration test apparatus (Z32 Erweka GmbH, Germany) according to Ph.Eur.10.

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Article information: M. Kokott, T. Okabayashi, A. Lura, R. Wiedey, J. Breitkreutz. Institute of Pharmaceutics and Biopharmaceutics, Heinrich Heine University, 40225 Duesseldorf , Germany.
DAICEL CORPORATION,1 8 23, Konan, Minato ku, Tokyo, 108 0075, Japan.

See also the Granfiller-D® video here:

https://youtu.be/C3cdEQnUj9I