Tablets & Capsules

TC0120

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Tablets & Capsules January 2020 32C reformulated ODTs pressed at several different compres- sion forces versus the hardness of the commercial CoQ10 ODT (88 newtons). When the compression force was increased from 5 to 20 kilonewtons, the hardness of the reformulated CoQ10 ODT increased from 60 to 150 new- tons. A compression force of 10 kilonewtons resulted in a hardness of 95 newtons, which was close to the 88-newton tablet hardness of the commercial product. Increasing the percentage of Kollidon CL-SF in the reformulated ODTs increased the tablet hardness, because the excipient also functions as a direct compression binder [3]. For example, at 10 kilonewtons of compression force, 10 percent Kollidon CL-SF produced ODTs with a hardness of 89 newtons while 15 percent Kollidon CL-SF produced ODTs with a hardness of 95 newtons. Next, the friability of the ODT products was measured using a model 10801 Vankel Vanderkamp friability tester. Reformulated ODTs made using 5 kilonewtons of com- pression force produced 0.5 percent friability, similar to products. ODTs dissolve rapidly in contact with saliva, eliminating the need to chew or swallow the tablet, which can improve compliance among the geriatric population. The drawback of poorly formulated ODTs is that they often have a sandy/gritty mouthfeel and lack the organo- leptic properties (taste and aftertaste) that patients desire. To fully meet consumers' needs and improve patient com- pliance, a CoQ10 ODT should disintegrate quickly with- out compromising taste and mouthfeel. This article describes a study that compared a commer- cial CoQ10 ODT product with a formulation designed to exhibit improved taste and disintegration characteristics. Reformulation methods and results A commercially available CoQ10 ODT with a round tablet profile, an active ingredient strength of 80 milli- grams, and a tablet weight of 500 milligrams was used as the reference product. The reformulated product also included 80 milligrams of CoQ10, along with Kollidon CL-SF (crosslinked polyvinylpyrrolidone), a water-insol- uble crospovidone with a strong disintegration capability; Ludiflash (D-mannitol, crospovidone, polyvinyl acetate, and povidone), a directly compressible excipient designed for ODTs; natural orange flavor; sucralose; Aerosil 200 (hydrophilic fumed silica); and magnesium stearate in the amounts shown in Table 1. The reformulated ODTs were of similar size and shape as the commercial ODT using 12-millimeter punches with a compound cup profile on a Korsch XL 100 tablet press. As Photo 1 shows, the surface of the commercial tablets had a significant number of yellow spots that may have been a result of insufficient blending. Because the refor- mulated ODT formulation was initially blended for 20 minutes with Kollidon CL-SF, which is known for dispers- ing agglomerated powders and improving flowability [2], the reformulated product had a smoother, more uniform tablet surface than the commercial product. Tablet hardness was measured using a Key International HT-300 tablet tester. Figure 1 shows the hardness of the Photo 1: Optical photos of commercial CoQ10 ODT (left) and newly prepared Ludiflash CoQ10 ODT (right). Table 1 Formulation of CoQ10 ODT Composition Weight (mg) w/w (%) CoQ10 80.0 16.0 Kollidon CL-SF 75.0 15.0 Ludiflash 334.5 66.9 Natural orange flavor 2.5 0.5 Sucralose 1.5 0.3 Aerosil 200 1.5 0.3 Magnesium Stearate 5.0 1.0 Total 500.0 100.0 Figure 1 Hardness of CoQ10 ODTs Hardness (N) Compression force (kN) Commercial ODT 180 150 120 90 60 30 0 5 10 15 20

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