Superdisintegrants for orally disintegrating and chewable tablets

INTERPharmaceuticalsPolyplasdone® CrospovidoneSuperdisintegrants fororally disintegratingand chewable tabletsRapid disintegration. Robust tablets. Smooth mouth feel.Fast dissolving, fast melting, chewable and orally dissolving ordisintegrating tablets are solid dosage forms that disintegrate rapidlyand dissolve in the mouth without water. These products have stayingpower in the marketplace because they appeal to consumers andsupport increased compliance among users as well as provide effectivelife-cycle management. The principle challenge with orally disintegratingtablets (ODTs) is to develop tablet formulations for standard directcompression processes that deliver rapid disintegration, pleasant mouthfeel and high breaking force for tablet robustness. Superdisintegrantsaffect a range of formulation parameters, including the rate of disintegration,tablet breaking force, and mouth feel. Polyplasdone XL-10superdisintegrant provides optimal performance in ODT formulations.Super disintegration efficiencyPolyplasdone crospovidone quickly wicks saliva into the tablet togenerate the volume expansion and hydrostatic pressures necessaryto provide rapid disintegration in the mouth. Unlike other superdisintegrants,which rely principally on swelling for disintegration, Polyplasdonesuperdisintegrants use a combination of swelling and wicking.When examined under a scanning electron microscope, Polyplasdonecrospovidone particles appear granular and highly porous (Figure 1).This unique, porous particle morphology facilitates wicking of liquidinto the tablet and particles to generate rapid disintegration.BenefitsProvides rapid disintegrationGives significantly higher tablet breaking force and lower friabilitySwells without gelling to provide rapid disintegrationand better textureAvailable in two particle sizes. Smaller particle size providessmoother mouth feel

PharmaceuticalsThe superdisintegrants were also evaluated in an ODT formulation(Table 1) containing 180-mg acetaminophen (APAP), a poorlycompressible material. The results show that Polyplasdonecrospovidones once again provide the highest tablet breakingforce over a range of compaction forces (Figure 6).Table 1: Acetaminophen (APAP) ODT formulationIngredient Amount %Encapsulated APAP* 17.90Mannitol (Spray Dried) 60.00Disintegrant 20.00Colloidal SiO 2 0.30Sodium Stearyl Fumarate 1.00Grape Flavor 0.50Sucralose 0.20Red Color 0.06Blue Color 0.04Total 100.00*Encapsulated APAP is 88% active acetaminophenSmooth mouth feelODTs with good mouth feel attributes support compliance andprovide a more pleasant consumer experience. The particle sizeof the superdisintegrant selected is one factor that impacts thetextural attributes of finished formulations. Large particles tendto provide a gritty feeling while smaller particles tend to supportsmooth texture. Polyplasdone XL-10 crospovidone provides thesmallest typical average particle size compared to other superdisintegrantsas shown in Table 2.In contrast to sodium starch glycolate and croscarmellosesodium, Polyplasdone superdisintegrants exhibit virtually notendency toward gel formation, even at high use levels. Disintegrantsthat gel can result in ODT and chewable products with anunpleasant, gummy texture. Polyplasdone superdisintegrantsprovide the best overall sensory experience as well as rapiddisintegration and robust tablets.Figure 6: Polyplasdone XL-10 superdisintegrant provides highesttablet breaking force in an acetaminophen ODT formulationBreaking Force (kp)201816141210864208.9 17.8 26.7Polyplasdone XLPolyplasdone XL-10Competitive CrospovidoneCroscarmellose SodiumSodium Starch GlycolateCompaction Force (kN)Table 2: Polyplasdone XL-10 crospovidone has smaller particlesDisintegrantTypical Average Particle Size(microns)Polyplasdone XL-10 ~25-40Polyplasdone XL ~110-140Croscarmellose Sodium ~50Sodium Starch Glycolate ~50To find additional ISP sales offices visit: ispcorp.comEMAIL: pharmaceuticalinfo@ispcorp.comBRAZILCHINATel: +55 11 3649-0455Tel: +86 21 6132-7888INDIAMEXICOTel: +9122 2837-0472Tel: +52 55 5276-6110GERMANY Tel: +49 (0) 2236 9649-260 UK Tel: +44 (0) 207 519-5054USA Tel: +1 973-628-4000CAN Tel: +1 905 607-2392Product Code: PH5284-I1-07/2009The information contained in this document and the various products described are intended for use only by persons having technical skill and at their own discretion and risk after they haveperformed necessary technical investigations, tests and evaluations of the products and their uses. While the information herein is believed to be reliable, we do not guarantee its accuracyand a purchaser must make its own determination of a product’s suitability for purchaser’s use, for the protection of the environment, and for the health and safety of its employees and thepurchasers of its products. Neither ISP nor its affiliates shall be responsible for the use of this information, or of any product, method or apparatus described in this document. Nothing hereinwaives any of ISP’s or its affiliates’ conditions of sale, and WE MAKE NO WARRANTY, EXPRESS OR IMPLIED, OF MERCHANTABILITY OR FITNESS OF ANY PRODUCT FOR A PARTICULAR USEOR PURPOSE. We also make no warranty against infringement of any patents by reason of purchaser’s use of any information, product, method or apparatus described in this document.INispcorp.com