Pharmaceutical Excipients and Coating Systems

1 PharmaceuticalExcipients andCoating SystemsKlucel hydroxypropylcelluloseKlucel hydroxypropylcellulose(HPC) provides a remarkable set ofphysical properties for tablet binding,modified release and film Coating . Itcombines organic solvent or aqueoussolubility, thermoplasticity andsurface activity. Low viscosity E andL types are widely used for premiertablet binding with low use levels(2-6%) and improved adhesion andflexible Coating applications. Regularparticle size materials are used in wetprocessing and the X-grind materialfor dry processing. Many viscositytypes are used for modified releasematrix Systems . Low molecularweight Klucel HPC polymers, duePharmaceutical Excipientsto their thermoplastic behavior andsuperior flow properties, findapplications in melt extrusion.

2 ThePHARM grades of Klucel HPCcomply with the monographrequirements of the NationalFormulary, European Pharmacopoeiaand the Japanese additional information on Klucel HPC,please refer to booklet 250-2F on the Aqualonweb site at hypromelloseBenecel hypromellose(hydroxypropylmethylcellulos e,HPMC) is widely used in thepharmaceutical industry due to theirability to thicken, bind and retainwater; emulsify; suspend particulates;stabilize; and form films. Thesepolymers are soluble in cold waterand some mixed solvents , butinsoluble in hot water due to products are supplied aswhite to off-white, free flowingpowders. Controlled release (CR)grades have a fine , narrow particlesize distribution that is optimized forhydrophilic matrix tablets.

3 AllBenecel products labeled withthe PH suffix are compliant withthe monograph requirements ofthe current editions of theNational Formulary, the EuropeanPharmacopoeia and the request literature or samples, please contact Aqualon Customer Service at1-877-5GO AQUA (1-877-546-2782) or e-mail us at HPCT ypical BrookfieldAt SolutionGrade (X = Fine)Viscosity ( )ConcentrationHF Pharm, HXF Pharm1,500 3,0001 %MF Pharm, MXF Pharm4,000 6,5002 %GF Pharm, GXF Pharm150 4002 %JF Pharm, JXF Pharm150 4005 % LF Pharm, LXF Pharm 75 1505 %EF Pharm, EXF Pharm300 60010 %ELF Pharm150 22510%USPB enecel HPMCN ominal USPS ubstitution TypeGradeViscosity (cps)MethylcelluloseA15C PH1500A4M PH40002910E3PH3E5PH5E6PH6E15 PH15E50 PH50E4M PH3600E4M PH CR3600E10M PH10000E10M PH CR100002208K100LV PH100K100LV PH CR100K4 MPH3600K4M PH CR3600K15M PH18000K15M PH CR18000K35M PH35000K35M PH CR35000K100M PH100000K100M PH CR100000K200M PH200000K200M PH CR200000 Aqualon and Blanose carboxymethylcelluloseAqualon and Blanose carboxymethylcellulose (CMC) isan anionic, water-soluble uses for CMC are in (a)ointments, creams, and lotions, as astabilizer, thickener and film-former,(b) jellies and salves, as a thickener,gelling agent, and protective colloidand film-former, (c) syrups andsuspensions, as a thickener andsuspending aid, (d)

4 Bulk laxatives,physiologically inert with high water-binding capacity, (e) mucoadhesivesfor its absorbency, (f) sustainedrelease, as a thickener and diffusionbarrier, and (g) tablet Coating as afilm-former. A variety of CMC gradesare available, with varying degrees ofsubstitution, viscosities and particlesizes. S-types provide smoothsolutions, based on uniformsubstitution. O-types providesolubility and viscosity stability onstorage in low pH media. Aqualon CMC grades designated P or PH arecompliant with the monographrequirements of the United StatesPharmacopoeia / National CMC grades designated Por PH are compliant with themonograph requirements of theEuropean Pharmacopoeia and theUnited States Pharmacopoeia /National additional information on Aqualon CMC,please refer to booklets 250-10H on theAqualon web site at CMCD egree of (1% concentration)1500-30007HF PH1000-28007H3SF PH1000-28007H3SF PHMedium (2% concentration)1500-31009M31F PH800-310012M31P400-8007MF PH7M8SF PH300-8009M8F PHLow (2% concentration)25-507LF PHExtra Low (4% concentration)50-2007L2 PBlanose CMCD egree of (1% concentration)

5 2500-45007H4F PH9H4F PH1500-25007HF PH1000-28007H3SF PH7 HOF PHMedium (2% concentration)1500-31007M31F PH9M31F PH12M31P200-8007M8SF PH12M8P400-6007MF PHLow (2% concentration)50-1007M1F PH25-507LF PHTo request literature or samples, please contact Aqualon Customer Service at1-877-5GO AQUA (1-877-546-2782) or e-mail us at ExcipientsAqualon ethylcelluloseAqualon ethylcellulose (EC) issoluble in a wide range of organicsolvents. Typically, EC is used as anon-swellable, insoluble componentin matrix or Coating Systems . EC canbe used to coat one or more activeingredients of a tablet to prevent themfrom reacting with other materials orwith one another. It can preventdiscoloration of easily oxidizablesubstances such as ascorbic acid,allowing granulations for easilycompressed tablets and other dosageforms.

6 EC can be used on its own orin combination with water-solublecomponents to prepare sustainedrelease film coatings that arefrequently used for the Coating ofmicro-particles, pellets and improved compressible grade,Aqualon ECTypical 5% BrookfieldEthoxylGradeViscosity ( )SubstitutionT10 Pharm8 - %N7 Pharm6 - %N10 Pharm 8 - %N14 Pharm12 - %N22 Pharm18 - %N50 Pharm40 - %N100 Pharm80 - %5% solution of 80/20 mixture of toluene/ethanolNatrosol HECT ypical 5% BrookfieldAt SolutionGrade (X = Fine)Viscosity ( )ConcentrationHHX Pharm3,500 5,5001 %HX Pharm, H Pharm1,500 2,5001 %M Pharm4,500 6,5002 % G Pharm250 4002 %L Pharm 75 1505 % Pharmaceutical ExcipientsAqualon T10 EC, was developedwith optimized compactibility (highethoxyl content and low viscosity) andgood powder flow (eliminating fineparticle size via micronization).

7 ThePHARM grades of Aqualon EC arecompliant with the monographrequirements of the United StatesPharmacopoeia/ National Formularyand the European hydroxyethylcelluloseNatrosol hydroxyethylcellulose(HEC) is a non-ionic water-solublecellulose ether. Natrosol HEC iseasily dispersed in cold or hot waterto give solutions of varying viscositiesand desired properties, thoughinsoluble in organic solvents . It isused in (a) solutions and gels, tocontrol rheology, providing thickeningand pseudoplasticity, (b) emulsions,for high salt tolerance and surfactantcompatibility, (c) modified releasematrix tablets where high-viscositygrades provides effective diffusionlimiting release of drugs with lowwater solubility and (d) tablet coatingwhere low viscosity grades impartflexibility to films while providing agood barrier to water and oxygentransmission.

8 The PHARM grades ofNatrosol HEC comply with themonograph requirements of theNational Formulary and the additional information, please refer toAqualon booklet 250-11G on the Aqualon website at request literature or samples, please contact Aqualon Customer Service at1-877-5GO AQUA (1-877-546-2782) or e-mail us at Coating systemsAquarius Coating Systems , afamily of dry, fully formulated filmcoatings Systems are availablefor both Pharmaceutical andnutraceutical solid-dosage formulators have access toan unrivaled range of cellulosicexcipients, enabling Aquarius Coating Systems to be tailored to meetexacting requirements. Immediaterelease coatings provide the optimumbalance of film strength andadhesion-even on challenging coreswithout impacting tablet Aquarius Coating Systems aresprayable at 20% solids, whichmeans faster throughput and reducedlabor and energy costs compared toconventional, lower-solids Coating Systems areavailable in clear, white, or full-colorformulation Systems to deliver asmooth, defect-free appearance withTablet Coatingcrisp logo definition.

9 Color formulationsare produced with the highest qualitycertified lakes, iron oxides, and naturalcolors. Aqualon can develop newcolors or expertly provide a customermatch using state-of-the-art colormatching software. We use theappropriate compendial grades of rawmaterials that are suitable for theintended application ( NF, USP, EPetc for Excipients and FCC, JECFA,etc. for nutra).Aquarius Coating Systems Product Line SummaryTypeClearWhiteColorAquarius CoatingSystemsNameIceCool VanillaArctic WhiteVariousTypical IngredientsPolymerHPMC1 HPC2 CMC3MC4 HPMC1 HPC2 HPMC1 HPC2 ColorantNoneTitanium OxideCalcium CarbonateTitanium OxideCalcium CarbonateFD&C LakesD&C LakesIron OxidesNatural Colors5 PlasticizerTriacetinPolyethylene GlycolGlycerinNone6 TriacetinPolyethylene GlycolGlycerinNone6 TriacetinPolyethylene 1%1 3%3 5%Advantages Excellent adhesion Superior durability Exceptional moisture resistancewith HPC Outstanding gloss especiallywith CMC Sprayable at 20% solids Brlilliant white High hiding Crisp logo definition Superior durability Calcium carbonate can be usedif titanium

10 Dioxide-free coatingsare preferred Sprayable at 20% solids Excellent adhesion Crisp logo definition Superior durability Custom matching available Formulated to meet marketregulatory requirements Ask to see Aquarius color kit1 Hydroxypropylmethylcellulose (hypromellose). from certification (CFR 21 Part 73).6 Using low glass transition temperature HPC can reduce or eliminate the need for request literature or samples, please contact Aqualon Customer Service at1-877-5GO AQUA (1-877-546-2782) or e-mail us at Coating systemsSustained-release Aquarius coatings are based on ethylcellulose(EC). These solvent-soluble Systems ,when coated onto drug-layeredpellets, provide precise drug-releaseprofiles. In addition, these coatingsare more stable than products madewith aqueous EC SRX Coating Systems areavailable in three different porositygrades, with the option of further finetuning the desired properties based onthe formulation additional information on Aquarius coatingsystems, please refer to booklet 250-57 on theAqualon web site at CoatingApplicationTypeGrade RecommendationsNo PorosityEX19093 Highly soluble drug,16 hrs + dissolution timesLow PorosityEKX19102 High to medium soluble drug,80% released in 10-16 hrsHigh PorosityEKX19103 Medium and low soluble drug,80% released in 3-12 hrsElimination of burst effectsin tabletsTo request literature or samples.