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1GENERAL TIPS Types of Tablet:-IPBPUSPUncoatedUncoatedCompressed/moldedFilm CoatedCoatedPlain CoatedEnteric CoatedGastro Resistent (Enteric Coated)Delayed ReleaseDispersible TabletDispersible TabletDispersible TabletModified Release TabletModified Release TabletExteded Release TabletSoluble TabletSoluble TabletSoluble TabletEffervescent TabletEffervescent TabletEffervescent TabletFor use in mouth (Chewable, Lozenges, Sublingual)For use in mouth (Chewable, Lozenges, Sublingual)Chewable/Buccal, SublingualOrodispersibleOrodispersibleOrodispersibleStandards for Tablets:-IPBPUSPContent of Active IngredientContent of Active IngredientContent of Active IngredientUniformity of weightUniformity of weightWeight VariationUniformity of ContentUniformity of ContentUniformity of ContentDTDTDTDissolutionDissolutionDissolution1) Content of Active Ingredient: -1) Assay of Active2) 20 tabs: -Limits 90% to 110%2) Uniformity ofWeight/Wt Variation:-20 tabs, calculate avg. wt NMT 2 deviate, nonetwice the limits.Weight Variation Limits:-1) For Tablets2) For Capsule:-IP/BPLimitUSP80 mg or less10%130mg or lessMore than 80mg or Less than 250mg7.5%130mg to 324mg250mg ormore5%More than 324mgFriability Test:-This test is additional to check crushing strength of tablet by this test one can check Capping &/or Lamination. USP limit is 0.5 to 1%. Rotation: -25 rpm or 100 rotations in 4 min.IPLimitLess than 300mg10%300mg or More7.5%
2USP 29-now<905>Uniformity of  Dosage Units≥25 mg & 25% of active ingredientUniformity of Content or Content Uniformity:-IP: -Active less than 10mg or 10%,BP:-Active less than 2mg or 2%,USP:-Active less than 25mg or 25%.-10 tabs limit NMT 1 tab deviate 85 –115% & none outside 75 –125% of the Avg value/IP/BP/USP (Relative Standard Deviation less than or equal to 6%),-If 2 or 3 individual values are outside the limits 85 –115% of the Avg value, & none outside 75–125% repeat for 20 tabs.-Complies when 30 tabs NMT 3 of the individual values are outside the limit 85 –115% of the Avg value, and none outside 75 –125%.Disintegration Time:-Uncoated TabletNMT 15 min, in water with Disc 370C ± 20CCoated TabletNMT 30 min, In water with Disc for Film Coated Tab, and NMT 60 min Other than Film coated tabletEnteric Coated TabIntact for 1 hr in 0.1 N HCl & disintegrate within 2 hr in Mixed 6.8 Phosphate buffer. According to USP 1 hr in Simulated gastric fluid, then in Simulated Intestinal Fluid.Dispersible/SolubleWithin 3 min in waterat 250C ± 10C (IP) & 15 –250C (BP)Orodispersible Within 1 minEffervescent Tab5minin 250 ml water at 20 –300C (IP) & 5  min in 200 ml water at 15-250C (BP)Buccal & SublingualNot Applicable but dissolve within 15 –30 min.DT Apparatus:-Mesh Apperture:-2mm (#10), Cycles:-28 –32 cycles/min, 50 –60 mm distance from bottom & top, Temp of water 370C ± 20C. If 1 or 2 tabs fail, repeat for 12 tabs.
3Solubility:-BP SOLUBILITIESCompressibility Index (Carr’s Index):-Angle of Repose:-Tapped Density –Bulk Densityx100θ = tan-1(h/r)Tapped DensityVery solubleless than 1 partFreely solublefrom 1 to 10 partsSolublefrom 10 to 30 partsSparingly solublefrom 30 to 100 partsSlightly solublefrom 100 to 1000 partsVery slightly solublefrom 1000 to 10,000 partsPractically insolublemore than 10,000 partsApproximate quantity of solvent by volume for one part of soluble by weight.For example, 1g of a very soluble substance dissolves in less than 1ml of solvent (1gm/ml).Flow propertyC.I(%)Hausner ratioExcellent ≤101.00 –1.11Good 11–151.12 –1.18Fair 16–201.19 –1.25Passable21 –251.26 –1.34Poor26 –311.35 –1.45Very  poor32 –371.46 –1.59Very, verypoor>38>1.60Flow propertyAngle of repose (degrees)Excellent25 –30Good31 –35Fair-aid not needed36 –40Passable –may hang up41 –45Poor –must agitate, vibrate46 –55Very poor56 –65Very, very poor>66
4Bioavailability:-The rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. For drug products that are not intended to be absorbed into the bloodstream, bioavailability may be assessed by measurements intended to reflect the rate and extent to which the active ingredient or active moiety becomes available at the site of action.ANDA -Abbreviated New Drug Application.IND –Investigational New Drug Application.NDA –New Drug Application.According to the BCS, drug substances are classified as follows:Class I -High Solubility, HighPermeabilityClass II -High Permeability, Low SolubilityClass III -High Solubility, LowPermeabilityClass IV -, Low Solubility Low PermeabilityA drug substance is considered HIGHLY SOLUBLE when the highest dose strength is soluble in <250 ml water over a pH range of 1 to 7.5. A drug substance is considered HIGHLY PERMEABLE when the extent of absorption in humans is determined to be >90% of an administered dose, based on mass-balance or in comparison to an intravenous reference dose. A drug product is considered to be RAPIDLY DISSOLVING when >85% of the labeled amount of drug substance dissolves within 30 minutes using USP apparatus Ior II in a volume of <900 ml buffer solutions. DISSOLUTION DETERMINATION USP apparatus I (basket) at 100 rpm or USP apparatus II (paddle) at 50 rpm. Dissolution media (900 ml): 0.1 N HCl or simulated gastric fluid, pH 4.5 buffer, and pH 6.8 buffer or simulated intestinal fluid. Compare dissolution profiles of test and reference products using a similarity factor (f2). AN ARRAY OF TABLET TYPESImmediate Release Uncoated Tablets: Usually no taste/stability issues.Coated Tablets: For taste/stability/identification (coated withwater-soluble/dispersible polymer–mixture of hydroxypropyl cellulose/hydroxypropylmethyl cellulose); coating readily ruptures in GI tract.Enteric-Coated Tablets: For drugs inactivated or destroyed in the stomach or for those causing irritation to the gastric mucosa; tablet passes through the stomach but disintegrates in the intestines where absorption takes place. Excipients used for enteric coating include cellulose acetate phthalate, mixtures of fats and fatty acids, etc.Multiple Compressed Tablets: Multiple-layered tablets manufactured by using more
5than one compression cycle. Each layer contains a different drug and each may be colored differently.Controlled Release Tablets: Improved therapy, less toxicity, improved patient compliance—using polymers such as methacrylates.Sublingual Tablets: Small, flat ovals such as nitroglycerin. They are ideal tablets for absorption of drugs which are destroyed by gastric juice or undergo first pass metabolism.Chewable Tablets: Disintegrate rapidly when chewed for patients with swallowing difficulty (children, elderly) and when there is no access to water. Most commonly used for multiple vitamins and antacids.Effervescent Tablets: In addition to the active, this product form contains sodium bicarbonate and citric acid. When water is added the ensuing chemical reaction forms carbon dioxide, which acts as a disintegrant and produces effervescence that hastens dissolution (antacids).Official Standards as per I.P. / B.P. / U.S.P.COMPARISON OF DIFFERENT PHARMACOPOEIAL QUALITY CONTROL TESTSPHARMACOPOEIASTYPE OF TABLETTESTS TO BE PERFORMEDBRITISH PHARMACOPOEIAFor all tabletsContent of active ingredientsDisintegrationUniformity of contentLabelingUncoated tabletDisintegration testUniformity of weightEffervescent tabletDisintegration testUniformity of weightCoated tabletDisintegration testUniformity of weightGastro resistant tabletDisintegration testModified release tabletUniformity of weightTablet for use in mouthUniformity of weight
6Soluble tabletDisintegration testUniformity of weightDispersible tabletDisintegration testUniformity of dispersionUniformity of weightINDIAN PHARMACOPOEIAUncoated tabletUniformity of container contentContentof active ingredientUniformity of weightUniformity of contentDisintegration testEnteric coated tabletDisintegration testDispersible tabletUniformity of dispersionDisintegrationSoluble tabletDisintegration testEffervescent tabletDisintegration/ Dissolution / DispersiontestUNITED STATES PHARMACOPOEIAPhysical tests applicable to tablet formulationBulk density /Tapped density of powderPowder finenessLoss on dryingDisintegration testTablet friabilityDissolution testDrug release testingUniformity of dosage formContainer permeation testLabeling of inactive ingredientsTablet Problems:-Capping:-‘Capping’ is the term used, when the upper or lower segment of the tablet separates horizontally, either partially or completely from the main body of a tablet and comes off as a cap, during ejection from the tablet press, or during subsequent handling.Lamination / Laminating:-Definition:‘Lamination’ is the separation of a tablet into two or more distinct horizontal layers.
7Chipping:-‘Chipping’ is defined as the breaking of tablet edges, while the tablet leaves the press or during subsequent handling and coating operations.Cracking:-Small, fine cracks observed on the upper and lower central surface of tablets, or very rarely on the sidewall are referred to as ‘Cracks’.Sticking / Filming:-‘Sticking’ refers to the tablet material adhering to the die wall.Filming is a slow form of sticking and is largely due to excess moisture in the granulation.Picking:-‘Picking’ is the term used when a small amount of material from a tablet is sticking to and being removed off from the tablet-surface by a punch face.The problem is more prevalent on the upper punch faces than on the lower ones. The problem worsens, if tablets are repeatedly manufactured in this station of tooling because of the more and more material getting added to the already stuck material on the punch face.Mottling:-‘Mottling’ is the term used to describe an unequal distribution of colour on a tablet, with light or dark spotsstanding out in an otherwise uniform surface.Double impression:-‘Double Impression’ involves only those punches, which have a monogram or other engraving on them.Problems for tablet coating:-Blistering:-It is local detachment of film from the substrate forming blister.Chipping:It is defect where the film becomes chipped and dented, usually at the edges of the tablet.Cratering:It is defect of film coating whereby volcanic-like craters appears exposing the tablet surface.Picking:It is defect whereisolated areas of film are pulled away from the surface when the tablet sticks together and then part.Pitting:It is defect whereby pits occur in the surface of a tablet core without any visible disruption of the film coating.Blooming:It is defect where coating becomes dull immediately or after prolonged storage at high temperatures.Blushing:It is defect best described as whitish specks or haziness in the film.Colour variation:A defect which involves variation in colour of the film.
8Infilling:It is defect that renders the intagliations indistinctness.Orange peel/Roughness:It is surface defect resulting in the film being rough and nonglossy. Appearance is similar to that of an orange.Cracking/Splitting:It is defect in which the film either cracks across the crown of the tablet (cracking) or splits around the edges of the tablet (Splitting).