Tablets

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Tablets

  1. 1. 11Tablets - lTablets - lBy fagosonBy fagosonDepartment of PharmacyDepartment of PharmacyNUBNUBPharmaceutical Technology
  2. 2. 22““A tablet is a solid single unit dosage formA tablet is a solid single unit dosage formcontaining one or more active ingredients withcontaining one or more active ingredients withor without auxillary substances, prepared byor without auxillary substances, prepared bycompression and molding.”compression and molding.”IntendedIntended mainlymainly for oral administrationfor oral administrationMost commonly are disk shaped with convex surfacesMost commonly are disk shaped with convex surfacesAvailable in special shape like round, oval, oblong,Available in special shape like round, oval, oblong,cylindrical, square, triangularcylindrical, square, triangularWidely used solid dosage form because they offer aWidely used solid dosage form because they offer anumber of advantages to the patient, prescriber,number of advantages to the patient, prescriber,manufacturer and manufacturing pharmacistmanufacturer and manufacturing pharmacist
  3. 3. 33Essential qualities of a good TabletsEssential qualities of a good Tablets--They should be accurate and uniform inThey should be accurate and uniform inweightweight--The drugs should be uniformly distributedThe drugs should be uniformly distributedthroughout the tabletsthroughout the tablets-The size and shape should be reasonable for-The size and shape should be reasonable foreasy administrationeasy administration--The tablets should not be too hard that it mayThe tablets should not be too hard that it maynot disintegrate in the Stomachnot disintegrate in the Stomach-There should not be any incompatibilities-There should not be any incompatibilities--They should be chemically and physicallyThey should be chemically and physicallystable during storage . Cont.stable during storage . Cont.
  4. 4. 44Essential qualities of a good TabletsEssential qualities of a good Tablets- They should not break during transportation- They should not break during transportationor crumble in the hands of the patientor crumble in the hands of the patient- They should be attractive in appearances- They should be attractive in appearances- There should not be any manufacturing- There should not be any manufacturingdefects like cracking, chipping discolourationdefects like cracking, chipping discolouration-- After disintegration it should release theAfter disintegration it should release thedrug readilydrug readily- They should be easy and economical in- They should be easy and economical inproductionproduction..
  5. 5. 55AdvantagesAdvantages- Offer greatest dose precision and the least- Offer greatest dose precision and the leastcontent variabilitycontent variability-- easy to be swallowed or administeredeasy to be swallowed or administered- easy to handle and carry by the patient- easy to handle and carry by the patient- economical, manufacturing cost are low,- economical, manufacturing cost are low,manufacturing speed is quite highmanufacturing speed is quite high- most stable with respect to physical, chemical- most stable with respect to physical, chemicaland microbiological attributesand microbiological attributes-- Bitter, unpleasant taste and nauseous odour ofBitter, unpleasant taste and nauseous odour ofmedicaments can be easily masked bymedicaments can be easily masked byadministering in the form of coated tabletadministering in the form of coated tablet
  6. 6. 66Advantage (Continued)Advantage (Continued)- product identification is probably the easiest- product identification is probably the easiestbecause of the variety of shapes and colours ofbecause of the variety of shapes and colours oftablets that are possibletablets that are possible- the lightest and the more compact of all dosage- the lightest and the more compact of all dosageformsforms- the easiest and the cheapest to pack and transport- the easiest and the cheapest to pack and transport- don’t require any measurement of dose- don’t require any measurement of dose
  7. 7. 77Advantage (continued)Advantage (continued)Can be divided into halves, quarters by drawingCan be divided into halves, quarters by drawinglines during manufacture to facilitate breakagelines during manufacture to facilitate breakagewhenever a fractional dose is requiredwhenever a fractional dose is requiredLend themselves to certain special release profileLend themselves to certain special release profilesuch as enteric or delayed release productssuch as enteric or delayed release productsAttractive and elegant in appearanceAttractive and elegant in appearance
  8. 8. 88In Summary Solid Dosage Forms, MostNotably Tablets Provide AdvantagesTo the pharmacistin storage, dispensing, and controlconvenience of useTo the patientTo the physiciancheaper due to mass productionand easier to manufacture,simplicity, economy, stability,and convenienceTo themanufacturerof product identification, dosageaccuracy and precision, improvedcontrol and more reliable therapy
  9. 9. 99DisadvantagesDisadvantagesAmorphousAmorphous and Low density drugs are difficult toand Low density drugs are difficult tocompress.compress.High dosesHigh doses are difficult to formulate as tablet dosageare difficult to formulate as tablet dosageform.form.BitterBitter tastingtasting and objectionableand objectionable odouodour drugs requirer drugs requirespecial treatment like coating or encapsulation andspecial treatment like coating or encapsulation andincrease the cost.increase the cost.Drugs that are sensitive toDrugs that are sensitive to oxygenoxygen or atmosphericor atmosphericmoisture may also require special coating as well as costlymoisture may also require special coating as well as costlypackaging which may increase the overall cost of finishedpackaging which may increase the overall cost of finishedproductproduct
  10. 10. 1010Disadvantage (Continued)Disadvantage (Continued)Drugs with poorDrugs with poor wettingwetting and slow dissolution propertiesand slow dissolution propertiesare difficult to convert into tablets which will provide fullare difficult to convert into tablets which will provide fulldrug bioavailability.drug bioavailability.Drugs that areDrugs that are liquidliquid at room temperature can not beat room temperature can not beformulated in tablet dosage formformulated in tablet dosage formA major disadvantage with respect to convenience ofA major disadvantage with respect to convenience ofpatients is the difficulty ofpatients is the difficulty of swallowingswallowing specially byspecially by childrenchildrenand ill patientsand ill patients
  11. 11. 1111DifferentDifferent TypesTypes of Tabletsof TabletsClassified into a number of categories, based onClassified into a number of categories, based ontheirtheir-Their methods of manufacture-Their methods of manufacture-Type of drug delivery system-Type of drug delivery system- Formulation and Functions- Formulation and Functions**Not all classes are entirely different but mostly**Not all classes are entirely different but mostlyoverlap each other, such as,overlap each other, such as,- Chewable and Effervescent tablets are single- Chewable and Effervescent tablets are singlelayered uncoated tabletslayered uncoated tablets
  12. 12. 1212Classification (continued)Classification (continued)Table1. Classified based on the method of manufacture andTable1. Classified based on the method of manufacture andtype of drug deliver systemtype of drug deliver system(A) Tablets ingested orally:(A) Tablets ingested orally:-- Compressed tablet, e.g. Paracetamol tablet– Multiple compressed tablet– Delayed release tablet, e.g. Enteric coated Bisacodyl tablet– Sugar coated tablet, e.g. Multivitamin tablet– Film coated tablet, e.g. Metronidazole tablet– Chewable tablet, e.g. Antacid
  13. 13. 1313Classification (continued)Classification (continued)(B) Tablets used in oral cavity :(B) Tablets used in oral cavity :– Buccal tablet, e.g. Vitamin-c tablet– Sublingual tablet, e.g. Vicks Menthol tablet– Troches or lozenges– Dental cone(C) Tablets administered by other routes:(C) Tablets administered by other routes:- Implantation tablet- Suppositories or Inserts, e.g. Clotrimazole tablet
  14. 14. 1414
  15. 15. 1515(D) Tablets used to prepare solution:(D) Tablets used to prepare solution:– Effervescent tablet, e.g. Dispirin tablet (Aspirin)– Dispensing tablet, e.g. Enzyme tablet (Digiplex)– Hypodermic tablet– Tablet triturates e.g. Enzyme tablet (Digiplex)
  16. 16. 1616Standard compressed tabletStandard compressed tablet-- Prepared by single compressionPrepared by single compression- employ any of the three basic methods of manufactures:- employ any of the three basic methods of manufactures: wetwetgranulation, dry granulation and direct compression.granulation, dry granulation and direct compression.- most of the tablets containing drugs intended to exert a local- most of the tablets containing drugs intended to exert a localeffect in the GIT are of this type (antacids and adsorbents)effect in the GIT are of this type (antacids and adsorbents)-- Other drugs in this group are intended to produce systemicOther drugs in this group are intended to produce systemiceffect.effect.-- Tablets break up and particle deaggregation are importantTablets break up and particle deaggregation are important
  17. 17. 1717Multiple compressed TabletMultiple compressed TabletTablets of this category are usually prepared for one ofTablets of this category are usually prepared for one ofthe two reasons:-the two reasons:-a. to separate physically or chemically incompatiblea. to separate physically or chemically incompatibleingredientsingredientsb. to produce repeat action or prolonged action productsb. to produce repeat action or prolonged action products-- layered tablets consist of parallel layers obtained bylayered tablets consist of parallel layers obtained bysuccessive compression of particles of different comp.successive compression of particles of different comp.- press coated or dry coated tablets are prepared- press coated or dry coated tablets are preparedby compressing a layer of granules over a previouslyby compressing a layer of granules over a previouslycompressed tablets. (manesty drycota).compressed tablets. (manesty drycota).
  18. 18. 1818The layered tablets are rapid, surface contact betweenThe layered tablets are rapid, surface contact betweenlayers is lessened, production is simpler so preferred.layers is lessened, production is simpler so preferred.The shortcomings of this category of dosage form forThe shortcomings of this category of dosage form forrepeat – action products is that its performance isrepeat – action products is that its performance ishighly dependant on gastric empting.highly dependant on gastric empting.XX,XX, If the second layer or core tablet quickly leaves theIf the second layer or core tablet quickly leaves thestomach following release of the initial fast releasestomach following release of the initial fast releasedose, an entirely different blood level profile resultsdose, an entirely different blood level profile resultsthan if there is a several hour or longer delay beforethan if there is a several hour or longer delay beforethe second fraction is emptied.the second fraction is emptied.- this is the reason that relatively few repeat –action or- this is the reason that relatively few repeat –action orcontrolled release products using this approach arecontrolled release products using this approach aremarketed.marketed.
  19. 19. 1919Repeat action tabletsRepeat action tabletsIn addition to compressed tablets, sugar coated tabletIn addition to compressed tablets, sugar coated tabletmay also employed.may also employed.The core tablet is usually coated with shellac or anThe core tablet is usually coated with shellac or anenteric polymer so that it will not release the loadingenteric polymer so that it will not release the loadingdrug in the stomach.drug in the stomach.The second dose of drug is then added in the sugarThe second dose of drug is then added in the sugarcoating.coating.
  20. 20. 2020Delayed action and enteric coated tabletDelayed action and enteric coated tabletThe delay action tablet dosage form is intended toThe delay action tablet dosage form is intended torelease a drug after some time delay or after therelease a drug after some time delay or after thetablet has passed through the part of GI tract intotablet has passed through the part of GI tract intoanother.another.The enteric coated tablet is the most commonThe enteric coated tablet is the most commonexampleexampleAll enteric coated tablets are a type of delayedAll enteric coated tablets are a type of delayedaction tablet but not all delayed action tablet areaction tablet but not all delayed action tablet areentericentericCellulose acetate phthalate, Polyvinyl acetateCellulose acetate phthalate, Polyvinyl acetatephthalate, Hydroxypropyl methyl cellulose phthatephthalate, Hydroxypropyl methyl cellulose phthatehave come into use for thishave come into use for this ..These polymers being acid esters, are insoluble inThese polymers being acid esters, are insoluble ingastric media that have a pH up to about 4.gastric media that have a pH up to about 4.
  21. 21. 2121Chewable tabletsChewable tabletsAre compressed tablets which have a smooth, rapiddisintegration when chewed or allowed to dissolve inthe mouth and contains a creamy base of a speciallyflavored and colored mannitol.Two major advantages are,Two major advantages are,a.The dose of most antacid is large so that the typicala.The dose of most antacid is large so that the typicalantacid tablet would be too large to swallowantacid tablet would be too large to swallowb.The activity of antacid is related to its particle size. Ifb.The activity of antacid is related to its particle size. Ifthe tablet is chewed prior to swallowing better acidthe tablet is chewed prior to swallowing better acidneutralizing may be possible from a given antacidneutralizing may be possible from a given antaciddosedose
  22. 22. 2222Xylitol may be used in the preparation of sugar-free chewable tablets. Xylitol is sweeter thanmannitol.lubricant and binders must not affect the textureor desired hardness of the tabletcolorant and tart or fruity flavorants arecommonly employed to enhance the appeal ofthe tabletsExamples of chewable tablets: Calciumcarbonate - antacids; Erythromycin - antibiotics;Didanosine - anti-infectives; Carbamazepine -anticonvulsants; Isosorbide dinitrate -vasodilator; Acetaminophen - analgesics;various vitamins and cold-allergy combinationtablet
  23. 23. 2323Tablets used in the oral cavityTablets used in the oral cavityThis type of tablet are placed in the mouth but notThis type of tablet are placed in the mouth but notswallowed.swallowed.*Buccal and sublingual tablets*Buccal and sublingual tabletsThese tablets , though not swallowed, are intended toThese tablets , though not swallowed, are intended toprovide systemic drug action.provide systemic drug action.These are small, flat, usually oval dosage forms to beThese are small, flat, usually oval dosage forms to beinserted in the buccal , or cheek, pouch (buccal tablet) orinserted in the buccal , or cheek, pouch (buccal tablet) orbeneath the tongue (sublingual tablets).beneath the tongue (sublingual tablets).The drug is absorbed directly through the oral mucosa,The drug is absorbed directly through the oral mucosa,thereby avoiding the acid and enzymatic environment ofthereby avoiding the acid and enzymatic environment ofthe stomach and the drug metabolizing enzymes of thethe stomach and the drug metabolizing enzymes of theliver.liver.
  24. 24. 2424Drugs are commonly administered by the oralDrugs are commonly administered by the oralmucosal routemucosal route::the vasodilator glyceryl trinitratethe vasodilator glyceryl trinitrate:: Steroids, such asSteroids, such asmethyl testosteronemethyl testosterone,, testosterone propionatetestosterone propionate,,estradioestradiol: and, possibly, some miscellaneousl: and, possibly, some miscellaneoushormones and drugshormones and drugs, such as, such as pancreaticpancreaticlipotropic hormone factors,lipotropic hormone factors, hesperidinhesperidin, and, andnicotinic acid.nicotinic acid.Drugs that may be absorbed via the oralDrugs that may be absorbed via the oralmucosa have several possible advantagesmucosa have several possible advantages::(1) Avoidance of the gastric environment and the(1) Avoidance of the gastric environment and thedecomposition it may produce with some steroids anddecomposition it may produce with some steroids andhormone (2) a more rapid onset of drug action thanhormone (2) a more rapid onset of drug action thanoccurs with tablets which are swallowed (3) Reduction ofoccurs with tablets which are swallowed (3) Reduction ofnausea, with drugs that produce this effect whennausea, with drugs that produce this effect whenswallowed (4) More efficient drug utilization (lower dose),swallowed (4) More efficient drug utilization (lower dose),owing to avoidance of inactivation by liver drugowing to avoidance of inactivation by liver drugmetabolising enzymes.metabolising enzymes.
  25. 25. 2525. Drugs absorbed from the gastrointestinal tract enter the mesenteric. Drugs absorbed from the gastrointestinal tract enter the mesentericcirculation which feeds directly into the liver via the portal vein. Drugcirculation which feeds directly into the liver via the portal vein. Drugabsorption from the oral cavity involves drug diffusion into the blood and lymphabsorption from the oral cavity involves drug diffusion into the blood and lymphcanals through the sublingual or oral mucosa. Blood is supplied to this regioncanals through the sublingual or oral mucosa. Blood is supplied to this regionvia the external carotid artery and is returned via the jugular veins into thevia the external carotid artery and is returned via the jugular veins into thegeneral circulation rather than going directly to the portal vein. Many steroidsgeneral circulation rather than going directly to the portal vein. Many steroidsare either relatively or totally inert if ingested owing to inactivation by liverare either relatively or totally inert if ingested owing to inactivation by liverenzymes. This loss of potency can be circumvented by other modes ofenzymes. This loss of potency can be circumvented by other modes ofadministration such as intramuscular injection, implantation of tablets, use ofadministration such as intramuscular injection, implantation of tablets, use ofvaginal suppositories, or absorption through the oral mucosa. The lattervaginal suppositories, or absorption through the oral mucosa. The lattermethod, in many instances, is preferable.method, in many instances, is preferable.Since most drugs, including weakly acidic drug moieties, are probablySince most drugs, including weakly acidic drug moieties, are probablyabsorbed primarily in the upper small intestine. The tablet must disintegrate,absorbed primarily in the upper small intestine. The tablet must disintegrate,the drug dissolve, and the stomach empty at least partially before drugthe drug dissolve, and the stomach empty at least partially before drugabsorption begin. Therefore , a time lag of 30 minutes or more (correspondingabsorption begin. Therefore , a time lag of 30 minutes or more (correspondingto the time required for the drug to be dissolved and leave the stomach) isto the time required for the drug to be dissolved and leave the stomach) istypical before a drug effect is exerted after swallowing a tablet. on the othertypical before a drug effect is exerted after swallowing a tablet. on the otherhand , total drug absorption typically occurs within 30 minutes after buccal orhand , total drug absorption typically occurs within 30 minutes after buccal orsublingual tablets have been administered and onset of action is common withsublingual tablets have been administered and onset of action is common withvasodilator drugs..vasodilator drugs..Buccal and sublingual tablets are designed not to disintegrate but to dissolveBuccal and sublingual tablets are designed not to disintegrate but to dissolveslowly over a 15 to 30 minute period. The tablet composition should notslowly over a 15 to 30 minute period. The tablet composition should notpromote salivation, which would result in swallowing dissolved drug, therebypromote salivation, which would result in swallowing dissolved drug, therebycircumventing the purpose of the buccal or sublingual tablets.circumventing the purpose of the buccal or sublingual tablets.
  26. 26. 2626Dental conesDental conesThe cones may contain an antibiotic orThe cones may contain an antibiotic orantiseptic typically in a filler of Sodiumantiseptic typically in a filler of Sodiumbicarbonate, sodium chloride, amino acid,bicarbonate, sodium chloride, amino acid,or lactose.or lactose.The cones are formulated and compressionThe cones are formulated and compressionso that a small volume of serum or fluid willso that a small volume of serum or fluid willcause disintegration and dissolution in 20 tocause disintegration and dissolution in 20 to30 minutes.30 minutes.
  27. 27. 2727Tablets administered by other routesTablets administered by other routesImplantation tabletsImplantation tabletsThis is also known as pellets, are small sterile tablets,This is also known as pellets, are small sterile tablets,cylindrical shaped and usually not over 8 mm. in length, forcylindrical shaped and usually not over 8 mm. in length, forsubcutaneous implantation in man or animals to providesubcutaneous implantation in man or animals to providevery prolonged drug effects – for 3 to 6 months or longer.very prolonged drug effects – for 3 to 6 months or longer.In man, use of this dosage form is limited to very potentIn man, use of this dosage form is limited to very potentdrugs which are not orally absorbed, notably steroids suchdrugs which are not orally absorbed, notably steroids suchas Desoxycorticosterone, testosterone, or estradiol.as Desoxycorticosterone, testosterone, or estradiol.The major advantage of the dosage form is to provideThe major advantage of the dosage form is to providecontinuous therapy over many months without the needcontinuous therapy over many months without the needfor repeated parenteral dosing. Over a long periods of timefor repeated parenteral dosing. Over a long periods of timethis form of therapy can be most economical. Also, it maythis form of therapy can be most economical. Also, it mayprovide the most even and uniform hormone therapy.provide the most even and uniform hormone therapy.
  28. 28. 2828Implantation tabletsImplantation tabletsThe immediate and potential disadvantage ofThe immediate and potential disadvantage ofimplantation therapy are:implantation therapy are:- the surgical technique which may be required- the surgical technique which may be requiredfor implantationfor implantation- the difficulty of maintaining a constant drug- the difficulty of maintaining a constant drugrelease rate as the pellet changes geometry withrelease rate as the pellet changes geometry withdissolutiondissolution- the possibility of a histopathological (tissue- the possibility of a histopathological (tissuetoxicity) reaction against the implanted ‘foreigntoxicity) reaction against the implanted ‘foreignbody’body’-the need to employ a surgical technique to-the need to employ a surgical technique toterminate the therapy should such terminationterminate the therapy should such terminationbecome necessarybecome necessary
  29. 29. 2929Vaginal tabletsVaginal tabletsAlso called inserts, are generally ovoid orAlso called inserts, are generally ovoid orpear shaped made by compression andpear shaped made by compression andintended to undergo dissolution and drugintended to undergo dissolution and drugrelease in the vaginal cavity.release in the vaginal cavity.The tablets are usually used in the treatmentThe tablets are usually used in the treatmentof trichomonas vaginitis andof trichomonas vaginitis andcontain organic iodine (iodochlor orcontain organic iodine (iodochlor oriodohydroxyquinoline compounds) or otheriodohydroxyquinoline compounds) or otherantiseptics, astringents, or steroids in aantiseptics, astringents, or steroids in asoluble base of lactose or sodiumsoluble base of lactose or sodiumbiocarbonate.biocarbonate.
  30. 30. 3030Effervescent tabletsEffervescent tabletsThese tablet produce effervescence whenThese tablet produce effervescence whenadded to cold water. Effervescence whichadded to cold water. Effervescence whichis usually carbon dioxide is generated dueis usually carbon dioxide is generated dueto chemical reaction which take placeto chemical reaction which take placebetween a Bicarbonate and an acid (citricbetween a Bicarbonate and an acid (citricacid and Tataric acid)acid and Tataric acid)The effervescence causes rapidThe effervescence causes rapiddisintegration of the tablet and alsodisintegration of the tablet and alsoincreases the palatabilityincreases the palatability ।।

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