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Definition of Tablets
Solid Dosage forms prepared by compression or molding of powdered/granulatied drugs and with the aid of suitable pharmaceutical excipients
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Charactistics of Tablets
- Most Frequently prescribed commerical dosage form
- Stable, elegant, and effective
- Convenient for handling, indentification and administration
- Commercially available only in fixed dosage strengths
- Many formats, sizes, colors, shapes, scoring, engraving
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How is format and size determined?
By the die and punch used, by the amount of fill and mount of pressure applied to the fill
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What are the types of tablets?
- Compressed
- Multiple Compressed
- Sugar-coated tablets
- Film-coated tablets
- Gelatin-coated (caplets)
- Enteric Coated
- Buccal
- Sublingual
- Chewable
- Lozenges, Troches, Drops or Pastilles
- Lollipops
- Effervescent
- Molded
- Triturates
- Rapid Dissolving
- Extended Release
- Vaginal
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Compressed Tablets
- Single compression of all ingedients
- Simple tablets
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Multiple Compressed Tablets
- For separation of incompatible drugs or for modified release
- Multiple-layered tablets: multiple feed and multiple compression of fill within a single die
- Tablet-within-a-tablet: core tablet is placed precisely within the die for compression with surrounding fill
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Sugar Coated Tablets
- Several Layers of colored or uncolored sugar solutions (sucrose, gelatin, acacia or PVP)
- Time and expertise
- Final table: increase up to 50% of size and weight of uncoated tablet
- Imprinting (FDA 1995) product specific identification codes and distinctive symbols
- Polishing: cloth of canvas impregnated with carnauba wax/beeswax or spraying with wax dissolved in acetone
- Final tumbling with talc for high luster
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Film-Coated tablets
- Thin layer of aqueous or non-aqueous polymer solution (plastic-like material): cellulose acetate phthalate; cellulose ether polymers
- Protection, Color, Durability, less bulkiness, less time consuming
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Gelatin-Coated (Caplet)
Capsule-shaped compressed tablet coated with gelatin
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Enteric coated tablets
- Protection of drug, patient gastric mucosa, or enhance absorption
- Based on transit time required for the passage of the dosage form from the stomach into the intestines or based upon the pH of environment
- Delayed-release features
- Whole tablet or drug particles or granules: single or multiple layers
- Materials: shellac, phthalate derivatives
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Buccal Tablets
Placed in the cheek pouch, dissolved slowly, absorption through the oral mucosa
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Sublingual Tablets
Placed under the tongue, prompt dissolution, absorption throughout the oral mucosa
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Chewable tablets
Chewed/dissolved in the mouth; made with creamy base, negative heat of solution leaves cool mouth feeling upon dissolution; flavored and colored; children and adults who have difficulty swallowing
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What are the creamy bases used in chewable tablets?
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Lozenges, Troches, Drops or Pastilles
- Hard candy-like (sugar or sugar-free) or gummy-like (gelatin-based)
- Dissolved or disintegrate slowly in the oral cavity
- High degree of compression
- Heat stable active ingredients
- Local effects
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Lollipops
Sugar-based lozenge on a stick (or sugarfree!)
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Fentanyl Actiq
- Used to relieve breakthrough chronic cancer pain
- Lollipops
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Effervescent Tablets
Cpmpression of effervescent salts that liberate carbon dioxide when dissolved in water, should NOT be swallowed whole
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Molded tablets
Molding and soft compaction: hand operated tablet press
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Tablet triturates
"Old Fashion" tablets containing small amounts of potent drugs and prepared with minimal compression to allow ease of crushing for compounding or rapid dissolution
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Rapid Dissolving Tablets
- Superdisintegrants
- Dissolution within 15-30 seconds and swallowing of the liquid
- Very water soluble excipients that attract water into the tablet
- children and elderly
- inherent problems, drug loading, taste masking, firability
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Zydis technology
lyophilization (foaming of a mixture of gelatin, sugars, drugs, etc and pouring into a mold)
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DuraSolv, OraSolv, Flashtab, Wowtab technologies
Compression (super-disintegrants + small quantity of effervescent material)
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Extended release Tablets
release of medication in a predetermined manner over an extended period
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Vaginal Tablets (inserts)
- Uncoated
- Vullet-shaped or ovoid
- Plastic/carboard inserter devices for admin.
- Local effects
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Types of Preparation of Compressed Tablets
- Wet Granulation
- All-in-One Granulation
- Dry Granulation
- Direct Compression
- Molding
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Tablets dedusting is done to
- remove loose powders
- elegance
- prior to coating
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What is Wet Granulation?
- Weighing and blending of powdered ingredients (drugs + fillers + disintegrating agents + others)
- Sifting of powders to eliminate clumps
- Mixing with liquid binders or adhesive mixture
- Damp mass
- pass through screen (6-8 mesh size)
- Dry themostatically controlled oven
- Sizing (12-20 mesh)
- Blending (granules + dry lubricants)
- Compression (tablet machine)
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Types of tablet machines?
- Single punch tablet press
- rotary tablet machine with multiple punches
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All-in-one-Granulation Method
- Sophisticated Machinery
- Granulation prepared by Fluid=bed process or Microwave vacumm process
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Dry granulation
- For materials that are degraded in presence of moisture or high heat
- Weighting and blending of powdered incredients: cohesive properties
- Binding agents
- powders compressed in slugging maching or roller compactor
- flat slugs or pellets
- slgs crushed and sized
- granuels and dry lubricant
- compression in tableting machine
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What are dry libricants
Mg/Ca/Zn Stearate/talc
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Direct compression
- Excipients have free-flowing and cohesive properties
- Potasium chloride, Methenamine, Dibasic calcium phosphate
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Molding
- Focing of a dampened mass into the cavities of a tablet mold (plastic or metal)
- Mold consists of two plates, one with a hole and the other with a peg
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Why are tablets coated?
- For protection of drug from air and humidity
- To protect gastruc mucosa of irritating drugs
- to mask taste
- For special release of drug (enteric coated)
- To provide aesthetics and distinction to a product (color, imprinting of manufacturer's symbol or information
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What does the USP need for quality control of tablets?
- Weight
- Content Uniformity
- Hardness, Breaking Strengh, Friabilty
- Thickness
- Disintegration
- Dissolution
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Weight
- Determined by the quantity of fill in the die of press
- Weight Variation for dosage form uniformity
- Assay for homogeneous drug distribution
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Content uniformity
active ingredient +/- 10%
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Hardness, Breaking Stregth, Friabilty
- Measurement of pressure/force to break each tablet
- Dpendons on type of tablet and degree of compression used during manufacture
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Friabilator does what?
- Measures the tendency of a tablet to crumle (rotaing tumbling conbtainer)
- Teablets are weighed before and after rotations and weight loss is determined (maximum loss allowed is 1%)
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Thickness
- Caliper, hang gauge or automated equipment
- Depends on:
- Diameter of the die
- Amount of fill
- Compaction characterists of fill
- Pressure applied
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Disintegration
Time required for a tablet to disintegrate
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Disintegration testing for compressed tab
appartus contiang water (30 min 37 C) or simulated gastric fluid 1 hr
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Disintegration testing for enteric coated tablets
simulated gastric fluid (1 hr) and intestingal fluid at 37 C
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Dissolution
- In vitro testing
- Product development
- quality assurance during manufacturing
- Bioequivalence from batch to batch: scale-up batches
- Mandatory for approval of marketing: FDA and regulatory agencies of other countires
- Influences the absorption and bioavailabilty
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Tablets packaged and stored?
- Contianers: Bottles, blister
- Light-resistant
- Desicant packet and cotton ball
- Types of container, reduced potency of volatile drugs
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How should nitroglycerin be packaged?
Glass container and no packing materials in contact with tabs
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