Dosage Forms Flashcards
composed of a solid or mixture of solids reduced to a FINELY DIVIDED and intended for internal or external use
Powder
composed of DRY AGGREGATES of powder particles that may contain one or more APIs, with or without other ingredients
Granules
solid dosage forms in which medicinal agents and/or inert substances are enclosed in a small SHELL OF GELATIN
Capsules
solid dosage forms usually prepared with the aid of suitable pharmaceutical EXCIPIENTS -> COMPRESSED
Tablet
semisolid preparations intended for external application to the SKIN or MUCOUS membrane
Ointment
are solid dosage forms intended for insertion into body ORIFICES where they melt, soften, or dissolve and exert local or systemic effects
Suppositories
liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of NATURALLY MISCIBLE solvents
Solutions
preparations containing finely divided drug particles (the SUSPENSOIDS) distributed somewhat uniformly throughout a vehicle in which the drug exhibits a MINIMUM degree of solubility
Suspensions
*dispersion in which the dispersed phase is composed of small globules of a LIQUID distributed throughout a VEHICLE in which it is IMMISCIBLE
*Select the oral dosage form, which contains one or more active ingredients that are unstable in the water phase but stabilized in oil-in-water dispersions; either or both phases may contain
Emulsions
PRESSURIZED dosage forms that, upon actuation, emit a fine dispersion of LIQUID and/or SOLID materials containing one or more active ingredients in a GASEOUS medium
Aerosols
- use repetitive, INTERMITTENT dosing of a drug from one or more immediate-release units incorporated into a single dosage form
- Do not produce or maintain uniform drug blood levels within the therapeutic range
- e.g., enteric-coated tablets, repeat-action tablet, prolonged action
Delayed-release systems
*achieves SLOW release of drug over an extended period of time
*non-constant
*First Order Kinetics
Sustained-release systems ***
*maintains therapeutic blood levels of
the drug for a PROLONGED period
Extended-release
*release at nearly CONSTANT RATE
*Zero Order
Controlled Release
delivery of a drug at a PREDETERMINED rate and/or location according to the needs of the body
Controlled Drug Delivery
targeting the diseased organ or tissue (or the adjacent parts)
Site-specific targeting
target: receptor within organ or tissue
Receptor targeting
pharmaceutical dispersed system that is a LOW VISCOSITY LIQUID preparation intended for application to the skin.
Lotion
8 (NMT 20% pass thru no. 60)
OFFICIAL DEFINITION OF POWDERS OF
ANIMAL AND VEGETABLE DRUGS
Very Coarse
20 (NMT 40% pass thru no. 60)
OFFICIAL DEFINITION OF POWDERS OF
ANIMAL AND VEGETABLE DRUGS
Chemical 20
Coarse
40 (NMT 40% pass thru no. 80)
OFFICIAL DEFINITION OF POWDERS OF
ANIMAL AND VEGETABLE DRUGS
Chemical 40
Moderately Coarse
60 (NMT 40% pass thru no. 100)
OFFICIAL DEFINITION OF POWDERS OF
ANIMAL AND VEGETABLE DRUGS
Chemical 80
Fine***
OFFICIAL DEFINITION OF POWDERS OF
ANIMAL AND VEGETABLE DRUGS
Sieve No. 80
No limit
Chemical 120
Very Fine***
- For NON-potent drugs
- NON-individual dosing
- Packaging - bottles (wide open), aerosols, sifter cans
Bulk Powder
What are the type of Bulk Powder (5)
- Dentrifices
- Oral powder
- Douches
- Insufflation
- Dusting Powder
- powder for cleaning TEETH
- Abrasive, anti-CARIOGENIC
Dentrifices
Intended to be SWALLOWED (dissolved in water prior to use)
Oral powder
- cleanse the VAGINA
- dispensed in the forms of tablets or powder
- powder is dissolved in warm (tepid) water
- pH usually 3.5 to 5 when the solution is prepared
Douches
- introduced into BODY CAVITY
- powder is placed in insufflator →squeeze the bulb to release particles trough the nozzle to the region for which the medication is intended.
- passed through a mesh # 100
Insufflation
- dusted on the skin by means of sifter-top containers
- provides NO systemic toxicity
- grit-free –> impalpable to touch
Dusting Powder
◼ Aka Chartula/Chartulae
◼ For POTENT drugs
◼ Powders divided into single doses
◼ Packaging: Individualized more accurate dosage form than bulk powder
DIVIDED POWDERS
TYPES OF PAPER USED FOR DIVIDED POWDERS
*transparent WAXY paper
*HIGHEST MOISTURE RESISTANT for drugs that are volatile, hygroscopic, deliquescent, efflorescent
Waxed Paper
TYPES OF PAPER USED FOR DIVIDED POWDERS
*LIMITED MOISTURE RESISTANCE
*also for volatile substances
*GLAZED transparent paper
Glassine Paper
TYPES OF PAPER USED FOR DIVIDED POWDERS
*LIMITED MOISTURE RESISTANCE
*thin, semi-opaque paper
Vegetable Parchment
TYPES OF PAPER USED FOR DIVIDED POWDERS
*NO MOISTURE RESISTANCE
*for non-volatile, or ingredients not adversely affected by air or moisture
Bond Paper
◼ powder + small amount of liquid FORMING A PASTE
◼ use of NON–volatile, NON-solvent known as LEVIGATING AGENT
◼ examples
1. Mineral oil (BEQ: aka liquid paraffin)
2. Castor oil
3. PEG
Levigation
◼ grinding using MORTAR & PESTLE
1. Glass Mortar
2. Porcelain/Wedgewood
◼intended both to MIX and COMMINUTE
Trituration ***
◼ use of VOLATILE solvent such as ALCOHOL (camphor reduction), ETHER (iodine reduction)
◼ applicable for GUMMY materials
Pulverization by Intervention
Mechanical method of particle size reduction
Milling
*Principle: CUTTING
*For comminuting
1. fibrous
2. crude drugs
Shear cutting cutting (in chikading song)
Shear Mill
*Principle: compression w/ application pressure
End Runner Mill
*Principle: Impact
*Comminuting ALMOST ALL drugs, except thermoLABILE substances
Hammer Mill
*Principle: Impact and attrition
*Ball as grinding medium
*Pin as impactor
Ball and Pin Mill
*Principle: attrition and compression
Rolling Mill
*Blending small amounts of powders by movement of SPATULA
*Not for LARGE-scale or POTENT powders
Spatulation (or small scale, non-potent)
*Small amount of POTENT drug substances + large amount of DILUENT
*to ensure the uniform distribution of potent drugs
Geometric Dilution
*Powder is enclosed in a LARGE container which rotates by a motorized process
* For large-scale mixing
Tumbling
*Use of a SIFTER
*Result: light, fluffy powder
*Not for POTENT drugs
Sifting
*Agglomerates of powders
*Requirement: 4-12 mesh sizes (or 0.2-4 mm)
Granules
Why granulate?
- ↑ FLOW and compaction
- ↑ COMPRESSIBILITY in tablet manufacturing process
- ↓ DUST during material processing
- UNIFORMLY distributes essential ingredients within the granules
*MOST WIDELY EMPLOYED method to produce compressed tablets
*Equipment: Fluid Bed Granulator
Wet Granulation
For drugs that are DEGRADED BY MOISTURE or elevated temperature required for drying the wetted material
Dry Granulation
OVERWETTING to resulting granules
Granules will be HARD
UNDERWETTING to resulting granules
Granules will be SOFT, tend to CRUMBLE
What are the DILUENTS/FILLERS (bulking agent, size enhancer)
Lactose - most common diluent
Mannitol
Xylitol
Starch
Kaolin
What are the DISINTEGRANTS (promote ↑ break-up)
Starch
Alginates
Cellulose
Clays
Gums
What are the BINDERS (gluers or ↑ adhesion)
Natural: Gums
Synthetic: Methylceullose, Ethylcellulose***
What are the GLIDANTS & LUBRICANTS (to improve flowability/flow activators)
Glidant example: colloidal silicon dioxide
-Mg stearate
-Ca stearate
Calamine is pink because of
Fe2O3
Use to disguise the bitter taste of Quinine
Yerba santa - Eriodictyon (best answer)
What is the BEST VEHICLE
1.Salty (e.g., Ammonium chloride)
2.Bitter (e.g., quinine)
3.Acrid or sour tasting (e.g., HCl)
4.Oily taste (e.g., castor oil)
BEST VEHICLE
1. Cinnamon Syrup
2. Cocoa (if not available, raspberry, cherry, cinnamon)
3. Raspberry
4. Aromatic rhubarb or sarsaparilla syrup
Flavoring Methodology
✓ Sour taste- FRUITY flavors, salty flavors
✓ Bitter – blended with salty, SWEET and sour tastes
✓ Chemicals used in blending: VANILLIN, MSG, benzaldehyde
Blending
Flavoring Methodology
✓ Addition of flavor whose intensity is longer and STRONGER than the obvious taste
✓ Methyl salicylate, Glycyrrhiza (Licorice), oleoresins
Overshadows
Flavoring Methodology
✓ Formation of INSOLUBLE compounds of the offending drug (e.g., SULFONAMIDE)
✓ EMULSIFICATION of oils, EFFERVESCENCE (magnesium citrate solution)
✓ High viscosity of fluids to LIMIT CONTACT OF DRUG with the TONGUE
✓ Mechanical procedures (COATING tablets)
Physical
Flavoring Methodology
✓ Absorption of the drug on a substrate or formation of COMPLEX of the drug with ion-exchange RESIN or complexing agents
Chemical
Flavoring Methodology
✓ Taste buds is ANESTHETIZED by MENTHOL or MINT flavors
Physiological
Methods of Coating Tablets
(SUGAR-COATING TABLETS) 5 Steps
- Waterproofing and Sealing
- Subcoating
- Smoothing and final rounding
- Finishing (and coloring, if desired)
- Polishing
Waterproofing substance
Shellac
How many subcoats of sugar-based syrups in Subcoating Step
3-5 subcoats
Subcoating substances:
sucrose solution (gelatin, acacia, or PVP)
In Step 3 of sugar-coating tablets, how many additional coatings of a thick syrup to complete the rounding?
5-10
Methods of Coating Tablets
(SUGAR-COATING TABLETS)
This step is performed in a clean pan
Step 4: Finishing (and coloring, if desired)
What is use in polishing step of coating tablets?
beeswax, carnauba wax
METHODS OF COATING TABLETS: (5) ***
- Sealing (waterproofing)
- Subcoating
- Smoothing (Grossing)
- Color coating
- Polishing (Polisher)
places a THIN, skin-tight coating of a PLASTIC-like material over the compressed tablet, to produce coated tablets having essentially the SAME weight, shape, and size as the originally compressed tablet
Film-coating tablets
*intended to pass through the stomach intact to disintegrate and release their drug content for absorption along the small intestine
*must resist the dissolution in the highly acid environment of the stomach
Enteric-coating tablets
Non-aqueous
Opaquants (?) and colorant ** (in hard gelatin capsule)
Opaquant (TiO2)
Steps in DRY Granulation (6)
- Weigh formulation/Milling
- Mixing
- Pre-compression/Slugging
- Sieving/Sieve slugs
- Final Mixing
- Compression
Steps in WET Granulation (6)
- Weigh & Mix Formulation
- Prepare Damp Mass
- Screening
- Dry the wet granulation
- Size granules by Dry Screening
- Lubricate & Compress
◼ Most common method of preparation
◼ Use of tablet machine (TM)
1. Single Punch TM
✓ Simplest of all machine type
Compression
✓ More cost efficient
✓ Preferred by industries due to its high
output.
Rotary Tablet Pressing Machine
PARTS OF A TABLET PRESS
Controls SIZE and SHAPE
Die
PARTS OF A TABLET PRESS
DIRECTS granules into the die
'’Directs means direction pag nag tatravel need mo ng SHOE’’
Feed shoe
PARTS OF A TABLET PRESS
Controls HARDNESS
'’Suntukin mo siya ng malakas’’
Punch
PARTS OF A TABLET PRESS
LOADS the granules
HOLDS/STORES material for compression
'’Hop in’’
Hopper
PARTS OF A TABLET PRESS
GUIDES punch movement
'’tourGUIDE needs a track’’
Cam track
Medicinal agents + inert substances + small shell of gelatin
Capsules
Parts of the Capsule
1. Shorter, wider
2. Taller, narrower
- Cap
- Body
What is the % of HGCs (hard gelatin capsules)
12-16% or 13-15%
a capsule composed of hard gelatin shell containing hundreds of tiny, coated beads/pellets of drugs for sustained release
Spansule
Method of capsule filling (small scale)
Punch Method
In Capsule Size
*The higher the number =
the smaller the capsule size (small)
- The LARGER size of capsule?
- The SMALLER size of capsule?
- 000
- 5
MATERIALS FOR MAKING CAPSULES
*partially hydrolyze COLLAGEN (connective tissues and bones of animals)
Gelatin
Weight in grams needed by a specified plunger to DEPRESS THE GEL (4mm) without breaking
Bloom Strength
*Encapsulate and hermetically SEAL LIQUIDS, suspensions, pasty materials, dry powders, and even pre-formed tablet
*Composition = GELATIN + SUGAR + WATER + PLASTICIZER
Soft -Gelatin Capsule
SGC Process
*more efficient
*GEL RIBBON brought together -> Fill is injected
-> Sealed (using pressure and heat)
Rotary or reciprocating die process
SGC Process
*using series of molds; oldest method
*Warm Gelatin sheet poured in MOLD -> Drug is placed -> Upper gelatin layer is added ->Capsule sealed by pressure
Plate process
*Dissolve or disintegrate slowly in the mouth
*Dosage form of Strepsils
Lozenges
1.Molded lozenges =
2. Compressed lozenges =
- Pastilles
- TroChes
Sugar-based LOZENGE on STICK
Lollipop
Sometimes known as BEADS
PELLETS
Small, ROUND with active ingredient
Pills
◼ AW = volatile oil + water immiscible
◼ Used as perfumed vehicle
◼ Storage: light resistant container (amber)
Aromatic Water
◼ = Acacia + Water
◼ thick, viscid, adhesive liquids
◼ Use: Suspending Agent
◼ Category: Aqueous (colloid) sol’n, suspending agent
Mucilage
◼ Treatment of EAR infection
◼ Impacted cerumen removal
Otic Solution (ear solution)
◼ restores MOISTURE to dry nasal passages
◼ curbs INFLAMMATION of mucus membrane
◼ cleanse nasal passages
◼ nasal DECONGESTANT
Nasal Solution
◼ mouth cleanser
◼ treatment of oral mucus membrane diseases
Mouthwash
◼ sterile
◼ eye irrigating solution
Ophthalmic Solution
◼ Use: Contain antiseptic to treat oropharyngeal condition
◼ swish & spit
Gargle
◼ = Fruit extract + H2O
◼ Flavored vehicle with preservative
Fruit Juice
◼ Diluted acid = conc. acid + purified water (PW)
◼ Diluted HCl = treatment of achlorhydria
◼ Conc Expression
1. % w/w = concentrated acid
2. % w/v = diluted acid
- typically: 10%w/v, except acetic acid: 6% w/v
Diluted Acids
◼ Aka Clysters
◼ Rectal injections
◼ Use:
✓ evacuation of bowel (laxative)
✓ retention enema (ulcerative colitis)
Enemas
◼ wash surgical wounds, incisions, and body tissues
◼ Requirements:
✓ sterile
✓ Passed Bacterial Endotoxin Test (BET)
✓ minimal amount of solid
Irrigation Solution
◼ Purified water + sucrose
◼ Methods of Preparation:
1. (+) heat
2. Agitation
3. Percolation
Syrup
◼Sucrose: 85g
◼SG = 1.313
◼Self-preserving
✓ 65 %w/w
✓ 85 %w/v
◼Prepared by Percolation
◼low solvent capacity
Simple syrup, NF
*Clear, pleasantly flavored solution for oral use
*Must contain alcohol (traditionally 5-40%)
*Iso-alcoholic elixir = low-alcohol (8-10%) + high-alcohol (73-75%)
Elixirs ***
*Aka Essences
* = Volatile oil + alcohol
1. HIGH Alcohol content: >60%
2. alcoholic or hydroalcoholic solution
3. medicinal agent
4. flavorant (orange spirit, cardamom)
5. Stored in light resistant container
6. Spirit + water = salting out
Spirits
Preparations obtained from vegetables & animal drugs
Extractives
- (hydro)Alcohol + chemical (or soluble components of vegetable drugs)
- Potency: 100mg/1mL = 10%
- Alcohol content: 15-80%
- Aging can cause precipitation of the inactive constituents (Mx: Glycerin)
- Storage: light-resistant container
Tinctures
10% opium tincture (17-21% alcohol)
Laudanum
10% potency (74-80% alcohol)
Comp benzoin tincture
- Aka 100% Tincture
- = Vegetable oil + alcohol + percolation
- Potency: 1g/1mL = 100%
Fluidextract
*COLLOIDON = Pyroxylin + 1 alcohol + 3 ether
*Flexible collodion = Collodion + 2% camphor +3% castor oil
*Salicylic acid collodion = flexible collodion + 10% salicylic acid
Ethereal Solution ***
Aka Embrocation
LinimEnts
It contains Vitamin A & D
Oleovitamins
Ex: eugenol - dental analgesic
Toothache drops
TYPES OF COLLOIDS
- Solvent-loving
- High affinity b/w dispersed phased and dispersion medium (solvation)
- NOT easily precipitated=thermodynamically stable
Lyophilic
Lyo - solvent
TYPES OF COLLOIDS
- Solvent-hating
- Low solvation
- EASILY precipitated=unstable
Lyophobic
*Surfactants
Micelles **
✓ Aggregates of surfactants dissolved in a dispersion medium
✓ Aggregation occurs over a NARROW concentration range (50 or more monomers)
✓ Use: to INCREASE the solubility of materials that are normally INSOLUBLE (Phenomenon: Micellar Solubilization)
Association (Amphiphilic)
Concentration at which MICELLES ARE FORMED is termed as
Critical Micelle Formation
COLLOID PROPERTIES (under Kinetic Properties)
RANDOM (zigzag) movement of particles due to collision
Brownian Movement
COLLOID PROPERTIES (under Kinetic Properties)
Movement of particles from an area of HIGH conc to an area of LOW conc
Diffusion
COLLOID PROPERTIES (under Optical Properties)
- When a light beam is passed through a colloidal sol, some may be absorbed, some is SCATTERED and the remainder is transmitted undisturbed through the sample
- FARADAY Effect: the sol. appears turbid due to light scattering
- Sig: measurement PS, shape as the turbidity depends in the size or MOLECULAR WEIGHT of the colloidal material involved
MNEMONIC: FRAday, saTURday, MOnday
Light scattering effect
COLLOID PROPERTIES (under Electrical Properties)
- Aka electrothermodynamic potential
- the difference in electric potential between the ACTUAL of the particle and the ELECTRONEUTRAL region
spirist Potential
COLLOID PROPERTIES (under Electrical Properties)
- aka electrokinetic potential
- the potential between the surface of the tightly bound layer (known as SHEAR/SLIPPING PLANE) and the electroneutral region of the solution
- governs the degree of REPULSION between adjacent, similarly charged, dispersed particles
- Sig: STABILITY of suspension
- High negative or positive values mean phase STABLE
- +50 mV(more stable form) vs +20 mV
- -50mV vs 5 mV
Zeta Potential ***
Factor that governs the degree of REPULSION in systems containing dispersed particles
Zeta Potential
INSOLUBLE particles (10-20microns)
Suspensoid
*lowers sedimentation (settling) rate; thickeners
*decrease settling
Suspending agent
Ideal Suspension (morse type BE)
Properties of a suspension
1. Settle __________ and readily ________
2. Particle size of suspensoid should remain fairly constant throughout periods of long-standing
3. Pour ___________ and evenly from its
container
- SLOWLY, REDISPERSIBLE
- READILY
GELS ***
1. water-based gel
2. freeze-dried
3. supercritical drying; extremely low density; Graphene aerogel
4. room temp. or vacuum; vacuum drying
- Hydrogel
- Cryogel
- Aerogel
- Xerogel
- Made up of either SMALL inorganic particles or of LARGE organic molecules enclosing and interpenetrated by a LIQUID
- Rendered jelly-like by the addition of GELLING agents
Gels
REVERSIBLE gel-sol property; thickens when standing, liquefies when shaken
Thixotropy
taking up of liquid WITHOUT increase in volume
Imbibition
taking up of liquid WITH increase in volume (lumaki)
Swelling ***
dispersing medium squeezed out; gel shrinks
Syneresis
Identify what type of Gelatin:
Acid hydrolysis
Type A Gelatin
Identify what type of Gelatin:
Base hydrolysis
Type B Gelatin