Dose Form Exam II Definitions

Solid dosage Form prepared by compression or molding of powdered/granulated drugs and with the aid o suitable pharmaceutical excipients

• Stable, elegant, effective
• Convenient for handling, identification and adminisration
• Many formats, sizes, colors, shapes, scored in halves with elegant engravings

• Compressed
• Multi Compressed
• Sugar Coated
• Film Coated
• Gelatin Coated
• Enteric Coated
• Buccal
• Sublingual
• Chewable
• Lozenges,Trochs, Drops, Pastilles
• Lollipops
• Effervesent
• Molded
• Tablet Triturates
• Rapid Dissolving
• Extended Release
• Vaginal Tablets

Single compression of all ingredients

For separation of incompatiple drugs or for modified release

• Multiple Compressed Tablets
• Multiple feed and multiple compression of fill within a single die

Core tablet is placed prescisly within the die for compression with surrounding fill

• Several layers of color or uncolored sugar solution (sucrose, gelatin, acacia or PVP = polyvinylpyrrolidone)
• Final tablet increased of up to 50% of size and weight if uncoated tablet
• Final tumbling with talc for high luster

Product specific indentification codes and distinctive symbols

Cloth or canvas impregnated with carnauba wax, bees wax or spraying with wax dissolved in acetone

• Thin layer of aqueous or non-aqueous polymer (plastic like material) cellulose acetate phthalate cellulose ether polymers
• Protection, color, durability less bulkiness, less time consuming

• Caplets
• Capsule-shaped compressed tablets coated with gelatin

• Protection of drug against patient gastric mucosa or enhanced 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 action
• Materials; shellac, phthalate derivatives

Placed in cheek pouch to dissolve slowly, absorption through the oral mucosa

Placed under the tongue, for prompt dissolution and absorption thoughout the oral mucosa

• Chewed and dissolve in the mouth made with creamy base (mannitiol, sorbitol, xylitol=sugar free)
• Negative heat of solution leaves a cool mouth feeling upon dissolution
• Flavored and colored
• For children and adults who have difficulty swallowing

• Hard candy like (sugar of sugar free) or gummy like (gelatin base)
• Dissolve or distintegrate slowly in the oral cavity
• Heat stable active ingredients
• Local effects

• Sugar based lozenge on a stick (also sugar based)
• Fentanyl

• Compression of effervescent salts that liberate carbon dioxide when dissolved in water
• Should not be swallowed whole

MOlding and salts compaction , hand operated tablet press

"Old Fashioned" tablet containing small amounts of potent drugs and prepared with minimal compression to allow ease of crushing for compounding and rapid dissolution

• SUPER DISINTEGRANTS
• Dissolution within 15 to 30 seconds
• Very water soluable excipients that attract water into the tablet

Drug loading, taste masking and friability

Release of medication in a pre-determined manner over an extended period

• Uncoated, bullet shape or ovoid
• Plastic or cardboard inserter device for administration
• Local Effects

• 1) Weigh and blending of drug. fillers, disintegrating agents. glidants
• 2) Sifting of powder to eliminate clumps
• 3) Mixing with liquid binder/adhensive agent, 10 to 20% aquous/alchoholic solution of corn starch, 25 to 50% solution glucose, molasses, gums such as acacia, solution of cellulose derivatives, gelatin
• 4) Damp mass, damped/ wet powder
• 5) Pass through screen 6 to 8 screen size
• 6) Drying: thermostatically controlled over
• 7) Sizing dry screening 12-20 mesh size
• 8) Blending of granules and lubricants (Mg/Ca/Zn Sterate/Talc/Stearic Acid)
• 9) Compression, tableting machine

• For materials that are degraded in the presence of moisture or high heat
• 1) Weighing blending of powdered ingredients, drugs, fillers, disintegrating agents, cohesive properties
• 2) Binding agents are added (methylcellulose/hydroxyl methylcellulose)
• 3) Powders are compressed in slugginh machine
• 4) Slugs crushed and sized
• 5) Granules and dry lubricants (Mg/Ca/Zn Sterate/ Talc)
• 6) Compression in tableting machine

• Excipients have free flowing and cohesive properties
• Potassium chloride, Methenamine, Dibasic Calcium Phosphate

• Forcing of a dampened mass into th cavities of a tablet mold (plastic or metal)
• Mold consists of two plates one with a hole and the other with a peg

• TO remove loose powder
• Elegance
• Prior to coating

• For protection of drug from air and humidity
• To protect gastric mucosa of irritating drugs
• Mask Taste
• To provide aesthetics and distinction to a product (color, imprinting and manufacturer symbol or information)

• Weight
• Content uniformity
• Hardness, breaking strength, Friability
• Thickness
• Disintegration
• Dissolution

• Weight variation for dosage form uniformity
• Assay for homogenous drug distribution

Active ingrediant between 90 and 110%

• Measurement of pressure/force to break each tablet
• Measure the tendency of a tablet to cumble (rotating tubling container)
• Tablet are weight before and after rotation and weight loss is determined (maximum loss allowed by USP is 1%)

• Caliper, hand gauge or automated equipment
• Depends on; diameter of the die, amount of the fll, compaction characterisics of fill
• Pressure applied

• The time required for a tablet to disintgrate
• Compressed tablets: Aparatus containing water ( 30 mins) at 37oC or simulated gastric fluid (1 hour)
• Enteric Coated: simuated gastric fluid (1 hour) and intestinal fluid at 37oC

• In vitro testing
• Quality assurance during manufacturing
• Bioequivalence from batch to batch; from the scale up batch
• Madatory for approval for marketing
• Influences the absorption and bioavailability

• Containers; bottles, blister
• Light resistant
• Desiccant packet and cotton ball
• Type of container: reduced potency of volatile drugs
• Nitroglycerin and no packing materials in catact with tablets

• Protection of injured area and rejuvenation of the skin,
• Hydration, Lubrication or emollient effect

• Specific effect
• Topically or systemically

• Skin
• Eye
• Nose
• Vagina
• Rectum

Deliver drug INTO the skin (the target) to treat dermal disorders (topical absorption)

Deliver drug through the skin (percutaneous absorption) to the general circulation for systemic effects (skin is not the target)

• Surface Area
• Condition of the skin
• Base/delivery system used
• Occlusive dressing
• Pressure/Rubbing

• Semisolid preparation for external application to the skin or mucous membranes.
• Soften or melt at body temperatures
• Spread easily
• Not gritty

To dry skin scaly lesions, skin mucosa, and eye

• Active drugs
• Ointment base (oleaginous, aqueous)
• Stiffeners: viscosity
• Humectants: escape of moisture
• Antioxidants: Rancidfication
• Penetration enhancers: penetration into the skin
• Preservatives: microbial growth

• Not water washable
• Emollient
• Insoluable in water
• Greasy
• Will not absorb water
• Occlusive

• White petrolatum
• White ointment

• Insoluble in water
• Not water washable
• Anhyrous
• Can absorb water
• Emmolient
• Occlusive
• Greasy

• Hydrophilic petrolatum
• Aquaphor
• Aquabase

• Insoluble in water
• Will absorb water
• Not water washable
• Contain Water
• Emmolient
• Occlusive
• Greasy

• Cold Cream
• Nivea
• Lanolin, hydrous
• Hydrocream
• Eucerin

• Insoluble in water
• Water washable
• Will absorb water
• Contains Water
• Not occlusive
• Not greasy

• Water soluble
• Water washable
• Will absorb water
• Anhydrous or hydrous
• Not occlusive
• Not greasy

PEG ointment

• None or very little skin penetration
• Type of base used oleaginous
• Refers to the external layer of the skin, epidermis

• Into the dermis
• Type of base used absorption base
• Refers to the internal layer of the skin, or dermis

• Yes into the skin and through the skin
• Type of base used emulsion and water soluble base
• Refers going through the skin

• Drug release rate
• Enhancement of percutaneous absorption Occlussion of moisture (If skin is dry wet ir, If it is wet dry it)
• Stability of drug
• Influence on other components of formuation (consistency)
• Patient Factors (dry skin, intact or broken skin)

• Trituration
• Levigation
• Spatulation
• Dissolution

• 1) Reduction of particle size
• Trituration,
• Levigation, low surface tension to improve wetting, minimum amount
• 2) Incorporation of solids to ointment by geometric method
• 3) Dissolution of solids in small amounts of solvent compatible with the base
• 4) Large volumes of liquids: use mortar pestle

• Specific Gravity 0.88
• Misciple with fix oils except for Castor Oil
• Uses; Oleagenous,Absorption, Water in oil emulsion bases

• Specific Gravity 1.26
• Misciple in water, Alcohol, Proplene glycol, PEG 400
• Imiscible, with mineral and fixed oils

• Specific gravity 1.04
• Miscible with water alcoholm glycerin and PEG 400
• Immiscible with mineral oil and fixed oils

• Specific gravity 1.13
• Miscible with water, alcohol, and propylene glycol
• Immiscible with mineral oil and fixed oils

• Specific Gravity 0.92
• Miscible with mineral oil and other fixed oils, castor oil
• Immiscible with water, alcohol, Glycerin, Propylene Glycol and PEG 400

• Specific Gravity 0.96
• Miscible with Alcohol and fixed oils
• Immiscible with water, Glcerin propylen glycol, PEG 400, mineral oil and fixed oils

• Tween 80
• Specific gravity 1.06-1.09
• Miscible with water, alcohol, glycerin, propylene glycol, peg 400, mineral oil and fixed oils

Melting of ingredients together and cooling with constant stirring until congealing

• 1 Oleaginous phase oils and waxes are melted together
• 2 Aqueous phase: solution of heat stabl and water soluble ingredients are heated to simlar temperatures
• 3 Pouring of aqueous into oily with stirring
• 4 Cooling with frequent stirring until congealing

• Not required to be sterile (except for ophthalmics)
• Antimicrobial preservatives
• Rectal urethral and vaginal: tested for yeast and molds

Clear or opaque plastic or glass, colored, sizes range from 0.5 oz to 1 lb

• Greater protection against external contamination and environmental conditions
• PLastic or aluminum coated with epoxy resin, vinyl or lacquer

Stored at room temperature, excessive heat will cause softening and separation phases

Need the route of administration and mode of administration

• Change in consistency
• Bleeding of iquid and phase separation: needs levigating agent
• Drying out of ointment: need humectant (glycerin, propylene glycol)
• Oleagenous and anhydrous bases: relatively stable
• Emulsion bases: less stable

• Semisolid dosage forms containing one or more drug substances dissolved or dispersed in a suitable base, they possess a relatively fluid consistancy and formulated o/w or w/o emulsion
• Opaque soft solids or very thick liquids for external application

Creams of the o/w emulsion type with a large percent of water and stearate soup-type emulsifiers (water evaporates leaving a thin film on the skin)

• Weeping or oozing lesions
• Drying effect: body fluids miscibl with cream aqueous external phase

• Thick stiff ointment that ordinally do not flow at body temperature and have reduced absorption
• To coat the affected area for protection

• For areas that require protection remains in place longer than ointments: sticky. Absorption of serious discharge from skin lesions. Less greasy feeling, not suited for hairy parts of skin
• If they are too stiff it is difficult to apply

• Semisolid system consisting of dispersion of small inorganic particles or large organic molecules interpenetrate by a liquid
• Are semisolid systems in shich the moement of the dispering medium is restricted by an interlacking three dimension network of particles

Excellent drug delivery system; oral, topical, nasal, vaginal, rectal, compatible with many different drugs and very efficacious

Taking up of liquid with no measurable increase in volume

Taking up of liquid in volume

Intense interaction between particles of the dispensed phase so that on standing the dispersion medium is squeezed out in droplets and the gel shrinks = instability

Reversible gel-sol formulation with chang in the volume of temperature

Removal of the liquid from a gel leaving only the framework gelatin in sheets, acacia, tears, tragacanth ribbons

• Gels may be as clear as liquid, others are terbid. Ingrediants not completly molecular dispersed or dissolved
• Most gels are water washable, water soluble, water absorbing and greaseless

Gels that contain linear or branched polymer macromolecules, that dissolve in water and have no apparent boundry with the dispersing medium

Single-phase gels made from synthetic or natural macromolecules

Gels that contain small discrete particle

semisolid on standing but liquid when shaken

Are two phase system with large particle size or floccule of small distinct

• Active drug does not interfere with the gelling process, add it prior to gelling for uniformly dispersion
• Active drug interferes with gelling process, place gel + active ingredient in a plastic bag, which is kneaded to thoroughly mix the drug, then cut corner of bag
• Gelling agents usually have 0.5 to 2 percent concentration

Sprinkling slowly very small particles of powder (through a sieve) into a rapid stirring liquid

Sonication

thicken the gel after the gelling agent is dispersed

• Adhesive masses spread on a backing of paper, fabric, moleskin or plastic
• Provide prolonged contact and effect at the site of application

Plastic masses containing gelatin (15%) glycerin (40%) water (35%) and medicinal ( 10%)

• Banage only if prescribed, open to the atmoshpere whenever possible
• Ointments creams and pastes, should not be substituted one for another by a pharmacist without the consent of the prescribing physcian

Liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutally miscible solvents

• Oral
• Topical
• Vaginal - douches
• Rectal - enemas
• Otic (arual)
• Nasal
• Ophthalmic
• Irrigating
• Parenteral

• Oral solutions
• Syrups
• Aromatic waters

• Tinctures
• Elixirs
• Other fluid extract
• Collodion
• Liniment
• Oleaginous solutions

• Homegeneous doses
• Immedient availability
• Most routes of administration
• Easy dose adjustment
• Enteral feeding
• Nursing home, psychiatric and incarerated patients

• Less stability
• Potential microbial contamination
• Solubility in acceptable solvents
• Taste and smells
• Bulk and weight
• Bulk containers

• Likes dissolves likes
• Inorganis compounds: high water solubiity
• Organic (weak acid or weak base) solubility depends on pH of the solvent
• Salts of organic compounds: high water solubility
• Heating of solvent: may cause precipitation
• Miscibility of liquids, oil and water immiscible

• Drug
• Solvent
• Sweetners
• Flavor/odorant
• Colorants
• Preservatives
• Buffers
• Stabilizers

look at book to finish

Generally Recognized As Safe

Nutritive sweetners may be converted to energy in the body

• Sugars: Sucrose, Dextrose (D-Glucose)(L-Glucose is salty), Fructose
• Non-sugars: Sorbitol, Glycerin, Propylene Glycol, Mannitol, Xylitol

Non-nutritive, non-caloric sweetners, sugar substitutes

• Natural: Not hydrolyzed, and not absorbed, methylcellulose, hydroxy ethy cellulose, stevia (heat stable)
• Artifical: Saccharin (sweet n low) unmetabolized, heat stable Cyclamate metabolized carcinogenicity and teratogenizity Aspartame (Equal, Nutrasweet) 3 metabolites, phenylalanine, aspartic acid, methanol, Heat labile Acesulfame Potassium, unmetabolized Sucralose (Splenda) unmetabolized heat stable Neotame similar to aspartame but with less amount of phenylalanine

10,000

The combination of flavor, smell, texture, temperature and color

SALTY

BITTER

sweeter it will be

Salty, Sweet, Bitter, Sour/Aicd, Oily, Metalic

• Yellow: Sulfur and riboflavin
• Blue: Cupric sulfate
• Red: Cyanocobalamine

Aniline ( derivative of benzene)

Interference with microbial growth, multiplication and metabolism

Water in a preparation that is not bound to other molecules

Determines the effective concentration of a preservative required for a given liquid (water based) formulation

• Alcohols and glycerols
• Ethyl Alcohol 95-96%, used 15-17.5%of the free water present in the preparation
• Propylene Glycol (same as ethyl alcohol)
• Glycerin (glycol) Preserve an equal eqilvalent quantity of volume
• Benzoyl Alcohol Bactericidal at 1-2% effectiveness not affected by pH of the solution

• Benzoic Acid, Na benzoate, K benzoate, [0.1-0.3%], for oral, topical and parenteral dosage forms
• Sorbic Aid, K [0.05-0.2%], for oral and opthalmic

• An ester and salt preservative up to 0.1%
• Most effective against fungi
• For all kinds of dosage forms
• Methyl Parabens, Methyl parabens sodium, propyl paraben, butyl paraben

• A topical (nasal, ophthalmic) and parenterals preservatives
• Phenylmercui nitrate (PMN) and Phenylmercuric acetate (PMA)
• Thimerosal

• Insufficient stability in aqueous medium to meet extended shelf-life
• Lyophilization or spray drying
• Refrigeration after reconstituion for 7-14 days

• Maintenance of Ideal pH for drug solubility, stability and product shelf life
• Attention to interactions with anti-microbil preservatives

• Any additional excipient required to maintain drug in solution, protect drug in its active form
• Keep compatability amoung all components, prevent degradation of drug or product

• SOlution with hydroalcoholic or alcoholic vehicle
• Maceration: softening due to soaking steepig
• May contain 15-80% of alcohol, self preserved

• Aqueous or oleaginous solutions
• Coarse droplets
• finely divided solids
• Nasopharyngeal
• Skin, antiseptis, local anesthetics, anitfungals
• Mehcanical devices: Break up solution into small particles
• Facilitate spraying of powder
• Spray bottels
• One way pumps
• Atonizer

• Douches, feminine hygiene or with anti infective agents for local actions
• Solutions prepated from powders

• Enemas rectal liquid preparation
• Retention: for local effect or systemic effect
• Evacuation: to clense bowel

Aqueous. sweetened. flavored, viscous solution

• Non-medicated: Flavored syrups, water soluble drugs, syrup NF 85% sucrose in pH20, ora-sweet: acidic pH and alcohol free
• Medicated: antiemetics, antihistamines, antitussives, antivirals

• Drugs: water solubility
• Solvents: Purified water, alcohol (low concentration)
• Pharmaceutical Ingredients: Seetening agents, Flavoring agents, Coloring agents, Antimicrobial/Antifungal preservatives

• With the aid of heat: sucrose syrups invert sugars, hydrolysis of sucrose to glucose and fructose, some artifical sweeteners are destroyed by heat
• Agitation
• HEat and agitation
• Percolation
• Maceration

per= through, colar= to strain, (preparation of coffee), extracts of crude drugs in comminuted form

To soak, a tea bag

• Drugs: alcohol-soluble and water-soluble components dissolved separately
• Solvents: water, alcohol, adjunet solvents
• Other pharmaceutical ingredients

• Sweetners
• Colorant
• Flavorant
• Preservatives: 10-15% is self preserved
• Stabilizers

• 0-6 years old: 0.5%
• 6-12 years old: 5%
• Adults: 10-15%

• Simple solution with agitation
• Mixture of alcoholic solution with aqueous solution added to Alocoholic
• Final concetration (talc) if separation of flavoring oils

Tight, light resistant container, protect from heat

• Topically applied to the eye
• Surface or introcular

For infections (bacterial, viral, fungal) allergies, inflammation, elevated intraocular pressure, dry eye

• Dropwise
• Thin ribbon to the lower lid margin
• Insertion of device for contiuouse release of drug

• Tear fluid in the cul-de-sac 7-8 mcl
• Nonblinking 30mcl vs blinking 10 mcl
• Blinking looses 80% of drop (50 mcl) is lost to tears and the nasolacrimal drainage

• Increase contact time
• Multiple- drop therapy: time intervals
• Suspension, ointment, Gels
• Inserts
• Oral or parenteral therapy

• Autoclave 121 oC for 15 minutes
• Bacterial 0.2 mcm pore size

Surgery, inserts, eye washes used in large quatities, single dose containers

• To make the osmotic pressure similar to the lacrimal fluid 0.9%
• FOr efficacy,safety and comfort ( no burning, tingling, swelling sensation)
• Only when it has the same osmotic pressure as some body fluid
• All the solutes contribute to osmotic pressure

It will draw water out of the eye and cause it to shrink

It will draw water into the eye and water enter the cells and may cause them to burst

• To maintain stability of drug
• Control therapeutic activity
• Reduce discomfort to the patient
• pH of eye is 7.4

• Boric Acid, 1.9% pH~5
• Isotonic phosphate, mixture of monobasic and dibasic salts of phosphat pH~ 5.9-8.0

Fast lacrimal drainage; liquids