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What is the most frequently prescribed dosage form?
What makes tablets so desirable?
What determines the size and format of a tablet?
- the die and punch used
- the amount of fill
- the amount of pressure applied to the fill
Why are tablets convenient?
- easy to handle
- easy to identify
- east to administer
Why would you make a multiple compressed tablet instead of a compressed tablet?
- if you need to separate incompatible drugs/ingredients
- for modified release (can administer 2 doses at once b/c the outside is the first dose and the inside will come later)
What are the 2 types of multiple compressed tablets?
- 1. multiple-layered tabs: multiple feed and multiple compression of fill within a single die
- 2. tablet within a tablet: core tablet placed precisely within the die for compression with surrounding fill
What are the different types of tablets?
- 1. sugar-coated
- 2. film-coated
- 3. gelatin-coated
- 4. enteric-coated (delayed release)
- 5. buccal
- 6. sublingual
- 7. chewable
- 8. lozenge/troche/drop/pastille
- 9. lollipops
- 10. effervescent
- 11. molded
- 12. tablet triturates
- 13. vaginal
- 14. extended release
- 15. rapid dissolving tablets (RDT)
What is PVP and what does it do?
- binding agent
What is another name for a sugar coated tab?
What is a sugar coated tab?
- several layers of colored or uncolored sugar solution
- -sugar solution made out of:
- -acacia or PVP
What are steps taken to make a sugar coated tab?
What are the disadvantages of sugar coated tabs?
- a lot of time required
- a lot of expertise required (difficult to make sugar even over whole tab)
- you get a lot of sugar in one day if you are taking multiple doses
- the final tab can increase in size and weight up to 50%
- have to have special imprinting on every tab per FDA
What is used to polish sugar coated tabs?
- a cloth or canvas impregnated with carnaubu wax/beeswax
- or a spray with wax dissolved in acetone
What is used to tumble sugar coated tabs?
talc for high luster
What is an advantage of sugar coated tabs?
they cover up bad taste and smell
What kind of tabs are 99% of those in the U.S.?
T/F: Tablets made for clinical trials do not and should not have marking on them.
What are some advantages of film-coated tabs vs. sugar coated?
- they are less time consuming to make
- they are less bulky
- they are durable
- they are colored
- they are protected
- they can be made with multiple layers of coating for different times of release (15min, 30min, 1 hour all in one tab)
What is a film coated tab?
- a thin layer of aqueous or non-aqueous polymer solution like plastic
- -cellulose acetate phthalate
- -cellulose ether polymers
What is an advantage of phthalates?
they are cheap and easy to make (colored, printed)
What are gelatin-coated tabs (caplets)?
capsule-shaped compressed tablet coated with gelatin
What is better about gelatin coated tabs?
- they could taste better and look better
- might go down easier
- faster acting than film coated
What are the characteristics of polymers, cellulose, and gelatins?
- Polymers: make plastics, there are different forms
- Cellulose: we cannot digest it, excreted through the feces
- Gelatin: will be absorbed and can be nutritive form of protein
What are enteric coated tablets?
- NOT the same as extended release!
- have DELAYed release properties
- made for the intestines, not the stomach
Why would we use enteric coated (delayed release) tablets?
- 1. protect the drug
- 2. protect patient gastric mucosa
- 3. enhance absorption of drug
What materials are used to make enteric coated tabs?
- shellac (#1 ingredient because it won't dissolve in the stomach)
- phthalate derivatives
What two factors do we base the formation of enteric coated on?
- 1. the transit time required for the passage of the tab from the stomach to the intestine
- 2. the pH of the environment
What are buccal tabs?
- placed in the cheek pouch
- dissolve slowly
- absorbed through the oral mucosa
What are sublingual tabs?
- placed under the tongue
- prompt dissolution
- absorption throughout the oral mucosa
- need to be under the tongue for at least 10 minutes
What are chewable tabs?
- chewed/dissolved in the mouth
- made with a creamy base like mannitol, xylitol, sorbitol
- xylitol is sugar-free
- flavored and colored
- good for kids and adults who have trouble swallowing
- NEED to be chewed, not sucked on!
What is it about mannitol, sorbitol and xylitol that makes them have a good sensation in the mouth?
their negative heat of solution leaves a cool mouth feeling upon dissolution
What are lozenges? And what are the 3 other names for a lozenge?
- AKA troche, drop, or pastille
- a hard, candy-like substance or gummy-like substance
- can be gelatin based
- can be sugar or sugar-free
- dissolve or disintegrate slowly in mouth
- highly compressed
- active drug should be heat stable
- made for local effects (if chewed you are defeating the true purpose so DON'T chew!)
What are lollipops?
- sugar-based lozenge on a stick (can be sugar-free)
- can make out of any drug or base
- less chance of patient trying to chew lollipop vs. a lozenge
- ex: Fentanyl Actiq relieves chronic cancer pain
What is an effervescent tablet?
- a compression of effervescent salts that release CO2 when dissolved in water
- DO NOT swallow whole!
What are molded tablets?
- hard to make uniform
- hand-operated tablet press used to mold and soft-compact
What are tablet triturates?
- "old fashioned" tabs containing small amounts of potent drugs
- prepared with minimal compression to allow ease of crushing for compounding or rapid dissolution.
- not used anymore
What are 3 problems of rapid dissolving tabs?
- 1. friability
- 2. taste is hard to mask because dissolve so fast
- 3. drug loading
What is friability?
how easily a tablet crumbles
How should RDTs be packaged?
wrapped individually to avoid coming in contact with each other and crumbling
What are RDTs?
- contain very water-soluble exicipients
Who should take RDTs?
children and elderly
What are the two types of technologies for creating RDTs?
- 1. lyophillization (foaming of ingredients and pouring into a mold)--> Zydis tabs
- 2. compression of super disintegrants with small amount of effervescent material)--> DuraSolv, OraSolv, FlashTab, WowTab
T/F: Vaginal tablets (inserts) can be termed suppositories.
What are vaginal tablets?
- uncoated because the enzymes in the vagina are not like those in the GI to break down coatings
- bullet-shaped or ovoid
- only for local effects
- aka ovules or inserts
What are extended release tablets?
- they release medication in a pre-determined manner over an extended period of time
- must be tested "in vivo" and "in vitro"
What are the 2 disadvantages of a rotary tablet machine?
What is the max amount of loss to crumbling allowed by USP?
What is the max amount of error allowed for the amount of active ingredient in a group of 10 tablets?
- should be between 90-110%
When making tabs by wet granulation, what ingredients are used to make the liquid binder/adhesive mixture?
- a 10-20% aqueous/alcoholic solution of cornstarch and PVP
- 25-50% soution of glucose, molasses, gums like acacia, cellulose derivatives, gelatin
When making tabs by wet granulation, which mesh size do you pass through first?
big (6-8 size) to obtain granules or pellets
When making tabs by wet granulation, which mesh size do you pass through last (during drying)?
small (12-20) to make granules smaller and uniform in size
Why do you need to dry the damp mass of granules during wet granulation of tabs?
to evaporate teh alcohol and PVP
What do you do with granules after drying them in wet granulation method?
blending- you add the granules to a dry lubricant such as talc, stearic acid, Mg Stearate, Ca Stearate, or Zn Stearate
What do you do after blending in the wet granulation method?
compression using either a single punch tablet press or a rotary tablet machine with multiple punches.
What is the all-in-one granulation method?
- uses sophisticated machinery
- the granulation is prepared by a microwave vacuum process or fluid-bed process
When would you use dry over wet granulation to make tablets?
- if the drug itself has its own binding properties
- if your drug is degraded by high heat or moisture
What are the binding ingredients used in dry granulation of tabs and how much?
6-12% methylcellulose or hydroxymethylcellulose
How are powders compressed during dry granulation?
using a slugging machine or a roller compactor
When would you use direct compression for tablets?
When the excipients have free-flowing and cohesive properties
What are some examples of direct compression drugs?
- Potassium Chloride
- Dibasic Calcium Phosphate
Why do we coat tablets?
- 1. to protect drug from air
- 2. to protect drug from humidity
- 3. to protect gastric mucosa from irritating drugs
- 4. to mask taste of drug
- 5. for special release (enteric coating)
- 6. to provide color, symbol, aesthetics
What are the 3 types of coating for a tablet?
- 1. sugar
- 2. enteric
- 3. film
What is a friabilator?
- a device that measures the tendency of a tablet to crumble while in a tumbling container
- helps determine how much powder is lost during transit
What 4 factors determine the thickness of a tablet?
- 1. pressure applied
- 2. amount of fill
- 3. diameter of the die
- 4. compaction characteristic of the fill
T/F: In vitro dissolution tests are mandatory for approval of marketing by FDA and other reg. agencies of other countries.
What is the purpose of a dessicant packet in a bottle of tablets?
to reduce humidity
What is the purpose of cotton/cotton balls in a bottle of tablets?
to maintain tight packaging and reduce crumbling
What is the difference between topical dermatological products and transdermal products?
- topical dermatological= deliver drug into the skin to treat dermal disorders (topical absorption)
- transdermal products= deliver drugs through the skin to the circulation for systemic effects (skin is not the target)
T/F: topical preps can be administered to the eye.
T/F: Transdermal topical products go through all layers of the skin, including the epidermis and dermis.
What are the 5 factors that affect drug penetration of topical preps?
- 1. occlusive dressings
- 2. surface area
- 3. condition of the skin
- 4. base used
- 5. pressure/rubbing
What are ointments?
- semisolid preps for external application to the skin or mucous membranes
- can be medicated or non-medicated
- applied to dry, scaly lesions on the skin, mucosa and eyes
What are 3 characteristics of a good ointment?
- 1. soften or melt at body temperature
- 2. spread easily
- 3. are not gritty
What does the word "unguent" refer to?
What ingredients can be found in an ointment?
- -active drug
- -ointment base
- -penetration enhancers
What are humectants used for?
to prevent loss/escape of moisture
What are antioxidants used for (in ointments)?
to prevent rancidification
What is a common penetration enhancer for ointments?
What are two examples of an oleaginous ointment base?
- white petrolatum
- white ointment
What are 4 examples of an absorption ointment base?
- hydrophillic petrolatum
- anhydrous lanolin
What are 5 examples of W/O emulsion ointment bases?
- hydrous lanolin
- cold cream
What are 4 examples of O/W emulsion ointment bases?
- hydrophillic ointment
What is an example of a water soluble ointment base?
Which ointment base has these characteristics?
-will not absorb water
-not water washable
-insoluble in water
Which ointment base has these characteristics?
-insoluble in water
-not water washable
-can absorb water
Which ointment base has these characteristics?
-insoluble in water
-will absorb water
-not water washable
W/O emulsion base
Which ointment base has these characteristics?
-insoluble in water
-will absorb water
O/W emulsion base
Which ointment base has these characteristics?
-anhydrous or hydrous
-will absorb water
water soluble base
What do emulsifiers do?
they allow water and oil to be mixed together by creating droplets of either the water or the oil
How far does an epidermic base penetrate and what is an example?
- it penetrates none or very little
How far does an endodermic base penetrate and what is an example?
- it penetrates into the dermis
How far does a diadermic base penetrate and what is an example?
- it penetrates into and through the skin (most penetration)
- water soluble
What are the 3 ways to manually prepare an ointment?
- 1. ointment tile + spatula
- 2. mortar and pestle (for more liquid preps like calamine lotion)
- 3. ziploc bag
What is the mechanical mortar and pestle called?
What do we call the 2 general methods for compounding ointments?
T/F: It is easier to mix oil and water with a large quantity mixer than by hand.
What do astringents do?
they close off top layer of skin cells and "create" a new layer (Glaucia's words)
What factors influence the selection of an appropriate ointment base?
- rate of drug release
- enhancement of percutaneous absorption
- occlusion of moisture
- stability of drug in presence of water
- influence of drug on other components of the formulation
- patient's skin factors (dry, intact, broken, oozing)
T/F: Petrolatum is not good for burns or cuts
False; it is good because it is very smooth
T/F: A lipid soluble drug should go into a water soluble base.
T/F: A highly lipid soluble drug should go into a lipid base because it will dissociate when it touches the skin.
False; should not go into a lipid base!
What is the main goal of incorporation?
to achieve uniformity
How much levigating material should be used to improve wetting?
If too much glycerin is added to a prep, what will be the result?
- reduced shelf life and
- reduced suspendability
T/F: You should not melt your ointment base to add your solid drug to it.
False, you can melt it
_____are used for more localized areas, while ________ are used for spreading across large areas of the skin.
T/F: We can dissolve solids in a small amount of solvent that is compatible with the base if we want something a little more liquid.
It is most important for the levigating agent to be miscible with: the drug itself or the base?
Which levigating agent can have a laxative effect?
Which levigating agent is good for mixing with greasy bases?
Which levigating agents are good for mixing with water-containing bases?
- propylene glycol
- PEG 400
- Tween 80
Which levigating agents are not good for mixing with water-containing bases?
- cottonseed oil
- mineral oil
- castor oil
Which levigating agent is pretty much miscible with water or any other oil or levigating agents?
What is coalescence?
- breaking of the emulsion (oil and water phases separate)
- don't want this!
What is the max capacity for an absorption base to accept liquids?
T/F: Alcohol will destroy an emulsion if too much is added.
Why are absorption bases more versatile?
because they can accept water or grease
T/F: with an emulsion base, you want to mix the drug with a levigating agent that is miscible with the external phase?
T/F: It would be possible to add 25 mL of liquid to 50g of an ointment?
T/F: Scents are essential oils so they can be added to oleaginous bases.
What is fusion?
melting of ingredients together and cooling with constant stirring until congealed
How do we prepare an emulsion ointment?
- Heat oils and waxes together
- Heat water and water soluble ingredients separately
- Slowly add water (aqueous phase) to oil phase with continous stirring
- Cool with frequent stirring until congealed
Are ointments required to be sterile?
No, but ophthalmic ointments are
What types of ointments need to be additionally tested for molds and yeasts?
what is the size range for ointment jars?
0.5 oz---1 lb.
what is the size range for tubes of ointment?
5, 15, 30g
T/F: Different bases work better in different areas of the body.
What temperature should ointments be kept at?
below 30 C (about room temp)
T/F: Tubes have greater protection against external contamination and environmental conditions than jars.
Which type of bases are relatively more stable (unless left in extreme heat)?
Which type of base is less stable?
What is the BUD for extemporaneous non-aqueous liquids or anhydrous preps that use NF products?
25% of time remaining on product exp. or 6 months, whichever comes first
What is the BUD for preps containing water?
2 weeks (14 days)
What is a cream?
- a very thick liquid for external application or an opaque soft solid
- easier to spread and remove than ointments
- for topical, rectal, vaginal
- drug is dissolved or suspended in W/O, O/W, or other water-washable bases
Why do we apply creams?
- to dry out weeping or oozing lesions
- the water from the lesion mixes with the water phase in the cream and is evaporated off the skin
What are pastes?
- thick, stiff ointments that don't flow at body temp. and have reduced absorption capabilities
- coat the affected area to protect
- contain at least 25% of solid materials that are undissolved in the base
How can we prepare pastes?
- fusion if need to increase workability of base
- can use base as a levigator
T/F: A gel is a solution.
False; a dispersion
Gels are excellent drug delivery systems for what areas of the body?
T/F: Gels are relatively easy to prepare, are efficacious and are compatible with many different drugs.
What is imbibition?
the taking up of liquid with no measurable increase in volume
what is swelling?
taking up of liquid with an increase in volume
What is syneresis?
the intense interaction between particles of the dispersed phase so that, on standing, the dispersion medium is squeezed out in droplets and the gel shrinks = instability
What is xerogel?
- the removal of the liquid from a gel, leaving only the framework
- -gelatin sheets
- -acacia tears
- -tragacanth ribbons
What is thixotropy?
- semisolid gel on standing, but when shaken becomes a liquid
- no change in temp or volume required to make this happen
What is the common concentration of gelling agents in a gel?
- must be less than 10% of prep
what are some characteristics of gels?
- -water washable
- -water soluble
- -clear or turbid
- -water absorbing
- -can be oleaginous or alcoholic components
- -disperse light
What preservatives should be used for gels/magmas?
- -sodium benzoate
- -benzalkonium chloride
What are single-phase gel systems?
gels that contain linear or branched polymer macromolecules that dissolve in water and have no apparent boundary with the dispersing medium
What are some examples of single-phase gel systems?
- -natural polymers (tragacanth)
- -semisynthetic cellulose derivatives (methylcellulose)
- -synthetic polymers (carbomers)
What are mucilages?
single phase gels made from synthetic or natural macromolecules
What are two phase gel systems?
- gels that contain small, discrete particles
- are thixotropic
What are some examples of two-phase gel systems?
- -aluminum hydroxide gel
- -bentonite magma, NF
What makes a gel a magma?
must be two-phase system with LARGE particles suspended or floccules of small, distinct particles
What are some common gelling agents?
- -xantham gum
- -alginic acid (seaweed)
- -animal/vegetable fat (lard, cocoa butter)
- -bentonite, veegum
- -Pluronic F-127
- -other methylcelluloses
- -carbomer resins
- -colloidal silicon dioxide
- -Polyvinyl alcohol (PVA)
- -mineral oil
- -polyethylene gel
T/F: the continuous phase of most gels is usually aqueous but can also be alcoholic or oleaginous.
What do neutralizers do for a gel?
they thicken the gel after the gelling agent has been dispersed
What are some examples of neutralizers?
- -Sodium hydroxide or Potassium hydroxide if alcohol content is less than 20%
- -Triethanolamine is alcohol is greater than 50%
- -sodium carbonate
What are plasters?
- adhesive masses spread onto the backing of paper, fabric, moleskin or plastic
- provide prolonged contact and effect at the site of application on the skin
- sized to fit area
What are glycerogelatins?
- plastic masses containing 15% gelatin, 4% glycerin, and 35% water, and 10% active drug
- similar to gummy base prep
- warmed and melted prior to application
What is an example of a glycerogelatin?
zinc gelatin for varicose ulcers
T/F: External wounds should be open to the atmosphere/air whenever possible.
True; unless there is an infection or prescribed to cover
T/F: A pharmacist can substitute one cream, ointment, or paste for another.
False; not without doctor's consent
what does supponere mean?
to place "under" the body
What are some advantages of suppositories?
- -avoid irritating the stomach
- -avoid gastric pH/enzymes
- -bypass the liver (partially avoid first pass effect
- -can be used for patients unable or unwilling to swallow
- -fast acting
- -can be used if patient is vomiting
What are factors that affect the absorption of a suppository?
- -lipid-water solubility
- -particle size of drug
- -base selection
- -colonic content
- -circulation route
- -pH and buffering capacity
What symptoms of the rectum might affect absorption of a suppository?
- -rectal tumors
T/F: Rectal fluids are relatively neutral in pH.
What are the 3 main types of suppositories and what are some other types of dosage forms for those areas?
- 1. rectal
- 2. vaginal
- 3. urethral
- -vaginal tablets
- -intrauterine contraceptive sponges
- -intrauterine drug delivery systems
- -ointments, creams
- -aerosol foams
What is the local effect of rectal suppositories?
- relief of hemorrhoids
- relief of constipation
what are some systemic effects of rectal suppositories?
About how long and how much does an adult rectal suppository measure?
How much does a child rectal supp weigh and how long is it?
What type of suppositories are used as a cathartic?
What should a patient first do with PEG or glycerinated gelatin supps before inserting?
moisten with warm water to aid with lubrication and dissolution
T/F: Suppositories can be frozen.
A PEG suppository with how much water should be dipped in water to prevent dehydration of rectal mucosa and stimulate peristalsis?
less than 20% water
What does "pessaire" mean in French?
What is the typical weight of a vaginal suppository?
up to 5 grams, but it can vary
What are the preferred bases to be used for vaginal suppositories?
Are there any systemic uses for a vaginal suppository?
Usually no, but can be progesterone for PMS
What are some local effects of vaginal suppositories?
- combat infections of genitourinary area
- restore vaginal mucosa to a normal state
What are some infections that can occur in the vagina and are treated with vaginal suppositories?
- Trichomonas vaginalis
- Candida albicans
- Haemophilus vaginalis
How do we treat Trichomonas vaginalis?
with a povidone-iodine suppository
How do we treat Candida albicans?
with nystatin, miconazole, clotrimazole, or terconazole suppository
How do we treat Haemophilus vaginalis?
sulfathiazole or sulfacetamide suppository
How do we restore the vaginal mucosa to a normal state?
with an estrogenic substance suppository
What drug can be used to prepare a contraceptive vaginal suppository?
What does "bougie" mean in French?
candle, in reference to a urethral suppository
What is the length of a typical female urethral suppository?
50 mm and 3-6mm in diameter
What is the length of a typical male urethral suppository?
140mm and 3-6 mm diameter
What is the main goal of inserting a urethral suppository?
- to be an antibacterial
- to be an anesthetic
What is Muse?
- a male urethral suppository used to treat erectile dysfunction
What are some characteristics of good suppository bases?
- chemically and physiologically inert
- compatible with many drugs
- stable during storage
- esthetically acceptable
- should melt or dissolve in body fluids
- should allow drug to be released
- have high melting points if using a drug like camphor, menthol, or phenol
What are the 4 main types of suppository bases?
- 1.fatty, oleaginous, or oil soluble bases
- 2. hydrogenated vegetable oils (emulsions)
- 3. water-soluble and water-miscible bases
- 4. miscellaneous bases
What is the most frequently used suppository base?
cocoa butter/theobroma oil
What is another name for cocoa butter?
At what temperature does a cocoa butter supp melt?
Why should cocoa butter be melted slowly in a water bath?
- because if heated to quickly at high heat and then quickly cooling will lead to a metastable crystalline form with much lower melting point
- supp will melt before you can even put it in
When should you add an emulsifier to your cocoa butter suppository?
when you are using water soluble drugs
Which type of drug should you not mix with cocoa butter to make a suppository?
fat-soluble drugs because they will not absorb in the body
What is an example of a fatty, oleaginous, oil soluble base for suppositories?
What are 2 examples of a hydrogenated vegetable oil (emulsion) base for suppositories?
What is fattibase/wecobee?
- supp base made from triglycerides from palm, palm kernel, and coconut oils
- emulsifiers and suspending agents added
- have a slightly higher melting point than cocoa butter
What are 3 examples of water-soluble/water miscible suppository bases?
- glycerinated gelatin
What are water-soluble/water miscible supp bases?
- when mixed with drug, they allow teh drug to dissolve and mix with aqueous body fluids
- can cause local irritation because they can dehydrate the rectal mucosa
What is the most popular water-soluble suppository base?
How are PEG bases made?
with polymers of ethylene oxide + water
T/F: PEG bases dissolve slowly in body fluids and do not melt.
Why do PEG suppositories need to be dispensed in glass or cardboard containers?
because the PEG interacts with polystyrene
What is the molecular weight of a solid, wax-like PEG?
greater than 1000
What is the molecular weight of a liquid PEG?
less than 1000
T/F: You can mix a low molecular weight PEG with a high molecular weight PEG by fusion to obtain a base with a specific consistency.
If you want a drug to be released slowly and you are using a PEG base suppository, should you use a high or a low melting point drug?
higher melting point
What is polybase?
- a water soluble supp base
- preblended homogenous mixture of Tween 80 and PEGs
- does not require mold to be lubricated
- stable at room temp
- can be mixed with water
What is glycerinated gelatin?
- a water soluble supp base
- absorbs water
- causes evacuation
- glycerin will pull water from atmosphere, so need to be stored in a tight container
- made of 70% glycerin, 20% gelatin, 10% water, and drug= RECTAL
- made of 60% gelatin and 20% glycerin=VAGINAL/URETHRAL
Why is a glycerinated gelatin base not recommended for systemic rectal suppositories?
- because of osmotic effect
- because of defecation reflex
T/F: Glycerinated gelatin vaginal and urethral suppositories are easier to insert than ones made with cocoa butter?
What are some miscellaneous supp bases?
- glyceryl monopalmitate
- glyceryl monostearate
- polyoxyl 40 stearate
What are the 2 types of miscellaneous supp bases?
- 1. mix of glycerin + high molecular weight fatty acids
- -fatty acids are: palmitic or stearic acid
- 2. mix of fatty bases with water-soluble emulsions (w/o emulsions)
- -stearates and glycols
What are the 3 methods used to make suppositories?
- hand molding
T/F: Hand molding of a suppository uses heat.
Which base is usually used to do hand molding of a suppository?
What method of suppository making would be used if your substances are insoluble in the suppository base or the medicinal agents are heat sensitive?
What substances can be used as a mold lubricant if you are making a supp with a water-soluble base?
- light mineral oil
- vegetable oil
What substances can be used as a mold lubricant if you are making a supp with an oleaginous base?
T/F: Lubricants are usually not needed for supp molds if they are heated and prepared properly.
Who should make simple syrup?
- Nobody is silly enough to make simple syrup!
What is a syrup?
an aqueous, sweetened, flavored, viscous solution
If a solution has a lot of alcohol in it, what is it then called?
What are the two different types of syrups?
- non-medicated (flavored vehicles)
What are the 3 types of non-medicated syrups?
- 1. Syrup, NF (simple syrup): 85% sucrose in water
- 2. Sucrose based:
- -cherry syrup (acidic medium)
- -chocolate syrup (bitter tasting drugs)
- -orange syrup (source of tartness, acidic medium)
- -raspberry syrup (disguise of sour or salty taste)
- 3. Commercial: both acidic and alcohol free
- -Ora-sweet SF
What are some examples of medicated syrups?
What are some components of syrups?
- water-soluble drug
- solvents: purified water, alcohol in [low]
- sweetening agents
- flavoring agents
- coloring agents
- antifungal/antimicrobial preservatives
What are some ways to prepare a syrup?
- 1. with the aid of a little heat
- 2. agitation
- 3. heat and agitation
- 4. addition of sucrose to a medicated and/or flavored liquid
- 5. percolation
- 6. maceration
Why don't we want to heat artificial sweeteners too much?
- some are destroyed by heat
- will get a different flavor if heated too much
T/F: Sucrose is a disaccharide of glucose + fructose.
Why should you not heat sucrose syrups too much?
- sucrose will be inverted to a mixture of monosaccharides, glucose and fructose
- becomes less sweet
- color turns darker
- more prone to microbial attack
What is an example of a syrup that is made by percolation?
What does "macerare" in maceration mean?
to soak, like a tea bag
What is an elixir?
a clear, sweetened, flavored, hydroalcoholic solution for oral use
What are the two types of elixirs?
- non-medicated: vehicles
T/F: A syrup may or may not have alcohol in it.
T/F: An elixir may or may not have alcohol in it.
What is the alcohol content of Aromatic Elixir, NF?
When making an elixir, how do we prevent it from being cloudy? (want it to be clear)
add water phase very slowly, with continuous stirring to alcohol phase
T/F: when making an elixir the alcohol-soluble and water-soluble components need to be dissolved separately.
What are some solvents used in elixirs?
- purified water
- propylene glycol
What is the alcohol content allowed in an elixir for a child under 6 years old?
What is the alcohol content allowed in an elixir for children 6-12 years old?
What is the alcohol content allowed in an elixir for adults?
How much alcohol in an elixir is considered self-preserving? (no extra preservative needed)
What are 2 methods used to prepare elixirs?
- 1. simple solution with agitation
- 2. mix alcoholic solution with aqueous solution
Why do we add the aqueous phase to the alcohol phase when making an elixir?
because whatever is soluble in water will also be soluble in alcohol so you ensure full dissolution of solids
How should elixirs be stored?
- in tight containers to prevent evaporation of alcohol
- in light resistant containers
- protect from heat
According to USP 23, what is a solution?
a liquid prep that contains one or more chemical substances dissolved (molecularly dispersed) in a suitable solvent or mixture of mutually miscible solvents
T/F: A solution should be clear, have nothing floating on it, and not be saturated.
Where can solutions be used in the body?
- vaginal (douches)
- rectal (enemas)
- otic (aural)
What are some advantages of solutions?
- doses are homogenous
- immediate availability for absorption
- dose is easily adjustable
- can be used for enteral feeding
- good for nursing home patients, incarcerated, psychiatric
- good for patients who can't swallow caps/tabs
What are some disadvantages of solutions?
- less stable than dry form of drug
- potential for microbial contamination
- package is bulky and weighs more
- can have dosage measurement errors
- need a solvent that will allow solubility
- need taste and smelling additives
What are some solutions that are classified by an aqueous type of solvent?
- oral solutions
- aromatic waters
What are some solutions that are classified by a NON-aqueous type of solvent?
- oleaginous solutions
How can we increase the solubility of a solution?
- -heat (but may cause precipitation in some drugs)
- -use a cosolvent (glycerin or propylene glycol, alcohol, benzyl alcohol
- -add salts of an organic compound
- -add inorganic compound (has high water solubility)
What do Diazepam, Taxol and Digoxin solutions all have in common?
they all have limited water-solubility so they require cosolvents like benzyl alcohol, propylene glycol, or alcohol so that they will go through a needle for delivery = SYRINGEABILITY
The solubility of an organic compound depends on ______?
the pH of the solvent
T/F: Weak acids like to dissolve in weak bases.
T/F: Miscibility of liquids is easily predicted.
Can you mix castor oil and mineral oil?
Can you mix cottonseed oil and mineral oil?
Can you mix water and alcohol?
Can you mix glycerin and water?
Can you mix glycerin and alcohol?
Can you mix alcohol and mineral oil?
Can you mix alcohol and castor oil?
yes (but 50/50 only)
T/F: Injectables for human use can have colorants.
False; only for veterinary inj.
What is the #1 solvent used for liquid preps?
What is a pyrogen?
- causes fever and chills
- comes from products of bacteria like lipopolysaccharides
Is Water for Injection, USP, sterile?
usually but not necessarily
Tell me about SWFI.
- It is sterile
- It is pyrogen free
- It comes in manufactured vials
- It should not be injected into anybody!
- It does not need to be sterilized afterward
T/F: Anything that is prepared with water for injection, USP, needs to be terminally sterilized after it is mixed.
Tell me about Bacteriostatic Water for Injection, USP (BWFI).
- It is sterile water with an antimicrobial preservative
- Cannot be used in preps for newborns or elderly because of the preservative is harsh on the liver
- Will have a longer shelf life than SWFI
What is the strength of Acohol, USP? aka ethyl alcohol or ethanol
What is the strength of Dehydrated alcohol, USP?
99.5% (nearly 200 proof)
What is the strength of Diluted Alcohol, NF?
What is the strength of Rubbing alcohol?
70% ethanol + denaturants
What is the strength of Isopropyl Rubbing Alcohol?
What are 2 oils that can be used as solvents due to their less irritating fatty acids?
What are the 3 methods by which purified water can be prepared?
- reverse osmosis
- ionic change
What are glycogenetic sweeteners?
- they are nutritive
- can be converted to energy in the body
What are some glycogenetic sugars?
- sucrose (sugar, agave nectar, fruit)
- dextrose (D-glucose, not L-glucose)
- fructose (levulose from fruits)
What are some glycogenetic non-sugars?
- propylene glycol
- **all are polyols/sugar alcohols
Why do we add sweeteners to solutions?
- to mask flavor of drug and overwhelm the tasting buds
- to make solutions thicker
Which gycogenetic sugar would be recommended for a patient with diabetes?
agave nectar because it transforms to glucose in the body very slowly and has a low glycemic index
What will happen if you heat D-glucose (dextrose) too much?
You will end up with L-glucose, which is salty
T/F: Glycogenetic non-sugars are less sweet, less viscous, and less antimicrobial than glycogenetic sugars.
Which non-sugar has 30% fewer calories than sugar?
What is a non-glycogenetic sweetener?
- has no nutritive value
- is a sugar substitute
- is non-caloric
What are some examples of natural non-glycogenetic sweeteners?
- -hydroxyethyl cellulose
- **all from plants
Which natural sweetener is heat stable and 30 times sweeter than sucrose?
What are some examples of artificial non-glycogenetic sweeteners?
- Acesulfame Potassium
- Sucralose (Splenda)
Which artificial sweetener was banned in 1969 for carcinogenicity and teratogenicity?
- *but still used in Coke Light in Europe
What artificial sweetener has been restricted in its use since 1977 and causes cancer in animals?
saccharin (sweet n low)
What are the 3 metabolites of Aspartame (Equal, NutraSweet)?
- 1. phenylalanine
- 2. aspartic acid
- 3. methanol
Why is phenylalanine bad?
it crosses the blood brain barrier and causes brain damage in people who can't metabolize this amino acid
What does heat-labile mean?
the substance can be warmed up but not baked with or it will be destroyed
What artificial sweetener has some heat stability, is unmetabolized, is 130 times sweeter than sucrose and is structurally similar to saccharin?
Acesulfame Potassium aka Sunett
What artificial sweetener is unmetabolized, heat stable, and 600 times sweeter than sucrose?
Sucralose aka Splenda
What artificial sweetener is an aspartame analog and is 30-60 times sweeter than aspartame, but with decreased amounts of phenylalanine?
What kinds of flavors do children prefer?
What kinds of flavors do adults prefer?
- less sweet
What things do patients expect with respect to flavorants?
- psychogenic balance with color
- immediate flavor ID and development
- acceptable feel in the mouth
- brief aftertaste
- no undesirable sensations
How many taste buds do we have?
What factors contribute to the taste of something?
T/F: Natural flavorings are more expensive than synthetic ones
What weight of salts are salty?
low MW (5,000 or less)
What weight of salts are bitter?
high MW salts (greater than 5,000)
What are the 3 types of flavorants?
- from spices
In an organic compound, what will more -OH groups taste like?
In an organic compound, what will esters, alcohols, and aldehydes taste like?
- will have a volatile odor
For newborns or elderly, what two components should not be added if possible?
- flavoring, but flavoring usually added for elderly
Where do 90% of synthetic colorants come from?
What are some agents with inherent color?
- cupric sulfate
- cyanocobalamine (vit B12)
Why do we use colorants?
- to enhance the appeal of a dosage form
- to reach a psychogenic balance with flavor
How do we select the proper colorant?
- dye chemical stability
- stability of other ingredients
- shelf life
- pH of prep
- water or oil solubility of prep
Which colorants are allowed for external application only?
FD&C Red #2 and #4
Which colorant must be listed on labels of food and is only allowed to be used in small amounts?
FD&C yellow #5
What is the difference between a bacteriocidal and a bacteriostatic?
- cidal= kills bacteria
- static= stops growth or multiplying of bacteria
T/F: Simple syrup, NF, is self preserved.
T/F: 15% of alcohol in an acidic media is self preserved?
T/F: 18% of alcohol in a basic/alkaline medium is self preserved?
T/F: Some flavoring oils and sweeteners have antimicrobial activity.
What are two flavoring oils that have antimicrobial properties?
T/F: It is okay to use preservatives in a prep for a newborn.
_______have a broad spectrum of antimicrobial capabilities so we use them a lot.
T/F: Large volume parenterals contain preservatives.
T/F: Some ophthalmics contain preservatives and some do not.
T/F: Refrigeration stops microbial growth/does not allow it.
False, only slows it down
What is free water?
- water in a prep that is not bound to other molecules
- available for attack
What is the role of free water?
it determines the effective concentration of a preservative required for a given liquid formulation
What are the different types of preservatives?
- 1. alcohols and glycols
- 2. organic acids
- 3. parabens
- 4. mercurial derivatives
- 5. salts of quaternary ammonium bases
- 6. chlorobutanol
Which type of preservative can cause allergies in a lot of people?
What is the most common type of preservative used in parenterals and ophthalmics?
salts of quaternary ammonium bases
What dosage forms are alcohols and glycols usually used for (as preservatives)?
oral and topical
Which preservative is approved for oral use but is not usually used because of its sharp, burning taste?
What are the 4 major alcohol/glycerol type of preservatives?
- ethyl alcohol
- propylene glycol
- benzyl alcohol
What are the 2 most common types of organic acid preservatives?
- benzoic acids, sodium benzoate, potassium benzoates
- sorbic acid, potassium sorbate
Which preservative is highly irritating to the skin?
sorbic acid, potassium sorbate
Which type of preservative is good for rectal, vaginal, and urethral dosage forms?
Which type of preservative is most effective against fungi?
Which type of preservative can be used for all dosage forms except parenterals?
What dosage forms can mercurial derivatives be used for?
What are the 2 most common mercurial derivative preservatives?
- phenylmercuric nitrate (PMN), PMA
What two types of preservatives can be used for both ophthalmics AND parenterals?
- salts of quat. ammonium bases
What are some common salt of quat. ammonium bases preservatives?
- cetylpyridinium chloride (in mouthwash)
- benzethonium chloride
- benzalkonium chloride
What preservative is only stable at an acidic pH?
What preservative should not be used in oral preps because it tastes like camphor?
T/F: All parenterals can be refrigerated.
T/F: Antimicrobial preservatives are ionic and highly active with buffers.
What do buffers do?
maintain ideal pH for drug solubility, stability, and product shelf life
What do stabilizers do?
- maintain drug in solution
- protect the drug in its active form
- keep all components compatible
- prevent degradation of drug or product
What is an example of a stabilizer (very general)?
Why should tinctures be dispensed in small volumes?
because of their high alcohol contents (15-80%)
Are tinctures for topical use or oral use?
What are tinctures?
- solutions with hydroalcoholic or alcoholic vehicle
- may contain dye
- contain a lot of alcohol
- simple solution of chemicals or plant materials
- made by percolation or maceration
What are sprays?
- not aerosols!
- aqueous or oleaginous solutions
- can be gel, cream, or lotion form
- may or may not be sealed
- do not contain a gas
What is a common vaginal solution?
What is a common rectal solution?
What are the two main goals/uses of an enema?
What are the 3 ways to apply ophthalmics to the eye?
- thin ribbon
- insertion of a device for continuous release
What are the only two places on the body that do not provide a systemic effect for drugs?
What does GRAS mean?
Generally recognized as safe
How much lacrimal fluid is in the culdesac of the eye?
How can we increase contact time of a drug with the eye?
- multiple drop therapy
- increase the viscosity
- make a suspension, ointment, cream or gel dosage form
- make an insert
- add on oral or parenteral therapy
Why do we need to have an increased concentration in ophthalmic dosage forms?
because 80% of a 50 microliter dose is lost in tears and nasolacrimal drainage within 5 minutes of administerine the drug
What is the amount of fluid in the eye when it is blinking and not blinking?
- Blinking: 10 microliter
- Not blinking: 30 microliter
What is the #1 type of sterility method used for ophthalmics?
filtration in the hood with a 0.2 micrometer pore size filter
When can a preservative be used in an ophthalmic prep?
- if the corneal membrane is intact
- ir you are making a multi-dose container
What does autoclaving an ophthalmic prep ensure?
that you are killing even viruses since filtration does not get rid of all viruses
At what temp and how long should you autoclave an ophthalmic prep?
121 C for 15 minutes
What ophthalmic products cannot have a preservative in them?
- single use products
- eye washes used in large quantities on burned or abnormal cornea
- preps used during an eye surgery
What are the most common preservatives used for ophthalmics?
- benzalkonium chloride
How can we combat Pseudomonas Aeruginosa since we cannot put a strong enough preservative in an ophthalmic to kill it?
- use more than 1 preservative or
- use a chelating agent like EDTA
What two ingredients can be added with a preservative in an ophthalmic to provide better action?
- chelating agents
What range of isotonicity do we allow in the eye (even though it will not be comfortable)?
- 0.6% -2%
- Normal range would be 0.9%
Why do we need isotonicity in the eye?
- for efficacy
- for safety
- for comfort
Which will exert a greater osmotic pressure? A given volume of an electrolyte solution or a given volume of a non-electrolyte solution?
electrolyte solution will exert a greater osmotic pressure
What makes two liquids isosmotic?
if they have the same osmotic pressure
What makes a liquid isotonic?
when it has the same osmotic pressure as some body fluid
What is the pH of lacrimal fluid?
What are two common buffers used for ophthalmics?
- boric acid (1.9%)
- isotonic phosphate
Why do we want ophthalmics to be thicker if possible?
- because the drug will remain in the culdesac longer
- enhances therapeutic effect
What is the most common thickening agent for ophthalmics?
methylcellulose and its derivatives
What are two factors that reduce bioavailability in the eye?
- binding (due to proteins in eye)
- destruction (due to lysozymes in lacrimal fluid)
How much protein do we have in our tears?
Why is Uveitis bad for our eyes?
because it is a disease that increases ocular protein levels, which is bad because protein binding inhibits drug actions
Do ionized or un-ionized drugs permeate the cornea easier?
un-ionized (lipids, lipid soluble)
What 4 criteria must an ophthalmic solution meet?
- be sterile
- be isotonic
- be aqueous
- be free of particulate matter
Why are ophthalmic suspensions better than solutions?
because they are thicker so there is extended contact for improved drug action
Tell me about the suspensoid in an ophthalmic suspension.
- it is very small and non-irritating to the eye
- agglomeration will not occur during storage
What is a disadvantage of an ophthalmic ointment?
- it causes blurred vision
- cannot be used with contacts
T/F: An ophthalmic ointment must be sterile.
What is the advantage of an ophthalmic ointment over a solution/suspension?
increased ocular contact time of the drug
What are ophthalmic gels designed to do?
extend drug action in the eye
What are two examples of ophthalmic gels?
- Timoptic XE
- Pilocarpine HS
T/F: Ophthalmic gels are more comfortable than ointments.
What are 4 things that ophthalmic preps must have to be effective?
What is the most common ingredient used in making ophthalmic inserts like Ocusert and Lacrisert?
What are all the different dosage forms that can be made for the nose?
- drops (solution)
- spray (solution)
- inhalant (solution)
What are some typical active ingredients found in nasal preps?
- adrenergic agents (decongestants)
- anti-inflammatory agents
- anti-allergic agents
- oxytocin (synthetic)
- insulin, growth hormone, other (occasionally)
What is rhinitis medicamentosa?
- rebound congestion
- instead of getting better, you make it worse because you use drug too much
T/F: Use of decongestants is addictive because of the drug.
False; addiction is to relief
What type of dosage forms can be made for the ear?
What is a cerumenolytic surfactant?
it breaks up and removes excess cerumen
What are some examples of cerumenolytic surfactants?
- hydrogen peroxide
- vegetable oils
- light mineral oil
- triethanolamine polypeptide oleate-condensate
- carbamide peroxide
What do hygroscopic co-solvents do for ear infections?
- reduce moisure in ear
- reduce bacterial growth
- reduce inflammation secretions
What are some hygroscopic co-solvents for the ear?