434 - Midterm 1 Flashcards
Magnesium Oxide
/Carbonate
ADSORBANT
Excipient to keep powders dry
- *ASCORBIC ACID**
- *asc**obyl palmitate, sodium ascorbate
- *ANTIOXIDANT**
- *ASC** the antioxidant
prevents oxidation
SHELLAC** + **GELATIN
COATINGS
Prevent degradation due to oxygen, light, moisture, mask unpalatable taste
(regular coatings)
Starches, calcium salts, lactose, Cellulose
(and other sugars including mannitol and sorbitol)
DILUENTS / FILLER
To add size to very small dosages.
- *SACCHARIN**
- *Mannitol / Sorbitol**
Syrups, oils, saccharin, lactose, mannitol, sorbitol, phenylalanine, xylitol
Flavoring Agents / Sweeteners
Masks bitter flavors, gives sweetness to a preparation.
MAGNESIUM STEARATE
calcium, PEG, glycerin, mineral oil
Lubricant / Anti-adherant
Helps keep ingredients from sticking to each other and to the equipment.
Sodium benzoate
benzoic acid
benzalkonium chloride
cetylepyridinium
PRESERVATIVES
BENZ / CETYL / PHENYL / PHENOL / PARABENS
Prevent growth of bacteria and other pathogens.
Mortar & Pestle
Coarse vs Smooth
•Coarse surface
•Particle size reduction of hard solids
•Emulsion formulation
•Caution – drug loss in mortar
Smooth = All other applications
COMMUNITION
Particle size reduction
Trituration – dry
Levigation – wet
Pulverization by intervention – dissolution and evaporation
for crystalline powders
Mechanical – electric grinder
Capsule Size
OPPOSITE DIRECTION
000 = LARGEST
2/3 = most common human caps
5 = smallest
Sweetener in oral Solutions
Saccharin, USP
0.02% to 0.1% w/w
Oil soluble;
bitter aftertaste
Saccharin Sodium, USP
Sweetener in Oral solutions
0.0075 to 0.6%
Water soluble;
bitter aftertaste
Stoke’s Law
Used to determine the
- *VELOCITY**
- Greater RADIUS = Faster Settling*
- *Rate of settling** can be modified by:
- Decreasing the difference between the density of the solid and liquid*
Increasing the viscosity of the fluid
Viscosity is best controlled by
adding viscosity enhancers or suspending agents
MethylCellulose
SUSPENDING AGENT
HydroPhylic Polymer
Grade number refers to the viscosity of a
2% aqueous solution
The greater the number, the greater the viscosity
4000cps = 4000x thicker than water
Prepared with
Heat & Tituration
Benzalkonium chloride NF
Polysorbate 20 NF (Tween 20)*
Polysorbate 80 NF (Tween 80)*
Sodium lauryl sulfate NF*
Sorbitan monostearate NF* (Span)
Glycerin
Mineral Oil**
Wetting/solubilizing agents
◦Used to lower surface tension between solid particles and liquids
◦Removes air from the powder in order to improve the ability of the powder to mix with the vehicle
Acacia, NF
Bentonite, NF
Bentonite Magma*
Carbomer resins, NF
Carboxymethylcellulose Sodium, USP
Colloidal Silicon Dioxide, NF
Tragacanth, NF
Xanthum Gum*
SUSPENDING AGENTS
Oral Suspension Components
◦Active drug
◦Inactive excipients:
Suspending agent/gelling agent
(surfactant, acacia, tragacanth, others)
Wetting agent
◦Sweetener (syrup)
◦Flavor
◦Color
Principles of Compounding Suspensions
WET HydroPhylic powders with?
HydroPhylic liquid** or **Surfactant
LIKE-LIKE
◦Thoroughly wet powders prior to adding the vehicle
◦Use the minimum amount of wetting agent required to produce the desired product
Principles of Compounding Suspensions
WET HydroPHOBIC powders with?
HydroPHOBIC liquid
LIKE-LIKE
◦Thoroughly wet powders prior to adding the vehicle
◦Use the minimum amount of wetting agent required to produce the desired product
EMULSIONS
3 Major Terms
Flocculation
controlled lacework-like structure of particles held together through weak van der Waals forces.
Creaming
Migration of the droplets of the internal phase to the top or bottom of the emulsion. The migration is caused by the difference in density between the two phases and the direction of the movement depends on whether the internal phase is more or less dense than the continuous or external phase.
Coalescence
The merging of small droplets into larger droplets with eventual complete separation of phases so that the droplets cannot be re-emulsified by simple shaking of the product. With coalescence, the barrier formed by the emulsifying agent is broken or destroyed.
This _irreversible_ coalescence of the droplets is also called cracking.
Desired properties of liquid emulsions
FINE DROPLET SIZES
Porcelain helps breaking up oil globules à uniform
Slow aggregation of droplets and product creaming
Most emulsions will eventually cream
Slow rate of creaming desired
Ease of redispersion when shaken
Aggregation and creaming may occur
Product should be formulated so that the internal phase readily redisperses to give a uniform emulsion when the product is shaken
◦Coalecence should not occur
Oleic Acid
Acacia
Span 80 = Sorbitan Monooleate
Tween 20
EMULSIFYING AGENTS
Different
HLB VALUE
HLB 10+ = HydroPhylic
HLB 10< = HydroPHOBIC
HLB > 10
Ex.
Tween 20
HydroPhylic
emulsifying agents
More WATER SOLUBLE
Forms better OIL in WATER EMULSIONS
O/W
HLB < 10
Ex.
Oleic Acid / Span 80
HydroPHOBIC
emulsifying agents
Better Water in Oil solutions
w/o
- *Emulsions:**
- *Considerations of what determines EMULSION TYPE?**
Emulsifier
Surfactants/emulsifying agents can form either w/o or o/w emulsions
Phase ratio
Ratio of internal phase volume to external phase volume
Order of mixing
The phase being added, usually by portions, tends to be the internal phase
The phase present in the greater concentration tends to be the external phase
If an excessive amount of internal phase is added any of the following may occur:
Internal Phase = Phase that is being ADDED
EX.
O/W –> Adding Oil so OIL = Internal Phase
HydroPhylic
It will all be emulsified and remain as separate droplets
◦The emulsion will coalesce
◦Phase inversion occurs
The external phase becomes the dispersed droplets (internal phase)
Continental method = Dry Gum
4:2:1
Initial emulsion formed with a prescribed ratio of ingredients
4 parts oil : 2 parts water : 1 part emulsifier
DRY = Oil is mixed with the Gum/emulsifier
VVV
As water is added LAST –> PHASE INVERSION
O/W Emulsion
What type of topical base?
White petrolatum
White ointment
Yellow petrolatum
Oleaginous Base
Hydrocarbons
Levigating Agent = Mineral Oil
Occlusive
What type of topical base?
Aquabase
Aquaphor
HydroPhilic Petrolatum
Absorption Base
Hydrocarbon + w/o Surfactant
2nd most Oily
Solid + Oils + Small # of aqueous solustions
Mineral Oil + Low HLB surfactant
What type of topical base?
Eucerin
Hydrocream
Nivea
W/O BASE
Hydrocarbon base + <45% w/w water + w/o Surfactant HLB _<_8
3rd most Oily
Moderate greasiness / occlusion
What type of topical base?
VANISHING CREAM
Hydrophilic Ointment
Dermabase
O/W BASE
Water-removable base
Hydrophobic compounds + water + o/w surfactant
Easy Spread / Washale / Hydrous
Glycerin + HIGH HLB surfactant
What type of topical base?
PEG Ointment
PolyBase
Water-Soluble Base
PEG
Easy spread/wash + not greasy
Glycerin + Propylene Glycol
What type of topical base?
MethylCellulose
Carbomer Gels
HydroPhylic Base = GELS
Methylcellulose or Carbomer Dispersion
>95% water content
Glycerin + High HLB Surfactant
Excipients
In Semisolid Dosage Forms
Stiffening Agents
Waxes w/ HIGH melting points
Blend into oleaginous bases to ↑viscosity, uses heat
Emulsifying Agents
- *Humectants**
- decrease the EVAP rate of water*
- *Preservatives**
- if there is WATER –> NEED THIS*
Absorption Enhancers
for TDDD
Ointment Preparation
What to Levigate the solid material with if…?
OIL = EXTERNAL PHASE
MINERAL OIL
Levigate the solid material in a vehicle in which it is INSOLUBLE WITH
to make a smooth dispersion
External Phase = Most used base
Ointment Preparation
What to Levigate the solid material with if…?
WATER = EXTERNAL PHASE
GLYCERIN
Levigate the solid material in a vehicle in which it is INSOLUBLE WITH
to make a smooth dispersion
External Phase = Most used base
Ointment Preparation
FUSION
all or some components of the ointment are
combined by being MELTED TOGETHER
&
Cooled w/ constant stirring –> CONGEALED
Glass Beaker or Porcelain Evap Dish
Materials w/ LOWEST Melting points –> added LAST
What type of Semisolid Dosage Form?
- *either**:
- *W/O emulsion** or O/W Emulsion
After applying –> water EVAPORATES
leaving a thin residue film of the oleaginous component
applied to:
Moist / Weeping Lesions
CREAMS
Cream Preparations
Incorporation into existing cream/base
titurate –> rubber spatula to remove from M&P –> ointment slab
- *Fusion Method**
- *oil soluble + Water soluble** –> into SEPERATE BEAKERS
Both phases heated ABOVE MP of highest MP component
remove both from heat then ADD:
AQUEOUS PHASE –> OIL PHASE
What type of Gel?
uniform distribution of gelling agent & Liquid
with no apparent boundaries
Gelling Agents = methylcellulose / tragacanth
SINGLE-PHASE GEL
What type of Gel?
consists of floccules of small distinct particles
often referred to as: MAGMA
Gelling Agents = methylcellulose / tragacanth
TWO-PHASE GELS
Suppository Bases
Oleaginous Fatty Base
MOST FREQUENTLY USED BASE
- *Cocoa Butter**
- low melting point* –> needs room temp / fridge
Hydrogenous Veggie Oils
palm / coconut oils
FattiBase** / **Witepsol** / **Fatty Blend
Suppository Bases
Water-Soluble Bases
Glycerinated Gelatin
70 parts glycerin / 20 parts gelatin / 10 parts water
does NOT melt –> DISSOLVES
can adsorb moisture
- *Polyethylene Glycol = PEG**
- does NOT melt* @ body temp –> DISSOLVED into BODY’s FLUIDS
- slower release of meds from the base*
Suppository Preparation
Lubrication for Water-Soluble Base?
OPPOSITE OF THE BASE
MINERAL OIL LUBRICANT
for water-soluble base
use minimal lubricant
excessive lube –> pools / misshapes suppositories
Suppository Preparation
Lubrication for Oil-Soluble Base?
OPPOSITE OF THE BASE
GLYCERIN or PEG lubricant
for oil-soluble base
use minimal lubricant
excessive lube –> pools / misshapes suppositories
Suppository Preparation
Levigate drug with what?
for Water-Soluble Base
- *GLYCERIN or PEG LUBRICANT**
- *Levigate with wetting agent = same property as base!**
Preparation:
Tituration of drug into uniform/small partical
Drug is mixed directly into base OR wetted b4 incorperation
Suppository Preparation
Levigate drug with what?
for Oil-Soluble Base
- *MINERAL OIL LUBRICANT**
- *Levigate with wetting agent = same property as base!**
Preparation:
Tituration of drug into uniform/small partical
Drug is mixed directly into base OR wetted b4 incorperation
What type of Troche?
Sugar + Carbs
corn syrup / water / drug
Smooth Surface texture
HIGH TEMP to prepare
154-160 degrees –> need to monitor closely
HARD TROCHES
What type of Troche?
PEGs + Acacia
drug / sugar / wax / various PEG’s
Flavored & colored
Slowly Dissolved in mouth or Chewed
SOFT TROCHES
pastilles
What type of Troche?
formulated with a:
GELATIN BASE = Jello
drug/gelatin / glycerin / water
Highly Flavored
CHEWABLE TROCHES
gummies
Sterile BUD - 797
CATEGORY 1
CAT 1 = Segregated Compounding Area
dirtier than cat 2
< 12 Hours @ Room temp
<24 hours @ Refridgeration
Sterile BUD - 797
Category 2
EVERYTHING IN COMPOUNDING HOOD/AREA
Must follow manufacturer’s guidelines - if BUD is shorter
Made from 1+ Non-sterile Component:
1 - 4 - 45 days
ONLY STERILE starting products:
4 - 9 - 45 days
Non-Sterile BUDs 795
ROOM TEMP
Solids = 180 days
Non-Aqueous (suppositories, ointments) = 90 days
Preserved Aqueous = 30 days
Refrigerator
Non-preserved Aqueous = 14 days
Suspensions / emulsions / gels / creams /sprays
