pharmaceutics exam 2 Flashcards
what is a capsule?
what is the active ingredient and where is it in reference to the capsule
what comes into play and where
“ A solid dosage form in which medicinal agents and inert substances (like excipients) are enclosed within a small shell of gelatin”
the active ingredient in powder surrounded by a capsule
excipient comes into play
what is made available when a patient is unable to swallow an intact solid dosage form like a capsule what can be given
chewable tablet, instant dissolving tablets, oral liquids, or suppositories are made available
capsules
Promote better patient compliance by being:
Capsules as such may not be filled
with liquids
what may the liquids be mixed with
- Solid dosage forms
- Medication is protected
- Easier storage and transport
Promote better patient compliance by being:
- Tasteless
- Easy to dose
- Capsules of specific designs provide
modified release
- Capsules as such may not be filled
with liquids
Capsules containing liquids must be sealed (requires industrial conditions)
The liquid may be mixed with an inert absorbent. The resultant solid mixture may be placed in capsules
Capsule forms
what is it filled with
what is its mold?
what are empty capsules often used for
what different sizes does it come in/what is the size from largest to smallest
is it usually concealed or open
Liquid-filled gelatin capsule
Capsule mold
Gelatin capsule- Empty capsule often used for
Extemporaneous compounding
of prescriptions
- come in different sizes (000 large, 5 small)
- usually concealed
what device do you use to ensure the correct filling of capsules?
what are the components of process?
use a torbial torsian balance
with this, you have an empty capsule on one side and another capsule of the same kind on the other side with the weight that you want the empty capsule to be in
let’s say that you have a 2g weight with the empty capsule on one and the empty capsule on the other side
the side with the 2g is heavier and you need to fill the empty capsule on the other side with 2g of substance in order to balance the scale
The formulation must be 2g otherwise It wouldn’t be accurate.
To compensate for the weight of the capsule being filled, the same capsule must be placed on the other side of the balance
How are capsules administered?
enteric coated
- what are they designed to do
extended released dosage forms
- what are they designed to do
what is the release of capsules based on
Enteric-coated:
– These are designed to
pass through the stomach
for drug release and
absorption in the intestine
Extended Release Dosage Forms:
These are designed to provide the release of the medication for an extended amount of time
what is the release of capsules based on - based on the coating outside of the capsule
Hard Gelatin Capsules
what is the empty capsule shell made of
how would you describe the capsule shell?
what description of capsules makes for higher patient compliance
Used to manufacture most of the
commercially available medicated capsules
Empty capsule shell made from:
–Gelatin, sugar and water
–They are clear, colorless, and essentially tasteless (want!)
–Most contain colorants & opaquants to make distinctive–for patient compliance
hard gelatin capsules Consist of two parts,
how is this dosage form intended to be used?
The content of capsules should be _______ in food or liquids only with the _______ of the _______
The base or body, which is longer and has a smaller diameter
The cap is designated to slide over the base portion and form a snug seal
This dosage form is intended to be swallowed whole.
The content of capsules should be opened and administered in food or liquids only with the concurrence of the pharmacist
Characteristics of Hard Gelatin Capsules
where is gelatin soluble
because gelatin is a protein, how is it digested?
what happens when gelatin is absorbed
how are most colored and made opaque, using what excipients
where does gelatin cycle through
Gelatin is soluble in hot water and in warm gastric fluids
Given that gelatin is a protein it is digested by proteolytic enzymes and absorbed
When gelatin dissolves it exposes its medicinal contents to the gastric (or intestinal) bodily fluids
Most are colored with FD&C and D&C dyes (colorants) and made opaque by adding titanium dioxide (opaquant).
gelatin cycles through the body
Where is the gelatin derived from to make capsules?
Gelatin is obtained by the partial hydrolysis of collagen obtained from
skin,
white connective tissue, and
bones of animals
While stable in air, gelatin is subject to microbial decomposition when moist–so needs preservative excipients
Hard capsules: contain between 13-16% moisture, but poor storage conditions can increase this level. Not good!
Avoid moisture in gelatin capsules, How?
what will moisture affect
what is used to protect against the absorption of atmospheric moisture
what are examples of dessicant materials
what must you leave inside
The moisture will affect hydroscopic agents (absorb moistrue from the air) in many capsules, therefore, small desiccant materials are used to protect against the absorption of atmospheric moisture.
Desiccant materials:
Dried silica gel, clay, and activated carbon
leave desiccant inside
Manufacturing hard gelatin capsule shells
capsule size
Capsule size: The sizes may vary but always determined by the amount of material to be incorporated
For human use: 000 (the largest) to 5 (the smallest) are commercially available.
There are 8 actual sizes [000,00,0,1,2,3,4 and 5]
Numerical designations are arbitrary and do not indicate the capsule’s capacity—000 is not the smallest but the largest
A pharmacist may compound capsules of a single medicinal agent, or combination of agents at the precise dosage prescribed for the patient
Developing the formulation
goal
what is the goal
what in what is important
lack in homogenity could result in what
what are ofetn used to produce the proper capsule fill volume and what are examples
Goal: Prepare a capsule with accurate dosage, good bioavailability, ease of filling and production, stability, and elegance.
Care in blending is important especially with low-dose drugs.
Lack of homogeneity could result in significant therapeutic consequences
Diluents or fillers are,
Often used to produce the proper capsule fill volume.
Offer bulk and cohesion
Examples:
Lactose, microcrystalline cellulose and starch
mixing only: glass mortar
Filling hard capsule shells
what method is used
what do you start with
what is placed on a sheet of paper
how to do the punch method
Pharmacists use “punch” method
Start with exact number of capsules to be filled
Powder to be encapsulated placed on sheet of paper, clean glass, or porcelain plate
Using a spatula powder is formed into a cake
Empty capsule body is held between the thumb and forefinger and “punched” vertically into the powder cake repeatedly until filled.
if making 10, make 11 to give room for error
Capsule sealing
what can capsules be sealed with
how can a capsule be sealed and what occurs during this
how many capsules can Industrial capsule sealing machines make
Capsules can be sealed with colored band of gelatin (KAPSEALS, Parker Davis)
Capsules can be sealed through a heat welding process that fuses the capsule cap to the body.
Industrial capsule sealing machines:
Can produce 60,000 to 150,000 gelatin banded, heat welded, or thermally coupled capsules per/hour
Cleaning and polishing capsules
Small amounts of powder may adhere to the outside of capsules after filling
Must remove before packaging and dispensing, wipe with clean gauze or cloth
On large scale cleaning, a vacuum can remove extraneous materials
Soft Gelatin Capsules
Pharmaceutically elegant and easily swallowed
Prepared to contain liquid, paste & dry fills
Liquids that can easily migrate through the capsule shell cannot be encapsulated into soft gelatin capsules.
When not to be used?:
When water content is > 5%
When low molecular weight water-soluble and organic compounds are employed such as,
alcohols, ketones, amines, and esters.
*Preservatives such as methylparaben and/or propylparaben used to retard microbial growth
Compendial requirements for capsules
Things added to preparations to facilitate their manufacture can only be used if,
Harmless (in the quantities used)
Do not exceed the minimum amounts required to provide their intended effect, if between 50mg or 10mg choose 10mg
Do not impair the bioavailability of the product
Do not interfere with assays to evaluate dosage form
Capsule within a capsule
The active ingredients can be separated from the other ingredients in a formulation.
In this case, you may fill a small capsule (i.e., No.5) with one powder, and then place that capsule along with the remaining ingredients inside a larger capsule.
The inside capsule should not be visible through the large capsule
used if contents will form eutectic mixtures if mixed so keep them separately so that it will not!
do not give if the internal capsule is seen if so, add powder on the walls of the cap. and put other cap inside
Tablet within a capsule
what can be placed in a capsule
Small commercially available tablets can be placed inside a capsule of a suitable size.
Small quantity of the additional powder should be deposited in the base before and after adding the tablet.
Similar to capsule inside capsule, tablet should not be visible through the filled capsule
Tablets
how often is it used in the commercial dosage form?
why is it liked so much
commercially available tablets can be made fast
how are tablets made
Most frequently prescribed commercial dosage form
Stable, elegant, and effective when made right
Commercially available tablets can be made at a rate of thousands per minute
Tablets are made primarily by compression with a limited number by molding
Tablets
size
grooved
Often vary in size,
shape, hardness, thickness
and in their ability to dissolve
In fluids.
These tablets are grooved
Are therefore intended
to be broken into two parts.
Why? Offers flexibility
Patients can swallow
them easily or use in divided
doses
they are scored so they can be broken and have some now or later
Definitions: types of tablets to know
Compressed tablets (C.T.):
Multiple compressed tablets (M.C.T.):
Sugar-coated tablets (S.C.T):
Film-coated tablets (F.C.T.):
Gelatin-coated tablets:
Enteric-coated tablets (E.C.T.):
Buccal or sublingual tablets:
Compressed tablets (C.T.):
Multiple compressed tablets (M.C.T.):
Sugar-coated tablets (S.C.T):
Film-coated tablets (F.C.T.):
Gelatin-coated tablets:
Enteric-coated tablets (E.C.T.):
Buccal or sublingual tablets:
Types of tablets continued
Instant Disintegrating/ Dissolving tablets
Extended Release Tablets (E.R.)
Vaginal Tablets:
Compressed tablets (C.T.)
Diluents or Fillers: Add bulk to prepare a certain size
Binder or Adhesives: Promote adhesion of the particles of the formulation
Disintegrants: Promotes breakup of tablets/drug availability
Antiadherents/ glidants/ or lubricating agents
Miscellaneous Adjuncts: Colorants and flavorants to enhance overall appearance
Multiple Compressed Tablets (M.C.T)
why stage at all
More than a single compression
Produces multiple-layered tablets or a tablet within a tablet
Each layer may contain diff. medicinal agents. Why?
Separation may be required to avoid chemical and physical incompatibility
Staged drug release
The general appearance of the multiple-layered tablet
core has an active ingredient/drug substance
has a compressed layer also has an active drug
why stage at all: extended released, drug bioavailable, MEC will differ if not staged
Sugarcoated tablets (S.C.T)
Compressed tablet can be covered with a colored or an uncolored sugar layer
The coating is water-soluble
The coating is quickly dissolved after swallowing
The coating protects the enclosed drug from the environment
The coating enhances the general appearance of tablets and permits imprinting of identifying manufacturer’s info.
Disadvantages to sugarcoating tablets are,
the time and expertise required in the coating process,
and the increase in size, weight, and shipping costs.
Maybe 50% larger and heavier than uncoated tablets (cause it’s bigger)
cannot be SCT and ECT, pick one!
Film-coated Tablets (F.C.T)
what is it coated with and what is it like
it is usually colored
what makes it better than sugar coatings
what is it designed to do
These compressed tablets are coated with a thin layer of a polymer capable of forming a skin-like film over the tablet
Usually colored ( for patient compliance)
More durable, less bulky, and less time-consuming to apply than sugar-coatings.
Designed to rupture and expose the core tablet at the desired location within the gastrointestinal tract–absorption other than standard sites; more options
all coated: what is the reason for coated
Gelatin-coated tablets
what is its abbreviation?
what does it look like
what does it facilitate
GElCAP,
Capsule-shaped compressed tablets
Facilitates swallowing and compared to unsealed capsules, gelatin tablets are more tamper-evident
Enteric-coated tablets (E.C.T)
Buccal and sublingual
what is the shape?
what is the intent/where does it need to be dissolved?
what is this an alternative for
what are buccal tablets designed for
what are SL tablets designed for
what does buccal and sublingual mean
what do these two drugs protect from
ECT:
Have delayed release characteristics
* Designed to pass unchanged through stomach intestines where the tablets disintegrate and allow drug dissolution.
* Mainly used when by-passing
the stomach to improve drug absorption
These are flat, oval tablets intended to be dissolved in the buccal pouch, or beneath the tongue through absorption through the oral mucosa
An alternative for drugs that are poorly absorbed from the G.I. Tract
Buccal tablets are designed to erode slowly
Sublingual tablets designed to provide rapid-release
Buccal: In the direction of the cheek
Sublingual: Below or beneath the tongue
protect drugs that are sensitive to gastric pH
Buccal drug delivery
must it remain in place?
what can be said about its taste? and why
what should the drug not do to the teeth
buccal:
sublingual:
The dosage form must remain in place
Total area of absorption is low compared to other routes- 100 to 170 cm2
Taste must be bland, or not acceptable for use
must also be a non-irritant
Drugs should not discolor or erode teeth
buccal: cheek
sublingual: below the tongue
Sublingual
Lining of the epithelium is keratinized for buccal and sublingual, but the epithelium for sublingual is thinner.
What does this tell us about drug absorption?-so drugs absorb faster for SL than buccal
layer that dosage form comes into contact with
Chewable Tablets
what base does it have and what is it colored with
what happens when it. is chewed or allowed to dissolve
who is it ideal for
when is it best used
why drink water after?
Have a creamy base usually of specially flavored and colored mannitol
Rapid disintegration when chewed or allowed to dissolve in mouth
Ideally suited for children and adults who have difficulty swallowing solid dosage forms.
use if difficulty to swallow
make sure active drug not get in teeth- so drink water
Molded Tablets (M.T.)
how may Tablet triturates (TT) be prepared
what is the appearance like
what is usually its diluent
what is it designed for
what can pharmacists insert inside to provide what
what else can they add
what should color match
Tablet triturates (TT) may be prepared by compression and by molding.
In terms of appearance very soft and soluble
Diluent: Lactose and Sucrose usually
Designed for rapid dissolution
Pharmacists may insert TT inside a capsule or dissolve it in liquids to provide accurate amounts of potent drugs.
add color and flavorant
red color should not taste like chocolate
orange. should not taste be like mint
Vaginal Tablets
Also called vaginal inserts
Uncoated and bullet or ovoid-shaped tablets
Inserted in vagina for localized effects
–Antibacterials for the treatment of Vaginitis caused by Hemophilus vaginalis or
–Antifungal for treatment of vulvo vaginitis candidiasis caused by Candida albicans and related species
not for systemic effects (like headache or neck pain)
the effect of density on gastric distribution
what does the absence of food effect
light objects float on gastric contents (food) if there is food/food is heavy
heavy objects fall to the base of greater curvature
The absence of food affects the med. will be made available –based on the meal
physiological pharmaceutics
meal makes a difference in what
on an empty stomach, what happens faster to ensure, and what does it result in
food has an impact on what
after breakfast, snack, lunch, snack, dinner:
meal makes a difference to when the med is absorbed
on an empty stomach: there is faster gastric emptying of the stomach and the drug will be absorbed faster
food has an impact on disintegrating tablet
after breakfast, snack, lunch, snack, dinner: gastric emptying takes a lot and the drug is not absorbed as fast
the effect of time of day on the route of gastric emptying
8am vs 8pm
8 am: less time it takes for gastric emptying to occur, there are fewer solids that remain in the stomach so gastric emptying is faster, and thus drug absorption is faster
8 pm: The more time it takes for gastric emptying to occur, there are more solids remain the stomach so gastric emptying is slow and thus drug absorption is slower
which of the following is used to improve flow properties of powder mic
colloidal silica
acacia
bentonite
A & B
A, B & C
colloidal silica
Ointments, Creams, and Gels
“Ointments, creams and gels are semisolid dosage forms intended for topical application”
Unmedicated ointments:
—Protectants (covers layer of skin, P), emollients (flexible & pliable, E), lubricants (where there is a lot friction, L)
Local or systemic absorption:
–Dermatologic applications treat the skin
Application sites include,
—Skin, nose, surface of eye, vagina or rectum
Ointment Bases
As classified by USP
Oleaginous bases = more fatty at top and more watery as you go down
Absorption bases- mostly fatty but has a little more water than oleaginous which has no water
Water-removable bases- water can remove it
Water-soluble bases = more water and more fatty as you go down, water can remove it
oleaginous: at the top is oleaginous, as you go down, fat decreases
100% oleaginous cannot be hydrophilic too
Oleaginous (hydrocarbon) bases
Application: skin use
Have an emollient effect, protecting against moisture escape
Effective occlusive dressings
One application for an extended
period without drying out
It does not wash off easily
–Petrolatum, USP
–White Petrolatum, USP
–Yellow Ointment, USP
–White Ointment, USP (see textbook)
Petrolatum, USP
Purified mixture of semisolid hydrocarbons obtained from petrolatum.
Color ranges from yellowish to amber
—-Melts at 38oC to 60oC because body temp. is 37*C
Used alone or in combination with other agents as an ointment base
Known as yellow petrolatum and petroleum jelly
—Vaseline (Chesbrough-Ponds).
Petrolatum, USP
vaseline, which is yellow in color
amber
White Petrolatum, USP
Decolorized purified mixture of semisolid hydrocarbons from petroleum
Lighter color compared to yellow petrolatum- Pharmacists prefer this variety
White petrolatum (White Petroleum Jelly)
Commercial product
—White vaseline (Chesebrough-Ponds)
–Product is all the way to the top so the cover is very close
–This product implies: it looks like this and is solid from top to bottom, but there could be less in there. But you could have more because we can get rid of air pockets. All depends on the drug product
Yellow Ointment, USP
is it prepared
Purified wax derived from the honeycomb of bee Apis mellifera.
How prepared?
-Melt yellow wax in a water bath (adding petrolatum until uniform mixture)
-Cool and stir
-The viscosity of yellow ointment is greater than plain petrolatum- viscosity is the reason why we have variety and why we want it to be a part of the product
Absorption Bases
Why are absorption bases not easily washed from the skin’s surface???
Type I: permit the incorporation of aqueous solutions, producing water-in-oil (w/o) emulsions (e.g., hydrophilic petrolatum*)
Type II: water-in-oil (w/o) that permits additional aqueous solutions (e.g., lanolin).
Useful for incorporating small amounts of aqueous solutions into hydrocarbon bases. How?
—By incorporating aqueous solution into the absorption base, and then incorporating the mixture into the hydrocarbon base.
Why are absorption bases not easily washed from the skin’s surface??? Because the oil absorbs onto the skin
Absorption bases (continued)
Lanolin, USP
-Obtained from sheep wool
-Cleaned, deodorized (otherwise it would smell) and decolorized
-No more than 0.25% water– do not need too much water
-Additional water may be added by mixing
Water-Removal Bases
These are oil-in-water (O/W) emulsions that closely resemble creams.
May be diluted with water (aqueous phase)
May absorb serous discharges
-Why are they referred to as water-washable bases?
-E.g., Hydrophilic Ointment, USP
Water-Removable Bases (continued)
Hydrophilic Ointment, USP (NOT OLEAGINOUS)
Ingredient Amount (grams) Methylparaben 0.25 Propylparaben 0.15 Sodium lauryl sulfate 10.00 Propylene glycol 120.00 Stearyl alcohol 250.00 White petrolatum 250.00 Purified water 370.00
Water-Soluble Bases
Water-soluble bases do not contain oleaginous components (aka~ greaseless)
Soften with the addition of water, will compromise dosage form, no need to add more water
Large amounts of aqueous solutions are not effectively incorporated in these bases
Normally used for the incorporation of solid substances
Polyethylene Glycol Ointment, NF
PEG 3350 400g
PEG 400 600g
PEG <600 Clear, colorless
PEG >600 ,<1000 Semisolid
PEG 1000 Wax-like
How is a base selected?
What should a Pharmacist consider?
Desired release rate of drug from the ointment base?
Desirability of topical or percutaneous drug absorption
Stability of drug in the ointment base
Effect (if any) the drug might have on characteristics of ointment base
Desire for a base to be easily removed with water
Characteristics of the surface to which the base is applied
The base providing the best combination of most desired attributes should be used
Good to know
Creams, applied to weeping or oozing surfaces
Lotions, usually applied to where friction may occur (under arm pits, thighs)
Ointments, applied to dry and scaly skin surfaces
Preparation of ointments (Incorporation of Solids)
Mix component until uniform mixture
Mortar and pestle
Spatula and ointment slab or parchment paper
Incorporation of solids
Use stainless steel spatula except when ingredients react with the stainless steel material (i.e., iodine). A Rubber spatula can replace stainless steel in this case – 2 options:
Thorough rubbing and working of the components together on solid surface until smooth and make preparation uniform.
Now separate freshly prepared base from the fine powder components used in the previous mixing step.
Add small amount of each together and mix until uniform.
Continue until all powder and base are combined and uniformly blended.
Levigation is often used to reduce powder particle size to reduce grittiness prior to incorporation of the solid material into the base.
For the selection of levigating agents.
Levigating agents should be physically and chemically compatible with drug and base.
Mineral oil is used for when oil is the external phase,
Glycerin is used when water is the external phase.
Preparation of ointments (Incorporation of liquids)
For incorporation of liquids…consider the capacity of ointment base
Note difference between oleaginous –vs- hydrophilic ointment
How to incorporate liquids into hydrophobic base?
Add solution to minimum amount of hydrophilic base, and then
Add this freshly prepared mixture to the hydrophobic base.
Small volumes of alcoholic solutions can be added to oleaginous vehicles or emulsions with ease. For example,
Natural balsams (i.e Peru balsams)
Preparation of ointments (Fusion method)
By this method, “all or some of the components of an ointment are combined by being melted together and cooled with constant stirring until congealed”
Main methods of fusion:
Heat-sensitive or volatile components are added when the temperature of mixture is low enough not to cause decomposition or volatilization.
In general, components having the highest melting points are heated to the lowest required temperature to produce a melt. Think of temp.
Two Alternative methods:
Melt the component with the lowest melting point first, followed by the addition of the remaining components in order of their melting points.
2) Melt all components simultaneously, increasing the temperature only as needed
Compendial Requirements
Microbial content-
Topical applications are not required to be sterile, but antimicrobial action is a must. Why?
Water content is an issue.
Staphylococcus aureus often found in dermatologic preparations
USP chapter titled, “Microbiological Attributes of Non-sterile Pharmaceutical Products,”
Deals with environmental control and application of good manufacturing practices to minimize both the type and the number of microorganisms in unsterilized pharmaceutical products.
USP states certain products should be tested routinely, these are:
Rectal,
Urethral, or
Vaginal
Due to the presence of Yeast and Molds at the site of application
General information for packaging semisolid preparations
Topical dermatologic preparations-
packaged in either jars, tubes or syringes
Ophthalmic, nasal, vaginal and rectal preparations-
—packaged in tubes or syringes
Packaging, Storage and Labeling
Large mouth containers or metal or plastic tubes
Store in cool place in sealed containers
Opaque or light sensitive containers used when necessary
Labels (for ointments, creams) include type of base (water soluble, water insoluble)
Creams
“Semisolid preparations containing one or more drug agents dissolved or dispersed in W/O or O/W emulsion or another water-washable base.”
Used topically, rectally and vaginally
—Generally when creams evaporate a thin residue film consisting of stearic acid (or other oleaginous components) is left behind.
Preferred over ointments by patients and pharmacists since they are easily removed
–Still, both options are generally made available.
What makes each of the following different from the rest?
ointments
Creams
Gels
Pastes
Plasters
Glycerogelatins
Creams
Gels
Pastes
Plasters
Glycerogelatins
Gels
“Semisolid systems consisting of dispersions of small or large molecules in an aqueous liquid, rendered jellylike by the addition of a gelling agent.”
Gelling agent- Carbomers (high MW, water-soluble polymers)
—Can be prepared to be used with various routes, including skin, eye, nose, vagina and rectum
The polymeric composition of Carbomers determines their viscosity.
NF contains monographs of 6, they are 910, 934, 934P, 940*, 941 and 1342.
Used as gelling agents at 0.5% to 2.0% in water
* 940 has the highest viscosity
Gels = Jellies
Carbomer: of the 5 circles, that they do not come together and aggregate, if they do then there will have inconsistent dosing of the drug
Should always be the same, little circles do not come together and do not aggregate
Cannot make a gel without a carbomer; must have a gelling agent
940* has the highest viscosity
Do not need much of it
0.5% vs 2.0% which one Is the most valuable if they both do the same job: want 0.5% is the minimum dose to do the job, ideally you do not want to add anything
Pastes
“Semisolid preparations intended for application to skin. They contain more solid material compared to ointments (~25%).This makes them a little stiffer.”
-Used to absorb serous secretions, remaining in place after application.
A portion of base is softened prior to incorporating the solids.
-A portion of the base is used rather than a liquid because the liquid will soften the base.
Plasters
“Solid or semisolid adhesive masses spread on the backing of paper, fabric, moleskin or plastic.”
-Adhesive tape- Adhesive plaster are used
Provide prolonged contact at the site.
–Unmedicated variety: provide protection or mechanical support at the application site
–Medicated variety: Concentration of salicylic acid used in commercial plasters (range from 10-40%) for the treatment of corns of feet.
Examples of other plaster products
hansaplast
corn removal plaster
Glycerogelatins
Plastic masses consisting of the following,
gelatin 15%
glycerin 40%
water 35%
medicinal substance 10% (i.e., zinc oxide)
Melted and cooled to just above body temperature before being applied to affected area.
Fine brush is used to apply the material, and is generally covered with bandage after hardening
Applied to skin for long-term.
Currently, zinc gelatin is used to treat varicose ulcers (aka~ Zing gelatin boot).
General Features
Features and use of,
Ophthalmic Ointments and Gels
Nasal Preparations
Dermatologic Preparations
Ophthalmic Ointments
Major route of drug transport in the eye is by simple diffusion via the cornea
If not efficient, secondary routes are conjunctiva and sclera.
Three layered structure of cornea
Lipophilic epithelial layer
Hydrophilic stromal layer
Less Lipophilic endothelial layer
on inside (inner layer)
USP sterility tests
Special considerations required- steam sterilization is ineffective because cannot penetrate the ointment base.
Dry heat can sterilize but too harsh. So end stage sterilization is not commonly practiced.
—–Instead, aseptic techniques are used when each component is added, including weighing of the ingredients.
Approved antimicrobial preservatives include,
Methylparaben, (0.05%)
Propylparaben, (0.01%)
Benzalkonium chloride, (0.008%)
All very small
Nasal Ointments
For nasal delivery ointments and gels are used.
Nasal passage is lined with thin layer of mucus produced by epithelial mucus glands.
-Ciliated epithelium assists with mucus movement
-Local effects is the primary treatment approach (i.e., nasal decongestants).
-Vascular region of the nasal passage does enable general circulation, so systemic absorption does occur.
-Can be used to deliver insulin, vaccines, polypeptides & proteins.
Delivered drugs to brain
Can use for local and systemic
Dermatologic preparations
Drug should both penetrate and be retained in the skin for a specified period
Factors affecting drug penetration include,
-Physicochemical properties of the drug
-Characteristics of the vehicle
-Concentration of drug in the vehicle
-Oil-water partition coefficient (PC)
-And general condition of the skin
The skin (like in transdermal delivery systems- TDDS) acts as a natural barrier controlling the rate and extent to which drugs can penetrate it.
However, unlike with TDDS, the therapeutic drug concentration delivered by a dermatologic preparation is not known. So, more qualitative measures are used.
Transdermal system vs ointment: ointment can retain drug substance; skin layer, temp. PC all affects how drug passes through the skin
Productt + the skin
Skin acts as barrier
Rate limitng: where absorption is the slowest
how to use derm. preps
For general use,
The patient must thoroughly clean the affected area with soap and water
Dry the area with clean soft cloth
Thin layer of medication is applied to skin area, and spread evenly.
Typically 1 to 3 mg of ointment or cream is applied per square centimeter of skin – thin layer
Area of application should remain uncovered unless otherwise stated
Clean hands immediately following use
What should a Pharmacist say to a patient?
Instruct patient of proper method of administration
Explain the frequency and duration of use
Any special warnings,
—For e.g., how should it be used during pregnancy?
Therapeutic goals and outcomes
Signs of an adverse response, and what to do if something goes wrong
When should treatment be discontinued?
Patient Counseling PointsFor all Ointments, Creams, Gels
Only a thin film should be applied
Unless otherwise instructed, remove a sufficient quantity from container, apply it, and gently rub into the affected area
Use a protective pad to protect area from being removed from the clothing
Use of lotions and creams should be avoided
Do not rub eyes or touch mouth during handling of application
If patient exhibits sensitivity or intolerance contact pharmacist or physician
