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OINTMENTS, CREAMS, AND GELS

OINTMENTS
OINTMENT BASES:
Oleaginous bases
Absorption bases
Water removable bases
Water soluble bases

Factors of Selecting Ointment Bases:


Physiochemical properties of
medicaments as stability in the base or
influence on consistency
Patients condition
Intended site of application
Characteristics of various vehicles
available
Oleaginous Bases
Hydrocarbon bases
Water-free
aqueous
preparations
may
be
incorporated in small amounts and with
some difficulty
Uses:
Emollient effect (not intended for
penetration into the skin)

Petrolatum, USP
Petroleum
jelly
,
Yellow
Petrolatum
Purified
mixture
of
semisolid
hydrocarbon obtained from petroleum
Yellowish to light amber
Insoluble in water
Widely used in cosmetic skin care
Devoid in taste and smell when pure
White Petroleum, USP
White Petroleum Jelly
Purified
mixture
of
semisolid
hydrocarbons from petroleum that has
been wholly or nearly decolorized
Lighter in color
Considered more esthetically pleasing
Commercial product: Vaseline
Uses:
Diaper rash
Dry skin
Yellow Ointment, USP
Purified wax obtained from the
honeycomb of the bee Apis Mellifera
Simple Ointment
Slightly greater viscosity than plain
petrolatum
May contain a suitable stabilizer

Unctuous mass of yellowish to white


amber color
Free or nearly free of odor and taste
White Ointment, USP
Consists of a white wax (bleached and
purified yellow wax) and white
petrolatum
Uses:
An emollient
Vehicle for other ointments
Absorption Bases
Two types:
Permit the incorporation of aqueous
solutions resulting in the formation of
water-in-oil emulsions
o Ex.
Hydrophilic petrolatum
Anhydrous lanolin
W/O emulsions that permit the
incorporation of additional quantities of
aqueous solutions
o Ex.
Lanolin (as emollient)
Cold Cream
Characteristics:
Not easily removed from the skin with
water
Hydrophilic Petrolatum, USP
Composed of stearyl alcohol, white
wax, cholesterol and white petrolatum
Characteristic:
Ability to absorb water with the
formation of water in oil emulsion
Commercial product:
Aquaphor
Aquabase
Anhydrous Lanolin, USP
Refined wool fat
May contain NMT 0.25% water
Characteristics:
Insoluble in water but mixes without
separation with about two times its
weight in water
Incorporation of water results in the
formation of a water in oil emulsion
Lanolin, USP
Obtained from Wool of sheep (Ovis
Aries)
Purified wax like substance:
Cleaned
Decolorized
Deodorized
Characteristics:
Water in oil emulsion that contains
between 25% to 30% water

Additional water may be incorporated


by mixing
Cold Cream, USP
Semi-solid water in oil emulsion
prepared with cetyl wax, white wax,
mineral oil, sodium borate, and purified
water
Uses:
Emollient
Ex.
Eucerin cream a water in oil emulsion
of petrolatum, mineral oil, mineral wax,
wool wax, alcohol, and bronopol
Water Removable Bases
Oil in water emulsion commonly called
creams
Aqueous external phase
Water-washable bases
Can absorb serous discharges
Characteristics:
Resembles creams in their appearance
May be diluted with water or with
aqueous solution
Hydrophilic Ointment, USP
Sodium lauryl sulfate (emulsifying
agent)
Stearyl alcohol and white petrolatum
(oleaginous phase of the emulsion)
Methylparaben
and
propylparaben
(antimicrobial preservatives)

Hydrophilic ointment and vanishing


cream (O/W)

Hydrous wool fat and cold cream (W/O)

Water Soluble Bases

Do not contain oleaginous components

Water-washable,
referred
to
as
greaseless

Soften greatly in water, large amount


of aqueous solutions not effectively
incorporated

Used
for
incorporation
of
solid
substances
These penetrates the skin and better
used for absorption of medicated and
therefore used for diadermic ointment.

Polyethylene Glycol Ointment, NF

A polymer of ethylene oxide and water


Molecular weight below 600 are clear,
colorless liquid

Molecular weight above 1000 are


waxlike white materials
Molecular weight in between are
semisolid

Greater molecular weight, greater


viscosity

Combining PEG 3350 (solid) with PEG


400 (liquid), results in a very pliable
semisolid preparation
Selection of the Appropriate Base
Desired release rate of the drug
substance from the ointment base
Desirability of topical or percutaneous
drug absorption
Desirability of occlusion of moisture
from the skin
Stability of the drug in the ointment
base
Desire for a base easily removed by
washing with water
Characteristics of the surface to which
it is applied
Preparation of Ointments
Incorporation
Fusion
Incorporation
Components mixed until a uniform
preparation is attained
In small scale or in extemporaneous
compounding of the Rx, the pharmacist
may use 2 means:
Mixing ingredients in a mortar and
pestle until smooth ointment is
produced
Use a spatula and an ointment slab (a
large glass or porcelain plate) to rub
the ingredients together (spatulation)
Incorporation of Solid
Particle size of a powder or crystalline
material is reduced
If the components react with metal
(such as Iodine, Tannins, Mercuric salts)
the harder rubber or silicone spatulas
may be used
The ointment base is placed on one
side
The powdered components is placed on
the other side
A portion of powder is mixed with a
portion of base until uniform
Repeat until all are combined
Thorough blending by continuous
movement of spatula
Incorporation of liquids
Small amounts of an aqueous solution
may be incorporated into an
oleaginous ointment
Bases, even if hydrophilic have limits to
retain liquids, beyond: becomes to soft
and semiliquid
Alcohol solution (small volume) may be
added easily to oleaginous vehicle or
emulsion bases

Large scale: roller mills force coarsely


formed ointments through stainless
steel rollers to produce ointments that
are uniform in composition and smooth
in texture
Small ointment mills: also used in
product development laboratories and
in small batch manufacture
Ointment Roller Mill /
Unguator
Electronic mortar and pestle
Ingredients are placed in a plastic
ointment jar with a special lid
Mixing blade is used to mix ingredients
in the dispensing container
Controlled manually or via computer
software
Fusion Method
All or some of the components of an
ointment are combined by being
melted together and cooled with
constant stirring until congealed
The heat labile substances and volatile
constituents are added last when
temperature is low enough not to
cause decomposition
Carried out:
Small scale: porcelain dish or glass
beaker
Large scale: large steam-jacketed
kettle

MISCELLANEOUS SEMISOLID
PREPARATIONS: PASTES, PLASTERS
AND GLYCEROGELATINS
Pastes
Semisolid preparations intended for
application to the skin.
Stiffer than ointments (due to
large proportion of solid material)
Prepared in the same manner as
ointments . (Direct mixing)

PASTES
When a levigating agent is to be
used to render the powdered
component smooth, a portion of
the base is often used rather than a
liquid, which would often the paste.
They remain in place after
application due to its stifness
Effectively employed to absorb
serous secretions
Not suited for application to hairy
parts of the body.

PASTES: LASSARS PLAIN ZINC


PASTE
It is prepared by mixing 25% each
of zinc oxide and starch with
white petrolatum.
It is very firm and is better able to
protect the skin and absorb
secretion than zinc ointment.
PLASTERS
Solid or semisolid adhesive masses
spread on a backing of paper,
fabric, moleskin, or plastic.
Adhesive material: rubber base/
synthetic resin
Applied to the skin to provide
prolonged contact at the site.
Non Medicated PLASTERS
Provide protection or mechanical
support at the site of application.
Adhesive tape used to be official
under the title adhesive plaster.
Medicated PLASTERS
Provide effects at the site of
application.
May be cut to size to conform to
the surface to be covered
Medicated PLASTERS: salicylic acid
Used on toes for the removal of
corns.
CORNS (clavi): are painful,
hyperkeratotic papules of the skin
that develop in response to excess
pressure on the bony prominences
of the feet and toes.
The outermost layers of the skin
are removed by the keratolytic
action of salicylic acid
Medicated PLASTERS: salicylic acid
10% - 40% concentration of
Salicylic acid used in commercial
corn plasters.
glycerogelatins
Plastic masses containing:
15% = Gelatin
40% = Glycerin
35% = Water
10% = Added medicinal
substances
glycerogelatins
Applied to the skin for the long
term.

Melted, Cooled, Applied, Covered.

Glycerogelatins: zinc gelatin


Most recent official glycerogelatin.
Used on the treatment of varicose
ulcers.
Also known as zinc gelatin boot
because of its ability to form a
pressure bandage
Glycerogelatins: Preparation
Softening the gelatin in the water
(10 mins)
Heating on a steam bath until
gelatin is dissolved.
Adding the medicinal substance
mixed with the glycerin.
Cool with stirring until congealed.

Topical dermatologic products


jars, tubes, or syringes.

Opthalmic, nasal, vaginal, and


rectal semisolid products are
always packaged in tubes or
syringes.
Ointment jars
Made of clear, opaque glass or
plastic.
Some are colored green, amber or
blue.
Opaque jars : for light sensitive
products. (White, dark green,
amber)
Size: 0.5 oz to 1lb
Commercial manufacture and
packaging of topical products:
Jars and tubes are first tested for
compatibility and stability for the
intended product.
This includes stability testing of
filled containers at room
temperature as well as under
accelerated stability testing
conditions.
tubes
Tubes used to package topical
pharmaceutical products are
gaining in popularity.
Light in weight, relatively
inexpensive, convenient for use,

and compatible with most


formulative components
Provide greater protection against
external contamination and
environmental conditions than jars.
Ointment tubes
Are made of aluminum or plastic
When the ointment is to be used
for ophthalmic, rectal, vaginal,
aural, or nasal application, they are
packaged with special applicator
tips.
Tube s of aluminum: coated with an
EPOXY RESIN, VINYL, OR LACQUER
to eliminate any interactions
between the contents and the
tube.
Types of Plastic tubes:
HDPE/LDPE,
PP
PET
Various plastic foil
paper laminates (10 layers thick)
Types of plastic tubes
LDPE (Low-density polyethylene)
Soft and resilient
Provides a good moisture barrier
2.
HDPE
(High-density
polyethylene)
Provides a superior moisture barrier
Less resilient
3. PP (Polypropylene)
High level of heat resistance
4. PET (Polyethylene terephthalate)
Transparency and a high degree of
product chemical compatibility.
Plastic tubes
The cylindrical bodies of plastic
tubes are made by extrusion and
then joined to shoulder, neck and
tip piece, which is made by
molding
Most multiple-dose tubes: Have
conventional, continuous thread
closures.
Single-dose tubes: prepared with a
tear away tip .
PLASTIC TUBES
STANDARD SIZES OF EMPTY TUBES
HAVE CAPACITIES OF
1.5 g

3.5 g
5g
15 g
30 g
45 g
60 g
120 g

Ointments, creams and gels : 5,


15, 30 g tubes.
OPTHALMIC OINTMENTS
Packaged in a small aluminum or
collapsible plastic tubes holding 3.5
g of ointment.
Tubes are sterilized before being
aseptically filled, are fitted with
narrow gauge tips,.
Either syringes for injection or
syringes for oral use have been
successfully used.

Filling ointment jars


Ointment jars are filled on a small
scale in the pharmacy by carefully
transferring the weighed amount of
ointment into the jar with a
spatula.
The jar size should allow the
ointment to reach near the top of
the jar
Ointments prepared by fusion may
be poured directly into the
ointment jar to congeal in it.
In large-scale manufacture of
ointments, pressure fillers force the
specified amount of ointment into
jars.
Filling ointment tubes
Tubes are filled from the open back
end of the tube, opposite from the
cap end
Ointments prepared by fusion may
be poured while still soft but
viscous directly into the tubes.
On a small scale, the tube may be
filled manually, or with a smallscale filling machine.
Tubes can also be filled using a
caulking gun system.
Automatic filling, closing, crimping
and labelling machines are used for
large-scale tube packaging.

Machines have the capacity to fill


1000-6000 tubes per hour.
Rotary machines have 4 stations
for feeding, cleaning, filling and
closing.
Plastic/Laminate tubes: sealed by
heat and crimping
Metal tubes: sealed by folding and
crimping with or without sealant.
Filling ointment tubes
Electronic mortars and pestles can
be used to prepare an ointment,
cream or gel in the dispensing
container.
Filling syringes
-Syringes can be filled either by
drawing the semisolid into the
barrel using the plunger or by by
removing the plunger and filling
through the back end of the
syringe.

Features and use of dermatologic


preparations

In treating skin diseases, the drug in a


medicated application should
penetrate and be retained in the skin
for a while.

Drug penetration into the skin depends


on a number of factors:
Physiochemical properties
Pharmaceutical vehicle properties
Condition of skin itself
Features and use
The skin is divided histologically into
the:
Stratum corneum (outer layer)
Living epidermis
Dermis, collectively a laminate of
barriers protecting against permeation
by external agents and loss of water
from the body.

Features and use


The stratum corneum
The stratum corneum is the
desquamating outermost layer. (10-15
mm thick layer of flat, partially
dessicated, dead epidermal cells.
composed of approximately 40%
protein and 40% water.

On the surface is a film of emulsified


material composed of a complex
mixture of sebum, sweat and
desquamating epidermal cells.
The stratum corneum
The film covering the stratum corneum
varies in composition, thickness, and
continuity.
It offers little resistance to drug
penetration.
Being keratinized, behaves as a
semipermeable membrane, and drug
molecules can penetrate by passive
diffusion.
The stratum corneum

Rate of drug movement across skin


layers depends :
- Drug concentration in the
vehicle
- Its aqueous solubility
- Oil-Water coefficient
between stratum corneum
and products vehicle
Good candidates for diffusion:
-Substances with BOTH aqueous
and lipid solubility characteristics

Skin Absorption occurs when the


topically applied chemical breaks
the skin barrier to reach the
bloodstream. Whether this
chemical becomes a risk is
determined by what occurs after
absorption. You body can filter
(The bouncers!) out the chemical
via bodily fluids, or
bioaccumulation (build up) occurs.

Inside stratum corneum

Drug blood levels achieved by


transdermal delivery systekms may
ba measurep and equated against
desired therapeutic effect same is
NOT true for topical nonsystemic
dermatologic

Topical Products Drug


Concentration on skin is not known.
Features and use of dermatologic
preparations
Factors of the base used and
product type:
- Difference in emollient and
occlusive effects and ease
of application and removal
between products
Oleaginous Bases- greater
occlusion and emollient effects
than hydrophilic bases
Pastes greater occlusion; more
effective than ointments
Creams- O/W emulsion; easy to
spread and remove
Water-soluble bases- non-greasy
&easy to remove

Application of dermatological
products
Clean thoroughly the affected area
Dry by patting with soft cloth
Apply a thin layer of medication is
spread evenly using gentle
pressure with fingertips
Usually abou 1-3mg of cream per
square centimeter of skin
A bandage should not be used
unless required by the physician.
Wash hands thoroughly.
Features and use of dermatologic
preparations
It is common to have an allergic
response such as skin rash, to a
topical product as a result of
sensitivity to the medicinal
compound used in the product.
To avoid these circumstances,
pharmacists should advised
patients that if symptoms or
irritations develop, discontinue the
use of the product and consult your
physician as soon as possible.
An alternative product that does
not contain the offending agent can
be use.
Some examples of dermatologic
ointments and creams:

Some examples of topical gels:


Features and use of opthalmic
ointments and gels
Presented by: Ira Sheinel Bascuguin
4
Application of medication to the
eye or conjunctival sac affects the
surfae of the eye and underlying
tissues as the drug penetrates/
Simple Diffusion avia the Cornea
- major route by which drug
enters the eye
Through Conjuctiva and Sclera
- route drugs that are poorly
absorbed by cornea

The cornea
3 layers: lipophilic epithelial layer,
hydrophilic stromal layer, less
lipophilic enothelial layer
The cornea
Drug penetration depends on a
drugs ability to pass through these
three layers.
Lipophilic Drugs- more capable of
penetrating than hydrophilic
compounds.

WHY? The transcellular passage of


drugs depends on their
permeability characteristics to
penetrate the lipid bilayer of the
epithelial cell membrane, which is
in turn dependent on the
lipophilicity of the drugs
Because of the corneas natural
resistance to drug penetration and
small surface of the cornea and
short residence time on the eye-drug penetration becomes limited.

bioavailability for absorption


into the ocular tissues
gives extended residence
time on the surface of the
eye.

Comparing ophthalmic solutions


with Ophthalmic Gels and
ointments

Ophthalmic Ointments
- cleared from eye slowly as
0.5% per minute
Ophthalmic Solution
- lose up to 16% of the
volume per minute

Comparing ophthalmic solutions


with Ophthalmic Gels and
ointments

Opthalmic Gels and Ointments


- increasing duration of
surface effects and

Selecting ointment base


Must NOT be irritating to the eye
Must permit the diffusion of
medicinal substance throughout
the secretions bathing the eye.
Have a softening point close to
body temperature (for comfort and
drug release)
Common bases
Usually- mixture of white
petrolatum and liquid petrolatum
(mineral oil) for both medicated
and non-medicated ointments
Water Absorbing agent can also be
used like lanolin
Gel base of PEG and Mineral Oil
this mixture allows water and
water- insoluble drugs to be
retained with the base
Fine milling
Where ointment is made uniform
and smooth
Medicinal agents can be added to
the ointment base as a solution or
as finely micronized powder
Quality standards of ophthalmic
ointments and gels
Must meet the USP sterility tests;
- Terminal Sterilization

Steam Sterilization or
Ethylene Oxide Methodneither cannot penetrate
the ointment base
Dry Heat Sterilization can
penetrate the ointment
base, but can pose threat to
the stability of the drug
substance and possible
separation of the base from
the other components may
occur because of the high
heat required

Because of the following


circumstances, sterilization
generally not taken
But, Sterility requirements must
still be meet such as:
- Each drug and nondrug
component must be
employed and rendered
sterile
Some antimicrobial preservative
when needed:
- combination of
Methylparaben (0.05%) &
Propylparaben (0.01%)
- phenylmercuric acetate
(0.0008%)
- Chlorobutanol (0.5%)
- Benzalkonium Chloride
(0.008%)
USP Test for metal particles
- test used is microscopic
examination of heat-melted
ophthalmic ointment
- -detected metal are
measured by a calibrated
eyepiece micrometer disk.
- Requirements are met IF the
total # of particles 50mm or
larger from ten product
tubes does not exceed 50
and IF not more than one
tube contains than eight
such particles
container
Must be packaged in collapsible
ointment tubes that have

elongated narrow tip to facilitate


application of narrow band of
ointment to the eye.
Preparation when applying
ophthalmic ointment
The ointment tube is held between
thumb and forefinger and the tip
placed near the eyelid without
touching it.
Patients head should be tilted back

Video:

Approximately 0.25 to 0.5 inch


should be placed inside of the
lower lid.
examples

Features and use of Nasal


ointments and gels
Presented by: Ira Sheinel Bascuguin
4
Nasal ointments and gels
Treatment of nasal mucosa
Nose
A respiratory organ serves as a
passage way for air to the lungs
Surface is covered with thin layer
of mucus produced by
subepithelial mucous glands.
Ciliated epithelium of nasal
passage- facilitates movement of
the mucous layer
Mucus contain:
Lysozyme
Glycoproteins
Immunoglobins
(act as a barrier and protection)

For local effects on the mucous


membrane and underlying tissues
Drug absorption into the general
circulation occur through the rich
blood supply feeding the nasal
lining.
Also used for systemic absorption

Butorphanol tartrate (Stadol NS,


Bristol-Myers Squibb)- analgesic
Cyanocobalamin (Nascobal Gel,
Schwartz) hematopoietic
Nafarelin Acetate (Synarel, Searle)
treatment of enometriosis
Nicotine- adjunct in smoking
cessation
Vaccines
Other polypeptides &proteins
Cyanocobalamin (Nascobal Gel)
intranasal administration
Used in treatment of Vit B12
defficiency, anemia
Self- adminitered nasal gel

ml of the gelo contains 500


mg of cyanocobalamin
Weekly
Efective absorption though nasal
mucosa to produce therapeutic
blood levels.