Features and use of ophthalmic ointments and

gels

Ointments and Gels
o Among the dosage forms used in the
topical treatment of conditions and
diseases of the eye
Other forms used:
o Solutions
o Suspensions
o Inserts
Systemic therapy
o Use of diuretics in the adjunctive
treatment of glaucoma
The major route by which drugs enter the eye
is simple diffusion via the cornea
Conjunctive and sclera
o Alternative route for drugs that are
poorly absorbed in the cornea
Cornea
o Three layered structure
A lipophilic epithelial layer
A hydrophilic stromal layer
A less lipophilic endothelial layer
on the inside
o Drug penetration depends on these 3
layers
o Lipophilic drugs are more capable of
penetration that hydrophilic
compounds
Ocular ophthalmic drug penetration is limited
by shirt residence time on the surface of the
eye because of rapid removal by tearing and
other natural mechanisms, the small surface
area of the cornea for the drug absorption, and
the corneas natural resistance to drug
penetration
Ophthalmic ointments and gels provide
extended resistance time on the surface of the
eye, increasing the duration of their surface
effects and bioavailability
Ophthalmic ointments are clared from the eye:
0.5% per minute
Ophthalmic solutions can lose ip to 16% per
minute
The ointment base
o Must not be irritating to the eye
o Must permit the diffusion of the
medicinal substance throughout the
secretions bathing the eye
o Should have softening point close to
body temperature
o Commonly used bases for medicated
and non-medicated (for lubrication):
white petrolatum and liquid
petrolatum (mineral oil)
o Lanolin-water miscible agent can also
be added
o Gel base of PEG and mineral oil: a
form that permits water and water-
insoluble drugs to be retained within
the base
Medicinal agents
o Can be added as a solution or finely
micronized powder
Ointment is made uniform and smooth by fine
milling
Ophthalmic ointments
o Must meet the USP sterility tests and the
test for metal particles in ophthalmic
ointments
o Rendering an ointment sterile requires
special technique and processing
o Steam sterilization or ethylene oxide
methods are ineffective bc neither is
capable to penetrate the ointment base
o Dry heat sterilization- can penetrate the
ointment base
The high heat required may pose
threat to the stability of the drug
substance and introduces the
possibility of components

Antimicrobial preservatives used:
o Methylparaben (0.05%)
o Propylparaben (0.01%)
o Phenylmercuric acetate (0.0008%)
o Chlorobutanol (0.5%)
o Benzalkonium chloride (0.008%0
Microscopic examination of heat melted
ophthalmic ointment- USP test for metal
particles
o detected metal particles are counted
and measured by a calibrated eyepiece
micrometer disk
o requirements are met if the total
number of particles 50 mcm or larger
from ten product tubes does not exceed
50 and if not more than one tube
contains more than eight of such
particles
USP directs that ophthalmic ointments must be
packaged in collapsible ointment tubes
o Collapsible ointment tubes have an
elongated narrow tip to facilitate
application of narrow band of ointment
to the eye
The applicator (caregiver) should hold the
ointment between the thumb and forefinger
and the tip placed near the eyelid without
touching it
Patient should be advised that blurred vision
will occur
It is advisable to administer eye ointment at
bedtime to prevent impairment of vision
Avoid touching the tip of the ointment tube to
prevent microbial contamination

Features and Use of Nasal ointments and gels

Ointments and gels
o Common dosage forms used
Others include
o Inhalants
o Solutions
o Suspensions
Nose
o Respiratory organ
o Passageway fro air to the lungs
o Surface coated with a continuous
thin layer of mucus produced by
subepithelial mucous glands
o Ciliated epithelium- facilitates the
movement of the mucous layer
o Mucus- contain lysozyme,
glycoproteins, and immunoglobulins
that act against bacteria and protect
against their entry into the lungs
o Ciliary action and sneeze reflex add
further defense against entry
Drugs introduced are primarily for local
effects on the mucous membrane and
underlying tissue
Nasal route of administration is also used
for systemic absorption of a number of
drugs
o Butorphanol tartrate (Stadol)-
analgesic
o Cyanocobalamin (Nascobal gel)-
hematopoietic
o Narfraline acetate (Synarel)-
treatment of endometriosis
o Nicotine (Nicotrol NS)- adjunct in
smoking cessation
Nasal route holds great promise for the
administration for insulin, vaccines,
polypeptides and proteins

Features and Use of Rectal Preparations

Oinments, gels, creams, creamlike aerosol
foams
o Dosage forms used in the treatment of
anorectal conditions
Solutions and suppositories
o Other dosage forms used
o Solutions-for enema or irrigation
Ointments, gels, and creams
o Are used for topical application to the
perineal area and for the insertion
within the anal canal
o Largely used to treat local conditions of
anorectal pruritus, inflammation, pain
and discomfort associated with
hemorrhoids
o Drugs include:
Astringents (ZnO)
Protectants and lubricants
(cocoa butter and lanolin)
Local anesthetics ( Pramoxine
HCl)
Anti-pruritics
Anti-inflammatory
(hydroscortisone)
Antiepileptics (Diazepam)
Perineal area
o Skin immediately surrounding anus
Anal canal
o Approximately 3cm long and connects
rectum
Both anal canal and rectum have mucosal
linings
Healthy perineal skin and mucosa
o Act as barrier to infection
Substances may be absorbed by Diffusion via
the network of 3 hemorrhoidal arteries and
accompanying veins
Rectal route
o Used for systemic absorption of
therapeutic level of drugs
o Used when oral administration induces
vomiting
Systemic effects of ointments, creams, and gels
intended for local action is usually limited by
the insolubility of certain drugs
Bases used for anorectal ointments and creams
include:
o Combination of PEG 300 and 3350
o Emulsion cream bases using cetyl
alcohol and cetyl esters wax
o White petrolatum
o Mineral oil
Antimicrobial preservatives (frequently used):
o Methylparaben
o Propylparaben
o Benzyl alcohol
o Butylated hydroxyanisole
Application
o Perineal skin must be cleanse first
o The ointment or cream is placed on a
piece of tissue
Products having water washable base are
easier to apply
Rectal ointments and creams are packaged
with special perforated plastic tips for products
to be administered in the anus primarily in the
treatment of pain and inflammation associated
with hemorrhoids
Application
o Patient lying down
o The rectal tip inserted
o Squeeze the tube
Rectal aerosol foam products
o Are accompanied with applicators to
facilitate administration
Features and Use of Vaginal Preparations

Ointments, creams, creamlike foams, and
gels
o Used in the topical treatment of
vovaginal conditions and diseases
Suppositories, vaginal inserts, transdermal
drug delivery systems, oral forms
o Other dosage forms used
Vaginal Surface
o Lined with squamous epithelium
cells and mucus produced by various
underlying glands
Topical products are used to treat
o Vulvovaginal conditions
o Vaginitis
o Endometrial atrophy
o Contraception with spermicidal
agents
Usual pathogenic organisms of vulvovaginal
infections and vaginitis
o Trichomonas vaginalis,
o Candida (Monilia) albicans,
o Haemophilus vaginalis
Anti-infective agents used for the diseases
above:
o Nystatin
o Clotrimazole
o Miconazole
o Clindamycin
o Sulfonamides
Endometrial atrophy
o May be treated locally with
hormones dienetrol and
progersterone w/c are used to
restore the vaginal mucosa to its
normal state
Nonoxynol-9 , Octoxynol
o Contraceptive preparations
o Used in combination with cervical
diaphragm
Preparations used in the vulvovaginal area
must be free from microorganisms, yeast,
and molds
Gels are subjected to bacterial growth
o Preserved with antimicrobial agents
Ointments, creams, and gels for vaginal
used: packaged in tubes
Vaginal foams: aerosol canisters
(packaging)
For intravaginal treatment
o Patient uses plastic applicator
o Application:
Applicator screwed on its
place
The tube is squeezed until the
applicator is filled
(note) Intravaginal products
are best accommodated when
the patient is lying on her
back
The applicator barrel must be
inserted into the vagina as far
as possible without causing
discomfort
Aerosol foams are used intravaginally in the
same general manner
Vaginal foams are oil in water emulsions
resembling light creams
o They are also water miscible and
nongreasy
Once a day administration is prescribed
and best done at bedtime to avoid leakage
and lessen soiling of clothing
Creams with water washable bases are
preferred to oleaginous bases
Tampons are not to be used in intravaginal
treatment
Unmedicated lubricant jellies are used by
physicians in rectal, urethral, and vaginal
examinations
All producats must be tightly closed when
not in use to prevent contamination
o if left unsealed, gels and jellies may
dry out
o