This document discusses various topical drug preparations including otic (ear) preparations, suppositories, vaginal suppositories and solutions, and enemas. It provides details on the composition, uses, and administration of these preparations. Otic preparations are used to treat ear infections and remove earwax. Suppositories are drug delivery systems inserted into body orifices for local or systemic effects. Vaginal preparations treat infections and restore tissue in the female genital tract. Enemas rapidly empty the lower intestines.

1. Dr. Asra Hameed
Pharm.D (JUW)
asra_hameed1@hotmail.com

3.  OTIC PREPARATIONS
 SUPPOSITORIES
 VAGINAL SUPPOSITORIES
 VAGINAL SOLUTIONS
 ENEMAS

4.  Otic preparations are sometimes referred to
as ear or aural preparations.
 Solutions are most frequently used in the
ear, with suspensions and ointments also
finding some application.
 Ear preparations are usually placed in the ear
canal by drops in small amounts for removal
of excessive cerumen (earwax) or for
treatment of ear infections, inflammation, or
pain.

5.  The auricle is the opening to the ear;
 The ear lobe surrounds the auricle;
 The external auditory canal starts at the
auricle and ends at the tympanic membrane

6.  Cerumen is a combination of the secretions of the sweat and sebaceous
glands of the external auditory canal. The secretions, if allowed to dry,
form a sticky semisolid that holds shed epithelial cells, fallen hair, dust,
and other foreign bodies that make their way into the ear canal.
Excessive accumulation of cerumen in the ear may cause itching, pain,
and impaired hearing, and it impedes otologic examination. If not
removed periodically, the cerumen may become impacted and its
removal made more difficult and painful.
 Through the years, light mineral oil, vegetable oils, and hydrogen
peroxide have been commonly used agents to soften impacted
cerumen for its removal. Recently, solutions of synthetic surfactants
have been developed for their ability to remove earwax. One
commercial product uses carbamide peroxide in glycerin and propylene
glycol (Debrox Drops, Murine Ear). On contact with the cerumen, the
carbamide peroxide releases oxygen, which disrupts the integrity of the
impacted wax, allowing its easy removal.
 Cerumen removal usually involves placing the otic solution in the ear
canal with the patient’s head tilted at a 45° angle, inserting a cotton
plug to retain the medication in the ear for 15 to 30 minutes, followed
by gentle flushing of the ear canal with lukewarm water using a soft
rubber ear syringe.

8.  Drugs used topically in the ear for their anti-infective activity
include such agents as ciprofloxacin,, colistin sulfate,
neomycin, ofloxacin, polymyxin B sulfate, and nystatin, the
latter agent used to combat fungal infections.
 These agents are formulated into eardrops (solutions or
suspensions) in a vehicle of anhydrous glycerin or propylene
glycol.
 These viscous vehicles permit maximum contact time between
the medication and the tissues of the ear.
 In addition, their hygroscopicity causes them to draw moisture
from the tissues, reducing inflammation and diminishing the
moisture available for the life process of the microorganisms.
 To assist in relieving the pain that frequently accompanies ear
infections, a number of anti-infective otic preparations also
contain analgesic agents, such as antipyrine, and local
anesthetics, such as pramoxine hydrochloride and benzocaine.
 Topical treatment of ear infections is frequently considered
adjunctive, with concomitant systemic treatment with orally
administered antibiotics.

9.  Liquid ear preparations of the anti-inflammatory
agents hydrocortisone and dexamethasone sodium
phosphate are prescribed for their effects against
the swelling and inflammation that frequently
accompany allergic and irritative manifestations of
the ear and for the inflammation and pruritus that
sometimes follow treatment of ear infections.
 In the latter instance, some physicians prefer the
use of corticosteroids in ointment form, packaged
in ophthalmic tubes.
 These packages allow placement of small amounts
of ointment in the ear canal with a minimum of
waste.
 Many commercial products used in this manner are
labeled eye and ear to indicate their dual use.

10.  Aside from the antibiotic–steroid combinations that are used to
treat otitis externa, or swimmer’s ear, acetic acid 2% in
aluminum acetate solution and boric acid 2.75% in isopropyl
alcohol are used. These drugs help to reacidify the ear canal,
and the vehicles help dry the ear canal. Drying the ear canal
keeps in check growth of the offending microorganisms, usually
P. aeruginosa.
 Pharmacists may also be called on for extemporaneous
preparation of a solution of acetic acid 2% to 2.5% in rubbing
alcohol (70% isopropyl alcohol or ethanol), propylene glycol, or
anhydrous glycerin.
 The source of the acetic acid can be Glacial Acetic Acid, USP, or
Acetic Acid, NF. Boric acid 2% to 5% dissolved in either ethanol
or propylene glycol has also been recommended for use in the
ear. This substance, however, may be absorbed from broken
skin and be toxic. Thus, its use is usually limited, especially in
children with burst eardrums.

11.  Pain in the ear frequently accompanies ear infection
or inflamed or swollen ear tissue. Frequently, the pain
is far out of proportion to the actual condition.
Because the ear canal is so narrow, even a slight
inflammation can cause intense pain and discomfort.
 Topical analgesic agents generally are employed
together with internally administered analgesics, such
as aspirin, and other agents, such as anti-infectives,
to combat the cause of the problem.
 Most topical analgesics for the ear are solutions, and
many contain the analgesic antipyrine and the local
anesthetic benzocaine in a vehicle of propylene glycol
or anhydrous glycerin (Antipyrine 54 mg, Benzocaine
14 mg, Dehydrated glycerin qs 10 mL).
 Again, these hygroscopic vehicles reduce the swelling
of tissues (and thus some pain) and the growth of
microorganisms by drawing moisture from the
swollen tissues into the vehicle.
 These preparations are commonly employed to relieve
the symptoms of acute otitis media.

12.  As determined on an individual product basis,
some liquid otic preparations require
preservation against microbial growth.
 When preservation is required, such agents as
chlorobutanol 0.5%, thimerosal 0.01%, and
combinations of the parabens are commonly
used.
 Antioxidants, such as sodium bisulfite, and other
stabilizers are also included in otic formulations
as required.
 Ear preparations are usually packaged in 5- to
15-mL glass or plastic containers with a dropper.

14.  Subtle differences in the formulation of otic suspensions may
be bothersome to the patient. This is so especially as it relates
to differences in inactive or inert ingredients that are
considered equivalent on the basis of active ingredients and
strength. For example, several suspension combinations of
polymyxin B sulfate, neomycin sulfate, and hydrocortisone have
been shown to be more acidic at pH 3.0 to 3.5 than the
standard product, Cortisporin-TC Otic (Monarch), whose pH is
4.8 to 5.1. Consequently, there is a risk that when drops are
legally substituted, a burning and stinging sensation can occur
when the drops are introduced into the ear of young children,
especially those with tympanostomies. It has also been
demonstrated that with time, the pH of these formulations,
including Cortisporin, becomes more acidic, possibly pH 3.0.
Thus, if it is stored over time, the acidity may irritate the ear
canal on later use. For this reason, this antibiotic–
hydrocortisone combination has been formulated into a new
suspension product, PediOtic (Glaxo Wellcome), with a
minimum pH of 4.1.

16.  When eardrops are prescribed, it is important for the pharmacist to
determine how the drops are to be used. For example, earwax
removal drops should be instilled and then removed with an ear
syringe. Drops intended to treat external otitis infection are intended
to be instilled and left in the ear.
 The pharmacist should make sure the child, parent, or caregiver
understands that administration is intended for the ear and the
frequency of application. To facilitate acceptance, the pharmacist
should point out that the bottle or container of medication should first
be warmed in the hands, and if the product is a suspension, shaken
prior to withdrawal into the dropper. The pharmacist should also
explain the need to store the medication in a safe place out of the
reach of children and away from extremes of temperature.
 When instilled into the ear, to allow the drops to run in deeper, the
earlobe should be held up and back. For a child, the earlobe should be
held gently down and back. For convenience, it is probably easier to
have someone other than the patient to administer the drops.

17.  Some eardrops by virtue of their low pH may cause stinging upon
administration. Parents and children should be forewarned,
especially if a child has tympanostomy tubes in the ear. The
patient or parent should also understand how long to use the
product. For antibiotic eardrops it is not necessary to finish the
entire bottle, because therapy could last 20 to 30 days,
depending upon the dosage regimen. Therefore, patients should
be instructed to continue using the drops for 3 days after
symptoms disappear. Products for otitis externa may take up to
7 to 10 days to demonstrate efficacy.
 If a child is prone to develop ear infections as a result of
swimming or showering, it might be advisable to recommend the
parents to consult a physician for prophylactic medication to use
during swimming season and consider using ear plugs that fit
snugly in the ear when swimming or showering. After the child
emerges from the water or shower, the parents can be advised to
use a blow dryer on a low setting to dry the ear quickly without
trauma. The dryer should not be held too close to the child’s ear.

19.  A suppository is a drug delivery system that
is inserted into the rectum (rectal
suppository), vagina (vaginal suppository) or
urethra (urethral suppository), where it
dissolves or melts and is absorbed into the
blood stream. They are used to deliver both
systemically and locally acting medications.

20.  Suppository bases may be conveniently
classified as according to their composition
and physical properties:
 Oleaginous (fatty) bases
 Water soluble or miscible bases

21.  Water soluble/water miscible bases are those containing
glycerinated gelatin or the polyethylene glycol (PEG)
polymers.
 Glycerinated Gelatin Suppositories
Glycerinated Gelatin is a useful suppository base,
particularly for vaginal suppositories. It is suitable for use
with a wide range of medicaments including alkaloids, boric
acid, and zinc oxide. Glycerinated gelatin suppositories are
translucent, resilient, gelatinous solids that tend to dissolve
or disperse slowly in mucous secretions to provide
prolonged release of active ingredients.it is may be prepared
by dissolving granular gelatin (20%) in glycerin (70%) and
adding water or solition or suspension of medication (10%)

22.  Fatty bases are perhaps the most frequently
employed suppository bases, principally because
cocoa butter is a member of this group of
substances. Among the other fatty or oleaginous
materials used in suppository bases are many
hydrogenated fatty acids of vegetable oils, such
as palm kernel oil and cottonseed oil. Also, fat-
based compounds containing compounds of
glycerin with the higher–molecular-weight fatty
acids, such as palmitic and stearic acids, may be
found in fatty bases. Such compounds, such as
glyceryl monostearate and glyceryl
monopalmitate, are examples of this type of
agent.

24. Suppositories can be extemporaneously prepared by one of three
methods.
1. Hand Rolling:
it is the oldest and simplest method of suppository preparation .
1. The drug is made into a fine powder.
2. It is incorporated into the suppository base by trituration in a
mortar.
3. Then the incorporated mass is rolled between fingers into rod
shaped units.
4.The mass is formed into a ball in the palm of the hands.
5. then rolled into a uniform cylinder with a large spatula.
6.The cylinder is then cut into the appropriate number of pieces
which are rolled on one end to produce a conical shape.
Effective hand rolling requires considerable practice and skill. The
suppository "pipe" or cylinder tends to crack or hollow in the
center, especially when the mass is insufficiently kneaded and
softened.

25. 2. Compression Molding
it is a method of preparing suppositories from a mixed mass of grated
suppository base and medicaments which is forced into a specialcompression
mold.
• In preparation for compression into the molds.
• the base and the other formulative ingredients are combined by thorough
mixing.
• the friction of the process softening the base into a pastelike consistency.
On a small scale, a mortar and pestle may be used. Heating the mortar in
warm water (then drying it) greatly facilitates the softening of the base and
the mixing.
On a large scale, a similar process may be used, employing mechanical
kneading mixers and a warm mixing vessel.

26. 3. Fusion Molding :
It involves:
• first melting the suppository base, and then
dispersing or dissolving the drug in the melted
base.
• The mixture is removed from the heat and
poured into a suppository mold.
• When the mixture has congealed, the
suppositories are removed from the mold.
• The fusion method can be used with all types of
suppositories and must be used with most of
them.

28.  These prep are used to control infections in
female genitourinary tract, to restore vaginal
mucosa and for contraception.
 The most common used base for
v.suppositories consist of combination of
various molecular wt. Polyethylene glycol nd to
this surfactants and preservatives are added.

29.  Wash your hands thoroughly before administering the
suppository.
 Remove the foil wrapper and moisten the suppository
with water or water-based lubricating jelly.
 Lie on your back with your knees bent. Hold the
applicator in one hand. Put the applicator into your vagina
(like you would a tampon) as far as you can. Slowly press
the plunger until it stops.
 Withdraw the applicator. The medicine will be left
behind in the vagina.
 Please lie for 10-15 min after insertion to ensure
absorption of medication.
 Wash the applicator with soap and water after every
use, rinsing and drying it well.
 While using this medicine, wear a sanitary pad to
protect your underwear.

30.  packed in plastic boxes
 glycerin and glycerinated gelatin supp. are
packed in tightly closed glass containers
 cool place.
 oleogenous suppositories should be place at
30c
 glycerinated gelatin at 20-25c.

32.  VAGINAL DOUCHES: powders are used to
prepare solution for vaginal douche that is for
irrigation, cleansing of the vagina.
 The powder them selves may be prepared and
packed in bulk or as unit packages.
 Among the components of double powder are the
following:
 Antiseptic ( Na borate)
 Astringent (K, Zn sulphate)
 Antimicrobial (povidone iodine)
 Detergent (Na lauryl sulphate)
 Oxidizing agent ( Na perporate)
 Salts (NaCl, Na citrate)
 Aromatics (menthol, Eucalyptus)

34.  An enema is the procedure of introducing liquids into the
rectum and colon via the anus. The increasing volume of
the liquid causes rapid expansion of the lower intestinal
tract, often resulting in very uncomfortable bloating,
cramping, powerful peristalsis, a feeling of extreme
urgency and complete evacuation of the lower intestinal
tract. An enema has the advantage over any laxative in its
speed and certainty of action, and some people prefer it
for this reason. Enemas can be carried out as treatment for
medical conditions, such as constipation and as part of
some alternative health therapies. They are also used to
administer certain medical or recreational drugs. Enemas
have been used for rehydration therapy (proctoclysis) in
patients for whom intravenous therapy is not applicable.

35. The main medical usages of enemas are:
 * As a bowel stimulant, laxative –
 * Enemas may also be used to relieve constipation and fecal
impaction, although in the U.S.A. and some other parts of the
world, their use has been replaced in most professional health-
care settings by oral laxatives and laxative suppositories.
 * Bowel stimulating enemas usually consist of water, which
works primarily as a mechanical stimulant, or they may be
made up of water with baking soda (sodium bicarbonate) or
water with a mild hand soap dissolved in it.
 * Cleansing the lower bowel prior to a surgical procedure such
as colonoscopy.
 * The administration of substances into the bloodstream. This
may be done in situations where it is undesirable or impossible
to deliver a medication by mouth, such as antiemetics given to
reduce nausea ( though not many antiemetics are delivered by
enema).

36.  * Additionally, several anti-angiogenic agents, which work
better without digestion, can be safely administered via a
gentle enema. Medicines for cancer, for arthritis, and for
age-related macular degeneration are often given via
enema in order to avoid the normally-functioning
digestive tract. Interestingly, some water-based enemas
are also used as a relieving agent for irritable bowel
syndrome, using in the colon and rectal area. Finally, an
enema may also be used for hydration purposes. .
 * Administration by enema avoids having the medication
pass through the entire gastrointestinal tract, therefore
simplifying the delivery of the medication to the affected
area and limiting the amount that is absorbed into the
bloodstream.
 * enema., anesthetic agents are used rectally to reduce
medically induced vomiting during and after surgical
procedures, in an attempt to avoid aspiration of stomach
contents.

37.  Cleansing enema:
 Cleansing enema: (high): Given to cleanse as much of the colon as
possible. Left lateral position to the dorsal recumbent position and
then to the right lateral position during the administration so that the
solution can follow the large intestine. The solution container is usually
held 12 to 18 inches above the rectum because the fluid is instilled
farther to clean the entire bowel. Cleansing enema (low): Cleanse the
rectum and sigmoid colon. Maintains a left lateral position during
administration.
 Carminative enema:
 Distends the rectum and colon with gas released from the enema
solution. For an adult, 60 to 80 mL is instilled.
 Retention enema:
 Introduces oil or medication into the rectum (types):
 1. Antibiotic:
 2. Anthelmintic:
 3. Nutritive:

39.  Improper administration of an enema may cause electrolyte
imbalance (with repeated enemas) or ruptures to the bowel or
rectal tissues resulting in internal bleeding. However, these
occurrences are rare in healthy, sober adults. Internal bleeding or
rupture may leave the individual exposed to infections from
intestinal bacteria. Blood resulting from tears in the colon may
not always be visible, but can be distinguished if the feces are
unusually dark or have a red hue. If intestinal rupture is
suspected, medical assistance should be obtained immediately.
The enema tube and solution may stimulate the vagus nerve,
which may trigger an arrhythmia such as bradycardia. Enemas
should not be used if there is an undiagnosed abdominal pain
since the peristalsis of the bowel can cause an inflamed
appendix to rupture.
 Recent research has shown that ozone water, which is sometimes
used in enemas, can immediately cause microscopic colitis.
 A recent case series of 11 patients with five deaths illustrated the
danger of phosphate enemas in high-risk patients.