Ophthalmic Formulations

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Ophthalmic preparations
Presented to: Ma’am Sana Inam

Presented by:
Noor Fatima 16942
Ifra 16943
Azka Fatima 16944
Tahira Zaheer 16957
Semester: 8th
Pharm D
Government College University Faisalabad
1
Contents
Ophthalmic preparation
Anatomy of eye
Mechanism of ocular absorption
Factors affecting intraocular bioavailability
Ophthalmic products
Ideal characteristics of ophthalmic products
Classification of ophthalmic products
Evaluation of ophthalmic preparations
Packaging of ophthalmic preparations
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Ophthalmic Preparation
Ophthalmic preparation is sterile product that is intended to
be applied to the eyelids or placed in the space between the
eyelids and the eyeball.
A drug delivery to circumvent ailments of the eye.
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3
Anatomy of eye
4
Mechanism of ocular absorption
Non-corneal absorption
• Penetration across sclera and conjunctiva into ocular tissues
• Non productive
Corneal absorption
• Outer epithelium:
Rate limiting barrier with pore size 60 Aᴼ.
Only access to small ionic and lipophilic molecules.
• Trans cellular transport:
Transport between corneal epithelium and stroma.
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Factors affecting intraocular
bioavailability
Physiological factors Formulation factors
Precorneal fluid drainage Sterility
Preservatives
Drug binding to tear proteins
Tonicity
pH and buffers
Melanin binding
Isotonicity
Drug metabolism Stabilizers and antioxidants
Viscosity
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Physiological factors
1. Corneal fluid drainage
 Precorneal fluid drainage is one of the main reasons for low ocular drug absorption.
 Naso-lacrimal drainage helps in maintaining the volume of precorneal fluid about 7 to 10 μL at
any time.
 Following are the factors influencing the drainage rate:
a) Instilled volume
b) Viscosity
c) pH
d) Tonicity and drug type
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2. Drug binding to tear proteins
 Tear fluid contains approximately 0.7 % of total body protein.
 Drug binding to these tear proteins may result in a reduction in concentration of total available
free drug for required pharmacological action at the target site.
3. Melanin binding
 The melanin pigment present in the iris and ciliary body may also change the ocular
bioavailability.
 Drugs such as ephedrine and timolol have a high binding capacity for melanin.
4. Drug metabolism
 Many enzymes such as cytochrome P450, aldehyde oxidase, aldo/ketone reductase,
cyclooxygenase, monoamine oxidase, hydrolase, and transferase are expressed in ocular tissues
such as cornea, lens, iris–ciliary body, and retina.
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Formulation / Product factors
1. Sterility
 Ideally, all ophthalmic products would be terminally sterilized in the final packaging.
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2. Preservatives
Ophthalmic products for individual use package in multi-dose containers.
1st dose is always sterile.
Other doses may cause infection to eyes due to

contamination.
So we add preservatives to prevent the growth or to destroy micro-

organisms. For example: Benzalkonium chloride (0.01%),
Phenylethanol (0.5%) etc.
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3. Tonicity
 The pharmacist should adjust the tonicity of an ophthalmic
products correctly (i.e.., exert an osmotic pressure equal to that of tear
fluid, generally agreed to be equal to 0.9% NaCl).
 A range of 0.5-2.0% NaCl equivalency does not cause a marked pain response and a range of
about 0.7-1.5% should be acceptable to most person.
 Commonly tonicity adjusting ingredients include : NaCl, KCL, buffer salts, dextrose, glycerin,
propylene glycol, mannitol etc.
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4. pH and buffers
pH adjustment is very important due to the following reasons:
 To render the formulation more stable.

 The comfort, safety and activity of the product.
 Eye irritation increase in tear fluid secretion rapid loss of medication.
 To enhance aqueous solubility of the drug.
 To enhance the drug bioavailability.
 To maximize preservative efficacy.
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4. pH and buffers (cont.)
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5. Isotonicity
Lacrimal fluid is isotonic with blood having an isotonicity value corresponding to

that of 0.9% NaCl solution.
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6. Stabilizers and antioxidants
 Stabilizers are ingredients added to a formula to decrease the rate

of decomposition of the active ingredients.
 Antioxidants are the principle stabilizers added to some

ophthalmic solutions due to following reasons:
a) Provide protection from oxidation.
b) Air is replaced by inert gas.
c) Gets oxidized in preference to medicament.
 Sodium metabisulphite, sodium thiosulphate, ascorbic acid
and acetyl cysteine etc. are few examples.
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7. Viscosity
 Extending the time period of contact with cornea,

there by decreasing the drainage rate, and improving bioavailability of substances
may be obtained by increasing formulation’s viscosity.
 Ideal thickening agent posses the following properties:
a) Easy to filter
b) Easy to sterilize
c) Compatible
d) Optimum refractive index
 Polyvinyl alcohol, methylcellulose, hydroxypropyl methylcellulose,
hydroxyethylcellulose, and carbomers are commonly used.
 Not used in eye drops and eye lotion.
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Drugs used in the eye
▶Miotics e.g. pilocarpine Hcl
▶ Mydriatics e.g. Atropine
▶ Cycloplegics e.g. Atropine
▶ Anti-inflammatories e.g. corticosteroids
▶ Anti-infectives (antibiotics, antivirals and antibacterial)
▶ Anti-glucoma drugs e.g. pilocarpine Hcl
▶ Adjuncts e.g. Irrigating solutions
▶ Diagnostic drugs e.g. sodium fluorescein
▶ Anesthetics e.g. Tetracaine
https://www.slideshare.net/ZahirKhan9/opthalmic-preparation-80338949
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Ophthalmic Products
 These are the sterile products meant for instillation in to the eye
in the space between eye leads and eye balls.
 These products must be sterile and are prepared under the same
conditions and same methods as other parenteral preparation.
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▶ Ophthalmic products include:
 Eye drops
 Eye lotion
 Eye ointment
 Eye suspension
 Contact lens solution
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Ideal characteristics
Good corneal penetration
Free from foreign particulate matter
Sterile
Isotonic with lachrymal secretion
Non-irritant and comfortable
Optimum viscosity (25-50cps)

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Classification of ocular drug delivery
system
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Eye drops
▶ Eye Drops are sterile aqueous or oily solutions or
suspension of drug that are instilled in to eye with the
help of dropper.
▶ The Eye Drops are usually contain drugs having

antiseptic, anesthetic, anti inflammatory, etc.
https://www.slideshare.net/srikanthavn/ophthalmic-preparations 22
▶ Essential characteristics of eye drops
 They should be sterile.
 They should be iso-osmotic with lachrymal secretion.
 They should be free from the foreign particles, fibers and

filaments.
 They should have almost neutral pH.
 They should be preserved with suitable bacterioside.
 They should remain stable during its storage.
https://www.slideshare.net/srikanthavn/ophthalmic-preparations 23
Example of eye drops
Rx
 Atropine Sulphate 1 g
 Phenyl Mercuric Nitrate 50.0
ml Solution 0.002 %
 Purified Water add up to 100

ml
▶ Direction : To be used as
directed
https://www.slideshare.net/PrashantBhagwanPatil/ophthalmic-preparation-90993197
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Eye lotion
▶ These are the sterile aqueous solutions used for washing for the eyes.
▶ The eye lotions are supplied in concentrated form and are required to be diluted
with warm water immediately before use.
▶ Eye lotions should be isotonic and free from the foreign

particles to avoid irritation to the eyes.
▶ Sodium Chloride and Sodium Bicarbonate eye lotion are commonly used for
removing foreign particles from eye.
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Example of eye lotion
▶ Rx
 Sodium Chloride 9gm
 Purified Water to produce 1000ml
▶ Rx
 Sodium Bicarbonate 35
 Purified Water to produce 1000ml
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Eye ointment
▶ Eye ointment are sterile preparations meant for application to the eye.
▶ These are prepared under aseptic conditions and packed in sterile

collapsible tubes.
▶ Example
▶ Rx
 Yellow Soft Paraffin 80gm
 Liquid Paraffin 10 gm
 Wool Fat 10 gm
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Eye suspension
▶ These are the preparations are not commonly used as compared to eye
drops.
▶ These are the prepared only those cases when drug is insoluble in
desired vehicle or unstable in liquid form.
https://www.slideshare.net/PrashantBhagwanPatil/ophthalmic-preparation-90993197 28
▶ Essential characteristics
 They should have desired viscosity.
 They should be isotonic.
 They should be sterile.
 The particle size of the eye suspension should be fine enough so that it should be non
irritating to the eye.
 They should be shaken thoroughly before use in order to distribute the drug particles uniformly.
 They should be packed in suitable container, so that it can be easily instilled in to eye.
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Contact lens solution
▶ Contact lenses are usually made form polymethyl methacrylate which is hard
hydrophobic plastic.
▶ Now a days some softer hydrophilic lenses are also used.
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▶ Hard contact lenses
Wearers of hard contact lenses generally used two solutions:
▶ Wetting solution
 It is used primarily for treating the lenses before insertation.
 It may contain wetting agent, thickening agent (Cellulose Derivatives),

antimicrobial agent, isotonicity adjusters
▶ Storage solution
 This solution is used for overnight cleansing, soaking, and storage.
 These storage solution are contain non ionic surface active agents.
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Soft contact lenses
▶ These are the soft flexible type lenses. For cleansing of these lenses used
heated 0.9% sodium chloride solution.
▶ The storage solution of these lenses should be sterile.
▶ The wetting of soft contact lenses are not problem because of its
hydrophilic nature.
https://www.slideshare.net/PrashantBhagwanPatil/ophthalmic-preparation-90993197 32
Strips
 Ophthalmic strips are made of filter paper and
are individually packed to ensure sterility until
the time of use.
 Sodium used as a diagnostic strips to

visualize defects or aberrations in the corneal
epithelium by staining the areas of cellular loss.
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Injections
 While injections are considered a dosage form
for nomenclature purposes, they are not treated
as a dosage form in this paper.
 It’s the new innovation of pharmaceutical

science.
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Implants
 Implants have been widely employed to

extend the release of drugs in ocular fluids
and tissues particularly in the posterior
segment.
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Evaluation of ophthalmic preparation
 Evaluation is a test of finished parenteral products, that either these are free from micro-
organisms or not.
 Evaluation of ophthalmic products is done by the following tests:
 Sterility test
 Leaker test
 Clarity test
 Metal particles in ophthalmic ointments
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Packaging of ophthalmic preparation
 Currently almost all commercially available ophthalmic products are packaged in plastic
containers.
 Obvious advantages-ease of use, less spillage, little breakage- have led to universal
acceptance of these plastic packaging components, consisting of bottles, fitment and closures.
 Alcon was the first company to introduce these packaging components, identified as a “Drop-
Tainer” for ophthalmic products, in the late 1940s and saw them adopted by the industry as
the standard for packaging topical ophthalmic products.
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Packaging of ophthalmic preparation
Plastic containers
 The plastic bottles for packaging of ophthalmic products are generally
made of low density polyethylene (LDPE), either with or without any
colorants or with opacifying agents.
 Polypropylene (PP) or high density polyethylene (HDPE) are also used
to meet specific product requirements.
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 Eye drops
Single dose containers:

 Plastic bottles (LDPE) are widely used.
Multiple dose containers

 Traditionally, glass bottles with rubber teat dropper were widely used.
 Now-a-days, plastic bottles (LPDE) are widely used.
.
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 Eye ointments
 Flexible plastic or collapsible metal tubes are used.
40
Caps or Closures
 Caps or closures are generally made from

polypropylene (PP) and basically seal the
container to prevent contamination or leakage of
the product.
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Ophthalmic cap color coding
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Glass container
 Neutral, boro-silicate type (Type 1 glass) were

widely used as a container for ophthalmic
preparations, but glass containers are not widely
used.
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References
 Pharmaceutical Dosage Form and Drug D
elivery System by Howard C. Ansel, Nicholas G. Popovich, Loyd V. Allen, Jr.
 https://
www.researchgate.net/profile/Abhirup-Mandal/publication/309591155_A_comprehensive_insight_on_ocular_pha
rmacokinetics/links/59fa2564458515d20c7cb2b9/A-comprehensive-insight-on-ocular-pharmacokinetics.pdf
 https://www.hindawi.com/journals/tswj/2014/861904/
 https://www.slideshare.net/srikanthavn/ophthalmic-preparations?next_slideshow=1
 https://www.slideshare.net/shubhrajit/opthalmic-preparation
 https://www.slideshare.net/PrashantBhagwanPatil/ophthalmic-preparation-90993197
 https://www.slideshare.net/ZahirKhan9/opthalmic-preparation-80338949
 https://www.ashp.org/-/
media/assets/policy-guidelines/docs/guidelines/pharmacy-prepared-ophthalmic-products.ashx
 https://www.slideshare.net/SunealSaini/evaluation-of-ophthalmic-preparation
 https://
www.slideshare.net/Abir420/packaging-of-ophthalmic-and-parenteral-products?fbclid=IwAR28Afpm-FcwWbU
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1

Presented to: Ma’am Sana Inam

1st dose is always sterile.

Other doses may cause infection to eyes due to

So we add preservatives to prevent the growth or to destroy micro-

 To render the formulation more stable.

Lacrimal fluid is isotonic with blood having an isotonicity value corresponding to

 Stabilizers are ingredients added to a formula to decrease the rate

 Antioxidants are the principle stabilizers added to some

 Extending the time period of contact with cornea,

 Contact lens solution

Free from foreign particulate matter

Isotonic with lachrymal secretion

Non-irritant and comfortable

Optimum viscosity (25-50cps)

▶ The Eye Drops are usually contain drugs having

 They should be iso-osmotic with lachrymal secretion.

 They should be free from the foreign particles, fibers and

 They should have almost neutral pH.

 They should be preserved with suitable bacterioside.

 They should remain stable during its storage.

 Phenyl Mercuric Nitrate 50.0

 Purified Water add up to 100

▶ Eye lotions should be isotonic and free from the foreign

 Sodium Chloride 9gm

 Purified Water to produce 1000ml

 Purified Water to produce 1000ml

▶ These are prepared under aseptic conditions and packed in sterile

 Yellow Soft Paraffin 80gm

 They should be isotonic.

 They should be sterile.

▶ Now a days some softer hydrophilic lenses are also used.

 It is used primarily for treating the lenses before insertation.

 It may contain wetting agent, thickening agent (Cellulose Derivatives),

 This solution is used for overnight cleansing, soaking, and storage.

▶ The storage solution of these lenses should be sterile.

 Sodium used as a diagnostic strips to

 It’s the new innovation of pharmaceutical

 Implants have been widely employed to

Single dose containers:

Multiple dose containers

 Flexible plastic or collapsible metal tubes are used.

 Caps or closures are generally made from

 Neutral, boro-silicate type (Type 1 glass) were

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