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Ophthalmic solution
Ophthalmic suspension
Ophthalmic ointments
Ophthalmic inserts (drug-impregnated and lenses)
Pharmacologic Categories of
Ophthalmic Drugs
Sterility.
Preservation.
Isotonicity.
Buffering.
Viscosity.
Ocular bioavailability.
Packaging.
0.004-0.01%
Benzethonium chloride
Chlorobutanol
0.01%
0.5%
0.004%
0.004%
0.005-0.01%
Measurement of Tonicity
1. Hemolytic method (a hypotonic solution liberates
oxyhemoglobin in direct proportion to the number
of cells hemolyzed). The vant Hoff i factor can be
determined.
2. A method based on any of the methods that
determine colligative properties. This method is
based on a measurement of the slight temperature
differences arising from differences in the vapor
pressure of thermally insulated samples contained
in constant humidity champers.
Freezing point of both the blood and lacrimal fluid
is -0.52 oC.
Freezing point of 0.9% NaCl is -0.52 oC (isotonic).
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1.
2.
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Class II Methods
White-Vincent Method
1. Addition of water to the drug to make an
isotonic solution
2. Addition of an isotonic or isotonic-buffered
solution diluting vehicle to bring the solution
to the final volume
Example: Make 30 ml of a 1% solution of
procaine HCl isotonic with body fluids. E for
procaine HCl is 0.21.
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Buffering
Ocular bioavailability
Factors affecting ocular bioavailability
Physiological factors
Protein binding:
Normally tears contain 0.6-2% protein, including albumin and
globulins but disease state can raise these levels.
Protein-bound drugs are incapable of penetrating the corneal
epithelium because of their size.
Protein binding is reversible but tear turnover results in loss of
both bound and unbound drug.
Drug metabolism:
Tears contain enzymes (lysozyme) capable of metabolic
degradation of drug substances.
The full extent to which the metabolism occurs and affects
therapeutic effectiveness is undetermined.
- Other considerations
Ophthalmic solutions must be clear and free of
particulate matter for comfort and safety.
The formulation of ophthalmic suspension is
undertaken when:
Drug particles
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Ophthalmic ointments
Ointments are greasy, semisolid preparations often anhydrous and
containing dissolved or dispersed medication.
Base requirements:
Non-irritating.
Permit diffusion of the drug.
Usually melt or soften at body temperature.
Mixture of petroleum & liquid petroleum.
Sometime water miscible base may be used (lanolin).
Ophthalmic inserts
They consist of inner core of the drug surrounded by
copolymer membrane through which the drug
diffuses (pilocarpine ocusert).
Membrane thickness and composition determine the
release rate.
Elliptical in shape (usually 13.4 x 5.7 x 0.3 mm).
Flexible.
They eliminate frequent, nighttime administration,
enhance compliance and reduce dose
Must be sterile and contains no preservative
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1.
Disadvantages:
They require an adaption period for the wearer (as long as a
week).
More easily dislodged from the eye.
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Disadvantages:
They have shorter life span than hard or RGP lenses.
The wearer must ensure the lenses do not dry.
They do not provide the same high level of visual acuity as hard
lenses.
Carry some risk of adsorbing medication concomitantly applied to
the eye.
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Chemical:
- Previously conducted with products that contained thimerosol, in
combination with either chlorhexidine or a quaternary ammonium
compound (sensitivity reactions).
- H2O2 was introduced. To prevent eye irritation from residual H 2O2,
the lenses must be exposed to a neutralizing agent.
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3. Wetting solution
Combination solution
They mix effects, such as cleaning and soaking, wetting
and soaking or cleaning, soaking and wetting.
They may lower the effectiveness of cleaning if the
concentration of the cleaning solution is low to
adequately remove the debris from the lens.
They should be reserved for wearers who need
simplification of lens care.
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Wearers normally do not have ocular pain. Pain is a sign of illfitting lenses, corneal abrasion, or other medical conditions. The
patient should be advised to counsel his ophthamologist.
Hard or soft contact lenses may occasionally cause superficial
corneal changes (painless and not evident to the patient)
therefore the eyes should be examined regularly to make certain
that no damage has occurred.
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