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35980lecture 3

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11 views16 pages

35980lecture 3

Uploaded by

muneeburrehmanmuneeburrehman8
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPT, PDF, TXT or read online on Scribd
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Types of Ophthalmic Dosage

Forms
Semi solid Dosage Forms
Ophthalmic Ointment
 Interferewith vision unless use is limited to
bed time instillation.
 Often used as adjunctive night time
therapy, with eye drops administered
during the day.
 Longer contact time and greater total drug
bioavailability, with slower onset & much more time
to reach peak absorption.
 Vehicle is usually a mixture of mineral oil &
white petrolatum.
Mineral oil is added to:
a)reduce the melting point.
b)Modify the consistency.
Petrolatum-based ointments are:
a)Bland.
b)Inert nature
which make them suitable
vehicle for moisture -
sensitive drugs.
 Ointments used as vehicles for
antibiotics, sulfonamides, antiviral,
antifungal, & anti-inflammatory
corticosteroids.
 Anesthesiologists may prescribe the
ointment vehicle for the surgical patient
undergoing general anesthesia to prevent
severe and painful dry eye conditions.
 The anhydrous petrolatum base may be
made more miscible with water through
the use of an anhydrous liquid lanolin
derivative , then aqueous drug solution
can be incorporated.
?How to use ophthalmic ointment
1. Wash hands.
2. Remove cap from the tube.
3. With one hand, gently pull the lower eye lid down.
4. While looking up, squeeze a small amount of
ointment (about ¼ to ½ inch) inside lower lid. Be
careful not to touch tip of tube to eye, eyelid,
fingers, etc.
5. Close eye gently and roll eyeball in all directions
while eye is closed. Temporary blurring may occur.
6. The closed eye lid may be rubbed very gently by a
finger to distribute the drug throughout the fornix.
7. Replace cap on tube.
Types of Ophthalmic Dosage
Forms
Solid Dosage Forms
Ocular Inserts
Non erodible Ocular Inserts
 In 1975, the first controlled release
topical dosage form was marketed in the
United States by the Alza Corporation
which was pilocarpine ocusert.
 Pilocarpine ocusert is an elliptical-
shaped membrane which is soft &
flexible designed to be placed in the cul-
de-sac between the sclera & the eye lid .
Intraocular Drug Delivery
Pilocarpine ocusert consists of :
-A rate controller, ethylene vinyl acetate (EVA) copolymer
membrane.
-A delivery portal, the copolymer membrane.
-Drug reservoir, pilocarpine, carrier material, alginic acid.

1,4. Rate
controlling
ethylene-vinyl
acetate copolymer
membranes
2. Annular opaque
ring
Intranasal and intraoccular drug delivery 03/10/2009
3. Drug reservoir
•Design 0f ocusert:
The ocusert is sterile, oval in shape & flexible,
It is made of a central core or reservoir which
contains the drug embedded in an alginic acid gel-like
base,
the drug reservoir is surrounded by a rate-limiting or
controlling membrane made of ethylene vinyl acetate
co-polymer which gives a steady and controlled drug
release for a certain period of time.
The device is bordered by a white annular ring
consisting of ethylene vinyl acetate co-polymer
impregnated with titanium dioxide (a powdered
pigment) that darkens the borders of the ocusert. The
border makes the ocusert easier for the patient to
Ophthalmic Inserts
Pilocarpine Insert
 The release rate of pilocarpine from this system is given by:
 (Fick’s law) dm ADKC
Where

dt h
dm/dt is the release rate
D is the diffusion coefficient of the drug in the membrane
K is the partition coefficient that is the ratio of drug concentration
at equilibrium inside the membrane to that outside the membrane
ΔC is the difference of the drug concentration between the inside
and the outside walls of the membrane (concentration gradient)
(The driving force of the release is the concentration of the drug in
the reservoir)
A is the area
h is the thickness of the system
Under routine conditions, the concentration of the drug in the tears
is negligible (2-3 µg/mL) compared to that inside the membrane,
which is essentially the solubility of the drug, so the equation can
be rewritten:
dm ADKS

dt h
Pilocarpine ocusert
•Used to treat Glaucoma because it reduces intraocular
pressure
• It is designed to release pilocarpine at a controlled required
rate (for example, 20 micrograms \ hour or 40 microgram or
80 microgram per hour), for a certain period of time (like 7
days), after 7 days the ocusert is removed & replaced by a new
one, so it’s more convenient than pilocarpine eye drops which
is used 4 times a day normally.

:Advantages over drop therapy for the glaucoma patient

Exposes the patient to only one-fourth to one-eighth the


amount of pilocarpine compared to drop therapy. (reduced
local side effects & toxicity.)
.It provides a continuous around – the clock- control of IOP
Patient convenience & improved compliance.(administered
only once per week.)
Erodible Ocular Inserts
 Why ?
1. They do not have to be removed
at the end of the therapy
2. Increase retention time
3. Increase penetration of the drug
4. Prolonged effect
Ex. Lacrisert
Lacrisert used to treat dry eyes,
keratitis, and decreased corneal
sensitivity
It contain 5 mg of HPMC in a
rod-shaped of about 1.27mm
diameter and 3.5mm long,
no preservative since it is
.anhydrous
It imbibes water from the tears
and forms a gel-like mass
after several hours, which
gradually erodes as the
polymer dissolves, it
thickens the tear film and
provides increased
lubrication. it used once or
Soft Contact Lens

Soft hydrophilic contact lens of the hydroxyl


ethyl methacrylate (HEMA) polymer to prolong
.delivery of pilocarpine
 Lens
is presoaked in a sterile
unpreserved solution of the drug.

 Placed in the eye over the cornea for a period


of time, usually few minutes to several hours
to increase the amount of drug absorbed or to
prolong the duration of effect.(reduce the
frequency of drug instillation & give diurnal control to the
treatment of glaucoma)
• Disadvantages: Uncontrolled nature to
the release of drug from it.
Potential for increased risks of
contamination since unpreserved drug
solutions must be used & the patient
must disinfect the lens himself.

 Example of contact lenses


 The Bionite lens which is made
from hydrophilic polymer (2-
hydroxy ethyl methacrylate ) has
been shown to produce a greater
penetration of fluorescein.

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