All ophthalmic products are required to be sterile and free from particulate matter.
They could be presented as single use or multiple use containers.
In multidose container preservative should be added.
Basic drugs are used as hydrochloric or sulfate or nitrate salt. Acidic drugs are used as
sodium salt.
Oily eye drops are seldom used and should be prepared in sterile oil ex: oily drops of
pilocarpine.
The therapeutic activity of the drug in eye drops may be affected by the pH value but
for stability reason the pH must be kept low.
1- The decrease in drop size to 20 or less decreases the drainage rate and increases the
residence time and bioavailability.
Practically there is difficulty in design safe eye droppers that will deliver volumes as
small as 5 or 10 µl.
Following installation of even a small drop, normal lachrymation will immediately
begin to dilute and wash away the drug.
Suspension
Suspension particles usually produce irritation and increase the rate of lachrymation
and blinking.
So the particle size of suspension particles should be very small.
Drugs with p.s. less than 10 µm are rapidly removed from the eye as are drugs in
solution.
Mixture of petrolatum and liquid petrolatum (mineral oil) is used as ointment base.
Addition of drug to ointment base could be by:
direct solution in oily basis (water soluble)
incorporation of very finely powdered drug into the base (insoluble)
Incorporation of aqueous phase drug into the ointment may require the addition of
hydrous wool fat or aliphatic alc. to increase its emulsifying capacity.
Addition of aqueous phase into the eye ointment may necessitate the addition of
buffering agents and antioxidant.
Advantage:
1) Decrease the frequency of administration
2) Ensure night time medication
3) Enhance patient compliance
The buffer capacity should be high enough to avoid change in pH during storage, and
low enough to significantly change the pH of the tear film within eyes.
Antioxidant
Ascorbic acid, acetylcysteine
The use of plastic dropper bottles which could permeable to gases increases oxidative
deterioration during storage of eye drops
Wetting and spreading agents
SAA disturb the integrity of tear film and are not often included in eye formulations
except in the form of antimicrobial preservatives.
It also may be included in suspension formulation to facilitate dispersion of the powder.
Nonionic SAA is preferred than anionic and cationic compounds.
Macrogol used as artificial tear to facilitate spreading over the eye surface.
Dextran and PVA are also used.
Preservatives
Added to prevent the growth of microorganism accidentally introduce during use in
multidose container.
Product used in traumatized eye or during surgery should not contain preservative.
Chlorhexidine
It is bisbiguanide bactericide effective in 0.01% against most bacteria.
Used more extensively in contact lens solutions.
It is cationic agent dose not have surface activity as benzalkonium chloride.
It is not stable in autoclave
Chlorbutol
Substituted alc., active against most bacteria and fungi.
Well tolerated by eye and compatible with most drugs used in ophthalmic.
It is volatile and can be lost during storage in plastic containers.
It is only stable in acidic solutions.
It can withstand sterilization.
All the previously mentioned preservatives are ineffective against some strains of
Pseudomonas aeruginosa.
The organism that can invade an abraded cornea causes ulceration and blindness.
Only mixture of 0.01% benzalkonium chloride and 1000 USP units of polymyxin B
sulfate is effective against this bacteria.