Podcast
Questions and Answers
What should a patient do to minimize taste and drainage after instilling eye drops?
What should a patient do to minimize taste and drainage after instilling eye drops?
When administering eye drops and ointments, what is the recommended order and time interval?
When administering eye drops and ointments, what is the recommended order and time interval?
What is a critical guideline for the storage of eye drop products?
What is a critical guideline for the storage of eye drop products?
What is a major pathway for ophthalmic drug absorption into systemic circulation?
What is a major pathway for ophthalmic drug absorption into systemic circulation?
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What action should be taken if multi-dose eye drops show signs of contamination?
What action should be taken if multi-dose eye drops show signs of contamination?
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Which of the following is NOT recommended when administering eye ointment?
Which of the following is NOT recommended when administering eye ointment?
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Which factor is NOT considered key in designing topical ophthalmic dosage forms?
Which factor is NOT considered key in designing topical ophthalmic dosage forms?
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What is the consequence of contamination in ophthalmic products?
What is the consequence of contamination in ophthalmic products?
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Which preservative is most commonly used in multi-dose eye drops?
Which preservative is most commonly used in multi-dose eye drops?
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Which statement about the GI tract absorption pathway for ophthalmic drugs is accurate?
Which statement about the GI tract absorption pathway for ophthalmic drugs is accurate?
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Why do single-use eye drops not require preservatives?
Why do single-use eye drops not require preservatives?
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What is a potential drawback of using Benzalkonium Chloride (BAK) as a preservative?
What is a potential drawback of using Benzalkonium Chloride (BAK) as a preservative?
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What percentage of an instilled ophthalmic dose can potentially be systemically absorbed?
What percentage of an instilled ophthalmic dose can potentially be systemically absorbed?
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Which preservative has seen a decline in use due to hypersensitivity concerns?
Which preservative has seen a decline in use due to hypersensitivity concerns?
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What is the ideal pH range for an ophthalmic product to avoid eye irritation?
What is the ideal pH range for an ophthalmic product to avoid eye irritation?
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What osmolarity is generally considered isotonic for ophthalmic formulations?
What osmolarity is generally considered isotonic for ophthalmic formulations?
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Which of the following viscosity modifiers is NOT commonly used in ophthalmic formulations?
Which of the following viscosity modifiers is NOT commonly used in ophthalmic formulations?
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What role do buffers play in ophthalmic formulations?
What role do buffers play in ophthalmic formulations?
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Which ingredient is intentionally hypertonic for treating corneal edema?
Which ingredient is intentionally hypertonic for treating corneal edema?
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What potential issue can arise from using excessive viscosity in ophthalmic formulations?
What potential issue can arise from using excessive viscosity in ophthalmic formulations?
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What is the primary form of liquid ophthalmics?
What is the primary form of liquid ophthalmics?
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What is the function of tonicity modifiers in ophthalmic solutions?
What is the function of tonicity modifiers in ophthalmic solutions?
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How are most solution formulations sterilized?
How are most solution formulations sterilized?
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What is the primary purpose of using finely micronized drug particles in suspensions?
What is the primary purpose of using finely micronized drug particles in suspensions?
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Why can't suspensions be filter sterilized?
Why can't suspensions be filter sterilized?
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What roles do chelating agents, like EDTA sodium, serve in ophthalmic products?
What roles do chelating agents, like EDTA sodium, serve in ophthalmic products?
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Which component is frequently added to ointments to reduce their viscosity?
Which component is frequently added to ointments to reduce their viscosity?
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What is the disadvantage associated with the use of ointments in ophthalmic applications?
What is the disadvantage associated with the use of ointments in ophthalmic applications?
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How do emulsions primarily differ from suspensions in terms of drug formulation?
How do emulsions primarily differ from suspensions in terms of drug formulation?
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What is the primary advantage of using gelling agents like carbomers in ophthalmic gels?
What is the primary advantage of using gelling agents like carbomers in ophthalmic gels?
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What type of ophthalmic product is commonly packaged in dropper bottles?
What type of ophthalmic product is commonly packaged in dropper bottles?
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Which of the following is a common surfactant used in ophthalmic products?
Which of the following is a common surfactant used in ophthalmic products?
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What is the primary use of suspensions in ophthalmology?
What is the primary use of suspensions in ophthalmology?
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Study Notes
Ophthalmic Drug Delivery
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The primary goal of ophthalmic drugs is local treatment, not systemic absorption. Absorption's significance depends on drug potency and strength.
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Systemic absorption pathways include:
- Nasolacrimal drainage: Drops drain through the nasal cavity.
- Nasal structures: Absorption in the nasal cavity, nasopharynx, and lacrimal sac is possible, including absorption through mixing with saliva.
- Gastrointestinal tract: Swallowed drugs are absorbed.
- Conjunctival absorption: Rich blood supply allows for more permeable absorption.
- Trabecular meshwork: Drainage through this meshwork allows drugs to enter the bloodstream.
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Over 50% of ophthalmic drugs can be systemically absorbed. Drugs absorbed via the GI tract bypass the hepatic first-pass effect.
Dosage Form Considerations
- Sterility: Crucial for ophthalmic products, similar to injectable drugs. Contamination can lead to serious consequences, including blindness.
- Pseudomonas aeruginosa is a significant corneal ulcer-causing organism.
- Sterility testing is mandated for commercially manufactured ophthalmic medications.
- Antimicrobial preservatives are necessary in multi-dose eye drops for sterility maintenance; single-use drops typically don't need these preservatives.
Preservatives
- Benzalkonium Chloride (BAK): Is the most commonly used preservative, effective against Pseudomonas aeruginosa, but can damage corneal epithelium at high concentrations.
- Alternatives include polyquad (polyquaternium 1), which is less sensitizing, and thimerosal.
- Oxidizing agents like sodium perborate are newer and act via oxidation of microbes.
pH and Osmolarity
- Ideal pH for ophthalmic products is around 6.6-7.8, matching tear film pH.
- Buffers (acetate, phosphate, citrate, borate) help maintain product pH stability, solubility, and patient comfort.
- Maintaining isotonicity (300mOsm/kg) like tears is crucial for patient comfort, although some products are intentionally hypertonic. (eg 5% NaCl)
- Viscosity Modifiers: Viscosity affects residence time and drug diffusion; increased viscosity can cause blurred vision, while prolonged contact and reduced drainage are benefits. (eg glycerin, cellulose derivatives, polyvinyl alcohol, polyethylene glycols (PEGs))
Ophthalmic Formulations
- Solutions: Most common form, involving dissolving the drug and excipients, followed by sterilization (heat or 0.2 micron membrane filtration).
- Suspensions: Finely micronized particles for minimized irritation and improved dissolution. Used for poorly soluble drugs or to enhance drug stability.
- Emulsions: Less common, employ lipophilic drugs dissolved in oil phase and emulsifiers for stabilization.
- Ointments/Gels: Prolonged contact time, commonly petrolatum-based ointments that can be sterilized. Gels use gelling agents like carbomers and cellulose derivatives to achieve extended contact.
Administration
- Wash hands, tilt head back, and pull down lower eyelid to create a pouch.
- Instill one drop precisely into the conjunctival sac and keep eye closed for 30 seconds.
- Avoid rubbing, wiping, or squeezing the eye. Replace the dropper tip cap without touching it.
- Consider waiting at least five minutes between consecutive drops.
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Description
Explore the essential aspects of ophthalmic drug delivery, focusing on local treatment methods and systemic absorption pathways. Understand key considerations for dosage forms, including sterility and potential absorption routes, to ensure effective and safe ocular therapies.