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Questions and Answers
What effect do multivalent cations have on activity?
What effect do multivalent cations have on activity?
Which of the following substances can reduce activity when heated with methylcellulose?
Which of the following substances can reduce activity when heated with methylcellulose?
What is the impact of heating in the presence of anionic surfactants?
What is the impact of heating in the presence of anionic surfactants?
Which cations are specifically mentioned as reducing activity?
Which cations are specifically mentioned as reducing activity?
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How does activity change in the presence of anionic surfactants?
How does activity change in the presence of anionic surfactants?
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What is the concentration at which chlorhexidine acetate or gluconate is typically used?
What is the concentration at which chlorhexidine acetate or gluconate is typically used?
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Which substance enhances the antibacterial activity of chlorhexidine?
Which substance enhances the antibacterial activity of chlorhexidine?
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Which of the following substances decreases the antibacterial activity of chlorhexidine?
Which of the following substances decreases the antibacterial activity of chlorhexidine?
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What role does disodium edetate play in the activity of chlorhexidine?
What role does disodium edetate play in the activity of chlorhexidine?
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Which statement about chlorhexidine's antibacterial activity is accurate?
Which statement about chlorhexidine's antibacterial activity is accurate?
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What is the primary use of benzalkonium chloride in the context described?
What is the primary use of benzalkonium chloride in the context described?
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Which type of drugs does benzalkonium chloride primarily enhance the passage for?
Which type of drugs does benzalkonium chloride primarily enhance the passage for?
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In which of the following scenarios would benzalkonium chloride be particularly beneficial?
In which of the following scenarios would benzalkonium chloride be particularly beneficial?
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How does benzalkonium chloride affect drug delivery?
How does benzalkonium chloride affect drug delivery?
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Which of the following statements about benzalkonium chloride is incorrect?
Which of the following statements about benzalkonium chloride is incorrect?
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Which of the following active ingredients requires protection?
Which of the following active ingredients requires protection?
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What is the role of sodium metabisulphite in ophthalmic products?
What is the role of sodium metabisulphite in ophthalmic products?
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What is the carbon dioxide reaction in sulfite antioxidation?
What is the carbon dioxide reaction in sulfite antioxidation?
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Which method is NOT used for sterilization of ophthalmic products?
Which method is NOT used for sterilization of ophthalmic products?
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What is the purpose of using a 0.22 µm pore size membrane filter?
What is the purpose of using a 0.22 µm pore size membrane filter?
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What is a potential consequence of prolonged usage of certain eye drops?
What is a potential consequence of prolonged usage of certain eye drops?
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What is the tolerated tonicity range for eye drops according to practical usage?
What is the tolerated tonicity range for eye drops according to practical usage?
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Which of the following correctly describes a condition that can arise from inappropriate eye drop usage?
Which of the following correctly describes a condition that can arise from inappropriate eye drop usage?
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Why should certain eye drops not be used for prolonged periods?
Why should certain eye drops not be used for prolonged periods?
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What is a safe characteristic of eye drops that ensures they are well tolerated by the eye?
What is a safe characteristic of eye drops that ensures they are well tolerated by the eye?
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What type of airflow conditions are required for filling procedures?
What type of airflow conditions are required for filling procedures?
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At what temperature and duration is dry-heat sterilization employed for non-aqueous preparations?
At what temperature and duration is dry-heat sterilization employed for non-aqueous preparations?
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Which of the following types of preparations typically undergo dry-heat sterilization?
Which of the following types of preparations typically undergo dry-heat sterilization?
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Which of the following statements is true regarding filling procedures?
Which of the following statements is true regarding filling procedures?
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Why is dry-heat sterilization used for certain pharmaceutical preparations?
Why is dry-heat sterilization used for certain pharmaceutical preparations?
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Flashcards
Multivalent Cation Inhibition
Multivalent Cation Inhibition
The reduction in activity of a substance in the presence of ions with multiple positive charges (like Mg2+ and Ca2+).
Methylcellulose Inhibition
Methylcellulose Inhibition
The ability of a substance to function is decreased when heated with methylcellulose.
Anionic Surfactant Inhibition
Anionic Surfactant Inhibition
The ability of a substance to function is decreased when formulated with negatively charged substances (like surfactants).
Surfactant
Surfactant
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Multivalent Cations
Multivalent Cations
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Mercurialentis
Mercurialentis
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Tonicity
Tonicity
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Tolerable tonicity range for eye drops
Tolerable tonicity range for eye drops
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Prolonged usage eye drops
Prolonged usage eye drops
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Mercury deposition in the eye
Mercury deposition in the eye
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Surface Activity of Benzalkonium Chloride
Surface Activity of Benzalkonium Chloride
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Transcorneal Passage
Transcorneal Passage
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Non-Lipid-Soluble Drugs
Non-Lipid-Soluble Drugs
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Carbachol
Carbachol
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How Benzalkonium Chloride Enhances Drug Delivery
How Benzalkonium Chloride Enhances Drug Delivery
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What is chlorhexidine used for?
What is chlorhexidine used for?
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What is the typical concentration of chlorhexidine?
What is the typical concentration of chlorhexidine?
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How can chlorhexidine's effectiveness be increased?
How can chlorhexidine's effectiveness be increased?
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What can decrease the effectiveness of chlorhexidine?
What can decrease the effectiveness of chlorhexidine?
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How does chlorhexidine's activity vary?
How does chlorhexidine's activity vary?
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Active ingredients in ophthalmic products
Active ingredients in ophthalmic products
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Antioxidants in ophthalmic products
Antioxidants in ophthalmic products
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Role of sulfite in ophthalmic products
Role of sulfite in ophthalmic products
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Autoclaving as a sterilization method
Autoclaving as a sterilization method
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Filtration sterilization for ophthalmic products
Filtration sterilization for ophthalmic products
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Grade A Laminar Airflow
Grade A Laminar Airflow
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Dry-Heat Sterilization
Dry-Heat Sterilization
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Non-aqueous Preparation
Non-aqueous Preparation
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Liquid Paraffin Eye Drops
Liquid Paraffin Eye Drops
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Sterilization
Sterilization
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Study Notes
Ophthalmic Preparations
- Ophthalmic preparations include eye drops, lotions, ointments, creams, gels, contact lens solutions, parenteral products, and ophthalmic inserts.
- Eye drops are solutions, emulsions, or suspensions of active medications for the conjunctival sac.
- Eye lotions are for irrigating and cleansing the eye surface, or for impregnating eye dressings.
- Eye ointments, creams, and gels contain active ingredients for application to the lids.
- Contact lens solutions are for contact lens care.
- Parenteral products are for intracorneal, intravitreous, or retrobulbar injections.
- Ophthalmic inserts release active ingredients over a prolonged period.
- Powders are for preparing eye drops and lotions.
Sterilization Requirements
- All ophthalmic preparations must be sterile and free from foreign particles.
Medicaments in Ophthalmic Products
- Anaesthetics: used topically in surgical procedures.
- Anti-infectives: antibacterials, antifungals, and antivirals.
- Anti-inflammatories: corticosteroids and antihistamines (non-steroid).
- Antiglaucoma agents: reduce intraocular pressure, such as beta-blockers.
- Astringents: such as zinc sulphate.
- Diagnostic agents: such as fluorescein, highlighting damage to the epithelial tissue.
- Miotics: constrict the pupil and contract the ciliary muscle, increasing drainage from the anterior chamber.
- Mydriatics and cycloplegics: dilate the pupil and paralyze the ciliary muscle, facilitating eye examination.
Eye Drop Formulation
- Active ingredient(s): to produce the desired therapeutic effect.
- Vehicle: aqueous, but occasionally oil.
- Antimicrobial preservative: to eliminate microbial contamination during use, maintaining sterility. Should not interact with active ingredients.
- Adjuvants: adjust tonicity, viscosity, or pH.
Antimicrobial Preservatives
- Preservatives should be included in all eye drops except those formulated for intraocular surgery or those supplied as single-dose preparations (tear replacements).
- Specific preservatives are suitable for specific eye drops (e.g., benzalkonium chloride and chlorhexidine acetate or gluconate).
- Important preservation factors include concentration and stability at autoclaving temperatures in specific eye drops (such as those not requiring autoclaving, like single-use formulations).
Benzalkonium Chloride
- One of the most common preservatives in eye drops (over 70% of commercially produced eye drops).
- Usually at 0.1% w/v.
- A mixture of alkylbenzyldimethyl ammonium compounds.
Benzalkonium Chloride - Activity
- Stable to sterilization by autoclaving.
- Rapid bactericidal action against Gram-positive and Gram-negative organisms.
- Destroys external cell structures.
- Activity reduced by multivalent cations (Mg2+, Ca2+).
- Activity reduced by heating with methylcellulose or anionic surfactants.
- Activity against Gram-negative organisms enhanced by chelating agents like disodium edetate.
- Surface activity enhances transcorneal passage of non-lipid-soluble drugs.
- Not suitable for preserving local anaesthetics; can abolish the blink reflex.
Chlorhexidine Acetate or Gluconate
- Cationic biguanide bactericide with antibacterial properties, similar to benzalkonium chloride.
- Used at 0.01% w/v.
- Antibacterial activity enhanced by aromatic alcohols and disodium edetate.
- Activity reduced by anionic surfactants.
Chlorobutanol
- Used at 0.5% w/v.
- MOA (mechanism of action) is unknown.
- Main disadvantages: volatility, absorption by plastic containers, and lack of stability at autoclave temperatures.
Organic Mercurials
- Phenylmercuric acetate, nitrate, and thiomersal.
- Used at low concentrations (0.001-0.004% w/v).
- Marked absorption by rubber.
- Should not be used in prolonged-use eye drops, because of intraocular mercury deposition.
Tonicity
- Eyes tolerate small volumes of eye drops with tonicities equivalent to 0.7-1.5% w/v sodium chloride.
- Best equivalent to 0.9% NaCl.
- Some preparations are hypertonic.
Viscosity Enhancers
- Increasing viscosity prolongs eye drop residence time, increasing drug penetration and therapeutic action.
- Important for artificial tears.
- Hydroxypropyl derivative of methylcellulose: the most popular cellulose derivative for enhancing viscosity.
- Polyvinyl alcohol, Polyvinylpyrrolidone, polyethylene glycol, dextrin, and sodium hyaluronate.
pH Adjustment
- pH offers best stability during preparation and storage.
- Also contributes to optimal therapeutic activity and patient comfort.
- Lachrymal fluid pH is 7.2-7.4, with considerable buffering capacity.
Buffers
- Example of buffers in practice using pilocarpine and its ion in a pharmaceutical or biological system.
Antioxidants
- Primarily reducing agents.
- Protect active ingredients.
- Examples of active ingredients requiring protection: adrenaline, proxymetacaine, sulfacetamide, tetracaine, phenylephrine, and physostigmine.
- Most used antioxidants: sodium metabisulphite and sodium sulphite.
Sterilization of Ophthalmic Products
- Methods: autoclaving (115-121°C), filtration (0.22 µm pore size), and dry-heat sterilization (160°C).
- Critical aspects of sterilization methods like filtering and autoclaving to sterilize the materials and products.
Instillation of Eye Drops
- Procedure for administering eye drops: tilt head back, pull down lower eyelid to form a pouch, drop in the prepared pouch, don't touch the eye, release the eyelid, and avoid excessive blinking.
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Description
Test your knowledge on the effects of multivalent cations and surfactants on the activity of chlorhexidine. This quiz covers its antibacterial properties, the role of various substances in enhancing or reducing its activity, and specific concentrations used in practice. Assess your understanding of the interactions between these compounds!