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Pharmaceutics III Lecture 12 Transdermal, Topical, Ophthalmic Delivery

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alchemist04's version from 2016-06-05 21:58

Section

Question Answer
T or F? Topical delivery is the delivery of drug to the skin surface and into the systemic circulatory system?False, Topical does not go into the the systemic. Transdermal goes into the system system
Which drug delivery moves across the cells and into the systemic circulation for drug delivery?Transdermal
Ointment, Creams, or Sprays are examples of .......... delivery system?Topical delivery
T or F? Topical delivers several hours and days of effect on the site of administrationFalse, Topical delivers hours only while Transdermal delivers for both hours and days.
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Question Answer
What are the main ingredients of ointment?Oils and Lipids
What are the main ingredients of Cream?Water embedded in Lipids
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Question Answer
Adv. of Transdermal (1)(1) Compliance and convenience
Adv. of Transdermal (2)(2) Localized and small dose is required
Adv. of Transdermal (3)(3) No 1st pass and liver metabolism
Adv. of Transdermal (4)(4) Controlled and Consistent metabolism is achieved (like Controlled Release delivery)
Adv. of Transdermal (5)(5) Minimal side effects
Adv. of Transdermal (6)(6) Reduction of peak and valley of blood concentration like in IR
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Question Answer
Disadv. of Transdermal (1)(1) Limited candidates to Transdermal
Disadv. of Transdermal (2)(2) Irritation at the site of application
Disadv. of Transdermal (3)(3) Not a fast onset (i.e. Slow onset)
Disadv. of Transdermal (4)(4) Skin could be a hinderance to permeability
Disadv. of Transdermal (5)(5) Size matters, drug with large size (more than 5-10 mg/day) cannot be delivered
Disadv. of Transdermal (6)(6) must be less than 500 daltons
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Question Answer
Factors affecting Transdermal drug Permeation are (Flick's Theory)(1) Diffusivity[D], (2) Lipophilicity[k] (3) Molecular size (4) Surface area (5) Thickness of the skin (6) Hydration of the Skin (7) Diseased skin/bruises (8) Age
T or F? in Reservoir Transdermal system, the drug in the Reservoir can be solution, suspension, liquid or gelTrue
What limits the rate of drug delivery of Reservoir Transdermal patch?The patch membrane/drug-release membrane
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Question Answer
What limits the rate of drug delivery in Matrix/Monolithic Transdermal System?The Stratum Corneum of the skin
T or F? Most marketed Path today are Matrix/Monolithic TransdermalTrue
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Question Answer
Counseling points (1)(1) Hydrated skin more permeable (2) Diseased skin more permeable (3) Inflammation helps with permeability, (4) Irritated, bruised, warm skin are more permeable
Counseling points (2)(1) Sunburned skin is initially none permeable but later permeable, Chemical peels, thermal burns or all kinds of burn renders the skin permeable
Counseling points (3)(1) Psoriatic skin (very thick) is less permeable
Counseling points (4)Rotate the site of application
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Question Answer
T of F? Damage to the Reservoir patch may cause toxicityTrue
T or F? Cutting Reservoir patch may result in changes in Rate of Drug librationTrue
T or F? Matrix path can be cut w/o compromising their release rateTrue
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Question Answer
What is the site of application of most ophthalmic dosage forms?Conjunctival Cul-de-sac
T or F? Drug penetration of Cornea is different form that of ConjunctivalTrue, because Cornea has both lipophilic and hydrophilic layers
Drug must process biphasic solubility characteristics to gain access to anterior chamber of the eye, T or F?True
T or F? Blood-eye barrier does not affect Ophthalmic drug deliveryTrue, it only affects the systemic administration
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Question Answer
What is the limitation of the Ophthalmic delivery per volume?It is limited to 10 mL
What is the limitation of Ophthalmic drug per bioavailability?Less than 5% will reach the target due to drainage, lacrimation, metabolism etc
Oral drugs are useless to treat Glaucoma/any eye problem because of Blood-eye barrier, T or F?True
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Question Answer
How does Drainage affect the administered dose(1) Occurs when the eye fluid exceeds that of Lacrimal fluids (7-10 uL) (2) restrict contact time to 2 mins
How does Lacrimation affect the administered doseby diluting the applied drug and causing drug loss
How does Metabolism affect the administered doseEnzymes in the eyes metabolized drug and could reduce the amt available for effect
How does Conjunctival absorption affect the administered drugConjunctival is well vascularized and some % are lost via systemic absorption
How does Cornea affect the administered doseLipophilic barrier (solves via Trancellular) and hydrophilic barrier (solves by paracellular)
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Question Answer
T or F? The condition of the eye require drug Solution with Isotonic, Sterile and pH range btw 6-8True
T or F? The condition of the eye require drug Suspension with particles less than 10 micronsTrue
The primary requirements for Ophthalmic drug are(1) Isotonic, (2) Sterile (3) Buffered at pH 7.2 (usually phosphate buffered)
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Question Answer
3 things about Ophthalmic Suspension (1)(1) Used for poor water-soluble drugs
3 things about Ophthalmic Suspension (2)(2) Provider longer duration of effect than Ophthalmic Solutions
3 things about Ophthalmic Suspension (3)(3) suspension w/ bigger particles causes irritation
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Question Answer
one thing about Ophthalmic Ointment (1)(1) Viscous and slow flowing
one thing about Ophthalmic Ointment (2)(2) Mineral oil, Petrolatum, Lanolin based
one thing about Ophthalmic Ointment (3)(3) Used when longer residence time of drug is required
one thing about Ophthalmic Ointment (4)(4) Night time use only
One thing about Ophthalmic Ointment (5)(5) Produced primarily to increase drug retention and increase mechanical resistance to tear flow
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Question Answer
What is the rational behind using Mucoadhensive formulations?It binds/adhere to conjunctival and causes prolonged residence or dose retention of drug
What is the rational behind using Prodrugs (inactive drug)?so that the prodrug can be metabolized and causes increased absorption in the conjunctival
What is the rational behind using Inserts?So that drug can be released continuously over several hours or days.
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