Dosage Forms Ii---Test Three---Advanced Parenteral Drug Delivery

Front 1

Where are depot injections injected?

Back 1

SC or IM

Front 2

Describe the four different approaches to delivery of a Depot Injection.

Back 2

1) Suspensions
2) Prodrugs
3) Binding to adsorbents
4) Bioerodible microspheres.

Front 3

In terms of a depot injection, what is the primary goal?

Back 3

The goal is to inject a drug product that slowly releases it ingredient.

Front 4

Describe the formulation of suspension depot injections?

Back 4

Depot suspensions are formulated in water oil (drug takes a long time to release or dissolve).

Front 5

Describe the mechanism of Prodrug depot injections.

Back 5

These are hydrolyzed to release the active drug. For depot injections, they are usually lipophilic (thus, low partitioning from oil (or fat) to interstitial fluid).

Front 6

Give an example of depot injections that bind to adsorbents?

Back 6

Vaccines bound to aluminum hydroxide get that slowly release antigen.

Front 7

Describe bioerodible microspheres.

Back 7

Microspheres are free-flowing polymer spheres of about 1 to 125 micrometers in diameter.

Front 8

Bioerodible microspheres act as ____ _____ _____ to prolong drug release.

Back 8

bioerodible matrix systems

Front 9

Give an example of a Bioerodible Microspheres.

Back 9

Lupron Depot (Leuprolide acetate).

These microspheres are prepared as a copolymer of poly (lactic acid) and poly(glycolic acid).
Note: Lactic Acid is product. Breaks down to lactic acid and glycolic acids.

Available as IM 1, 3, and 4 month controlled release injections.

Front 10

Where are Depot implants placed?

Back 10

Subcutaneously.

Subcutaneous tissue: rich in fat, poor in hemoperfusion and nerves, and relatively low reactivity to foreign matter (can enamble the implant to remain for a long time; common in abdomen and inside arm).

Front 11

What are the three main types of depot implants?

Back 11

1) Polymer
2) Osmotic
3) Mechanical

Front 12

Describe Polymer Implants.

Back 12

Membrane-controlled (reservoir).

Front 13

Polymer Implants: Where diffusion from a ____ ____ (reservoir) is controlled by polymer membrane.

What type of order release is this?

Back 13

saturated solution, zero-order release.

Front 14

Polymer Implants: These products generally require surgical insertion and ___ ____.

True or False. It is biodegradable.

Back 14

Surgical removal

False. Not Biodegradable.

Front 15

One implant (4 cm in length with a diameter of 2mm) contains __ mg etongestrel _____ embedded in a ___ ethylene vinyl acetate (EVA) polymer ____

Back 15

69 mg

Crystal

Note: Implantation provides approximately three years of contraception.

Solid

Matrix

Front 16

Describe a Histrelin acetate implant.

Back 16

One non-biodegradable implant, diffusion-controlled HYDRON polymer reservoir containing histrelin acetate.

Matrix reservoir: zero order release.

Immediate release from membrane, followed by a year of steady release.

Front 17

What are the two different types of Histrelin implants?

Back 17

1) Suprellen LA: for central precocious puberty

2) Vantas: for the palliative treatment of advanced prostate cancer.

Front 18

True or False. Suprellan LA and Vantas are similar in their delivery rates.

Back 18

False.

Suprellan LA and Vantas DIFFER in their delivery rates.

Front 19

True of False. Bioerodible matrix implant are composed of bioerodible polymers with uniformly dispersed drug, which have to be removed.

Back 19

False.

Bioerodible matrix implant are composed of bioerodible polymers with uniformly dispersed drug, which DO NOT have to be removed.

Front 20

Give an example of a bioerodible matrix drug.

Back 20

1) Zoladex

2) Gliadel Wafer: an intracranial implant of cammustine homogenously dispersed in a bioerodible polymer matrix.

Polymer degrades at surface, slowly releasing drug.

Protects drug from degradation; drug unstable.

Front 21

True or False. Some wafers can be implanted into the cavity that remains after a brain tumor resection.

Back 21

True.

Front 22

Describe Eligard?

Back 22

Its a bioerodible matrix. Supplied as a two-syringe product that are mixed prior to SC injection.

ATRIGEL and leuprolide acetate are mixed.

Atrigel: tissue water causes the polymer to precipitate and trap the drug in a solid implant.

Front 23

Describe Osmotic Implants.

Back 23

Where osmotic pressure governs the release.

Front 24

Give an example of an osmotic implant.

Back 24

Vladur (leuprolide acetate). A metal implant that functions as a osmotically controlled system.

Front 25

What are the components of Vladur?

Back 25

1) Drug Reservoir

2) Membrane-allows water entry

3) Osmotic Tablets

4) Piston: pushed by the expanding polymer, it forces the drug out of a laser-drilled hole.

Front 26

Describe mechanical implants.

Back 26

Implantable infusio pumps. Pumps are positive pressure to deliver the medication.

Front 27

Implantable infusion pumps are ____ ____ units consisiting of a ___ _____ drug reservoir, and _____ that can be surgically implanted in a subcutaneous pocket.

Back 27

self-contained

pumping mechanism

catheter

Front 28

Mechanical Implants are usually made up of this material.

True or False. Mechanical implants can be used for both spatial and temporal control of drug delivery.

Back 28

Titanium, which has god biocompatibility.

True.

Front 29

Give an example of a mechanical implant.

Back 29

SynchroMed.

The drug solution is pumped from a reservoir into a catheter by a peristaltic mechanism.

Front 30

Describe Minimed.

Back 30

A type of mechanical pump. These use a piston to force fluid out, thus is gentler on insulin (approved in EU for continiuous intraperitoneal insulin deliver)

Front 31

Give some important features of mechanical implants.

Back 31

1) A particular site can be catheterized

2) Certain models can be programmed externally, using telemetry, for constant infusion or circadian patterns.

Front 32

Describe Amulatory (External) Infusion Pumps.

Back 32

Similar to implantable pumps: use positive pressure to deliver the medication.

Front 33

Describe the available types of Ambulatory (External) Infusion Pumps.

Back 33

1) Continous infusion, intermitted infusion, or bolus dosing.

2) Single or multiple solution delivery.

Front 34

What are some of the therapeutic applications of Amulatory (External) Infusion Pumps?

Back 34

1) Patient-controlled analgesia (PCA)

2) Mainly IV

3) Lockout interval-specifies the minimum amt. of time between doses.

4) Cancer Chemotherapy

5) Antimicrobials and TPN solutions.

6) Insulin: Continous sub-Q insulin infusion (tight glucose control).

Front 35

What are the two marketed particulate types of Spatial Control Parenteral Drug Delivery?

Back 35

1) Liposomes nanoparticles

2) Albumin nanoparticle

Front 36

Liposomes:

Hydrophillic drugs may be contained within the aqeous interior.

Lipophillic and amphipillic drugs may be contained within the bilayer membranes.

(Statement, not a question).

Back 36

Statement, not a question.

Front 37

What are some problems and prospects for lipsomes?

Back 37

The Mononuclear Phagocyte System (MPS): includes macrophages in the liver, lung, spleen, and intestine.

Front 38

Describe the prospect of the Mononuclear Phagocyte System.

Back 38

As particulates, lipsomes are recognied as foreign and will be engulfed by macrophages.

Macrophages, and the organs that contain them can be passively trageted.

Front 39

Describe the Problem associated with the Mononuclear Phagocyte System (MPS)

Back 39

Other Diseases where the MPS needs to be avoided.

Front 40

Describe a solution to the MPS problem.

Back 40

"Stealth" liposomes. These are liposomes with PEG chains attached to the lipid headgroups.

PEG chains shield the liposomes from MPS recognition.

PEG chains are very hydrated, making the liposome difficult to distinguish from surrounding plasma.

Front 41

Give an example of "Stealth" liposome.

Back 41

Doxil (doxorubicin liposomes): for Kaposi's Sarcoma.

Front 42

What are the characteristics of Doxil?

Back 42

1) The drug is water-soluble: increased Doxuribacin half-life

2) Improved parameters: Also localized the drug to tumor sides, with possible reduced cardiac toxicity!

Front 43

Give an example of other liposome products.

Back 43

Ambisome (amphotericin B liposomes): antifungal product.

Decreased renal accumulation of Amphoteracin B. Less nephrotoxicity.

Front 44

What are Albumin nanoparticles?

Back 44

These are albumin particles with a mean diameter of nanometer proportions.

Front 45

Give an example of Albumin nanoparticles

Back 45

Paclitaxel (Abraxane Injectable Suspension)

Front 46

Paclitaxel is a very ____ drug that is formulted with ____ (Cremophor EL) and 50% alcohol.

Back 46

lipophilic drug

surfactan.

Significant hypersensitivity, requires pre-med Glucocorticoids.

Front 47

In Abraxane, albumin nanoparticles are coated with paciltaxel, and not formulated with surfactant and alcohol.

(Statement, not a question)

Back 47

Statement, not a question.

Front 48

Abraxane (True or False)

Cemphor/Alcohol needed.

No need for glucocorticoid premed.

Back 48

FALSE.

NO NEED Cemphor/Alcohol needed.
----------------------------------------
TRUE.

No need for glucocorticoid premed.

...remember that paclitaxel needs glucocorticoids.