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S3 Case 3 - Musculoskeletal > Principles of Depot Injections + Formulations > Flashcards

Principles of Depot Injections + Formulations Flashcards

1
Q

What are the advantages of long acting injectables?

A

Predictable drug release profile
Better patient compliance
Ease of application
Avoidance of 1st pass
Reduced dosing
Decrease incidence of side effects
Cost reduction

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2
Q

What are the different route of applicable injection?

A

SC
IM

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3
Q

What’s good about SC?

A

Greater surface area
Shorter needles
Less discomfort
Better safety profile

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4
Q

What’s bad about SC?

A

Limited to no more than 1-2ml

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5
Q

What is SC the primary route for?

A

Protein-based drugs

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6
Q

What’s good about IM?

A

Greater injection vol

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7
Q

What are the types of long acting injectable formulations?

A

Oil-based solutions
Drug suspension
Polymer-based

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8
Q

What are oil-based solutions suitable for?

A

Steroid esters
eg. contraception, hormone replacement therapy + antipsychotics

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9
Q

What is the route of injection for oil-based solutions?

A

IM

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10
Q

What is the important formulation consideration of oil-based solutions?

A

Drug solubility
Drug partitioning
Vehicle viscosity

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11
Q

What are the properties of oil vehicles?

A

Vegetable oil
Synthetic fatty acid esters
Castor oil

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12
Q

What is the partition coefficient?

A

Ratio of drug activities in 2 immiscible solvents comprising the partitioning system

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13
Q

What is the rate-limiting step of drug absorption in drug suspensions?

A

Dissolution of drug particles

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14
Q

What are poorly water-soluble salt formations used for in drug suspensions?

A

Control dissolution rate of drug particles to prolong the absorption

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15
Q

What are polymer-based systems suitable for?

A

Macromolecules - eg. peptides, proteins

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16
Q

What are the advantages of polymer-based systems?

A

In vitro + in vivo stabilisation of macromolecules
Extension of biological half life
Improvement of systemic availability

17
Q

What polymer properties play a role into drug release?

A

Composition of copolymer ratios
Hydrophilicity/hydrophobicity
Molecular mass
Glass transition temperature

18
Q

What is an example of appropriate polymers?

A

Biodegradable microspheres

19
Q

How does the release process of microspheres work?

A

From surface, through pores, diffusion through polymer barrier, diffusion through water-swollen barrier, polymer erosion + bulk degradation

20
Q

What are in situ-forming gels?

A

Made of biodegradable products, injected into body then congeal to form solid implant

21
Q

Describe how in situ-forming gels work

A

Drug-polymer solution injected in a suitable solvent system
Solvent diffuses out = water insoluble polymer solidifies + entraps drug
Drug slowly released from biodegradable depot

S3 Case 3 - Musculoskeletal (14 decks)

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