Formulation and delivery of Insulin Flashcards Preview

PM3B: Autumn > Formulation and delivery of Insulin > Flashcards

Flashcards in Formulation and delivery of Insulin Deck (15):
1

What are the main differences between a small molecule and therapeutic protein

Small molecule: typical drug
Carbon chain
Low homogenous
Site of action delivery

Therapeutic protein:
Hydrophilic to polypeptide
High single protein with moderate heterogeneity
Site of action: Insulin, flu vaccines

2

What are the four categories for biologicals and give examples of each

1. Gene therapy (nucleic acid)
Gendicine

2. Polypeptides
Proteins and peptides- insulin, growth hormone, clotting/blood factors

3. Monoclonal antibodies
Trastuzumab- herceptin
Rituximab- Mabthera
Infliximab- Remicade

4. Vaccines
Influenza vaccine
BCG tuberculous vaccine
Hepatits B

3

What are the three challenges for all biologics

Complexity- higher than normal drugs

Instability- biological origin makes it more unstable

Availability- often limited by large molecular size

4

What is immunogenicity

Immune response to drug (hypersensitivity)

Leads to loss of efficacy and more serious adverse effects

5

Why are biologics so unstable

Biological origin

Conditions must be compatible with biological molecules- good food for microbes

Proteins have 3-4 layers of vital structure that can degrade with reactions via H2O and O2- irreversible change

6

What are the four protein structures and describe each one briefly

Primary structure- amino acid sequence

Secondary structure- regular sub structures (alpha helix and beta sheet)

Tertiary structure- 3D structure

Quaternary structure- complex protein molecule

7

How do you normally deliver biologics and why these routes

Biologics have large molecular size

1. Permeability through epithelia (biomacromolecules wont pass through here though)

2. Access to tissues from blood vessels

3. Cell membranes- although drug target not normally within cells

8

What are the two methods of manufacturing proteins and examples of proteins made by each of these methods

Biotechnology: Produced in microbial or animal cell cultures and isolated via chromatographic and filtration steps
Example: Insulin, erythropoietin, monoclonal antibodies and interferons

Isolate from blood:
Examples: albumin and blood clotting factors
focused on reduction of viral contamination

9

What are the four different types of insulin

Rapid Acting
Short Acting
Intermediate Acting
Long Acting

10

Describe rapid acting insulin and give some examples

Short onset of action and short duration time

examples:
Insulin Lispro (Humalog)
Insulin Aspart (NovoRapid)
Insulin glulysine (Apidra)

11

Describe long acting insulin and give some examples

Longer effect than intermediate acting insulins

Normally used ONCE daily to maintain basal insulin level (2-4 days achieves steady state)

Examples:
Insulin glargine (LANTUS)
Insulin determir (levemir)
Insulin degludec (tresiba)

12

What are the different ways insulin forms are modified

Modification of aggregation, quaternary structure and crystallinity alters SOLUBILITY and AVAILABILITY

13

What are the three basic insulin regimes and describe each of them

1. ONE, TWO or THREE insulin injections per day:
Short acting or rapid acting insulin analogue with an intermediate acting insulin

2. MULTIPLE DAILY INJECTIONS
Short acting or rapid acting insulin analogue injected BEFORE MEALS
Can be used together with one or more separate daily injections of intermediate acting or long acting

3. CONTINUOUS SUB CUTANEOUS INSULIN INFUSION
Includes: Programmable pump that delivers a regular continuous amount of insulin that is short or long acting- via subcutaneous needle or cannula

14

What are the different devices available for insulin administration

1. Pre-filled injectors (subcutaneous)

2. Syringe and needle

3. Injectors and auto injectors

4. Needle free injectors

5. Pumps

15

What are the future insulin delivery methods that are thought to be in development

Needle free injectors

Inhaled

Transdermal

Oral insulin- micro encapsulation