AP - Eye & Ear, Parenteral, Nasal & Pulmonary Drug Delivery Flashcards

1
Q

Preformulation information?

A
  • solubility
  • pKa
  • stability (in solution, formulation and API itself)
  • log P
  • toxicity profile
  • analytical assay
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2
Q

Auricular or Otic or Aural drug delivery means drug delivery to the…

A

ear.

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3
Q

Since drug is only applied to outer part of ear, drug is not absorbed ________.

A

systemically. Therefore, topical drug delivery rules apply.

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4
Q

In order to have a stable suspension, and want some interaction between a drug with average-low water solubility, and the solvent, you can add a ________.

A

Wetting agent - surfactant

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5
Q

What can modify viscosity?

A

Gelling agents

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6
Q

Name a few flocculating agents.

A
  • Electrolytes (sodium salts - acetate, phosphate)
  • ionic surfactants
  • polymeric agents
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7
Q

How do you prepare a suspension

A

Dissolve buffer in solvent. Add buffering agent, preservative and gelling agent (viscosity modifier) and mix to get uniform clear solution. Add the API last and mix thoroughly.

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8
Q

During suspension preparation, why is the API added last?

A

To ensure only API is suspended and not the other excipients such as gelling agent.

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9
Q

What are the stability tests for suspensions? (Three things)

A
  • Particle size analysis (make sure it hasn’t increased in size as this can cause local irritation)
  • Viscosity
  • Degree of flocculation
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10
Q

Ocular drug delivery are used for…

A

the eye.

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11
Q

Eye formulations are delivered ______

A

locally.

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12
Q

Solutions can be dispensed as _____ and _____

A

drops and irrigation solutions

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13
Q

Suspensions can be dispensed as ______

A

drops.

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14
Q

Particle size for eyes must be

A

< 100um

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15
Q

Eye drops or anything administered to eyes MUST be

A

sterile.

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16
Q

Buffering capacity for eye should have a pH of _____

A

7.4

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17
Q

Define parenteral drug delivery.

A

Administration of drug not through alimentary canal but rather by injection through an alternate route e.g. subcutaneous (under skin), IM (depot injections - oily solutions), IV (can be short acting/ long acting infusions), IA (infusions), IS (anti cancer, epidural), ID (vaccines), IC (adrenaline) e.t.c.

18
Q

What are some reasons for using parenteral drug delivery?

A
  1. If drug is not stable in GI tract and cannot go through any other route of administration e.g. insulin
  2. GI enzymatic activity
  3. Low absorption –> 1st pass metabolism
  4. Variable absorption from patient to patient
19
Q

Advantages of parenteral?

A
  • Quick drug delivery
  • Rapid onset of action
  • Ideal alternative when oral therapy is not possible
  • Accurate dosage
  • Used for systemic and local effect
  • Implants and depot for prolonged action
  • Suitable for parenteral nutrition and for continuous medication
20
Q

Disadvantages of parenteral?

A
  • Patient compliance
  • Administered by trained medical professionals
  • Once administered, no way it can be altered –> nearly impossible to reverse the effects
  • Stringent manufacturing and packing requirements leading to higher production costs
21
Q

Types of parenteral formulations

A
  • Solutions (can be dispensed individually as powders with a separate solvent)
  • Suspensions (can be dispensed individually as powders with a separate vehicle)
  • Liposomes
  • Emulsions
22
Q

What is the dose for small volume parenteral products?

A

0.1ml - 1.5ml

single bolus injection suitable for i.m, s.c, i.v etc

23
Q

What is the dose for large volume parenteral products?

A

> 100ml

usually for parenteral nutrition

24
Q

Choice of small volume or large volume depends on…

A

if you want it to act immediately (SVP) or over a long period of time (LVP).

25
Q

Disadvantage of SVP?

A
  • Fixed conc (manufacturer regulated)

- If frozen –> thawing –> can lead to altered product stability.

26
Q

What are the excipients for injections?

A

PASSBV

  • Preservatives
  • Antioxidants
  • Solvents; aqueous - water for injection; aqueous miscible - propylene glycol, glycerol, PEG
  • Solubilising agents e.g. surfactants
  • Buffers; salts e.g. NaCl
  • Viscosity modifiers e.g. methylcellulose
27
Q

Water for injection is obtained by which process? ______ or _______ _______

A

Distillation or Reverse osmosis

28
Q

Water for injection is free from _____, ______ and _______

A

particulates, pyrogens and bacteria.

29
Q

Water for injection; quick production to utility to minimise _________

A

contamination.

30
Q

Water miscible solvents are used as co-solvents to increase _______/ _______.

A

solubility/ stability.

31
Q

Non aqueous are usually used for _______

A

intramuscular depot injections

32
Q

Preservatives are used at much lower concentrations for parenteral injections than topical formulations. Why?

A

Because they are sterile manufactured or stabilised. Therefore, need to keep small amounts to maintain sterility.

33
Q

What are buffer salts used for in parenteral drugs?

A

To stabilise the drug.

34
Q

What is blood osmolality value?

A

280 - 303 milliosmoles.

35
Q

Which is preferred hypertonic or hypotonic?

A

Hypertonic

36
Q

Nacl, dextrose and mannitol are all?

A

Tonicity modifiers

37
Q

What are some buffers used in parenteral products?

A
Ammonium
Acetate
Bicarbonate
Citrate (used for acidic)
Phosphate (used for ph 5-7)
38
Q

If parenteral product is sterile, only need to add preservative if… ?

A

multi dose units are used

39
Q

If a drug has poor water solubility what can you do?

A
  • pH manipulation –> make it more acidic/ alkaline
  • use co-solvents
  • surfactants
  • complexing agents
  • emulsions
  • NEED TO ANALYSE STABILITY OF FINAL PRODUCT BEFORE GOING AHEAD.
40
Q

Particle size for suspension in injections is

A

< 5um

41
Q

What are some adverse effects following parenteral administration

A
  • Precipitation
  • Haemolysis due to hypotonic formulations
  • Pain (IM route due to pH or co-solvent conc)
  • Phlebitis - pain, oedema
42
Q

What is the QC or injections?

A

sterility test
pyrogen test
particulate matter
microscopic test