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Gary's lecture (Pharmaceutics) > Solutions and solubility: Pharmaceutical oral solutions > Flashcards

Solutions and solubility: Pharmaceutical oral solutions Flashcards

1
Q

Give an example of an extemporaneous formulation?

A

Thiamine (Vitamine B1) HCL oral liquid

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2
Q

What s solubility affected by?

A
  • pH

- Temperature (Drug should be in solution at all strengths

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3
Q

List the four different types of solutions?

A
  • Oral solutions
  • Oral elixirs
  • Oral syrups
  • Others including mouthwashes, gargles, rectal solutions and enemas
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4
Q

What are pharmaceutical oral solutions?

A

These are liquid preparations in which the therapeutic agent and the various excipients are dissolved in the chosen solvent system.

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5
Q

Pharmaceutical solutions for parental administration, or specific formulations require aseptic manufacture. TRUE OR FALSE?

A

TRUE

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6
Q

What are the advantages of using oral solutions?

A
  • Ease of use/ administration (i.e children or elderly)
  • The drug is dissolved and readily available for absorption (As long as the drug is soluble in stomach it will have a greater bioavailability than solid dosage form)
  • Modification of taste can improve compliance of bitter tasting drugs.
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7
Q

What are the disadvantages of using oral solutions?

A
  • Stability (cannot be used for drugs that are not stable in water e.g aspirin)
  • Limited by the solubility of some drugs (only suitable for drugs with particular solubility profiles)
  • Expensive to transport, compared to other dosage forms
  • Bulky for patients to carry with them
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8
Q

List the common types of excipients?

A
  • Flavours and colours (sweeteners, dyes)
  • Preservatives
  • Vehicle (purified water)
  • Co-solvents (glycerol, ethanol)
  • Solubility enhancing agents (surfactants)
  • Viscosity modifiers
  • Buffers
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9
Q

Solute-solute interactions are unfavourable but it is entropically viable. TRUE OR FALSE?

A

TRUE

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10
Q

What are homogenous products?

A

Product must be in solution throughout all of the drugs shelf life, including excipients as well

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11
Q

Solubility at selected pH may be high , moderate and low. TRUE OR FALSE?

A

TRUE

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12
Q

What are the factors affecting solubility?

A
  • Crystal form (polymorphism)
  • Melting point
  • Chemical factors (lipophilicity, ability to ionise)
  • pH will affect the solubility of acids and bases
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13
Q

At pH above the pKa, the solubility of acidic drugs increases. TRUE OR FALSE?

A

TRUE

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14
Q

At pH below the pKa, the solubility of basic drugs increases. TRUE OR FALSE?

A

TRUE

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15
Q

How do zwitterions behave?

A

They behave as acidic at basic pH and bases at acidic pH

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16
Q

Which one of the following is most stable form of paracetamol, Monoclinic or Orthorhombic?

A

Monoclinic

17
Q

Orthorhombic undergoes plastic deformation due to a wellodefined planar structure and is suitable for direct compression. TRUE OR FALSE?

A

TRUE

18
Q

Are salts forms more water soluble than free acids/bases and more stable?

A

YES

19
Q

How can you optimise solubility?

A
  • Salt form - more water soluble than free acid/base and more stable
  • Modify pH - so salt form and ionised form predominates and solubility increases
  • Co-solvents - Improves solubility for chemicals with poor aqueous solubility, but offer issues with toxicity
20
Q

What is Cyclodextrin used for?

A

Used for masking properties of drug

21
Q

What is Calixarene used for?

A

Used for masking properties of drugs, however, this is three dimensional. (they rotate and produce different conformations)

22
Q

Give an examples of aqueous vehicle?

A

Purified water Bp or USP prepared by distillation, ion exchange or reverse osmosis

23
Q

Purified water is not to be used for parental formulation ,water is used for injections. TRUE OR FALSE?

A

TRUE

24
Q

Give examples of co-solvents?

A

Glycerol - miscible in water
Alcohol USP
Surfactants

25
Q

Give examples of what do buffers do and provide examples?

A

Control pH, in doing so they maintain pH dependant solubility and optimise the product

  • They enhance stability of drugs that may be susceptible to acid or base catalysed hydrolysis
  • for example Acetates/citrate/phosphate buffered saline
26
Q

Give examples of Sweetening agents?

A

Sucrose/liquid glucose/glycerol

27
Q

Give examples of Viscosity modifiers?

A

Non ionic cellulose derivatives/ ionic polymers

28
Q

Give examples of the excipient antioxidants?

A

Sodium sulphite/ formaldehyde

29
Q

What are preservatives used for and give examples?

A

Used to control the microbial load in a formulation which should be kept below the minimum inhibitory concentration
-E.g Parabens/ sodium benzoate

30
Q

Preservatives are not affected by other ingredients such as buffers, micelles or hydrophilic polymers. TRUE OR FALSE?

A

FALSE

Gary's lecture (Pharmaceutics) (7 decks)

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