Oral Solution Dosage Forms - ALL NOTES Flashcards

1
Q

How can rate of absorption be limited?

A

-By precipitation when a solution is overly concentrated so will come out of solution

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2
Q

What is a pharmaceutical solution?

A

-Liquid preparations in which the therapeutic agent and the various exipients are dissolved in the chosen solvent system

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3
Q

What are advantages of pharmaceutical products as solutions?

A

-Aids young children and people that struggle;e to swallow
-Can be flavoured
-Drug is already dissolved so quicker uptake

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4
Q

What are disadvantages of pharmaceutical products as solutions?

A

-Not as stable as a tablet
-bulky to store, ship and carry
-Bottle could break
-Not suitable for drugs that are hydrolised or insoluble

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5
Q

What is an example of a co-solvent?

A

-Ethanol
-Glycerol

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6
Q

What is an example of an antioxidant ?

A

-Ascorbic acid

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7
Q

What is an example of an antimicrobial preservative ?

A

-Benzalkonium chloride

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8
Q

What is an example of a pH adjuster?

A

-citric acid

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9
Q

What is an example of an isotonic adjuster?

A

-Sodium chloride
-glucose

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10
Q

What is an example of a viscosity enhancer?

A

-Hydroxmethylcellulose

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11
Q

What is an example of a chelating agent?

A

-EDTA

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12
Q

What is an example of a natural sweetener?

A

-Sucrose

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13
Q

What is an example of an artificial sweetener ?

A

-Aspartame

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14
Q

What kind of water must be used in parenteral solutions?

A

-Distilled then further purified to remove pyrogens

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15
Q

What kind of water must be used in non-parenteral solutions?

A

-Distilled

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16
Q

What is high solubility?

A

-Readily incorporated into the vehicle and formulated as an oral solution

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17
Q

What is moderate solubility?

A

-Solubility enhanced using co-solvents or related methods

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18
Q

What is low solubility?

A

-Formulated as an alternative dosage form eg suspension

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19
Q

What physicochemical factors affect solubility of therapeutic agents?

A

-Molecular weight
-Particle size
-Number of hydrogen bonds
-Hydrophilic groups
-Amorphous properties

20
Q

What happens if the pH>pKa of an acid drug?

A

-Solubility of acidic drug increases

21
Q

What happens if the pH<pKa of a basic drug?

A

-Solubility of basic drug increases

22
Q

Aspirin pKa =3.0
pH stomach = 1.2
Will the weak acid more mainly ionised or unionised?

A

-Unionised

23
Q

Aspirin pKa =3.0
pH stomach = 6.8
Will the weak acid more mainly ionised or unionised?

A

-ionised

24
Q

Chlorpromzine pKa = 5.0
pH stomach = 1.2
will the weak base more mainly ionised and unionised?

A

-Ionised

25
Q

Chlorpromzine pKa = 5.0
pH stomach = 6.8
will the weak base more mainly ionised and unionised?

A

-unionised

26
Q

What is the acceptable pH range for oral administration?

A

-5 to 8

27
Q

How can pH be optimised?

A

-use of a buffer

28
Q

How can you convert a weak acid to a salt?

A

-If you increase the pH in the diffusion layer the dissolution rate and saturation solubility will increase even though the bulk pH is the same

29
Q

Why can’t some weak acids be converted to salts to increase solubility?

A

-May be more prone to hydrolysis, chemical stability, manufacturability

30
Q

How can co-solvents increase solubility?

A

-Used as well as water to enhance the solubility by allowing more ionisation

31
Q

How does micellar solubilisation work?

A

-Incorporates drugs into or onto micelles

32
Q

What is cyclodextrin complexation?

A

-Enzymatically modified starches composed of glucopyranose with a hydrophobic cavity, hydrophilic exterior that holds a hydrophobic drug with poor water solubility

33
Q

What approaches can help drug solubilisation?

A

-pH
-Co-solvent
-Complexation
-Change to salt
-Disperse phase
-More amorphous

34
Q

What is a vehicle ?

A

-Drugs can put themselves in to be transported

35
Q

What is pourability?

A

-How well a solution can be poured, relates to viscosity

36
Q

What is palability?

A

-How agreeable the taste of a solution is

37
Q

What are the purposes of excipients ?

A

-Facilitate administration
-Protect the formulation from issues regarding physical and chemical stability

38
Q

What are the purposes of buffers?

A

-Control pH of the formulated product to maintain solubility and enhance stability

39
Q

What are the purpose of sweetening agents?

A

-Increase the palatability of the therapeutic agent

40
Q

What are the purpose of viscosity-enhancing agents?

A

-Ensure the accurate measurement of the volume to be dispensed

41
Q

How is viscosity increased?

A

-The addition of non-ionic or ionic hydrophilic polymers

42
Q

What is the purpose antioxidants ?

A

-Enhance the stability of therapeutic agents that are susceptible to chemical degradation by oxidation

43
Q

What are chelating agents?

A

-Form complexes with heavy metal ions involved in oxidative degradation of therapeutic agents

44
Q

What do preservatives do?

A

-Control the microbial bioburden of the formation

45
Q

What are the ideal properties of preservative?

A

-Broad antimicrobial spectrum
-chemically and physically stable over the shelf life
-low toxicity