Solutions Flashcards

1
Q

what is a solution

A

a homogenous one-phase system consisting of two or more components

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2
Q

solvent

A

phase in which the dispersion occurs

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3
Q

solute

A

the component which is dispersed as small molecules or ions in the solvent

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4
Q

types of solution

A

aqueous or non-aqueous

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5
Q

advantage of solutions as oral dosage form

A
  1. easy to swallow (peds)
  2. drug immediately available for absorption
  3. uniform distribution
  4. less irritation than capsules
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6
Q

disadvantage of solutions as oral dosage form

A
  1. bulky and inconvenient to transport or store
  2. poor stability (esp if drug susceptible to hydrolysis)
  3. prone to microbial growth/ contamination
  4. unpleasant taste of drug
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7
Q

types of preparations to be made

A
  1. potable water
  2. purified water BP
  3. water for injection BP
  4. water free from carbon dioxide or air
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8
Q

cosolvency

A

solubility of a weak electrolyte or non-polar compound in water can be improved by the addition of a water-miscible solvent in which the compound is also soluble

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9
Q

what are cosolvents

A

vehicles used in combination to increase the solubility of a drug

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10
Q

what is the solubility of a drug affected by

A

dielectric constant of solvent system, ideally dielectric constant should be 25-80

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11
Q

pH control

A

if drug is either a weak acid/base, its degree of ionisation and consequently its solubility are influenced by the pH of the solubility, ensure pH does not conflict with other product requirement

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12
Q

solubilization

A

concentration of surfactant used should be above its critical micellar concentration- micellar solubilization

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13
Q

what is the range of values for hydrophilic surfactant to be a useful solubilising agent

A

above 15 HLB value

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14
Q

how can solubility be improved

A

adding surfactant, however a large excess of surfactant is undesirable

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15
Q

factors that affect choice of solubilising agents

A
  1. toxicity and irritancy
  2. miscibility with solvent system
  3. compatibility with other components
  4. odour and taste
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16
Q

example of solutions with solubilising agents

A
  1. fat soluble vitamins + polysorbates
  2. iodine + macrogol ethers
  3. steroids + polyoxyethylated castor oil
  4. cresol + chloroxylenol + potassium soap of fatty acids
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17
Q

example of combi of cosolvent and solubilising agents employed to improve solubility

A
  1. vitamin A + polysorbate 80 + glycerol

2. chloroxylenol + potassium ricinoleate + ethanol terpineol

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18
Q

chemical modification

A

involves synthesis of soluble salts of the drug; soluble salt which may not have any activity is converted back to active base in biological system

19
Q

example of chemical modification

A
  1. sodium phosphate salts of hydrocortisone, prednisolone, and betamethasone
  2. sodium succinate salt of chloramphenicol
20
Q

particle size reduction

A

size and shape of very small particles (< 1 micron) can affect their solubility, but less commonly employed to improve solubility

21
Q

how are particle size commonly reduced

A

milling

22
Q

non-aqueous solutions

A

solvents are classified as

  1. fixed oils of vegetable origin,
  2. alcohols,
  3. polyhydric alcohols,
  4. mineral oils
  5. and others
23
Q

why are non-aq solution employed

A
  1. prepare solution of drugs which are unstable in water

2. prepare intramuscular injections of drugs for depot therapy

24
Q

alcohol for external use only

A
  1. industrial methylated spirit (ethanol with 5% methanol as denaturant)
  2. isopropanol
25
Q

alcohol

A

commonly employed in low concentration, as a cosolvent with water in the formulation of aqueous solution for oral and parenteral use

26
Q

polyhydric alcohols

A

commonly used as cosolvent with water in the formulation of injections

27
Q

example of polyhydric alcohol

A
  1. glycercol (E & I): phenol ear drops BPC 1973
  2. propylene glycol (E & I): Digoxin injection BP, Phenobarbitone Injection BP, Chloramphenicol Ear Drops BP
  3. Polyethylene glycols of low MR (E&I): Erythromycin Ethylsuccinate injection BP
  4. Dipropylene Glycol, Diethylene glycol, Ethylene glycol (E only cause toxic): veterinary and horticultural use
28
Q

Mineral oils

A

internal external use, limited use as solvent in pharma preparation due to oily tacky nature; veg oil preferred; more often used in formulation of emulsion

29
Q

what are not for internal use

A
  1. xylene (eardrops)
  2. ethyl ether (cosolvent with OH in collodions, extraction of crude drug)
  3. isopropyl myristate, isopropyl palmitate (cosmetics)
  4. dimethylsulphoxide, dimethylformamide, dimethylacetamide (veterinary)
  5. kerosene (insecticides)
30
Q

buffers

A

employed to resist any change in pH when acid/alkali added

31
Q

example of buffers

A

carbonates, citrates, gluconates, lactates, phosphates, tartrates, borates

32
Q

color

A

employ to improve attractiveness and enable easy identification of products

33
Q

how may stability of color be affected by

A

pH, ultraviolet radiation, presence of oxidizing or reducin agents

34
Q

types of colors

A
  1. natural: show variation in chemical composition and are less stable, but more widely accepted (carotenoids, chlorophylls, anthocyanins)
  2. synthetic: coal tar dyes, brighter n=more stable colors (sodium salts of sulphonic acids)
35
Q

natural sweetening agent

A

sucrose, fructose, sorbitol, mannitol, glycerol, xylitol, hydrogenated glucose syrup, isomalt, honey , liquorice

36
Q

artificial sweetening agent

A
intensify sweeteners (<0.2%); tendency to impart bitter/ metallic after taste
eg: saccharin, aspartame, acesulfame, potassium, thaumatin
37
Q

flavours

A

employed to make oral products more palatable while fragrances improve the appeal of the product

38
Q

eg of flavor/fragrance

A

fruit juice, aromatic oils, herbs, spices

39
Q

preservative

A

prevent microbial contamination of product

40
Q

antioxidants

A

prevents degradation of compounds by oxidation

41
Q

isotonicity modifiers

A

adjust tonicity of large volume solutions for parenteral and ophthalmic use

42
Q

density modifiers

A

to adjust the density of spinal anaesthetics

43
Q

how are pharmaceutical solutions manufactured

A

mixers: propeller, turbine, paddle

44
Q

how are pharmaceutical solutions evaluated for quality

A

drug content, density, tonixity, viscoxity (topical), clarity/particulate, color, sterility (parental/opth)