Lecture 1 Flashcards

1
Q

Solution

A

Homogeneous molecular dispersion

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2
Q

Emulsion

A

Oil in water, water in oil, looks like bubbles

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3
Q

Suspension

A

Solid in water or oil, looks like dirt

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4
Q

Solution dosage form examples

A

Injectables, nasal solutions, opthalmic solutions, otic solutions, irrigation solutions, enemas, douches, gargles, mouthwashes, juices

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5
Q

Advantages of solution dosage forms

A

Homogeneous no problems of content uniformity, easy to manufacture, good bioavailability

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6
Q

Components of solution dosage forms

A

Active ingredient = drug
Solvent = water, vegetable oils
Cosolvent = ethanol, glycerin, propylene glycol
Buffering agent
Preservative
Antioxidant, chelating agent
Flavor and sweetener = sucrose, sorbitol

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7
Q

Buffer

A

Solution of weak acid and salt of its conjugate base

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8
Q

Weak acid removes

A

added base

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9
Q

Salt removes

A

added acid

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10
Q

Henderson hasselbalch equation

A

ph=pka + log A-/HA

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11
Q

Buffering capacity

A

Ability of a buffer to resist a change in pH due to added OH or H

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12
Q

Van slyke equation

A

b=2.3C ka[H3O]/Ka+[H3O]^2
C = total buffer concentration
Max when pH=pka

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13
Q

Selection of pH

A

Use pH that provides maximum stability for drug
Minimize irritation with parenteral, opthalmic, or nasal dosage forms by adjusting to be the same pH of body fluid

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14
Q

pH of blood, interstitial fluid, and tears

A

7.4

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15
Q

Other ways to minimize buffering capacity besides pH

A

Minimize volume, administer slowly

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16
Q

Antimicrobial preservative purpose

A

protect patient from pathogens
maintain potency and stability of dosage forms

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17
Q

Antimicrobial preservative mechanism of action

A

Preservatives adsorb to bacterial membrane and disrupt it. Bacterial membrane is lipophilic and has a net negative surface charge

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18
Q

Adsorption due to lipid solubility

A

alcohols, acids, esters

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19
Q

Adsorption due to electrostatic attraction

A

Quaternary ammonium compounds

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20
Q

Ampules allowed bacterial content

A

Must be sterile, single dose, no preservative needed

21
Q

Multiple dose vial allowed bacterial content

A

must be sterile, may contain 10 doses, need a preservative to kill microorganisms introduced during use

22
Q

Opthalmic solution allowed bacterial content

A

must be sterile, must contain a preservative if packaged in multiple dose container

23
Q

Oral liquid allowed bacterial content

A

need not be sterile but should not contain pathogens. FDA limits number of organisms to be less than 100 per mL, need preservative for multiple dose packages

24
Q

Oral solids allowed bacterial content

A

Less likely to carry bacterial than liquid forms, test raw materials to be sure manufacturing facility is clean

25
Q

Ideal preservatives

A

effective in low concentrations against a wide variety of organisms
soluble in formulation
non toxic
stable

26
Q

Pharmaceutical preservatives

A

Alcohols, acids, esters of p hydroxybenzoic acid (parabens), quaternary ammonium compounds

27
Q

Alcohols

A

Ethanol, benzyl alcohol, chlorobutanol

28
Q

Ethanol

A

requires greater than 15% limited to oral products, may be lost due to volatility

29
Q

Benzyl alcohol

A

Local anaesthetic action, burning taste (not use orally), water soluble, stable over wide pH range, widely used in parenterals

30
Q

Chlorobutanol

A

Campor like odor and taste, not used orally, used in parenterals and Opthalmics, volatile, lost through rubber stoppers and plastic containers

31
Q

Acids

A

only active in unionized lipid soluble form

32
Q

benzoic acid

A

pka 4.3, used in oral products

33
Q

Sorbic acid

A

pka 4.8, used in oral products, excellent in molds and yeast

34
Q

Esters of p-hydroxybenzoic acid (Parabens)

A

Widely used orally, hydrolyze rapidly at pH values above 7, anesthetize tongue
Low solubility is problem, causes skin sensitization when used in dermatological products

35
Q

Propyl paraben and butyl paraben

A

Most lipophilic esters, best against mold and yeast

36
Q

Methyl paraben and ethyl paraben

A

Lease lipophilic esters, best against bacteria

37
Q

Quaternary ammonium compounds

A

Benzalkonium chloride (zephirin), cetyltrimethylammonium chloride (cepryn), widely used in opthallmics, water soluble and fast killing, incompatibility issues due to positive charge

38
Q

pH affect on preservative action

A

Only unionized species of weak acids are effective as preservative, add more total weak acid when pH is above pka to have effective concentration of unionized species

39
Q

Complex formation effect on preservative action

A

Only uncomplexed free preservative is active

40
Q

Adsorption by solids effect on preservative action

A

only the unadsorbed preservative is active

41
Q

Chemical stability effect on preservative action

A

Consider the shelf life

42
Q

Antioxidants

A

Drug substances that are less stable in aqueous media than in solid dosage forms, reactions may occur from ingredient-ingredient interactions/container product interactions

43
Q

Oxidation

A

Main degradation pathway of pharmaceuticals, initiated by heat, light, peroxides, metals (copper or iron)

44
Q

Auto-oxidation

A

automatic reaction with oxygen without drastic external interference

45
Q

Free radical scavengers

A

retard, delay oxidation by rapidly reacting with free radicals

46
Q

Examples of free radical scavengers

A

Propyl, octyl, dodecyl esters of gallic acid, BHA, BHT, tocopherols, Vitamin E

47
Q

Reducing agents

A

Have lower redox potentials than drug, more readily oxidized

48
Q

Examples of reducing agents

A

Sodium bisulfite, ascorbic acid, thiols

49
Q

Chelating agents

A

Antioxidant synergists, little antioxidant effects, remove trace metals like citric acid, EDTA