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Pharmaceutics I > Final Exam > Flashcards

Final Exam Flashcards

1
Q

ointments, creams, pastes, gels, foams, suppositories

A

pharmaceutical semisolids

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2
Q

intended for application to the skin surface (dermal, transdermal), mucous membranes (ophthalmic, nasal, oral cavity, rectal, vaginal), body cavities (suppositories, rectal, vaginal, urethral)

A

semisolids applications

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3
Q

most difficult epidermal barrier for drugs to cross

A

stratum corneum

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4
Q

drugs are applied to the skin to provide effects:
1. on the skin surface (protective film, sunscreen, surface cleansing, antiseptic)
2. within the stratum corneum layer of skin (several skin diseases like psoriasis, eczema, zerosis - moisturizers and drug reservoir of depot)
3. for deep-seated conditions requiring penetration of drugs into the epidermis and dermis (dermal products for acne, cellulitis, dermatitis)
4. for systemic therapeutic outcomes (transdermal products for systemic bioavailability)

happens along the hair follicular duct and sweat gland or through the epidermis

A

semisolid drug delivery to the skin

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5
Q

most transdermal drugs are absorbed through the ______

A

epidermis because the amount of hair follicles/sweat glands is different from person to person and epidermis is much larger surface area for drug absorption

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6
Q
  1. absorption and penetration (skin permeability, nature of drug/excipients/drug products)
  2. effect on skin function
  3. miscibility and compatibility with skin secretions and serum
  4. freedom from irritant effect
  5. emollient properties (moisturizing components)
  6. ease of application and removal (washability)
A

dermatological factors of semisolids

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7
Q
  1. biological factors (related to the skin)
    - skin condition, age, site of application
    - blood flow to the skin
    - skin metabolism
    - skin hydration, pH, temperature
  2. physiological factors (related to the drug and drug product)
    - partition coefficient, lipophilicity, solubility
    - drug concentration, type of dosage form, type of base
    - molecular size, pH, ionization
    - excipients (penetration enhancers, antioxidants, etc.)
A

factors influencing dermal penetration of drugs

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8
Q
  1. intercellular lamellar lipids
  2. diffusion path length
  3. natural moisturizing factor (NMF) - complex mixture of low-molecular-weight, water soluble compounds (humectant, helps retain/attract moisture), urea, lactic acid, amino acids, PCA
  4. degree of exfoliation - counseling point to avoid shaving before transdermal application
A

percutaneous absorption depends on these things

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9
Q

keratin (fibrous proteins), natural moisturizing factors (NMFs), and 15-20% water

A

corneocytes in stratum corneum

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10
Q

barrier for hydrophilic drugs, hold the cells together and keep the skin elastic/pliable

A

intracellular lipids of stratum corneum

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11
Q

disruption of the barrier by irritants and allergens, sensitization and inflammation of the skin and mucus membrane (allergic reactions), increased epidermal proliferation and changes in differentiation, changes in lipid composition, impaired barrier function

A

skin permeability barrier function impaired in eczema (atopic dermatitis)

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12
Q

ointments may be easily spread on skin (external, local action, site specific), provide lubricating/emollient effects that may reduce trauma or inflammation of the affected site, persist at site of application (infected/irritated skin, hemorrhoids, eyes, etc.), avoidance of first pass metabolism and GI transit, convenient for patient having difficulty swallowing, patient on polypharmacy (multiple medications)

A

advantages of semisolids

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13
Q

dose accuracy (may not be as accurate as unit dosage forms), skin irritation or contact dermatitis may occur due to drug and/or excipients (sensitivity/allergic reactions), possibility of allergic reactions due to additives like preservatives and fragrances, bulky to handle, may cause staining, poor permeability of some drugs through the skin because of properties of drug, can only be used from drugs that require very small plasma concentration for action (transdermal), large molecular weight drugs/drugs with larger particle sizes are not easy to penetrate through the skin (diffusivity)

A

disadvantages of semisolids

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14
Q

smooth texture, elegant in appearance, not causing dehydration, non-gritty, non-greasy and non-staining, non-hygroscopic

A

ideal physical properties of semisolids

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15
Q

non-irritating (less or no allergic reaction), do not alter membrane/skin function unless intended to do so (permeation enhancers increase drug penetration through the skin), miscible with skin secretion

A

ideal physiological properties of semisolids

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16
Q

easily applicable with efficient drug release, water washability (rinsability without the use of soap or detergents which could be skin irritants)

A

ideal application properties of semisolids

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17
Q

advantage of overcoming first pass metabolism of drugs, deliver drugs with a short half lifetime more easily and eliminate frequent administrations to maintain constant drug delivery (sustained release, controlled release for steady delivery and blood levels), transdermal patches for accurate dosing, better patient compliance

A

transdermal drug delivery

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18
Q

body site (skin thickness), number and cell size of the epidermis and stratum corneum, skin pH, density and distribution of hair follicles, skin hydration, sweat pores
stick to manufacturers recommended site of application

A

skin permeability varies according to these things

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19
Q

skin barrier function is reduced in children and neonates (large surface area to body weight, risk of overdosing or adverse effects)
in adults the skin barrier does not appear to be affected by aging - with increasing age the epidermis thins and keratinocytes are less adherent to each other, age-related changes in hydration and lipid structure, result in an increased barrier function of stratum corneum but only significant for hydrophilic compounds
transdermal drug delivery can be alternative route of administration for geriatric patients

A

skin permeability and age

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20
Q
  1. selection of vehicle (ointment base, TD patch) - drug stability, intended product use, site of application, product type
  2. physiochemical properties of drug - drug release from a vehicle, concentration of drug, solubility of drug in vehicle, partition coefficient of the drug between the vehicle and skin
A

formulation considerations of semisolids

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21
Q
  1. inert, non-irritating, non-sensitizing
  2. compatible with skin pH and drug
  3. good solvent/emulsifying agent
  4. emollient, protective, non-greasy, easily removable
  5. release medication readily at site of application
  6. elegant and good stability
A

ideal properties of base for semisolids

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22
Q

what is the function of butylated hydroxyanisole (BHA)?

A

antioxidant (BHA and BHT/toluene are fat-soluble antioxidants that prevent rancidification of fats and oils

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23
Q

skin can act as a barrier but with these things the penetration of drug through the skin can be improved - oleic acid, PCA, ethanol, glycol, PEGs, surfactants

A

permeation enhancers

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24
Q

hygroscopic substance, used to…
1. increase solubility of active ingredient
2. enhance skin penetration
3. hydrate skin
4. glycerin, urea, hyaluronic acid, glycolic acid, propylene glycol, sorbitol, olive oil, honey

A

humectant

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25
Q

providers assurances of batch-to-batch quality, reproducibility, reliability and performance

A

quality control

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26
Q

semisolid dosage forms intended for external application to the skin or mucous membranes (medicated and non-medicated), contain less than 20% water and more than 50% hydrocarbons waxes polyols, routes of administration include ophthalmic, topical, rectal, vaginal, nasal, transdermal

A

ointments

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27
Q

semisolid products consisting of oil-in-water emulsions, aqueous microcrystalline dispersions of long chain fatty acids or alcohols, high water content up to 50%, water-washable and more cosmetically and aesthetically acceptable, routes of administration include topical (dermal, nasal, rectal, vaginal), transdermal, NO ophthalmic products

A

creams

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28
Q

hydrocarbon, absorption, water-removable, water-soluble

A

types of ointment bases

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29
Q

also known as oleaginous bases, have no or only small amounts of aqueous components, can keep medicaments in prolonged contact with the skin and act as an occlusive dressing, have an emollient effect (softening or soothing the skin) and are difficult to wash off, do not dry out or change noticeably on aging (stable, longer shelf life), examples include hard paraffin, mineral oil, microcrystalline wax, petrolatum

A

hydrocarbon ointment bases

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30
Q

two groups:
1. anhydrous base that permits the incorporation of aqueous solutions to form a w/o emulsion (hydrophilic petrolatum, anhydrous lanolin)
2. water in oil emulsion base (creams) that permits the incorporation of additional aqueous solutions (lanolin)
exhibit a beneficial emollient effect

A

absorption bases

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31
Q

wax secreted by the sebaceous glands of wool-bearing animals

A

lanolin

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32
Q

mixture of hydrocarbons obtained from crude oil

A

petroleum

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33
Q

refined, purified, and processed petroleum

A

mineral oil

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34
Q

natural wax produced by honeybees

A

beeswax

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35
Q

wax produced by de-oiling petrolatum, removing the oil with a solvent

A

microcrystalline wax

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36
Q

washable, creams (o/w emulsion, hydrophilic ointment), more acceptable for cosmetic purposes, some medications may be more effective in these bases than in hydrocarbon bases, may be diluted with water and accept/absorb serious discharges in dermatological conditions (weeping skin), low or no occlusive property

A

water-removable base

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37
Q

o/w cream, white petrolatum, stearyl alcohol (hydrocarbon part, emollient), water, sodium dodecyl sulfate (emulsifier), propylene glycol (cosolvent), methyl and propyl parabens (preservatives), also known as vanishing creams (water evaporates from the skin for cooling effect and leaves undetectable film)

A

hydrophilic ointment

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38
Q
  1. action desired (site of application)
  2. nature of medication to be incorporated (drug’s properties, chemical stability)
  3. based on the bioavailability and stability (rate of drug release)
  4. effect of therapeutic agent on the quality of the finished product (viscosity)
A

choice of ointment base depends on these things

39
Q

which formulation provides the longest shelf life?

A

ointment

40
Q

drug material is levigated with a small amount of vehicle (the base or a levigating agent) to form a concentrate that is then diluted in geometric proportions with the remaining base
mineral oil is a levigating agent for oleaginous base

A

levigation method in ointment preparation

41
Q

use of heat, components of the base are melted together and further congealed at a constant cooling rate, heat-labile substances (APIs) or any volatile substances (perfume) are added when the temperature of the base is low enough to prevent ant decomposition or loss

A

fusion method of ointment preparation

42
Q
  1. preparation of the oil phase - heating may be required to melt some ingredients (melt the highest melting point ingredient first)
  2. hydration of aqueous phase ingredients - emulsifiers, stabilizers, preservatives dispersed in water, heating may also be used to accelerate process, heating the aqueous phase also helps to mix with the oil phase
  3. forming the emulsion - two phases are blended under vigorous agitation to form the emulsion
  4. dispersion of active ingredients and other excipients like perfume or volatile ingredients
A

preparation of creams

43
Q

parabens, phenoxyethanol, benzyl alcohol

A

commonly used preservatives in creams

44
Q

adding an emulsion into a gel (gelling agent or already formed gel)

A

emulgels

45
Q
  1. dissolution and release of drug from vehicle/formulation (concentrated in the base and SC)
  2. partition of the drug into the stratum corneum (solubility, permeability, thickness)
  3. diffusion of the solubilized drug across the stratum corneum
  4. penetration of the drug into the layers of the skin
A

percutaneous drug absorption

46
Q

apply onto only the indicated area, do not apply to large surface area, do not apply to damaged skin, do not occlude skin unless indicated, avoid excessive rubbing/heat, stop use if skin gets irritated, wash hands

A

patient counseling points on ointments/creams

47
Q

semisolid dosage forms that contain a high percentage (often up to 50%) of finely dispersed solids
- stiff consistency (don’t flow at body temp)
- stays over the area to which they are applied (don’t spread over healthy skin)
- serve as protective coatings (but not occlusive since pastes are porous)
- used in treatment of oozing lesions (absorb secretions)

A

pastes

48
Q
  1. single-phase aqueous (aqueous gel)
  2. fatty (hydrocarbon base)
A

types of pastes

49
Q

triamcinolone acetonide dental paste (topical corticosteroid for oral lesions, mouth sores, decreases inflammation), adhesive base suitable for application to oral cavity (Oromuco-adhesive paste) - gelatin, pectin, carboxymethylcellulose sodium, plasticized hydrocarbon gel

A

aqueous paste (single phase)

50
Q

zinc oxide paste for diaper rash
- ricinus communis (castor) seed oil
- mineral oil
- paraffin
- balsam tolu resin
- petrolatum
- preservative free

A

fatty paste

51
Q
  1. hydrocarbon base (soft paraffin and liquid paraffin)
  2. water miscible base (emulsifying ointment, plasticized hydrocarbon)
  3. water soluble bases (PEG bases)
A

bases for pastes

52
Q

melt all bases and wax with continuous stirring, add powdered ingredients, continuous and constant stirring until cool

A

fusion method of preparation of pastes

53
Q

melt the base, take powder drug and triturate with melted base (concentrate), triturate the concentrate with the remaining base (heat may be used to facilitate mixing)

A

fusion and trituration method of preparation of pastes

54
Q
  1. additional/alternative hydrophobic solvents (polydimethylsiloxane - liquid silicone, vegetable oils - canola oil, sunflower oil, corn oil, soybean oil, organic esters - isopropyl myristate)
  2. preservatives if necessary
  3. antioxidants - lipophilic antioxidants BHA/BHT, hydrophilic antioxidants sodium metabisulfite
A

commonly used excipients in pastes

55
Q

semisolid systems consisting of colloids as either:
- small inorganic particles (colloidal suspensions)
- large organic molecules (interpenetrated by a liquid)
based on external liquid phase, these can be classified as polar/aqueous (hydrogels) or nonpolar/lipids (organogels)

A

gels

56
Q

two-phase systems (inorganic particles and the continuous gel phase, aluminum hydroxide gel, bentonite magma), colloidal dispersion, pseudoplastic non-Newtonian flow behavior (viscosity decreases with increased shear force - shear thinning and thixotropic, due to break down of the structure of the system)

A

inorganic gels

57
Q

single-phase system (no apparent boundaries between particles and gels), contain gelling agents (natural or synthetic polymers)

A

organic gels

58
Q

water-swollen structures composed mainly of hydrophilic polymers (natural, synthetic, semisynthetic), hydrophilic polymers are rendered insoluble due to the presence of crosslinks (entanglements, crystallites, van der Waals interactions, pi pi stackings, hydrogen bonds)

A

hydrogels

59
Q

organic (non-polar) solvents (hexanes, isopropyl myristate, sunflower oil, corn oil), gelatin process involves the self-assembly of low-molecular-weight gelators (LMWGs) to give polymer-like fibers (acrylic polymers, lecithin, polyethylene)

A

organogels

60
Q

taking up of water or solvent by the gel and increase in volume, gel-gel interactions are replaced by the gel-solvent interactions

A

swelling/imbibition of gels

61
Q

opposite of swelling/imbibition, many gels often contract spontaneously on standing and exude some fluid medium, becomes more obvious as the concentration of the gelling agent decreases, occurs in both organic and inorganic gels

A

syneresis or weeping of gels

62
Q

some gels turn into a sol on shaking and reset to gel on standing, reversible gel-sol transformation, time-dependent shear thinning property

A

thixotropy

63
Q

most hydrogels show a drastic change in their properties in response to external stimuli (smart hydrogels) - pH, temp, ionic strength change, biological (enzymes, antigens, antibodies)

A

stimuli-responsive gels

64
Q

gels in which the vehicle has been removed leaving a polymer network/films - dry gelatin, tragacanth ribbons, polystyrene
have porosity and high surface area

A

xerogel

65
Q

dispersed system (liquid in gas), packaged in pressurized containers or special dispensing devices, contain dispersed gas bubbles usually in a liquid continuous phase, forms a fluffy semisolid when dispensed
attractive drug delivery system for cosmetic, pharmaceutical, medical applications
- ease of application (spread uniformly, fill the area of application, increase contact time)
- allows for better coverage (hard to reach areas, wrinkles, skin folds)
- enhanced patient acceptance/compliance
- useful for application on highly inflamed, swollen, abraded, infected, sensitive skin (minimize the need for touching/rubbing)
- offer cooling, soothing, emollient, moisturizing effects

A

foams

66
Q

solid/semisolid masses that adhere to the skin being applied in the form of pieces of fabric that contain a layer of medication
- provide protection and mechanical support
- provide occlusive and macerating action
- apply medication into close contact with surface of the skin
- medicated pain relief (lidocaine)
- prototype for transdermal delivery systems

A

plasters/pads

67
Q

external applications resembling ointments, used as a covering or protection
- xeroform (petrolatum) is a sterile gauze with white petrolatum, used as a bandage for various types of wounds, used in skin graft

A

dressings

68
Q

semisolid dosage forms intended for insertion into body cavities (rectum, vagina, urethra), either melt (fatty base) or dissolve (water soluble base), exert a local or systemic effect

A

suppositories

69
Q

__________ route of administration is useful if patient is unconscious, vomiting, nauseated, unable to take orally (pediatric)

A

rectal

70
Q

the ability of a solid to exist in more than one crystal form, cocoa butter has 4 of these (alpha, beta, beta prime, gamma)

A

polymorphisms

71
Q

which polymorph of cocoa butter is appropriate for rectal use?

A

beta (34-35 C)

72
Q

saturated triglycerides, dehydag, fattibase, suppocire, witepsol

A

synthetic/semi-synthetic fatty bases

73
Q

dissolve in the mucosal fluid and release the drug, glycerinated gelatin, glycerin retains moisture and provides lubrication for aid of insertion

A

glycerol-gelatin bases

74
Q

composed of PEGs with different molecular weights (polypeg, polybase), water soluble, suitable for both hydrophilic and lipophilic drugs, offer good bioavailability

A

polyethylene glycol bases (PEG bases)

75
Q

non-ionic surfactants, polyoxyethylene fatty acid esters, polyoxyethylene stearate, facilitate drug delivery

A

surfactant suppository bases

76
Q

hardness (for proper handling and delivery), shape (for comfortable insertion/retention), solubilization of drug in suppository matrix, rapd melting or dissolving after application

A

important characteristics for suppositories

77
Q

has a direct effect on patient safety and therapeutic efficacy, instability or degradation of drug product can lead to deviations from the labeled potency, reduction in therapeutic effect, creation of toxic byproducts, change in appearance, drug release, or function

A

drug product stability

78
Q

must be safe and effective demonstrated in clinical trials, must be reproducible and high quality (manufacture must meet Current Good Manufacturing Practice - CGMPs, chemical physical and microbiological stability based on stability testing, establish shelf life and storage conditions)

A

FDA-approved drug product

79
Q

duration for which product meets specifications after manufacture when stored and used as directed

A

shelf life

80
Q

date (month/year) until which batch meets specifications when stored and used as directed, each batch tested when manufactured and periodically over the shelf life (not beyond the shelf life)

A

expiration date

81
Q

active ingredients in a product must remain within the 90-110% of label strength during the shelf life for efficacy, safety, and consistency
+/-10% variation commonly used as general benchmark
allows for some degree of decreased potency due to chemical or physical processes
allows for batch-to-batch variability during manufacture

A

potency specification

82
Q

occurs when drug molecules interact with water

A

degradation by hydrolysis

83
Q

process of electron loss due to the interaction of the drug with atmospheric oxygen

A

degradation by oxidation

84
Q

degradation catalyzed by absorption of light in the UV range, drugs that are susceptible to this should be in suitable packaging (amber bottles, tablet coating - titanium dioxide, capsules)

A

degradation by photolysis

85
Q

process by which an epimer is transformed into its counterpart, considered degradation in cases in which the action of a drug on a receptor is stereoselective (for example only the L enantiomeric form of epinephrine is active in treatment of anaphylaxis)

A

epimerization

86
Q

understand drug reactivity, protect from moisture, light, atmospheric air (packaging), storage conditions (humidity, temp, fridge or freeze if appropriate), appropriate dosage form, excipients, and manufacturing process

A

ways to improve chemical stability

87
Q

protect against low levels of contamination during normal storage and use, must be present in some products and good to have in others (multidose liquids/semi-solids containing water, some solids with high moisture content (ODTs), non-sterile liquids with high risk of contamination)

A

antimicrobial preservatives

88
Q

package in direct contact with the product

A

primary package

89
Q

package outside of the primary one, usually not critical to stability of the drug

A

secondary package

90
Q

applies to repackaged/manipulated commercial products, pill organizer, compounded products
shorter than expiration date (manufacture guidance, general guidelines, consider situation, professional judgement and literature)

A

beyond use date

91
Q

batch or lot specific, problem with manufacture, stability, package, label

A

recall

92
Q

product-specific, problem with safety or efficacy, FDA approval revoked

A

withdrawal

93
Q

product-specific, company stopped the sale of the product

A

discontinuation

Pharmaceutics I (4 decks)

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