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IDM > TBL 4 - Pharmaceutical formulations > Flashcards

TBL 4 - Pharmaceutical formulations Flashcards

1
Q

What is a drug?

A

The active pharmaceutical ingredient (API) is a chemical compound with pharmacological (or other direct) effect intended for use in the diagnosis, treatment or prevention of disease.

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2
Q

Why can’t be the API be given along?

A

Using API in its pure state is rare due to low doses being administered in therapeutic state. Usually between 50 to 500mg of API per dose.

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3
Q

Why is it acceptable to add additional material to API?

A

As if the pure state of API by itself yields small quantities so material are added to the API to yield product (e.g. a tablet) of acceptable size for patient use.

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4
Q

What would happen if tablets were smaller from its recommended size?

A

Tablets any smaller would be difficult to manufacture and would affect patient compliance.

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5
Q

what would the reason be for API to be unsuitable in it’s pure form?

A

In some cases exhibits unfavourable physical and chemical properties e.g. API shows poor aq solubility, may not survive the acidic environment of stomach or may exhibit unfavourable physical characteristic such as poor powder flow.

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6
Q

what is a pharmaceutical formulation?

A

a specific combination of API’s and excipients.

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7
Q

What are excipients?

A

are pharmacologically inert ingredients used to give the final dosage form (tablet, capsule, cream etc) body (mass) or to control its characteristics. - excipients serve as a medium or vehicle for one or more API’s.

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8
Q

What is a dosage form?

A

a physical form in which an API is given to patients.

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9
Q

What are examples of solid dosage forms?

A

tablets, capsules, powders

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10
Q

What are examples of semi-solid dosage forms?

A

creams, ointments

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11
Q

What are liquid dosage forms?

A

injectables, syrups

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12
Q

what does the dosage form of a pharmaceutical product show?

A

its method of entry/delivery (route of administration) into a biological system.

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13
Q

What is the choice of dosage form dependent on?

A

the physical/chemical properties of API, intended site of action and required onset of action.

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14
Q

What is enteral (oral) administration?

A

Is the dosing of a drug for the system-wide effects but delivery is via GI tract. - most common route - from mouth to G-tube.

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15
Q

What are the pros of oral administration (4 things)

A
  • Non-invasive
  • can be modified for extended release
  • convenient
  • usually less expensive then other forms
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16
Q

What are the cons of oral adminsteration (7 things)?

A
  • Not appropriate for unconscious patients
  • requires time for absorption and distribution
  • Patients may be unable to swallow
  • Absorption time affected by food, drugs, stomach acid and condition of gut
  • Metabolic processes in the GI tract may be problematic for some drugs
  • May cause patient discomfort/nausea
  • Sublingual/buccal tablets may not be taken correctly if patient is not appropriately instructed/counselled
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17
Q

what is a bulk powder?

A

are multi-dose preparations consisting of solid, loose, dry particles of varying degrees of fineness. - contain 1 or more active ingredients with or without excipients also has cooling matter and flavouring substances.

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18
Q

what does the pharmaceutical bulk powders usually contain?

A

contains non-potent medicaments (substance used for medical treatment) such as antacids since the patient measures a dose by volume using 5ml medicine spoon.

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19
Q

what is a powder dispersed in?

A

dispersed in water- effervescent powders dissolved before taking.

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20
Q

what is divided powders?

A

are single-dose presentations (e.g. small sachet) that are intended to be issued to patient to take in or with water e.g. Lemsip sachets.

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21
Q

what are granules?

A

are agglomerates (collect or form into mass) of powder mixes , usually of drug plus excipients.

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22
Q

How can pharmaceutical granules be prepared?

A

can be bulk or divided and could be prepared by wet or dry granulation.

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23
Q

How can some granules be taken?

A

some granules are placed on the tongue and swallowed with water, whereas other are intended to be dissolved in water before taking

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24
Q

What do the effervescent granules evolve?

A

evolve carbon dioxide when added to water.

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25
Q

What are tablets?

A

are solid dosage forms consisting of active ingredients and suitable pharmaceutical excipients

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26
Q

What are the advantages of tablets to the patient (5 things)?

A
  • Accuracy of dosage
    • compactness
    • portability
    • blandness of taste
    • ease of administration
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27
Q

What are the advantages of tablets to the manufacture (6 things)?

A
  • simplicity
    • economy of preparation
    • stability
    • convivence in packaging
    • shipping
    • Dispensing
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28
Q

What are the disadvantages of tablets?

A
  • drugs with poor wetting
    • Slow dissolution
    • intermediate to large doses difficult to formulate/manufacture as tablet to provide adequate or full drug bioavailability
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29
Q

What does paracetamol resist?

A

resists compression into dense compacts.

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30
Q

what do drugs that are bitter tasting, objective odour or sensitive to oxygen or moisture require?

A

encapsulation or entrapment prior to compression or tablets may require coating

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31
Q

Filler (or diluent) is a common type of excipient used in tablets what is the most common filler?

A

Lactose is included to increase size of tablet - necessary as amount of API is so tiny so tablet would be too small to handle it.

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32
Q

When is a filler not necessary?

A

when the dose of a drug is high

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33
Q

What could be a potential alternative excipient to produce tablets with improved physiochemical and biopharmaceutical performance?

A

engineered xylitol (used as sugar substitute)

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34
Q

What is a binder?

A

for example starch paste added to promote granulation to ensure free flowing properties of the particles.

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35
Q

Why is using a binder important?

A

in order to promote cohesive compacts during direct compression and ensure tablet remaining intact after compression.

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36
Q

What is distintegrant?

A

for example starch helps the tablet break down into small fragments, when it’s ingested. - helps the medicine to dissolve and taken up by the body so it can act more quickly.

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37
Q

what is the most traditional distintegrant in tablets?

A

starch - conc up to 10%

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38
Q

What does glidants improve?

A

improve the flowability of tablet granules or powder by reducing the friction between particles, preventing the formation of lumps.

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39
Q

What is the most commonly used glidants?

A

Colloidal silica (aerosil), 0.2% by weight

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40
Q

What is anti-adherent used for?

A

e.g. magnesium stearate, stop the powder from sticking to the equipment as the tablet is being made.

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41
Q

What is a lubricants?

A

e.g. aluminium stearate, talc and PEG, ensure that the tablet has a smooth surface. They reduce friction that occurs between the wall of the tablets and walls of the die cavity when the tablet is ejected.

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42
Q

Why are colourants added to tablets?

A

are added to help you to recognise your tablet make it easier to take your medicine correctly

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43
Q

Why are flavouring agents used?

A

help improve tablets taste. - limited to chewable tablets or tablets that are intended to dissolve in mouth, to impart pleasant taste, masking unpleasant tasting APIs.

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44
Q

What are capsules?

A

solid dosage forms in which medicinal agents and/or excipients are enclosed within a small shell (often of gelatin).

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45
Q

what are gelatin capsules composed of?

A

sugar, gelatin and water

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46
Q

What are the advantages of capsules over liquid forms?(3 things)

A
  • efficiently manufacture
    • produced at low cost
    • more stable with longer half-life
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47
Q

What are the advantages of capsules over solid dosage forms (5 things)?

A
  • being more elegant
  • generally improved bioavailability
  • Versatile forms - can carry liquid, semisolid or solid drugs
  • easily prepared extemporaneously
  • easily protected from light (opaque shell)
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48
Q

What are oral solutions?

A

are homogenous liquid preparations for oral use containing one or more active ingredients dissolved in a suitable vehicle (commonly water)

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49
Q

What should oral solutions be clear and free from?

A

precipitate

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50
Q

What would a change in colour or cloudiness of solutions indicate?

A

indicates degradation or microbial contamination

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51
Q

What are the PROS of oral solutions?

A
  • Solutions are absorbed faster than solid dosage forms
  • Generally cause less GI irritation
  • phase separation is not a concern with solutions as it may be for suspensions and emulsions
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52
Q

What are the CONS of oral solutions?

A
  • Susceptible to microbial contamination
  • possible hydrolysis of APIs in aq solutions
  • taste of some drugs is more unpleasant when in solution
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53
Q

What are the additives used in the formulation of oral solutions (4 things)?

A
  • buffers
    • flavouring agents
    • antioxidants
    • preservatives
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54
Q

Who is the target audience for the administration of oral solutions?

A

young children

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55
Q

What are oral emulsions?

A
  • liquid preparations for oral use containing 1 or more active ingredients.
  • Stabilised oil-in-water dispersions
  • Either or both phases contain dissolved solids.
  • solids may also be suspended in oral emulsions
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56
Q

What state is emulsions in for oral administrations?

A

oil (active ingredient) in water and facilitate the administration’s of oily substances such as castor oil or liquid paraffin in a more palatable form

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57
Q

what are oral suspensions?

A

liquid preparations containing one or more active ingredients suspended in suitable vehicle

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58
Q

What are suspensions useful for?

A

useful for administrating insoluble or poorly soluble drugs

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59
Q

What forms a simple syrup?

A

a liquid preparation of liquid in water forms simple syrup (e.g. 85% sucrose) to which one or more active ingredients can be added to form a medicated syrup.

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60
Q

Why are syrups often used?

A

often used as flavouring syrups to mask the unpleasant taste of some APIs, predominantly for administration in children (e.g. amoxicillin or paracetamol syrup)

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61
Q

Why are syrups popular in the treatment of coughs or sore throats?

A

as their increased viscosity allows them increased contact time with the affected sites.

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62
Q

What is an elixir?

A

a liquid oral preparation that usually contains either potent or unpleasant-tasting drugs.

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63
Q

what is the colour of the formulation of elixirs?

A

they are clear

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64
Q

What does elixirs contain?

A

contains a high proportion of sugar or other sweetening agent, included to mask the offensive or nauseating taste.

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65
Q

what are paediatric elixirs formulated with?

A

formulated with fruit syrups as a base flavouring agent

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66
Q

What are paediatric elixirs contained with?

A

Non-aq solvents (alcohol, glycerine or propylene glycol) form a significant proportion of the vehicle used in elixirs or solubilising agents.

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67
Q

What is a linctus?

A

a liquid oral preparation used for demulcent, expectorant or sedative purpose to treat a cough.

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68
Q

What is demulcent?

A

forms a soothing film over a mucus membrane, relieving minor pain and inflammation.

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69
Q

what is expectorant?

A

increases the production of hydration of secretions

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70
Q

How is linctus intended to be taken?

A

intended to be sipped slowly, coating throat in an undiluted form. So, linctus is formulated to be viscous solution containing sugars.

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71
Q

What are oral drops?

A

liquid preparations intended to be administered in small volumes with the aid of a suitable measuring device. may be solutions, suspensions or emulsions

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72
Q

What are parenteral administration?

A

Is the dosing of a drug for systemic (whole body distribution) via route other than the GI system.

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73
Q

What is an example of a parenteral administration?

A

medicines given by injections - some drugs only available in injectable form and this route is a fast drug action

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74
Q

Routes that injections can take are…. (5 things)

A
  • Subcutaneous
    • intramuscular
    • intravenous
    • transdermal
    • implantation
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75
Q

What are the PROS of parenteral administration?

A
  • Drug does not pass through intestinal tract
  • provides a fast acting drug action
  • eliminates many factors that might affect absorption rates
  • can be used for unconscious patients, those who cannot swallow and patients who are nil by mouth
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76
Q

What are the CONS of parenteral adminsteration?

A
  • Invasive
    • may introduce bacteria in to the system
    • painful/frightening
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77
Q

What is an injection?

A

An injection is an infusion method of putting liquid into the body, usually with a hollow needle and a syringe which is pierced through the skin to a sufficient depth for the material to be forced into the body.

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78
Q

What is an Intravenous (IV) adminsteration?

A

Involves administrating the drug through a needle placed directly into a vein. IV preparations are usually solutions that must be sterile and free of particulate matter.

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79
Q

What are the PROS of IV adminsteration?

A
  • drug doesn’t pass through intestinal tract
  • fast onset of action
  • eliminated many of the factors that might affect absorption rates
  • immediately available to the body cus introduced directly into the bloodstream
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80
Q

What are the CONS of IV adminsteration (6 things)?

A
  • Invasive
    • may introduce bacteria into the system
    • painful/frightening
    • recovery is much more difficult if a medication error or and adverse reaction occurs
    • Requires a functioning cannula
    • Cannula are prone to infection, tissuing
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81
Q

What is an intravenous injection?

A

a liquid administered direct into the bloodstream via a vein. it is advantageous when a rapid onset of action is needed.

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82
Q

What does an intramuscular administration (IM) involve?

A

Involves a direct injection into a large muscle mass.

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83
Q

What can IM medications be?

A

Solutions or suspensions and some formulations can be given either IV or IM

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84
Q

What are the PROS of IM adminsteration (4 things)?

A
  • Drug does not pass through the intestinal tract
  • fast on set action (but not as fast as IV
  • eliminated many factors that might affect absorption rates.
    • can be formulated for extended release
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85
Q

What are the CONS of IM administration (6 things)?

A
  • Invasive
    • may introduce bacteria into the system
    • painful/frightening
    • drug absorption may be erratic depending on the site used, the muscle mass of the patient, and the amount of exercise performed by the patient
    • may cause bruising
    • difficult to reverse drug action once its been injected
    • not appropriate for a patient with decreased muscle mass or bleeding problem
86
Q

what is an IM injection?

A

injection of a substance directly into a muscle e.g. vaccines. Depending on chemical properties of drug medication may either be absorbed very quickly or gradually

87
Q

Where is IM injections given?

A

deltoid, vastus lasteralis, ventrogluteal and dorsogluteal muscles.

88
Q

What is a complication that may arise with IM injections?

A

Injection fibrosis is a complication that may occur if injections are delivered with great frequency or with improper technique

89
Q

What is involved in subcutaneous adminsteration?

A

Subcutaneous (SC) administration involved injecting small amount of solution or suspension immediately under the skin

90
Q

What are the PROS of subcutaneous adminsteration?

A
  • drugs does not pass through intestinal tract
  • patients can be taught to self-administer
91
Q

What are the CONS of subcutaneous adminsteration (5 things)?

A
  • Invasive
  • may introduce bacteria into the system
  • limit to the volume of medication that can be injected
  • may be difficult for patients with thin or frail skin
  • rate of absorption is slower then IV or IM routes
92
Q

What is an intradermal adminsteration?

A

it is inserted in the top layers of the skins and is not as deep as the SC injection.

93
Q

What is the intradermal adminsteration used for?

A

used for allergen testing

94
Q

What is an intra-articular adminsteration?

A

involves injecting meds directly into a joint such as the knee

95
Q

What is intra-arterial adminsteration?

A

involves injecting meds directly into a joint such as the knee

96
Q

What is intra-arterial adminsteration?

A

involved injecting a drug directly into an artery. This method delivers the drug directly to the desired location, so decreases the side effects to other parts of the body.

97
Q

What kind of drug is an example of intra-arterial adminsteration?

A

Cancer chemotherapy drugs - but extreme caution should be used cus these drugs are toxic

98
Q

What is intra-cardiac adminsteration?

A

involved injection directly into heart muscle. This method only used in extreme life-threatening emergences.

99
Q

Who is qualified to preform and intra-cardiac adminsteration?

A

only healthcare personnel’s trained and experienced in preforming this type of injection should attempt it cus there’s a risk of rupturing the heart

100
Q

What is an intraperitoneal adminsteration?

A

Involves injection into the peritoneal or abdominal cavity. This method of injection is often used to administer antibiotics needed to treat infections in the abdominal cavity such as peritonitis resulting from a ruptured appendix.

101
Q

What is intrapleural administration?

A

injection of a drug into the pleura or the sac surrounding the lungs. May be done to eliminate or prevent excessive amounts of fluid from building up in the pleural sac surrounding the lungs

102
Q

What is intravitreal adminsteration (hint: eye)?

A

injection into the vitreous, which is a jelly-like substance inside the eye. It is performed to place meds inside eye near the retina

103
Q

What are implants (Hint: pump)?

A

A medication pump e.g. insulin pump or medical device that is inserted into the body either permanently or for a prescribed amount of time and it is designed to provide continuous adminsteration of a drug over a predetermined amount of time.

104
Q

What is a topical administration?

A

topical adminsteration brings drug formations into contact with the skin. Drug can treat surface conditions with little or no penetration into skin or is designed to penetrate skin to provide therapeutic effect.

105
Q

What are the PROS of the topical administration (2 things)?

A
  • Application can be direct to the site of action
  • Some products can produce a systemic effect by having drug diffuse through the skin and into the bloodstream
106
Q

What are the CONS of the topical adminsteration (2 things)?

A
  • Skin acts as natural barrier that will affect rate and amount of absorption
  • conc needed to provide a therapeutic effect is difficult to determine
107
Q

What is a semisolid dosage form?

A

are products of semisolid consistency to be applied to skin or accessible mucous membranes for therapeutic protection or cosmetic function.

108
Q

What are the advantages of a semisolid dosage form (2 things)?

A
  • Flexible dosing
  • Suitability for local and systemic drug delivery.
109
Q

What are the disadvantages of semisolid dosage forms (3 things)?

A
  • Less stability
    • contamination
    • dosing errors
110
Q

What are the common sites for semisolid dosage forms?

A

Skin, eyes, nose, vagina, urethral membrane and rectum

111
Q

What is the ideal physiochemical properties for semisolid dosages forms (6 things)?

A
  • smooth texture
    • non-dehydrating
    • non-gritty
    • pharmaceutically elegant
    • non-greasy and non-staining
    • not hygroscopic
112
Q

What are the ideal physiological properties for semisolid dosage form (4 things)?

A
  • Non-irritating
    • Miscible with skin secretions
    • low sensitisation index (hypoallergenic)
    • Do not alter membrane/skin functionality
113
Q

What is the ideal application properties (2 things)?

A
  • easy to apply and wash off
    • efficient drug release
114
Q

What is the drug action of semisolids?

A

includes releasing the drug onto the skin surface then diffusion of the drug molecules through the different layers of the skin to reach the intended site of action.

115
Q

What are ointments?

A

They are greasy preparations with permissible addition of up to 25% of powder by weight, that are good for areas of the skin that need protection.

116
Q

What are the dosage forms of ointments?

A

dosage forms are homogenous, translucent, viscous semisolids preparations intended for external applications

117
Q

What conditions are ointments useful for?

A

any condition characterised by dry skin (e.g. atopic dermatitis).

118
Q

Why are ointments used?

A

used due to their emollient (softening) effects or used as a medication vehicle. Ointments soften and do not met upon application to skin.

119
Q

What can ointments be classified as (3 classifications)?

A
  • Epidemic(antiseptics/protectives)
    • Endodermic (emollients/moisturising)
    • Diathermic (systemic)
120
Q

What is the base of an ointment?

A

the base is anhydrous and immiscible with skin secretions

121
Q

What are creams?

A

are combinations of water, oil and other substances that have softer consistency and are less greasy in comparison to ointments and components are absorbed into the skin.

122
Q

Ointment vs Cream….:

A
  • Ointement: oleaginous base, low water content (<20%), more greasy (volatiles)
    • Cream: Greater water content (>20%), less greasy (volatiles)
123
Q

What can creams be a combination of? Hint:(O/W) OR (W/O)?

A

Creams can either be oil in water (O/W) or water in oil (W/O) emulsions and contain preservatives to prevent bacterial/fungal growth.

124
Q

What is the most commonly used preservatives?

A

Parabens

125
Q

What is the difference between oil in water emulsions and water in oil emulsions?

A

oil in water emulsions rub into skin and could easily washed off whereas water-in-oil emulsions are greasier.

126
Q

What are pastes?

A

contain one or more drug incorporated in a base with large proportions of finely dispersed powders.

127
Q

What are the advantages of pastes (6 things)?

A
  • Less penetrating, less macerating and less heating then ointments
  • Makes a good protective barrier when placed on skin
  • solid they contain absorb and neutralise certain noxious chemicals before they ever reach the skin
  • like ointments, paste form an unbroken relatively water-impermeable film.
  • unlike ointments the film is opaque and can be used as sun block
  • pastes less greasy cus of absorption of fluid hydrocarbon fraction to the particulates
128
Q

What is gel?

A

Is a dispersion of small or large molecules (gelling agents) in an aq liquid vehicle (solid drugs in a jelly-like substance). Gels are semi-colloids

129
Q

What are gels used for?

A

medication, lubrication and carrier for spermicidal agents to be used intra-vaginally with a diaphragm. Gels are a common form for acne preparations (e.g. acnederm)

130
Q

How can gels be classified?

A

based on mode of gel formation, chemical nature and source/origin

131
Q

What happens during single phase gels?

A

gelling agent in uniformly distributed throughout liquid and no apparent boundaries exist between them

132
Q

What happens during a 2-phase gels?

A

consist of floccules of small, distinct particles

133
Q

What are hydrogels?

A

are hydrophilic polymeric gelling agents in water

134
Q

What are organogels?

A

are thermoplastic (thermoreversibale) materials containing liquid organic phases (e.g. organic solvents, mineral oil and vegetable oil) entrapped in a 3D cross-linked network of gelling agents.

135
Q

What are plasters?

A

solid or semisolid adhesive ,asses spread onto backing paper or fabric for a local effect. applied to skin to being medication in close prolonged contact with skin surface.

136
Q

What are plasters main uses?

A
  • provide protection and mechanical support - Furnish an occlusive and macerating action
  • Bring medication into close contact with the surface of the skin
137
Q

What are liniments?

A

are fluid or semi-fluid or semi-solid preparation for application to skin - might be alcoholic or oily solutions or emulsions

138
Q

How should liniments be applied?

A
  • must be massaged into the skin (e.g. friction)
  • liniments should not be applied to broken skin
139
Q

What are lotions?

A

these are fluid preparations (aq) for external application without friction. either dabbed on the skin or applied on suitable dressing and covered with a waterproof dressing to reduce evaporation

140
Q

What is collodion?

A

is a solution of nitrocellulose in ether acetone, sometimes with addition of alcohols.

141
Q

what is collodion’s generic name?

A

pyroxylin solution

142
Q

What does collodion becomes when solvent evaporates?

A

highly flammable, solvent evaporates dries to a celluloid-like film

143
Q

What does collodion do?

A

used to seal minor injuries (artificial skin), used to bring the API into contact with the skin and hold it in place

144
Q

what does compound wart remover consist of?

A

consists of acetic acid and salicylic acid in an acetone collodion base used in treatment of warts by keratolysis

145
Q

What are paints?

A

paints are liquid for application to the skin or mucous membranes. Skin paints contain volatile solvent that evaporates quickly to leave dry resinous film of medicament

146
Q

What are throat paints?

A

are more viscous due to high content of glycerol, designed to prolong contact of the medicament with the affected site.

147
Q

What are the mouthwashes, throat sprays and gargles considered to be?

A

considered as topical agents since they are used to target a local site of action (the mouth or throat) - used to relieve minor sore throat pain and to improve bad breath

148
Q

What is a dusting powders?

A

is finely divided insoluble powder containing ingredients such as talc, zinc oxide or starch as its base. An API can be added to give powder a therapeutic activity (e.g. as an antiseptic or antifungal)

149
Q

What do dusting powders absorb?

A

absorb moisture (e.g. an astringent) which discourages bacterial growth. Others are used for their lubricant properties.

150
Q

What is a poultices?

A

paste-like preparations used externally to reduce pain and inflammation cus they retain heat well.

151
Q

What happens to poultices after heating?

A

After heating, the preparation is spread thickly on dressing and applied as hot as the patient can bear, to the affected area.

152
Q

What are PROS of inhalation (2 things)?

A
  • very rapid absorption to the huge surface area of the respiratory endothelium
  • Bronchodilators and inhaled steroid can be targeted to lungs with low levels of systemic absorption
153
Q

What are the CONS of inhalation (2 things)?

A
  • Bioavailability depends on patient’s inhaler technique and the size of drug particles generated by delivery technique
  • Inhaled corticosteroids can cause mouth and tongue soreness, hoarseness of voice and oral thrush
154
Q

What are metered dose inhalers?

A

Inhalers are solutions, suspensions or emulsion of drugs in a mixture of inert propellants held under pressure in an aerosol dispenser.

155
Q

What is the method of metered dose inhalers?

A

release of dose of the medicament in form of droplets of 50 um diameter or less from the container through a spring-loaded valve incorporating a metering device.

156
Q

How does the patient inhales the drug?

A

inhales through the mouthpiece as patient pressed down on the value using finger pressure.

157
Q

What conditions are inhalers and nebulisers used to treat?

A

asthma and other respiratory problems.

158
Q

What is a nebuliser?

A

a device to administer medication to people in forms of liquid mist to the airways.

159
Q

What is the process of nebuliser?

A

pumps air or O2 through a liquid medicine to turn it into vapour, which is then inhaled by the patient.

160
Q

What is the transdermal route of adminsteration?

A

The transdermal route of administration involved delivery of the drug across the top of the skin for percutaneous absorption to facilitate a systemic effect

161
Q

What are the PROS of the transdermal route of adminsteration (2 things)?

A
  • The skin assists in controlling the rate of absorption and delivery to the bloodstream
  • Drug does not pass through the intestinal tract
162
Q

What are the CONS of the transdermal route of adminsteration (1 thing)?

A
  • May cause skin irritation or reactions
163
Q

What is a transdermal patch?

A

is a dosage form that is applied to skin and release drug over a period of time. In transdermal products drugs pass through the skin and enter the general circulation

164
Q

What are the advantages of transdermal products (4 things)?

A
  • Avoiding hepatic first-pass metabolism
  • Enhanced therapeutic efficacy/minimum side effects
  • Improve patient compliance
  • Abrupt termination of drug effect by wiping the drug off the skin and allowing high local conc.
165
Q

What are the disadvantages of transdermal products (3 things)?

A
  • Irritation
  • side effects due to systemic drug absorption
  • may wipe away easily
166
Q

What does the rectal adminsteration involve?

A

Involved inserting a drug through the anus into the rectum.

167
Q

What are rectal suppositories?

A

Are solid dosage forms formulated in a base that is intended to melt and dissolve and release the medication after it is inserted

168
Q

Where is the suppositories medication absorbed through?

A

absorbed through the rectal mucosa to provide systemic effect or it may exert a topical (local) effect.

169
Q

What are the PROS of suppositories (2 things)?

A
  • Good absorption - the haemorrhoidal veins drain directly into the inferior vena cava
  • avoiding hepatic first pass metabolism
170
Q

What are the CONS of suppositories (2 things)?

A
  • may not be suitable after rectal or anal surgery
  • some patients dislike suppositories
171
Q

What are suppositories?

A

are small solid medicated masses, cone-shaped that are inserted into the rectum where it melts at body temp. A suppositories dissolved after insertion.

172
Q

What can rectal suppositories produce?

A

can produce local (to treat haemorrhoids and ulcerative colitis) or systemic effect - e.g. anti-emetic effect

173
Q

What is an enema?

A

an enema is the procedure of introducing liquids into the rectum and colon via the anus.

174
Q

What are the 2 forms of an enema?

A

Evacuant enema and Retention enema

175
Q

What is an evacuant enema?

A

Used as a bowl stimulant to treat constipation (e.g. soap enema and magnesium sulphate enema). Volume is 2 litres, should be warmed to body temp before adminsteration.

176
Q

What is a retention enema?

A

their volume dose not exceed 100ml - no warming needed

177
Q

What does the retention enema exert?

A
  • exert a local effect or systemic effect allowing adminsteration of APIs into the bloodstream.
  • used when impossible to administer orally.
178
Q

When does nutrient enema contain?

A

carbohydrates, vitamins etc.

179
Q

What are vaginal suppositories or tablets intended for?

A

intended for insertion into the vaginal canal and designed to melt or dissolve and release the medication. - may contain medication intended to be absorbed or topical effect limited to vaginal area

180
Q

What do vaginal suppositories (pessaries) produce?

A

produces a local antimicrobial effect

181
Q

What are pessaries?

A

pessaries are solid medicated preparations designed for insertion into the vagina

182
Q

What are the 3 types of pessaries?

A
  • Moulded pessaries
    • Compressed pessaries
    • Vaginal capsules
183
Q

What are moulded pessaries?

A

they are cone-shaped and prepared in a similar way of moulded suppositories

184
Q

What are compressed pessaries?

A

made in a variety of shapes and are prepared by compression in a similar manner to oral tablets.

185
Q

What are vaginal capsules?

A

similar to soft gelatin oral capsules differing only in size/shape

186
Q

What are vaginal rings?

A

are doughnut-shaped polymeric drug delivery services designed to provide controlled release of drugs in the vagina over extended periods of time.

187
Q

What is a intrauterine device (IUDs)?

A

IUDs/’coils’ are small, T-shaped contraceptive devices constructed of copper and plastic which is inserted into the uterus.

188
Q

What are the advantages of IUDs (2 things)?

A
  • Long-acting reversible contraception
    • IUD stays in place for 5 to 10 years
189
Q

How are solutions instilled into the eye?

A

By tipping head back and placing the required number of drops inside the lower lid of eye while looking up.

190
Q

How are solutions instilled into the eye?

A

By tipping head back and placing the required number of drops inside the lower lid of eye while looking up.

191
Q

How are ophthalmic ointments applied?

A

Pulling down lower lid and applying a thin ribbon of the ointment along the inside of the lid.

192
Q

What are ocular inserts?

A

are solid devices placed in eye and release a drug at constant rate, minimising side effects due to rapid absorption

193
Q

How are otic preparations administered?

A

solutions/suspensions administered into ear canal and contain analgesics, antibiotics and anti-inflammatory agents.

194
Q

How are nasal solutions administered?

A

administered to the nasal passages in the form of drops or sprays - may be suspensions or emulsions.

195
Q

What are the PROS of ocular, otic and nasal routes of adminsteration?

A
  • Direct application
196
Q

What are the CONS of ocular, otic and nasal routes of adminsteration (Hint: all just relating to eyes)?

A
  • For eyes: must be sterile and free of any particulate matter that irritate the eye
  • For eyes: care taken to avoid touching eye with tip of dropper/ointment tube
  • Ocular inserts: cumbersome to insert properly and insert must be removed from eye after drug is released
197
Q

What are eye drops?

A

are saline-containing drops used as a vehicle to administer APIs in the eye

198
Q

What should eye drops be?

A

must ne isotonic to eye and are sterile (aseptic) products

199
Q

What are ophthalmic ointments and gels?

A

these are sterile semi-solid preparations intended for application to conjunctiva or eyelid margin.

200
Q

What are ear drops?

A

are solutions, suspension or emulsions of drugs that are instilled into the ear with a dropper.

201
Q

What are ear drops used to treat?

A

treat/prevent ear infections - infections of outer ear/ear canal used to treat build up of ear wax.

202
Q

Why should the use of oily nasal drops be avoided?

A

cus of possible damage to the cilia of the nasal mucosa.

203
Q

What are the main 4 things that makes an ideal dosage form for a drug?

A
  • serves as the optimal vehicle for maintaining efficacy of the drug
  • able to survive the body’s metabolic process and get to site of action
  • can be successfully manufactured
  • will survive the journey from production to administration
204
Q

What is Class I according to Biopharmaceutical classification system (BCS)?

A

High permeability, high solubility

205
Q

What is Class II according to Biopharmaceutical classification system (BCS)?

A

High permeability, low solubility

206
Q

What is Class III according to Biopharmaceutical classification system (BCS)?

A

Low permeability, High solubility

207
Q

What is Class IV according to Biopharmaceutical classification system (BCS)?

A

Low permeability, Low solubility

208
Q

When is a drug substance considered highly soluble?

A

When highest dose strength is soluble in <250 ml water over a range pH range 1 to 7.5

209
Q

When is a drug substance considered highly permeable?

A

when absorption in humans is >90% of an administered dose, based on mass-balance or in comparison to an intravenous reference dose

210
Q

When is a drug product considered to be rapidly dissolving?

A

When >85% of the amount of drug substance dissolved within 30 mins using USP apparatus or II in a volume of <900 ml buffer solutions

211
Q

What is primary manufacturing?

A

where API is made - achieved by synthesis, biosynthesis or fermentation

IDM (8 decks)

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