Lab 3 Flashcards
1
Q
Ointment - Definition
A
Ointments are semi-solid dosage forms able to treat skin and mucosa. They contain the components homogenously dispersed (solved, suspended, emulgeated) in an ointment base.
– Homogenous
– Do not dissolve at body temperature
– Do not contain solid particles
2
Q
Differents bw. ointments and cream, pasta and gel
A
-Cream: contains more water, than ointment
-Paste: contains a large proportion of solid powder finely
dispersed (also oral application)
-Gel: Gels consist of liquids gelled by means of suitable gelling agents (also oral application).
3
Q
Ointment - Usage
A
– Local administration
– Systemic effect: high lipophilicity or appropriate vehicle (e.g. DMSO)
4
Q
Ointment - Composition
A
- Active compounds: antibiotic, antimicotic, antiviral agent, NSAID’s, glucocorticoids, antihistamin, coating, disinfecting agents etc. -Ointment base components: Ingredients without or with low water solubility: * Plant and animal lipids * Hydrocarbons * Waxes & wax alcohols - Water soluble ingredients: *Plants and animal polymers *Synthetic polymers - Hydrophobic ointments - Water-emulsifying ointments - Hydrophilic ointments
5
Q
Ointment - Examples on plant and animal lipids
A
- Fats
- Cocoa butter (Fatty bases Theobroma Oil BP)
- Oils (sunflower oils, castor oil, flax oil, cod-liver oil etc.)
- Hydrolysis: glycerol, fatty acids
6
Q
Ointment - Examples on hydrocarbons
A
- Soft paraffin
- Liquid paraffin
- Hard paraffin
- Vaseline
7
Q
Ointment - Examples on waxes & wax alcohols
A
• Wool wax (adeps lanae) (hydrous wool fat, Lanolin 25% water) Lanalcol, Wool-fat alcohol • Honey bee wax Myristyl alcohol • Sperm Whale wax (Physeter macrocephalus) Cetostearyl alcohol
8
Q
Ointment - Examples on plants and animal polymers
A
- Methylcellulose
- Hydroxiaethylcellulose
- Agar
- Gelatine
- Starch: potato, wheat etc.
9
Q
Ointment - Examples on synthetic polymers
A
- Macrogols (polyoxyethylenes)
* Polysorbates (Tweens)
10
Q
Ointment - hydrophobic ointments; types and advantages/disadvantages
A
– White soft paraffin and yellow soft paraffin can be used as ointment bases.
– In case of skin irritation or when protective effects is needed.
– The disadvantage of paraffin usage on the skin is the prevention of the skin from perspiration
11
Q
Water-emulsifying ointments
A
– Water emulsifying hydrocarbon waxes and ointments, capable of oil-in-water emulsion formation: • anionic emulsifying wax • nonionic emulsifying wax • cetomacrogol emulsifying ointment • anionic emulsifying ointment – Water-emulsifying hydrocarbons, capable of water-in-oil emulsion formation: • simple ointment, • paraffin ointment • hydrous ointment.
12
Q
Hydrophilic ointments
A
– Are miscible with water
– They can be applied when greater body surface area is
treated or when the ill animal is sensitive to hydrocarbons.
13
Q
What are macrogol ointment?
A
Hydrophilic oitmentcontains that contains two types of polyethylene glycols; macrogol 4000 and macrogol 300.
14
Q
Ointment - Dispensation
A
- Jar
* Tube
15
Q
Ointment - Prescription
A
„For external use only!”
• Official preparations (BP)
• Prepared preparations
• Licensed preparations
16
Q
Eye ointment - Definition
A
Sterile, soft, homogenous ointments intended for application to the conjunctiva. Prolonged effect (eye-drops), a bit more preferable in cats (nasolacrimal duct).
17
Q
Eye ointment - Composition
A
- Active substance: AB, glucocorticoids, Vit. A, etc.
* Eye ointment bases: simple eye ointment, hydrous eye ointment
18
Q
Eye ointment - Dispensation
A
– Not more than 5-10 grams (open package stability)
– In sterilised tubes with a cannula
19
Q
Eye ointment - Prescription
A
– Official preparations
– Prepared preparations
– Licensed preparations
20
Q
Oral gel and oral paste - Usage
A
– Orally
21
Q
Oral gel and oral paste - Composition
A
- Active substance: anthelminthics, AB, sedatives, probiotics etc.
- Vehicle: gel or paste
22
Q
Intramammary preparations - Definition
A
Sterile, soft preparations (suspensions, emulsions, solution) able to treat or prevent the diseases of the mammary gland.
They can be introduced into the mammary gland via the teat canal.
– Dry-cows = non-lactating cows
– Lactating cows
23
Q
Intramammary preparations - Usage
A
– Udderwash
– Udder-disinfection
– Milking-out
24
Q
Intramammary preparations - importances in case of lactating/dry animals
A
– In case of lactating animals, after 12 hours milk-out, then reapplication
– Dry cows: after last milk-out, long WP!
25
Intramammary preparations - Composition
– Active compound: AB, antimycotics, antiseptics, GC (their form changes whether lactating or not!)
– Vehicle: liquid paraffin, beeswax etc.
– Auxiliary subst.: stabilizing suspension and emulsion (eg. DMSO), preservatives (eg. Benzyl alcohol)
26
Intramammary preparations - Dispensation
– Plastic syringes with special injector (single doses)
– For the treatment of a SINGLE teat canal
– /Rarely multidose formulations/
27
Intramammary preparations - Prescription
– Official preparations (BPV) - rare!
| – Licensed preparations
28
Suppositories - Definition
Solid, single-dose preparations, that will dissolve on body temperature.
The shape, volume and consistency are suitable for rectal administration (+ vaginal formulations)
29
Suppositories - Usage
– Mainly in small animals
– Local effect: disinfectant, adstringent, emolliating
– Systemic effect: sedative, anticonvulsive, NSAID’s etc.
(avoiding liver first pass)
30
Suppositories - Composition
* Active substance: e.g. sedative, NSAID (powder or liquid)
| * Suppository bases: hard fat , cocoa butter, supplemented hard fat, macrogol mass
31
Suppositories - Dispensation
Aluminium foils + box
32
Suppositories - Prescription
– Official preparations
– Prepared preprations
– Licensed preparations
33
Electuaries - Usage:
– Orally
| – Not precise: only safe ingredients
34
Electuaries - Composition
* Active substance: powder form, safe
| * Vehicle: syrup (prepared), jam (homemade)
35
What are tranquilizers?
sedatives / neuroleptics (phenothiazines, butirophenons,Rauwolfia alkaloids)
36
Tranquilizer sedatives - Pharmacological effects
* decreased motoric activity, decreased aggression
* reduced response to stimuli and fear, indifference to the surroundings
* No analgesic activity, but they potentiate the activity of analgesics (neuroleptanalgesia) ↔ slight analgesic activity can be observed by butyrophenones
* Increasing the dose lengthens the duration of sedation, not the depth (they do not cause hypnosis)
37
Tranquilizer sedatives - Receptorial effects
* Anti – α1-activity: hypotension (!) – horse: paradox-reaction
* Anti – dopamine activity: mainly responsible for sedative effect. Antiemetic effect. PRL-secretion increases: contraindicated for pseudopregnant animals
* Anti – histamine (H1) activity: antiallergic effect
* Anti – serotonine activity: versatile actions, e.g. inhibited regulation of body temp.
* Anti-muscarine effect: constipation, dry mouth (markedly in humans)
* FSH-secretion decreases: fertility rate decreases
38
Tranquilizer sedatives - Side effects
* Hypotension: can cause collapse in severely dehydrated, exsiccated animals (boxers very sensitive!)
* Paradox-reaction might be present in the horse
* Tissue irritation (e.g. chlorpromazine can cause muscle necrosis given im.)
* They can induce epileptic seizures (anti-D-effect)
* Hypothermia in cold places, hyperthermia in hot places
* Can exacerbate the symptoms of pseudopregnancy
* Slow metabolism and excretion: must not be given directly before slaughtering
* Can cause penis-prolapse in stallions (especially propionilpromazine, acepromazine)
39
Tranquilizer sedatives - Indications
* Sedation (e.g. transportation, capturing)
* Antiemetic (against vomiting and nausea)
* Neuroleptanalgesia in combination
40
Tranquilizer sedatives - Active substances
```
a) Phenothiazines: used to treat schizophrenia and manifestations of psychotic disorders:
– Chlorpromazine
– Propionil-promazine
– Acepromazine
– Thiethylperazine
– Promethazine
b) Butyrophenones: induce a state of apathy and mental detachment in patients with dysharmonious brain function
• Azaperone
• Droperidol
• Fluanison
```
41
Tranquilizer sedatives - Chlorpromazine:
-Type of phenothiazine
-Chlorpromazini hydrochloridum
-Paradox-r., muscle necrosis, very slow excretion from the body
• A.U.V.: -
• Human:
42
Tranquilizer sedatives - Propionil-promazine
-Type of phenothiazine
• A.U.V.: -
• Human: -
43
Tranquilizer sedatives - Acepromazine
-Type of phenothiazine
-The time to reach maximal effect depends on the formulation (gels↔tablets)
• A.U.V.: ACP inj., tablet, Vetranquil inj., Sedalin oral gel
• Human: -
44
Tranquilizer sedatives - Thiethylperazine
-Type of phenothiazine
-Pronounced antiemetic activity
• A.U.V.: -
• Human: Torecan inj., dragee, suppository
45
Tranquilizer sedatives - Promethazine
-Type of phenothiazine
-Promethazini hydrochloridum
-Pronounced antihistamine activity
• A.U.V.: -
• Human: Phenergan (Pipolphen) tablets, inj., suppositories
46
Tranquilizer sedatives - Butyrophenones
* Slight analgesic activity!
* Compensation of the respiratory depressant effect of opiates excellent for neuroleptanalgesia (e.g. droperidol + fentanyl) --> Cardiovascular depression and inhibition of temperature centre is less.
47
Tranquilizer sedatives - Azaperone
-Type of butyrophenone
-For sedation of pigs, reducing the stress (i.m!)
• A.U.V.: Stresnil inj.
• Human: -
48
Tranquilizer sedatives - Droperidol
-Type of butyrophenone
-Droperidolum
-Neuroleptanalgesia
• A.U.V.: -
• Human: Inapsine inj.
49
Tranquilizer sedatives - Fluanison
-Type of butyrophenone
-Neuroleptanalgesia, especially in small, laboratory animals
• A.U.V.: Hypnorm inj. (+fentanyl)
• Human: -
50
LIQUID DOSAGE FORMS - definition
Disperse systems where different liquids are used as dispersive phase.
51
LIQUID DOSAGE FORMS - types
- Homogeneous disperse systems: Solution
- Intermediate categories: Emulsoid (Microemulsion), Suspensoid (Microsuspension)
- Non-homogeneous disperse systems: Emulsion, Suspension
52
Solution - DEFINITION
- Homogeneous liquid system, clear (transparent) and free from particles and deposit
- Ingredients are dissolved in suitable liquid vehicle
53
Solution - USAGE
* Oral: local or systemic effect
* Uterine or udder treatment
* Topical treatment of skin and mucous membranes
* Ophtalmic use
* Ear drop, nasal drop
* Injection, infusion
54
Solution - “Sterile solutions” and "isotonic and isohydric"
for parenteral use or for the treatment of mucous membrane of eye, vagina,
uterus and udder
- Injections, infusions, intramammary products and
eye drops have to be isotonic and isohydric
55
Solution - CONTAINERS
- Vials, Glass, Bottle, Plastic flask
- Plastic tops or special closers, children resistant
closer (mainly for elixirs, syrups), multidose formulations with Pump-system
- Dark (i.e. brown) glass or UV resistant “covered” plastics containers
56
Solution - SEVERAL SPECIAL FORMS
(direct intake, favourable taste)
• Elixir: clear, flavoured (high proportion of sucrose), alcohol (diluted ethanol or other polyhydric alcohols) and aromatic compounds (e.g. orange extract, cocoa, cinnamon)
• Syrup: concentrated, viscous aqueous solutions with high amount of sugars plus aromatic compounds
• Mixture: dispersed active ingredients in suitable liquid, less transparent, less amount of sugars, suspended solids may separate slowly
57
Emulsion and Suspension - DEFINITION
Liquid preparations in which the active ingredient(s) is/are dispersed (suspended/emulsified) in a suitable liquid vehicle (dispersive phase)
- In case of the emulsions the dispersed phase is liquid
- In case of the suspensions the dispersed phase is solid
58
Emulsion and Suspension - IMPORTANCES
- During the storing/ on standing suspensions can get
sediment - deposit formation
- They have to be suitable for redispergation
- Label/Sig. contains the terms ‘shake well before use’
59
Emulsion and Suspension - USAGE
- External: topical preparations (local or systemic)
| - Internal: enteral, parenteral
60
Emulsion - COMPOSITION
- Active agent - Vehicles:
*Distilled water or aqueous liquid, the active agent is fat-soluble, O/W (oil in water) type
*Vegetable oils (corn oil, cottonseed oil, peanut oil, sesame oil), the active ingredient is water-soluble, W/O (water in oil) type
-Auxiliary substances: the use of emulsifying (suspensifying) agents is required to minimize the surface tension existing between the two different phases
O/W-type emulsifiers: soaps, sorbitan esters, PEGs
W/O-type emulsifiers: wool fat, wool alcohol or stearin
61
Emulsion and Suspension - CONTAINERS
Same as solutions:
- Vials, Glass, Bottle, Plastic flask
- Plastic tops or special closers, children resistant
closer (mainly for elixirs, syrups), multidose formulations with Pump-system
- Dark (i.e. brown) glass or UV resistant “covered” plastics containers
62
Suspension - COMPOSITION
Dispersed powder in a liquid dispersive phase
63
Injection and infusion - DEFINITION
Sterile liquid preparations are
- Solutions
- Emulsion or micro-emulsions
- Suspension or micro-suspensions
64
Injection and infusion - USAGE
intended for parenteral use
65
Injection and infusion - Administration route
IV., IM., SC., IP., IC., IO, ID etc.
- IV: oily solutions, NOT suspension/emulsion
- Except micro-emulsions, micro-suspensions
66
Difference bw. injection and infusion
Infusions are intended for slower or faster IV application
67
Injection and infusion - SIGNIFICANCE
- The effects of the enteral or parenteral applied drugs
differ from one another (e.g. MgSO4)
- Rapid effect is required (shorter absorption half-life)
- Compound irritates the mucous membranes of GI
- The stomach (i.e. low pH, enzymes) decomposes the
drug
- The oral treatment is impossible (because of injuries or
the patient is unconscious /comatose/)
- The drugs should not pass through the liver first
68
Injection and infusion - CONTAINERS
- Human injections and veterinary single dose formulations (in vials, less than 10 ml)
- Veterinary multidose formulations (10-100< ml) in sterile glass bottles, closed with rubber-stoppers
- Infusions (100-1000 ml) are dispensed in glass bottles, plastic bags
69
Extraction - DEFINITION
- Traditionally prepared from one or more medicinal herbs
- In case of non-watery and true extracts the active ingredient content is extracted by the pharmacists or
manufacturers (industrial conditions)
- Watery extract can be prepared by both pharmacist and
owners
70
Extraction - CLASSIFICATIONS
1. Based on their solid matter content
2. Based on their extracting agents
3. Based on principles of procedures
71
Extraction - solid matter content
- Liquid extraction (at least 50% extracted liquid material)
- Semi-liquid extraction: solid matter content is bw 50-70%
- Semi-solid extraction: solid matter content is bw 70-80%
- Solid extraction degree of humidity: maximum 6%
- Preparation, reconstitution of solutions
- Can be used as sweetening or flavouring agents
72
Extraction - their extracting agents
a) Watery /Aqueous/ extraction:
* Decoction (ingredients are extracted by cooking)
* Infusion (soaking in hot water)
* Extraction (soaking in tepid - lukewarm - water)
* Applied: Externally (rinsing and cleansing of surfaces), Orally or Inhaling
b) Alcoholic extraction; tinctures
- Adm: Externally (use on body surface or wounds)or Orally (mainly as appetizers)
c) Ethereal extraction
d) or other organic solvents (heptanes)
73
Extraction - principles of procedures
Soaking, wet steaming, percolation (permanent flow of extracting agent through the percolator)
74
Extraction - CONTAINERS
Tinctures are daylight sensitive
75
Liniment - Definition
Thick, lotion-consistency dosage form for topical administration.
76
Liniment - Usage
– Rare
– Skin diseases, rheumatism
– Horses: soreness, stiffness, cooling (alcohol+volatile oils)
77
Liniment - Prescription
```
– Official preparations (White liniment BP)
– Prepared preparations (rare)
– Licensed: infrequent (GSL, P)
*animal health care products
- ”Only for external use”
```
78
Gaseous dosage forms
```
For inhalation:
• Gases (N2O)
• Aerosols – For inhalation
For other:
• Aerosols – For topical use
• Foams
• Impregnated/Smoking strips
```
79
Aerosols - DEFINITION
Aerosols (sprays) are based on solids (fine powders) or
liquids
- Delivered in the form of an aerosol
(appropriate valve or a suitable atomising device)
- The sizes of particles have to be smaller than 5 µm
80
Aerosols - USAGE
- External use: Treatment of skin and mucous membrane surface
- Internal use: Intrapulmonary, via inhalation
81
Aerosols - COMPOSITION
- Active agents: disinfectants, AB, antifungals, parasiticides and anti-inflam agents
- Vehicles (i.e. solvents): distilled water, diluted alcohol,
propylene glycol etc.
- Propellant gases: propane-butane, compressed air
-Pressurised form (pressure is app. 250 kPa)
-Non-pressurised form (suitable pump-system and dispersing)
82
Aerosols - CONTAINERS
- Sprays should be supplied in well-closed containers
| - No opening or burning of the empty pressurised containers is allowed because of the risk of accident
83
Impregnated/Smoking strips - Definition:
• Dosage forms intended for antiparasitic treatments of honey bees.
• Impregnated strips: put in the bee-hive check
the effect after 24 h
• Smoking strip: ignition--> put in the bee-hive in smoking state --> check the effect after 24 h
• The expelled mites should be burnt.
84
Impregnated/Smoking strips - Prescribing
• Licensed
85
Impregnated/Smoking strips - Example
E.g. Bayvarol impregnated strip
86
Stability
In the given storage time interval the difference of the measured and the declared physical and chemical parameters′ values must be not greater than ± 5-10%
87
Determinant factors of stability
a) Physical factors:
• Homogeneity (macroscopic, microscopic): description to a homogeneous drug preparation
• Emulsion stability
b) Chemical factors:
• Decomposition of the active substance
• Interactions: other active substances, vehicle, package material
• Environmental effects: air, light, temp, humidity
88
Stability tests types
• Long term: 25°C, 60% RH: 0, 3, 6, 9, 12, 18, 24 and 36 months
• Accelerated: 40°C, 75% RH: 0, 3 and 6 months
• In use:
– Medicated drinking water: 0, 6, 12 and 24 hours
– Medicated feeds: 0, 1, 2 and 3 months
– Opened package: 0, 2 and 4 weeks
– On going: 25°C, 60% RH: 0, 3, 6, 9 and 12 months
89
Measured parameters of stability tests
```
– Content of active substances
– Concentrations of impurities
– Homogeneity: macroscopic, microscopic (particle size)
– Microbiological tests: e.g. sterility
– Density
– Viscosity
– pH
```
90
Colloid chemical classification of drug formulations
INCOHERENT FORMULATIONS:
a) Heterogeneous>500nm: powders, emulsion,
suspension, granules
b) Colloidal (1-500 nm): colloidal solution, some stock
solutions
c) Homogenous (<1 nm): solutions, tinctures
COHERENT FORMULATIONS:
a) Heterogeneous: ointment, pastes, creams, tablets,
suppositories
b) Colloidal: gels
91
Stability of emulsion
* Phase separation
* Phase inversion
* Aggregation processes
92
Pharmaceutical ingredients for suspension preparation
• Solubilizing agents: Polysorbate 20, 60, 80, Sodium lauryl sulfate
• Viscosity increasing agent: HEC, HPC, Silica colloidal anhydrous/hydrated
• Microbiological conservants/preservatives: Sorbic acid,
Preservative solution
• Other ingredients: Flavoring agents
93
Terpineol containing suspension (Expectorant)
• In mortar the pulverized terpineol (Terpinum) should be
mixed thoroughly and gradually with portions of HEC
(Mucilago hydroxyaethylcellulosum).
• The suspension should be diluted with purified water, then it should be transferred to the bottle with given portion of water.
• Preservative solution (Solutio conservans) and peppermint stock solution (Diluendum menthae) should
be added and the liquid should be mixed thoroughly.
94
Terpineol containing suspension: LABELLING
* Internally, shake it well before use
* Storage: 1 months, store at low temperature
* Th: Expectorant
95
Semisolid preparations:
• OINTMENT
• CREAM
* OINTMENT - an ointment consists of a single-phase base in which solids or liquids may be dispersed.
* CREAM: multiphase preparations consisting of a lipophilic phase and an aqueous phase
96
Antirheumatic ointment - LABELLING
- Externally. Keep in cold place.
| Th: Antirheumaticum. Rubefaciens.
97
Moisturizing cream - LABELLING
Externally. Keep in cold place.
| Th: Moisturizer.
