Medical Sticks and Suppositories Flashcards by Cole Binsfeld

What is a main difference between soft and hard sticks?

hard sticks require moisture to activate them; hard sticks not really used in pharmaceutics anymore

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How are medical sticks made?

Molding/fusion

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Fatty base agents for sticks?

cocoa butter, vegtable oils, hydrogenated vegtable oil, waxes

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Water-soluble bases agents for sticks?

Sodium stearate, glycerol PEGs

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Case: Why use a suppository for an infant for constipation?

Acts quickly, safe, localized absorption

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Suppository definition?

A solid dosage form used for rectal, vaginal, or urethral admin
Consists of a dispersion of active ingredient in an inert matrix (rigid/semi-rigid)

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What are advantages of suppositories?

less invasive than injectables?
limit first pass effect
limit DI’s when given in combo w/ other therapies
can be used for local or systemic effect
accomadates pts who have difficulty swallowing
accomodates admin in unconscious pt or infants
Increases F of drugs

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What are the limitations of suppositories?

not for long-term treatment (lower acceptance rate)
user discomfort
Special storage condtions like low temp
Difficult for self admin for some pts

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Explain which vein is systemic and wich is not in rectal absorption of drugs

Absorbed through inferior middle rectal vein that leads into inferior vena cava –> direct systemic absorption
Superior rectal veins drain into portal vein which bases into liver prior to reaching systemic absorption

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Steps of rectal absorption

Fusion.dissolution –> diffusion –> mucus layer –> rectal mucosa –> transport

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What formulation factors can impact drug absorption?

pKa
physical state of the drig in formulation
solubility; degree of ionization and particle size
solubility of drug in rectal fluid
Partition coefficient of drug
particle size (want lower)

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What physiological factors impact drug absorption?

Anatomical size
site ofdrug delivery in the rectum
change in rectal pH based on age or disease conditions
presence of stool in the rectum
frequecny of bowel movements
pathological chagnes in tissue integrity ; changes in thickness of mucosa

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Sizes/shapes of Rectal, Vaginal, and Urethral suppositories in Adults/children?

Rectal: 2g/1g bullet/ torpedo shaped (32mm long)
Vaginal: 5g(varies) globular, oviform or cone shaped(pessaries)
Urethral: Males: 140 mm x 3-6mm ~4g shape: slender, pencil shaped

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Why use suppostory over oral?

poorly absorbed orally
taste unacceptable
irritates GI
drug of abuse
Acid liable drugs
Drugs prone to enzymatic degradation

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What characteristics should a vehicle/base have for suppository sticks?`

Able to:
melt
soften
dissolve at body temp
promote drug release
stay stable during manufacturing and storage
inert
esthetically acceptable

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What are bases used for suppositories?

Fatty: cocoa butter, hydrogenated vegtable oil, hydrogenated palm oil
Water: glycerine, PEG

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When do you use a fatty or water-soluble base for a suppository?

Fatty: if drug is highly soluble in water, low solubility in fat
Water: drug highly souble in fat, low soluble in water
This is because it promotes drug release

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Characteristics of Cocoa Butter?

Natural TG
Melting Point: 31-35 (low)
Solid @ 25
4 polymorphic forms w/ different MP’s (major limitation)
Requires lubrication of the mold when compounding

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Characteristics of hydrogenated vegtable ois (witepsol)

Suppocire
Semi-synthetic –> resistant to oxidation/hydrolysis
Waxy solids
MP: 33-45
No polymorphism
more flexible and less brittle character
lower viscosity –> separation/sedimentation risk of API while cooling (lack of uniformity potential)
Self lubricating but, contract in mold

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Acid value and Hydroxyl nomber for Cocoa butter, hydrogenated oil, suppocire?

<5, 0
<2, 5-30
Low, <10-30

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Characteristic of glycerol-gelatin base?

Rare to use b/c not inert (laxative effect)
hygroscopic so storage condtions very important
dissolution varies w/ age of suppository –> unpredictable API response

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Characteristics of PEG?

slow drug release
MP’s differ based on combination components
Chemically stable but not physically stable, inert compatible
Limited by:
- hygroscopic
- incompatabilities w/ API’s
- May become brittle on storage
Prepared by molding and compression, no lubrication needed

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What additives are used to improve incorporation of API’s?

Fixed oils (levegate solids), water

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What additives are used to increase hydrophilicity and dissolution characteristics?

Ionic surfactants (Anionic, SDS, SLS, TEA-stearate), non ionic surfactants (TWEEN)

What additives are used to improve viscosity?

Al-monostearate, glyceryl monostearate, steryl/myristyl/ - cetyl alcohols, bentonite, colloidal silica

What additives are used to modify MP?

FA's, fatty alcohols, waxes

What additives are used to protect against degradation?

antimicrobial, antifungal, antioxidant

When should you consider rectal route as a pharmacist?

peds pts w/ dysphagia pts w/ N&V refusal of oral meds/ spitting out tablets pts w/ GI blockage/obstruction pts w/ esophageal stricture or malignancy loss of consciousness/palliative care decreased mental status

When should you not consuder rectal route as pharmacist?

neonatal pts pts w/ conditions assocaited w/ meutropenia thrombocytopenia chronic constipation increased GI motility (diarrhea) placement of medication causes pain

What are the preparation steps for suppositories?

Mold prep Mold calibration Base prep API incorporation mixing and pouring cooling and finishing packaging, storage and labelling

What is the displacement factor?

Measures amount of ctive substance that dispalces 1 gram of suppository base Available in literature for common drugs Affects final suppository wt and dosing uniformity of the formulation especially for drugs which exhibit high displacement factors

Benefits of cold compression?

increased rate of production No sedimentation problems eliminates temp changes related problems suitable for thermoliable and insoluble drugs

How does cold compression work?

base and drug mixture is forced into a mold under pressure using a wheel operated pressing into open molds

Disadvantages of cold compression?

Requires finely powdered excipients Not used for extemporaneous compounding

What are the problems w/ hand rolling? When is it used?

tedious, not very uniform Usually used for cocoa butter

How are suppositories usually packaged?

Individually wrapped Fatty base: 2-8 Water base: tightly closed containers to avoid moisture PEG can be stored at room temp

What causes craching, splitting, and pitting? How can it be fixed?

Excipient contracts strongly, large time gap between pouring and cooling --> temp fluctuations Fix: Use an excipient which crystalizes slower, maintain optimum control of steps pouring and cooling to minimize temp changes

What causes sticking to mold? Fix?

fatty molds (gaps between molds upon closure), premature removal from mold, insuffeceint cooling, insuffecient lubrication Fix: Use appropriate equipment, prolong molding period/cooling period, use an excipient whcih crystalzies more rapidly, reduce cooling temp, sufficient lubrication

What causes thickening prior to pouring? fix?

High proportion of finely powedered API's, high viscosity base mixtures. Fix: PEG select the mixture of right PEGs, adjust [ ] of the API in the dosage form

What causes poor product homogeneity?Fix?

dispalcement factor not taken into account, cooling to slow or too weak leading to drug sedimentation. Fix: calculation should be carefully perfomed, increase vsicosity of the base

What causes product insufficiently solid? FIx?

Inclusion of air Fix: check the stirring levle and limit formation of air bubbles

What cuases surface anomalies? Fix?

High melting point excipients, >60 MP = longer residence in mold leading to shape abnormalities, excipient to API ratio Fix: Ensure mold is appropriately sealed, use excipients to stabalize the system such as surfactants

Patient counseling points for supositories?

follow package instructions to lubricate use water soluble (do not use petrolatum jelly) Insert the medication about a finger length into rectum and place against rectal wall close legs and sit or lay still for ~15 minutes avoid emptying bowels for about 1 hour Avoid exercise and excessive movement for about 1 hour Vaginal and urethral almost always come w/ applicator

What is needed to activate hard sticks?

moisture

Which base contracts in the mold?

Hydrogenated oils (witepsol)

Which base needs lubricating when compounding?

cocoa

Which form of cocoa butter is needed

beta

What does a high melting point of base tell us?

sustained release

Which base is not inert?

glycerol-gelatin= laxative

How does age effect glycerol bases?

changes dissolution= not always the same dose

Which bases need to be stored in a cool place?

fatty

What type of lube should be used for insertion?

water soluble

How far to insert?

finger length

How long to sit still after application?

15 min

How long should you avoid BM and exercise?

1 hour

What is always given with a urethral suppository?

applicator

How far do you insert for vaginal and urethral?

as far as comfortable