Solid Systems Flashcards by Kayley Donovan

Solid dosage forms

earliest and largest form of administering drugs

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Solid dosage forms

Important system. tablets, gelatine capsules, granules, powders, release pellets.

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Earliest oral solid dosage form

1500 BCE, 4000 BCE medical preparations (ancient greece)

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Bulk solids

handled without count in large volume (incalculable)

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Troubling behaviour of bulk solids

move awkwardly, affect and are affected by surroundings, change in behaviour (pattern and time), hypersensitive

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Awkward moving behaviour of bulk solids

poor/excess flow, tacky/sticky, pack/bridge, form piles, bounce/roll

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Surroundings effect on bulk solids

abrasive/corrosive/toxic/explosive, high heat capacity, dusty, adhesive. friable (crumble), degradable, contaminable, absorb, wall friction, sensitive to pressure

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Change in behaviour of bulk solids

hygroscopic, electrostatic, segregate, fluidisation, shear thinning, asymmetry. compacting, permeate, phase separate, salt bridging, settle

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Hypersensitivity of bulk solids

particle size and distribution, surface texture/chemistry, shape

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Flow properties of bulk solids

Powders don’t flow well so are hard to transport

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Angle of repose

steepest angle of descent relative to horizontal plane that material can be piled without slumping.

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Angle of repose and flow properties

angle decreases, flowability increases
angle < 25 flow = excellent
angle > 40 flow = poor

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Granulated

grained mixture.

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Granules

finely powdered particles

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Granulation

physical process making small particles into agglomerates.

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Reasons for granulation

improve flowability, dosage control, reduce segregation, easy transport, better wetting and physical properties

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Granule products

fertilizer, coffee, milk powder, dog food

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Granulation steps

actives mixed with excipients, liquid binder added, drying

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How do granules form

adhesion and cohesion, liquid bridge, solid bridge, van der waals, form bonds

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Principle mechanisms of granulation

layering, crushing and layering, coalescence, abrasion transfer

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Layering granulation

powder mix forms surface layer to increase granule size

Crushing and layering granulation

granules break into fragments that adhere to other granules

Coalescence granulation

two or more granules join to form larger granule

Abrasion transfer

material abraded adheres to other granules

Wet granulation

liquid binder is sprayed onto particles moving around and the liquid then solid bridge forms into blackberry structure (agglomerate)

Dry granulation

Used when API is temperature or moisture sensitive. Slugging or roller compaction

Slugging

compressing machine turns powder into tablets which are crushed into granules

Roller compaction

rolling machine agitates powder into long (lasagne) sheets which are then crushed into granules

Fluidisation

high shear and air flow turns solid powder into liquid

Pharmaceutical tablets

convenient and inexpensive processing, excipients and API's mixed together higher shear and pressed together (punch and die).

Effervescent

Fizz/bubbles produced from acid/base(carbonate) reaction

Tableting punch and die

upper punch and lower punch 1 compression each, have specific shapes for tablets

Compression pressure of tablets

Compression force/punch tip area p = F/A

Porosity of tablet

1 - density of tablet/particle density ε = 1 - ρ(c)/ρ(p)

Porosity means

measure of empty space within material (pores in the compressed powder)

Excipients in tablets

antiadherents (stearates), binders (starch/glucose), disintegrants (starch/alginates), antioxidants, fillers, colours, flavours, glidens

Types of tablets

plain (active + excipient, cheap), coated, multi actives, matrix tablets (swelling and non-swelling), chewable, effervescent

Non-swelling matrix tablets

API is released slower through permeable matrix.

Swelling matrix tablets

Polymer matrix, water contact makes it swell and drug is released through pores (sponge)

Tablet coating benefits

mask taste/odour, protect, easy swallowing, prevent irritation, easy handling, packaging speed, identification

Types of coatings

sugar, film

Sugar coating

cheap, safe, can colour, tasteful but time consuming and unhealthy

Film coating

polymer film around tablet, easy

Coating pan

spray coating into metal pan and while it is turning hot air is blown to coat and dry

Quality control tests

content of API, uniformity, disintegration time, hardness, friability, dissolution

Organ specific tablet

drug delivery systems specifically target release in organs/tissue

Capsule

encapsulating powder, granules, pellets, liquids and semi-fluids.

Hard shell capsules

contain dry powdered ingredients, made out of gelatin, made in two halves (smaller and bigger).

Soft-shell capsules

used for oils and for active ingredients dissolved or suspended in oil

Gelatine

hydrolysed collagen, structural protein in extracellular matrix in connective tissue (abundant in mammals - marrow)

Capsule quality control

permeability and sealing, weight variation, uniformity, disintegration, dissolution