Capsules Flashcards

1
Q

What are capsules?

A

Solid dosage forms in which the drug substance and/or excipients are enclosed within a soluble container or shell or coated on the capsule shell. The shells may be composed of two pieces (body and cap) or a single piece

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2
Q

What are the shell materials?

A

Gelatin: traditional polymer for capsules

Hydroxypropyl methylcellulose: plant based material

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3
Q

What are the advantages of hard capsules?

A
  • Mask unpleasant taste and odor of drug
  • better bioavailability
  • allow powders to be dispensed in an uncompressed form
  • versality for multiple filling formulations
  • may be easier for some people to follow
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4
Q

What are the cons of hard capsules?

A
  • easily affected by humidity
  • might not be easy for some people to swallow
  • filling speed of capsule machines is slower than tablets
  • can be tampered
  • not compatible with certain materials
  • cost of capsule shells and manufacturing
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5
Q

What are the properties of gelatin?

A
  • produced by hydrolysis of collagenous materials
  • moisture content is 13-16%
  • produces strong flexible film
  • consistent dissolution
  • cross linking can happen and modify dissolution
  • mechanical stability depends on water content

Type A - pork skins via acid processing
Type B - bones and animal skins by alkaline processing

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6
Q

What are the gelatin capsule shell ingredients?

A

Gelatin, water, colouring agents, flavouring agents, processing aids (SLS), preservatives (parabens)

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7
Q

What is the dip molding process?

A
  • Pair of dipping pins put inside a warmed, aqeuous gelatin solution to form a film around the pins
  • The pins are withdrawn and rotated around to distribute and cool down the film
  • dried film is removed and cut to length
  • two parts are joined to the pre locked position
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8
Q

What are the properties of HPMC?

A
  • plant origin, non ionic polymer
  • immediate or modified release
  • low moisture content (2-9%)
  • consistent dissolution with no cross linking
  • great physical stability (break less in dry conditions)
  • prepared by dip molding process or thermogellation
  • rough capsule surface
  • harder to produce uniform colouring
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9
Q

What are the hard capsule fillings?

A

Dry powders, pellets, granules, tablets, semi solids, non aqueous liquids

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10
Q

What are the two filling methods for extemporaneous compounding?

A
  • punch method (hand filling)

- capsule filling machines

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11
Q

What are the packing stats? What is the procedure?

A
  • how much powders fits into the capsule
  • capsule body is 100% filled
  • capacity is dependent on the density of the powder
  • determines capsule size needed
  1. Tare the weight of an empty capsule shell
  2. Fill 5 capsules with each ingredient
  3. Weigh each filled capsule and get an average
  4. Record the weight for that capsule size to obtain the packing stats for the individual ingredient
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12
Q

What are the filling step requirements for industrial methods?

A

powder flow, lubricity, compressibility (carr’s index 18-35)

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13
Q

What are the common excipients of dry powder capsules?

A

Fillers (MCC, Lactose), Disintegrant (Croscarmellose, sodium starch glycolate), Lubricant (Mg stearate)

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14
Q

What are the dependent methods?

A

Volume of capsule shell controls the dose
Requires it to be 100% filled for correct weight uniformity
Auger or screw method

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15
Q

What are the independent methods?

A

Dosator, dosing disc and vacuum filling

Dosator - suitable for >/= 20 mg, not suitable for highly cohesive powders
Dosing disc - >30 mg
Vacuum filling - low dose inhalation products

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16
Q

What are the liquid and semi solid fillings?

A
  • sealing step required
  • easier tech than softgel capsules

Excipients:
Lipophilic - vegetable oils, esters, fatty acids, fatty alcohols
Hydrophilic: PEG 3000-6000
Amphilic: poloxamers, lecithin, PEG esters

17
Q

What are soft gels?

A

A liquid or semi solid matrix inside an one piece plastizicized gelatin shell

18
Q

What are the pros of soft gels?

A
  • improved drug bioavailability
  • increased dose uniformity and reproducibility
  • easy to swallow, lack of odour and taste
  • avoid formation of dust
  • oils and low mp drugs that cannot be compressed
  • enhanced drug stability
19
Q

what are the cons of softgels?

A
  • subject to effects of humidity (8-16%)
  • difficult for some people to swallow
  • more expensive, specialized equipment, formulation optimization requires more expertise
  • drugs can migrate from oily vehicle into shell
  • unsuitable for aqueous liquids
20
Q

What are the softgel shell ingredients?

A

gelatin (type B), water, plasticizers (glycerin, propylene glycol, sorbitol), preservative, colour and opacifier

21
Q

What are the properties of fill formulations?

A
  • capacity to dissolve the drug dose in small volume
  • fast and uniform rate of dispersion in the GI tract
  • compatibility with softgel (pH shoild be 2.5 to 7.5)
  • prevent precipitation of solubilized drug
  • withstand high temp during sealing step (60-70)
22
Q

what are the types of fill formulations?

A

solutions, suspensions, emulsions, microemulsions, self emulsifying drug delivery system, self microemulsifying

23
Q

What are the hydrophilic liquids?

A

PEG 400 and 600, propylene glycol, glycerin
Ethanol and water below 5-10%
Problem with drug precipitation when it contact with water in GI tract
Examples: Ibuprofen, Naproxen sodium, Nifedipine

24
Q

What are the lipophilic liquids?

A

tryglyceride oils

solution fills: calcitriol, valproic acid
suspension fills: progesterone, ranitidine

25
Q

what are the self emusifyinf/micro/nano emulsifying drug systems?

A

oil phase + non ionic surfactants

  • spontaneous emulsion formed in the GI fluid, stable for longer time
  • Higher SA due to surfactant
  • cyclosporin A, Ritonavir
26
Q

What are the softgel manufacturing processes?

A
  • Rotary die process

- Seamless process

27
Q

how is the unformity of dosage units ensured?

A

weight variation using 10 caps, CU: HPLC

28
Q

What are the other quality control tests?

A

disintegration, dissolution, stability testing, moisture permeation test (single unit and unit dose containers, samples exposed to known relative humidity, colour change/weight pre and post test)

29
Q

What are lozenges, troches and lollipops?

A
  • dissolve or disintegrate slowly in mouth
  • made by compression/molding
  • hard lozenges: hard sugar candy base, soft lozenges: PEG base or acacia base, chewable lozenges: glycerinated gelatin abse
30
Q

What is chewing gum used for?

A
  • smoking cessation, gingivitis, pain relief and motion sickness
  • localized delivery of drugs in mouth
  • made by compression or mixing ingredients with melted gum base, rolling and cutting finished untis