pharmaceutics exam 2 Flashcards
what is a capsule?
what is the active ingredient and where is it in reference to the capsule
what comes into play and where
“ A solid dosage form in which medicinal agents and inert substances (like excipients) are enclosed within a small shell of gelatin”
the active ingredient in powder surrounded by a capsule
excipient comes into play
what is made available when a patient is unable to swallow an intact solid dosage form like a capsule what can be given
chewable tablet, instant dissolving tablets, oral liquids, or suppositories are made available
capsules
Promote better patient compliance by being:
Capsules as such may not be filled
with liquids
what may the liquids be mixed with
- Solid dosage forms
- Medication is protected
- Easier storage and transport
Promote better patient compliance by being:
- Tasteless
- Easy to dose
- Capsules of specific designs provide
modified release
- Capsules as such may not be filled
with liquids
Capsules containing liquids must be sealed (requires industrial conditions)
The liquid may be mixed with an inert absorbent. The resultant solid mixture may be placed in capsules
Capsule forms
what is it filled with
what is its mold?
what are empty capsules often used for
what different sizes does it come in/what is the size from largest to smallest
is it usually concealed or open
Liquid-filled gelatin capsule
Capsule mold
Gelatin capsule- Empty capsule often used for
Extemporaneous compounding
of prescriptions
- come in different sizes (000 large, 5 small)
- usually concealed
what device do you use to ensure the correct filling of capsules?
what are the components of process?
use a torbial torsian balance
with this, you have an empty capsule on one side and another capsule of the same kind on the other side with the weight that you want the empty capsule to be in
let’s say that you have a 2g weight with the empty capsule on one and the empty capsule on the other side
the side with the 2g is heavier and you need to fill the empty capsule on the other side with 2g of substance in order to balance the scale
The formulation must be 2g otherwise It wouldn’t be accurate.
To compensate for the weight of the capsule being filled, the same capsule must be placed on the other side of the balance
How are capsules administered?
enteric coated
- what are they designed to do
extended released dosage forms
- what are they designed to do
what is the release of capsules based on
Enteric-coated:
– These are designed to
pass through the stomach
for drug release and
absorption in the intestine
Extended Release Dosage Forms:
These are designed to provide the release of the medication for an extended amount of time
what is the release of capsules based on - based on the coating outside of the capsule
Hard Gelatin Capsules
what is the empty capsule shell made of
how would you describe the capsule shell?
what description of capsules makes for higher patient compliance
Used to manufacture most of the
commercially available medicated capsules
Empty capsule shell made from:
–Gelatin, sugar and water
–They are clear, colorless, and essentially tasteless (want!)
–Most contain colorants & opaquants to make distinctive–for patient compliance
hard gelatin capsules Consist of two parts,
how is this dosage form intended to be used?
The content of capsules should be _______ in food or liquids only with the _______ of the _______
The base or body, which is longer and has a smaller diameter
The cap is designated to slide over the base portion and form a snug seal
This dosage form is intended to be swallowed whole.
The content of capsules should be opened and administered in food or liquids only with the concurrence of the pharmacist
Characteristics of Hard Gelatin Capsules
where is gelatin soluble
because gelatin is a protein, how is it digested?
what happens when gelatin is absorbed
how are most colored and made opaque, using what excipients
where does gelatin cycle through
Gelatin is soluble in hot water and in warm gastric fluids
Given that gelatin is a protein it is digested by proteolytic enzymes and absorbed
When gelatin dissolves it exposes its medicinal contents to the gastric (or intestinal) bodily fluids
Most are colored with FD&C and D&C dyes (colorants) and made opaque by adding titanium dioxide (opaquant).
gelatin cycles through the body
Where is the gelatin derived from to make capsules?
Gelatin is obtained by the partial hydrolysis of collagen obtained from
skin,
white connective tissue, and
bones of animals
While stable in air, gelatin is subject to microbial decomposition when moist–so needs preservative excipients
Hard capsules: contain between 13-16% moisture, but poor storage conditions can increase this level. Not good!
Avoid moisture in gelatin capsules, How?
what will moisture affect
what is used to protect against the absorption of atmospheric moisture
what are examples of dessicant materials
what must you leave inside
The moisture will affect hydroscopic agents (absorb moistrue from the air) in many capsules, therefore, small desiccant materials are used to protect against the absorption of atmospheric moisture.
Desiccant materials:
Dried silica gel, clay, and activated carbon
leave desiccant inside
Manufacturing hard gelatin capsule shells
capsule size
Capsule size: The sizes may vary but always determined by the amount of material to be incorporated
For human use: 000 (the largest) to 5 (the smallest) are commercially available.
There are 8 actual sizes [000,00,0,1,2,3,4 and 5]
Numerical designations are arbitrary and do not indicate the capsule’s capacity—000 is not the smallest but the largest
A pharmacist may compound capsules of a single medicinal agent, or combination of agents at the precise dosage prescribed for the patient
Developing the formulation
goal
what is the goal
what in what is important
lack in homogenity could result in what
what are ofetn used to produce the proper capsule fill volume and what are examples
Goal: Prepare a capsule with accurate dosage, good bioavailability, ease of filling and production, stability, and elegance.
Care in blending is important especially with low-dose drugs.
Lack of homogeneity could result in significant therapeutic consequences
Diluents or fillers are,
Often used to produce the proper capsule fill volume.
Offer bulk and cohesion
Examples:
Lactose, microcrystalline cellulose and starch
mixing only: glass mortar
Filling hard capsule shells
what method is used
what do you start with
what is placed on a sheet of paper
how to do the punch method
Pharmacists use “punch” method
Start with exact number of capsules to be filled
Powder to be encapsulated placed on sheet of paper, clean glass, or porcelain plate
Using a spatula powder is formed into a cake
Empty capsule body is held between the thumb and forefinger and “punched” vertically into the powder cake repeatedly until filled.
if making 10, make 11 to give room for error
Capsule sealing
what can capsules be sealed with
how can a capsule be sealed and what occurs during this
how many capsules can Industrial capsule sealing machines make
Capsules can be sealed with colored band of gelatin (KAPSEALS, Parker Davis)
Capsules can be sealed through a heat welding process that fuses the capsule cap to the body.
Industrial capsule sealing machines:
Can produce 60,000 to 150,000 gelatin banded, heat welded, or thermally coupled capsules per/hour
Cleaning and polishing capsules
Small amounts of powder may adhere to the outside of capsules after filling
Must remove before packaging and dispensing, wipe with clean gauze or cloth
On large scale cleaning, a vacuum can remove extraneous materials
Soft Gelatin Capsules
Pharmaceutically elegant and easily swallowed
Prepared to contain liquid, paste & dry fills
Liquids that can easily migrate through the capsule shell cannot be encapsulated into soft gelatin capsules.
When not to be used?:
When water content is > 5%
When low molecular weight water-soluble and organic compounds are employed such as,
alcohols, ketones, amines, and esters.
*Preservatives such as methylparaben and/or propylparaben used to retard microbial growth
Compendial requirements for capsules
Things added to preparations to facilitate their manufacture can only be used if,
Harmless (in the quantities used)
Do not exceed the minimum amounts required to provide their intended effect, if between 50mg or 10mg choose 10mg
Do not impair the bioavailability of the product
Do not interfere with assays to evaluate dosage form
Capsule within a capsule
The active ingredients can be separated from the other ingredients in a formulation.
In this case, you may fill a small capsule (i.e., No.5) with one powder, and then place that capsule along with the remaining ingredients inside a larger capsule.
The inside capsule should not be visible through the large capsule
used if contents will form eutectic mixtures if mixed so keep them separately so that it will not!
do not give if the internal capsule is seen if so, add powder on the walls of the cap. and put other cap inside
Tablet within a capsule
what can be placed in a capsule
Small commercially available tablets can be placed inside a capsule of a suitable size.
Small quantity of the additional powder should be deposited in the base before and after adding the tablet.
Similar to capsule inside capsule, tablet should not be visible through the filled capsule
Tablets
how often is it used in the commercial dosage form?
why is it liked so much
commercially available tablets can be made fast
how are tablets made
Most frequently prescribed commercial dosage form
Stable, elegant, and effective when made right
Commercially available tablets can be made at a rate of thousands per minute
Tablets are made primarily by compression with a limited number by molding
Tablets
size
grooved
Often vary in size,
shape, hardness, thickness
and in their ability to dissolve
In fluids.
These tablets are grooved
Are therefore intended
to be broken into two parts.
Why? Offers flexibility
Patients can swallow
them easily or use in divided
doses
they are scored so they can be broken and have some now or later
Definitions: types of tablets to know
Compressed tablets (C.T.):
Multiple compressed tablets (M.C.T.):
Sugar-coated tablets (S.C.T):
Film-coated tablets (F.C.T.):
Gelatin-coated tablets:
Enteric-coated tablets (E.C.T.):
Buccal or sublingual tablets:
Compressed tablets (C.T.):
Multiple compressed tablets (M.C.T.):
Sugar-coated tablets (S.C.T):
Film-coated tablets (F.C.T.):
Gelatin-coated tablets:
Enteric-coated tablets (E.C.T.):
Buccal or sublingual tablets:
Types of tablets continued
Instant Disintegrating/ Dissolving tablets
Extended Release Tablets (E.R.)
Vaginal Tablets:
Compressed tablets (C.T.)
Diluents or Fillers: Add bulk to prepare a certain size
Binder or Adhesives: Promote adhesion of the particles of the formulation
Disintegrants: Promotes breakup of tablets/drug availability
Antiadherents/ glidants/ or lubricating agents
Miscellaneous Adjuncts: Colorants and flavorants to enhance overall appearance
Multiple Compressed Tablets (M.C.T)
why stage at all
More than a single compression
Produces multiple-layered tablets or a tablet within a tablet
Each layer may contain diff. medicinal agents. Why?
Separation may be required to avoid chemical and physical incompatibility
Staged drug release
The general appearance of the multiple-layered tablet
core has an active ingredient/drug substance
has a compressed layer also has an active drug
why stage at all: extended released, drug bioavailable, MEC will differ if not staged
Sugarcoated tablets (S.C.T)
Compressed tablet can be covered with a colored or an uncolored sugar layer
The coating is water-soluble
The coating is quickly dissolved after swallowing
The coating protects the enclosed drug from the environment
The coating enhances the general appearance of tablets and permits imprinting of identifying manufacturer’s info.
Disadvantages to sugarcoating tablets are,
the time and expertise required in the coating process,
and the increase in size, weight, and shipping costs.
Maybe 50% larger and heavier than uncoated tablets (cause it’s bigger)
cannot be SCT and ECT, pick one!
Film-coated Tablets (F.C.T)
what is it coated with and what is it like
it is usually colored
what makes it better than sugar coatings
what is it designed to do
These compressed tablets are coated with a thin layer of a polymer capable of forming a skin-like film over the tablet
Usually colored ( for patient compliance)
More durable, less bulky, and less time-consuming to apply than sugar-coatings.
Designed to rupture and expose the core tablet at the desired location within the gastrointestinal tract–absorption other than standard sites; more options
all coated: what is the reason for coated
Gelatin-coated tablets
what is its abbreviation?
what does it look like
what does it facilitate
GElCAP,
Capsule-shaped compressed tablets
Facilitates swallowing and compared to unsealed capsules, gelatin tablets are more tamper-evident
