Lecture 2 Capsules Flashcards
What are the capsule components?
Active ingredients, Diluent or filler, Disintegrant, and Lubricant/glidant
What is an example of diluent or filler in a capsule?
lactose, microcrystalline cellulose (brand name Avicel), and starch(absorbs moisture)
What does a disintegrant do?
facilitates break-up and distribution of the capsule’s contents. Helps break it up once its in the body.
What is an example of a disintegrant?
pregelantinized starch, croscarmellose, and sodium starch glycolate
What does a lubricant/glidant do?
improve powder flow (want to use small amount)
What is an example of a lubricant/glidant in a capsule?
Fumed silicon dioxide, magnesium stearate, calcium stearate, stearic acid, or talc
How do you select a capsule size?
Trial and error but you can narrow your search by: Compare formulation characteristics to the characteristics of a known drug, volume occupied, The rule of sixes, the rule of sevens.
What do you convert to when using rules of 6’s and rules of 7’s?
grains (65 mg in 1 grain)
What does a hard gelatin capsule made of?
A body and a cap.
When compounding a control substance you make extra capsules. T/F
False
When developing the formulation and selection of capsule size you need to consider…
Accurate dosage, good bioavailability, ease of filling and production, stability, and elegancy(want them to look full and no powder on side).
When compounding a potent powder what do we need to consider?
it needs to be evenly distributed (geometric dilution)
What would you put a tablet within a capsule?
Protect from light, clinical trials (all look the same).
What types of quality control would you do on capsules?
Drug content, fill weight, disintegration, dissolution, and stability.
What types of preparations are there of capsules?
Extemporaneous (punch method and small capsule filling machines, 100-3–), Industrially (automated filling machines)
What is disintegration testing?
Test drug by assimilating conditions in body (37 C temperature, gastric juices,) to see if drug will disintegrate in body.
What is dissolution testing?
Test to see if the drug has actually gone into solution.
What can the weight variation be according to USP?
Capsule shall not be less than 90 percent and not more than 110 percent of the theoretical calculated weight of each unit.
What is content uniformity?
The amount of active ingredient should be within 85 to 115 percent of the label claim for 9 out of 10 dosage with no unit outside of 70 to 125 percent of label claim.
What is the content labeling requirement?
Capsules must be labeled to express the quantity of each active ingredient in each dosage unit.
What is stability testing?
Intrinsic stability of active drug molecule under different environmental factors (temperature, humidity, light, formulation components, and container and closure system).
What is the USP 795 require in regards to stability?
6 months if prepared from USP/NF ingredients or 25% of remaining expiration dating if prepared from commercial products unless evidence is available to support other dating
What is the moisture permeation test?
single-unit and unit-dose containers to ensure stability for packaging.
What is a solid dosage form inn which the durg is enclosed within a hard or soft soluble container or shell. The shells are usually made from gelatin; however, they may also be made from starch or other suitable substances
Capsules
What are the advantages of capsules?
Mask unpleasant tastes, aromas and appearances of a drugEasy to prepareCan vary dosage and combination of drugsEasy to swallowSolubilityStabilityEasy to carry
What are the disadvantages of capsules?
Easily tampered withsensitive to humidity and microbial contaminationDifficult for some populations to swallowUnsuitable for aqueous liquidsNot suitable for administering very soluble ionic salts
How is gelatin obtained?
From partial hydrolysis of collagen from skin, white connective tissue and bones of animals.
Hard Gelatin Capsules are stable in air when dry, but subject to microbial decomposition when moist. T/F
True
Hard Gelatin Capsules contain no moisture. T/F
False, they contain 13-16 percent moisture
Hard Gelatin Capsules may absorb additional moisture and lose their rigid shape in high humidity. T/F
True
Hard Gelatin Capsules may gain moisture in extreme dryness. T/F
False, Hard Gelatin Capsules may lose normal moisture in extreme dryness which leads them to become dry and brittle.
What sizes do capsules run in? What is largest and what is smallest?
000 (largest) to 5 (smallest)
How do you select an appropriate capsule size?
Compare formulation characteristics to the characteristics of a known drugVolume occupiedThe rule of sixesThe rule of sevens
What is the rule of sixes?
Bulk densities of many powders average about 0.6 g/mL
What is the rule of sevens?
Convert formulation weight to grains (65mg in 1 grain), subtract from seven; use table to determine appropriate size. *Only works if calculated values are between -3 and 5.
How do you measure how much of the drug is being released?
By measuring the concentration of drug in the solution by dissolution testing.
What is the capsule weigh variation?
Capsule weight should be not less than 90% and not more than 110% of the theoretical calculated weight of each unit.
What is the content uniformity variation?
The amount of active ingredient should be within 85% to 115% of the label claim for 9 out of 10 dosage units assayed, with no unit outside of 70% to 125% of label claim.
