Untitled Flashcards Set

erview of Capsules

Are solid dosage forms in which medicinal agents

and/or inert substances are enclosed in a small shell of

gelatin.

From the Latin word "capsula" meaning a small

container.

Hard or Soft

Body and a cap

Not suitable for efflorescent materials & deliquescent

materials.

API (Active Pharmaceutical Ingredient) - It refers to the

main ingredient in a drug that is responsible for its

therapeutic effects.

Immediate release -when no effort has been made to

modify the API release date

Type A (Cationic) - derived from acid treated precursor

at pH-9, mainly from animal bones

Type B (Anionic) - derived from alkali treated precursor

at pH-4.7, mainly from pork sin

Hard Gelatin Capsules

Most commercial medicated capsules

Empty shells are made of gelatin, sugar and water, and

plasticizer

May be colored with various FD&C and D&C dyes

Titanium dioxide - pacifying agent in capsules

Many capsules are packed along with a small packet or

cylinder of a desiccant material

Desiccant material used are dried silica gel, clay and

activated charcoal

Prolonged exposure to high humidity can affect in vitro

capsule dissolution

Different kinds of hard capsules:

Vegetarian capsules

Cellulose based

Consists of Hydroxypropyl methy|cellulose (HPMC) and

purified water

Contains no preservative, gelatin, wheat, animal by-

products or starch

Made from cellulose of pine or poplar

Fast dissolving

GMO free, gluten free and no preservatives

Special capsules shells for:

Sodium lauryl sulfate-free capsules

Opaque white capsules w/o titanium oxide

Liquid fill

Inhalation powders

Hygroscopic fill

Gelatin

Obtained by partial hydrolysis of collagen from white

connective tissue and bones of animals

Available in fine & coarse powder, shreds, flakes, or

sheets

Stable in air when dry but subject to microbial

decomposition when moist

Contains 13%-16% of moisture

Soften in cold water through absorption of water up to

10 times its weight of water

Soluble in hot water and in warm gastric fluid

Digested by proteolytic enzymes

Methods to track passage of capsules:

Tracking capsuled in the gastrointestinal tract to map

their transit time and drug-release patterns

Gamma scintigraphy - a noninvasive procedure that

entails the use of gamma ray-emitting radiotracer

incorporated into the formulation with a gamma camera

couple to a data recording system

Pharmacoscintigraphic evaluation

when scintigraphy and pharmacokinetic studies

combine

Provides information about transit and drug-release

patterns as well as the rate of drug absorption

Useful in:

A

Determining whether a correlation exists

between in vitro and in vivo bioavailability for

immediate-release products

B.

Assessing the integrity and transit time of

enteric-coated tablets

C. Drug and dosage form evaluation in new

product development

pH- sensitive nondigestible radiotelemetric device

(Heidelberg capsule)

approximate size of No. O capsule

sinas been use as a nnacuve means o

measure gastric pH in fasting and nonfasting human

subjects

Manufacture of Hard Gelatin Capsule Shells

Manufactured in two sections, body and shorter cap

The pegs are made of manganese bronze - affixed to

plates, each capable of holding up to 500 pegs

Dipping - Simultaneous cap and body formation

Spinning - Uniform gelatin distribution and bead prevention

Drying - The gelatin is dried by cool air to form a hard shell

Stripping - Capsule stripping by bronze jaws

Trimming and Joining - The stripped cap and body portions

are trimmed to the required length by stationary knives, then

joined and ejected from the machine as complete capsules

Polishing:

Pan Polishing - Acela-cota pan is used

Cloth Dusting - Rubbed with cloth

Brushing - Feed under soft rotating brush

Capsule shell design

Snap-Fit

Enables two halves of the capsule joined by locking

grooves in the shell walls

The two grooves fit into each other and thus ensure

reliable closing of the filled capsule

Modern Capsule-filling machines

Produces more than 180,000 capsules/hour

Splitting (telescoping) and denting of the capsule occur

with the slightest contact between the two rims when

they are joined

Coni-Snap

The rim of the capsule body is not straight, but tapered

slightly

Reduce the risk of capsule rims touching on joining and

eliminates problem of splitting during large-scale

operations

Coni-Snap Supro

Upper capsule part extends so far over the lower part

and the only rounded edge of the latter is visible

Less gripping in lower surface means increasing the

security of the contents

Capsule Sizes

000 (the largest) to 5 (the smallest) are commercially

available.

Larger capsules are for veterinary use

Size to use is determined by:

amount of material to fill (drug dose)

density

compaction/compressibility

Formulation and Selecting the Capsule Size

Goal is to prepare a capsule with accurate dosage, good

bioavailability, ease of filling and production, stability, and

elegance.

In dry formulations, the active and inactive components

must be blended thoroughly to ensure a uniform powder mix

for the fill.

low-dose drugs - lack of homogeneity in blending may result

in significant therapeutic consequences.

Preformulation studies are performed to determine

whether all the formulation's bulk powders may be

effectively

Uniform drug distribution can be achieved when density

and particle size of the drug and non-drug are similar

Particle size may be reduced by milling (50-1000 mcm)

Milled powders may be blended through a powder mix when

the drug's dosage is 10mg or greater

Micronization - used for drugs of lower dose or when

smaller particles are required

Produces particles about (1 to 20 mcm)

EXCEPIENTS in capsule formulation:

Diluents or Filler - fill the capsule volume

Example: Lactose, microcrystalline cellulose, starch

Disintegrants - assist in breakup and distribution of API in

the stomach

Example: Pregelatinized starch, croscarmellose, sodium starch

glycolate

Lubricant or glidant (0.25% to 1&)

Lubricant (magnesium stearate) -has waterproofing

characteristics and can retard penetration by the

gastrointestinal fluids and delay drug dissolution and

absorption

Lubricant (sodium lauryl sulfate) - a surface-active

ingredient used to facilitate wetting by the

gastrointestinal fluids

Glidant (talc) - commonly used to enhance flow

Generic substitution - inserting tablets or small capsules

into capsules in commercial production of capsules

to separate chemically incompatible agents or to add

premeasured amounts of potent drug substances

using prefabricated tablets to insert into a capsule as

an alternative instead of weighing

Coated pellets - designed for modified-release of drugs

(commonly placed in capsule shells)

Some liquids such as fixed or volatile oils do not interfere

with the stability of the gelatin shells may be placed in

locking gelatin capsules

Eutectic mixtures - have a propensity to liquefy when

admixed

To prevent: mix with a diluent or absorbent such as

magnesium carbonate, kaolin, light magnesium

oxide

In most instances, the amount or drug in a capsule is a

single dose. When the usual dose of the drug is too large for

a single capsule, two or more capsules may be required

To determine capsule size - amount of material to fill (drug

dose), density, and compaction/compressibility

In extemporaneous compounding, best capsule size is

determined by trial

A properly filled capsule should have its body filled with the

drug mixture, not the cap

Density is used to determine

Filling the capsule shells