Pha 041 sas 3

PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Lesson title: Solid Dosage Forms: Powders, Granules, Capsules
PART I
Materials:
Book, Pen and SAS
Lesson Objectives:
At the end of the lesson, you should be able to:
1. Identify and different types of solid dosage forms: Powders,
Granules and Capsules
2. Describe the various solid dosage forms their preparations and
methods
References:
Ansel’s Pharmaceutical Dosage
Forms and Drugs Delivery Systems
9th Edition
Productivity Tip: Think of the most convenient dosage form you had taken. If you are taking vitamins or
medicines everyday have you wondered why it is in such a form?
A. LESSON PREVIEW/REVIEW
Introduction (3 mins)
In this section, it is important to be able to differentiate each solid dosage forms and its preparations and
methods. From a pharmaceutical standpoint, solid dosage forms are efficiently and productively
manufactured; they are packaged and shipped by manufacturers at lower cost and with less breakage than
comparable liquid forms. They are also more stable and have a longer shelf life than do their liquid
counterparts.
Powder is defined as a dosage form composed of a solid or mixture of solids reduced to a finely
divided state and intended for internal or external use.
Granules are defined as a dosage form composed of dry aggregates of powder particles that
may contain one or more active pharmaceutical ingredients with or without other ingredients.
Capsules are solid dosage forms in which medicinal agents and or inert substances are enclosed
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
in a small shell of gelatin.
Solid-dosage forms are efficiently and productively manufactured; they are packaged and
shipped by manufacturers at lower cost and with less breakage than comparable liquid forms. They are also
more stable and have a longer shelf life than do their liquid counterparts.
1) Activity 1: What I Know Chart, Part 1 (2 mins)
Instructions: In this chart, reflect on what you know now. Do not worry if you are or not of your
answers. This activity simple serves to get started on thinking about our topic. Answer only the first
column, “what I know”. Leave the third column “what I learned” blank at this time.
What I Know
Questions:
What I Learned (Activity 4)
1.What is a solid dosage form?
Give 3 examples
2.What’s the difference between
powders and granules in terms of
flowability?
3.What does volatile substance
means?
B.MAIN LESSON
Activity 2: Content Notes (18 mins)
Powders
Properly prepared, powders have a uniform, small particle size that has elegant appearance. In
general, powders are more stable than are liquid dosage forms and rapidly soluble, enabling drug to be
absorbed quickly.
Before their use in the preparation of pharmaceutical products, solid materials first are characterized to
determine their chemical and physical features, including morphology, purity, solubility, flowability,
stability, particle size, uniformity and compatibility with any other formulation.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Powders have qualities that make them an attractive dosage form for certain situations. It
provides a rapid onset of action because they are readily disperse, have a large surface area, and usually
require only dissolution, not disintegration, before absorption. Although the use of medicated powders
per se in therapeutics is limited, the use of powdered substances in the preparation of other dosage
forms is extensive. The particles of pharmaceutical powders and granules may range from being
extremely coarse to extremely fine.
Particle size and Analysis
Type
Description
Very coarse (No.8) powder
All particles pass thru no. 80 sieve and NMT 20% pass thru no. 60
Coarse (No.20) powder
All particles pass thru no. 20 sieve and NMT 40% pass thru no. 60
Moderately coarse (No.40)
powder
All particles pass thru no. 40 sieve and NMT 40% pass thru no. 80
Fine (No.60) powder
All particles pass thru no. 60 sieve and NMT 40% pass thru no. 100
Very fine (No.80) powder
All particles pass thru no. 80 sieve
Particle size can influence a variety of important factors:
• Dissolution rate of particles
• Suspendability of particles
• Uniform distribution of drug substance
• Penetrability of particles
• Lack of grittiness of solid particles in dermal ointments, creams, and ophthalmic
preparations
Methods for Determination of Particle size (Found in your book on Chapter 6: Powders and Granules
• Sieving, in which particles are passed by mechanical shaking through a series of sieves
of known and successively smaller size and the proportion of powder passing through
or being withheld on each sieve is determined.
• Microscopy, in which sample particles are size through the use of a calibrated gird
background or other measuring device
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
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Sedimentation rate, in which particle size is determined by measuring the terminal
settling velocity of particles through a liquid medium in a gravitational or centrifugal
environment, it can also be calculated from Stokes law.
Light Energy Diffraction or Light Scattering or light scattering, in which particle size
is determined by the reduction in light reaching the sensor as the particle, dispersed
in a liquid or gas, passes through the sensing zone
Laser Holography, in which a pulse laser is fired through an aerosolized particle spray
and its photographed in three dimensions with a holographic camera, allowing the
particles to be individually imaged and sized
Cascade Impaction, which is based on the principle that a particle driven by an
airstream will hit a surface in its path, provided its inertia is sufficient to overcome the
drag force that tends to keep it in the airstream. Particles are separated into various
size ranges successively increasing the velocity of the airstream in which they are
carried
Good to Know!
Micromeritics is the science of small particles; a particle is any unit of matter having defined physical dimensions. It is
important to study particles because most drug dosage forms are solids, solid are not static systems, the physical state of
particles can be altered by physical manipulation, and particle characteristics can alter therapeutic effectiveness.
Comminution of Drugs
Comminution, reduction of the particle size of a solid substance to a finer state, is used to
facilitate crude drug extraction, increase the dissolution rates of drug, aid in the formulation of
pharmaceutically acceptable dosage forms and enhance the absorption of drugs. Grinding a drug in a
mortar to reduce its particle size termed as trituration or comminution.
Levigation is commonly used in small-scale preparation of ointments and suspensions to
reduce the particle size and grittiness of the added powders.
Blending Powders
When two or more powdered substances are to be combined to form a uniform mixture, it is best
to reduce the particle size of each powder individually before weighing and blending. Depending on the
nature of the ingredients, the amount of powder, and the equipment, powders may be blended by
spatulation, trituration, sifting and tumbling.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Spatulation is blending small amounts of powders by movement of a spatula through them on a
sheet of paper or an ointment tile. It is not suitable for large quantities of powders containing potent
substances, because homogeneous blending is not certain as other methods.
Trituration may be employed both to comminute and to mix powders. If simple admixture is
desired without special need for comminution, the glass mortar is usually preferred. When a small
amount of a potent substance is to be mixed with a large amount of diluent, the geometric dilution
method is used to ensure uniform distribution of the potent drug. This method is especially indicated
when the potent substance and other ingredients are the color and a visible sign of mixing is lacking.
Powders may also be mixed by passing them through sifters like those used in the kitchen to sift
flour. Sifting results in a light, fluffy product. This process is not acceptable for the incorporation of the
potent drugs into a diluent powder.
Another method of mixing powders is tumbling the powder in a rotating chamber. Mixing by this
process is thorough but time consuming. Such blending is widely employed in industry, as are
More terms to remember!
Medicated Powders
Eutectic powders may become sticky or
pasty, or they may liquefy when mixed
together.
Hygroscopic powders will absorb moisture
from the air.
Deliquescent powders will absorb moisture
from the air to the extent that they will
partially or wholly liquefy.
Efflorescent powder is a crystalline powder
that contains water of hydration or
crystallization. This water can be liberated
either during manipulations or on exposure
to low-humidity environment. If this occurs,
the powder will become sticky and pasty or
it may even liquefy.
mixers that are motorized blades to blend powders in a large
vessel.
Segregation is an undesirable separation of the different
components of the blend. Segregation may occur by sifting or
percolation, air entrapment (fluidization), and particle
entrapment (dusting). Fine particles tend to sift or percolate
through coarse particles and end up at the bottom of the
container and actually lift the larger particles to the surface.
Fine, aerated powders with differences in particle size or density
may result in a striation pattern and may occur during powder
transfer. Dusting occurs when the finer, lighter mixture and
repeating this until all of the diluent is incorporated.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Some medicated powders are intended to be used internally and other externally. Most can be
taken orally after mixing with water and some are inhaled for local or systemic effects. Examples are
Aerosol powders, Bulk and Divided powders. Divided powders may be prepared by the pharmacist
depending on the potency of the drug substance. Powder papers are used and may be of any size
convenient to hold the amount of powder required. The papers may be:
Types of Paper
Description
Simple bond paper
Not used for volatile components or substances affected by
moisture
Vegetable parchment
Semi-opaque and has limited moisture resistance
Glassine
Transparent paper and has limited moisture resistance
Waxed paper
Transparent and a water-proof paper for volatile substance
Types of Mortar and Pestle and uses
Type
Use
Glass mortar
Used in preparing solutions and suspensions
Wedgwood
Suited for crystalline solids
Porcelain
For soft aggregates or crytals
Types of Powder
Description
Aerosol powders
Medicated powder administered by inhalation with the aid of dry
powder inhalers which deliver micronized particle of medication in
metered quantities
Bulk powders
Medication in bulk quantities is limited to nonpotent substances and
controlled dosage should not be dispensed in this manner
Divided powders
After a powder has been properly blended it maybe divided into
individual dosing and is suitable for potent drugs
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Advantages and Disadvantages of Powders
Advantages
• Flexibility in compounding
• Good chemical stability
• Preferred as oral dosage form for
those with difficulty in swallowing
• Preferred when dose is too bulky to
be made tablet or capsule Faster
• dissolution rate
Disadvantages
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Time-consuming in preparation
Not well suited for dispensing
For bulk powders, inaccuracy of dose
Granules
As indicated previously, granules are prepared agglomerates of smaller particles of powder.
They are irregularly shaped but may be prepared to be spherical. Granules flow well compared to
powders because of its flow properties, granulations are commonly used in tablet making to facilitate
free flow of material from the feeding container. A number of commercial products containing antibiotic
drugs that are unstable in aqueous solution are prepared as small granules for constitution by the
pharmacist with purified water just prior to dispensing.
Granules are prepared by wet methods and dry methods.
Wet method
Wet method is to moisten the powder or powder mixture and then pass the resulting paste
through a screen of the mesh size to produce the desired size of granules. The granules are placed on
drying trays and are dried by air or under heat. The granules are periodically moved about on the drying
trays to prevent adhesion into a large mass.
Another type of wet method is fluid bed processing, in which particles are placed in conical piece
of equipment and are vigorously dispersed and suspended while a liquid excipient I sprayed on the
particles and the product dried, forming granules or pellets of defined particle size.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Dry method
Dry granulation method may be performed in a couple of ways. By one method, the dry powder
is passed through a roll compactor and then through a granulating machine. A roll compactor also called
a roll press or roller compactor processes a fine powder onto dense sheets or forms by forcing it through
two mechanically rotating metal rolls running counter to each other, the surface of the compacting rolls
may be smooth or may have pockets indentations or corrugations that allow compaction of different
forms and textures. The compacted powder is granulated to uniform particle size in a mechanical
granulator.
An alternative dry method, termed slugging, is the compression of a powder or powder mixture
into large tablets or slugs on a compressing machine under 8000 to 12000lb of pressure, depending on
the physical characteristics of the powder. The slugs are generally flat-faced and are about 2.5cm in
diameter. The slugs are granulated into the desired particle size, generally for the use in the production
of tablets.
Effervescent Granulated Salts
Effervescent salts are granules or coarse to very coarse powders containing a medicinal
agent in a dry mixture usually composed of sodium bicarbonate, citric acid, and tartaric acid. When added
to water, the acids and the base react to liberate carbon dioxide, resulting in effervescence. The
combination of citric acid and tartaric acid avoids certain difficulties. When tartaric acid is used alone,
the resulting granules readily lose their firmness and crumble. Citric acid alone results in a sticky mixture
difficult to granulate.
When medications are to be administered orally to adults, capsules and tablets are usually
preferred because they are conveniently carried, readily identified and easily taken. Capsules and tablets
are available for many medications in a variety of dosage strengths, providing flexibility to the prescriber
and accurate individualized dosage for the patient.
Advantages of Granules
• Better flow
• More stable in the presence of atmospheric air
• Less likely to cake
• Easily wetted
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Patient Counseling
Reconstituted suspensions should be thoroughly mixed or shaken before use to resuspend the
dispersed particulates. This is especially true if suspension preparations dosed from multiple-dose
containers. For particularly viscous suspensions prone to air entrapment, instructions may advise the
user how to shake the preparation to resuspend settled particles while minimizing air entrapment.
Capsules
When medications are to be administered orally to adults, capsules and tablets usually are
preferred because they are conveniently carried, readily identified and easily taken.
Numerous characteristics help to identify capsules and tablets, including the shapes and colors
of capsules and tablets. Capsules and tablets are available for many medications in a variety of dosage
strengths, providing flexibility to the prescriber and accurate individualized dosage for the patient.
Capsules’ medicinal agents are enclosed in a small shell of gelatin. Gelatin is obtained by the
partial hydrolysis of collagen obtained from the skin, white connective tissue and bones of animals.
Gelatin is stable in air when dry but is subject to microbial decomposition when it becomes moist. The
shells may be composed of two pieces or single piece. Capsule shells are usually made from cellulose
polymers or other suitable material. Two-piece capsules are commonly referred to as hard-shell capsules
and one-piece capsules are often referred to as soft-shell capsules.
Types of Gelatin capsule shell
Hard gelatin capsule shells are used in most commercial medicated capsules. It is stable in
air when dry but is subject to microbial decomposition when it becomes moist. Normally, hard gelatin
capsules contain 13-16% of moisture. Capsule shells are usually made from gelatin however they may
also be made from cellulose polymers or other suitable material.
Soft gelatin capsule shells are made of gelatin to which glycerine or polyhydric alcohol such
as sorbitol has been added. It may contain more moisture than hard capsules, may have a preservative
to retard microbial growth. Soft gelatin capsules are used to encapsulate and hermetically seal liquids,
suspensions, pasty materials, dry powders and even preformed tablets. Soft gelatin capsules are
pharmaceutically elegant and are easily swallowed.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Capsule sizes
For humen use, empty capsules, 000 is the largest and 5 is the smallest.
Preparation of Filled Hard Gelatin capsules
1. Developing and preparing the formulation and selecting the size capsule
2. Filling the capsules shells
3. Capsule sealing
4. Cleaning and polishing the filled capsules
Preparation of Soft Gelatin capsules
1. Plate process
2. Rotary die process
3. Reciprocating die process
Compendial requirements for Capsules when substances are added
• harmless in the quantities used
• does not exceed the minimum amounts required to provide their intended effect
• does not impair the product’s bioavailability, therapeutic efficacy and safety
• do not interfere with requisite compendial assays and tests
Oral Administration of Solid Dosage Forms
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Solid dosage forms (capsules and tablets) for oral administration are best taken by placing the
dose upon the tongue and swallowing it with a glassful of water or beverage. Ingesting solid dosage
forms with adequate amounts of fluid is important. Some patients attempt to swallow a tablet or capsule
without water, but this can be dangerous because of the possibility that it will lodge in the esophagus.
If patient cannot swallow a solid dosage from, the pharmacist can suggest a chewable or liquid
form of the drug. If these are not available, an extemporaneously compounded liquid form may be
prepared. Extemporaneous compounding involves a pharmacist preparing a dosage form suitable for an
individual patient.
Activity 3: Skill-building Activities (20 mins)
Provide the following:
I.
List 4 counseling points for proper administration of capsules:
1. ________________________________________________________________________
________________________________________________________________________
2. ________________________________________________________________________
________________________________________________________________________
3. ________________________________________________________________________
________________________________________________________________________
4. ________________________________________________________________________
________________________________________________________________________
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
Activity 4: What I Know Chart, part 2 (2 mins)
Instruction: To review what was learned from this session, please go back to “What I Learned”
column. Notice and reflect on any changes in your answers.
Activity 5: Check for Understanding (10 mins)
Instruction: Now it’s time for you to figure this one out on your own! Take time to read, analyze and
understand the following scenarios.
A. Identify the following:
HYGROSCOPIC 1. Substances that absorbs water from air but do not liquefy
5
2. The smallest capsule size
GELATIN 3. Obtained in partial hydrolysis of collagen obtained from the skin, white connective tissue
and bones of animals
VERY FINE 4. Refers to all particles pass through sieve no. 80
LEVIGATION 5. It is used in small scale preparation of ointments and suspensions to reduce particle size
and grittiness of the added powders
PORCELAIN 6. A type of mortar and pestle used for soft aggregates
GRANULES 7. A dosage form that has a better flow and more stable in the presence of atmospheric air
13-16% OF MOISTURE 8. Moisture content of a hard gelatin capsule
VOLATILE 9. A substance easily evaporated
WAXED PAPER 10. A type of paper used in for divided powders that is ransparent and a water-proof
paper for volatile substance
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
C. LESSON WRAP-UP
Activity 6: Thinking about Learning
A. Work Tracker: You are done with this session! Let’s track your progress. Shade the session number you
just completed.
P1
1
2
3
P2
4
5
6
7
8
9
10
B. Think about your Learning: Tell me about your thoughts. Today’s topic is all about Powders, Granules
and Capsules. What surprised you about the lesson today? Explain why.
____________________________________________
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____________________________________________
____________________________________________
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FAQs
1. Is it needed to drink fluids in taking solid dosage forms? Ans. Yes, ingesting solid dosage forms with
adequate amounts of fluid is important to avoid possibility that it will lodge in the esophagus. A
glassful of water or beverage can be given.
2. Why some medications intended for oral administration needs to be reconstituted? Ans. Some oral
administration are relatively unstable in liquid form so they are provided to the pharmacist by the
manufacturer as a dry powder or granule for constitution with specified quantity of purified water at
the time of dispensing. Under labelled conditions of storage, the resultant product remains stable
for the prescribed period of use generally 2 weeks.
This document is the property of PHINMA EDUCATION
PHA 041: Pharmaceutical Dosage Forms and Drug Delivery Systems
Student Activity Sheet
MODULE # 3
Name: ______________________________________________________ Class number: ______ Section:
____________ Schedule: _______________________________ Date:______________
This document is the property of PHINMA EDUCATION
Name:
Description:
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