III.

Solid Dosage Forms

Mary-Ann B. Sapnu, RPh, MSc
Learning Objectives
At the end of this session, the students will be able to:
◂ Demonstrate knowledge of the characteristics,
advantages and disadvantages various solid dosage forms

◂ Demonstrate understanding of the uses/applications and

administration of various solid dosage forms

2
Course Outline
◂ Powders and Granules
◂ Tablets
◂ Capsules
◂ Other solid dosage forms for oral
administration
◂ Lozenges (Troches)
◂ Lollipops
◂ Pellets
◂ Pills
◂ Bolus tablets
3
Powders

4
 Powders

◂ powders have a uniform, small particle size that has

an elegant appearance.

◂ In general, powders are more stable than are liquid

dosage forms and are rapidly soluble, enabling the
drug to be absorbed quickly.

5
 Powders

◂ Powder dosage forms have a large surface area that is

exposed to atmospheric conditions. Thus, powders
should be dispensed in tight containers.

◂ They are more reactive in nature because of their large

surface area.

6
Advantages

◂ Flexibility in compounding
◂ Relatively dry and devoid of moisture
◂ Stable than other dosage forms

7
Disadvantages

◂ It is not easily wetted

◂ It is not suitable for dispensing
◂ Inaccuracy of the dose to be given
◂ Some powders are hygroscopic and
deliquescent

8
Particle Size Analysis

◂ Purpose of obtaining quantitative data in

terms of size, distribution and shaping of
drug particles.

9
 Factors Influenced by Particle Size
◂ 1. Dissolution
◂ PS, DR
◂ e.g. Micronization
◂
◂ 2. Suspendability
◂ PS, S

10
 Factors Influenced by Particle Size
◂ 3. Penetrability
◂ Through Passive Diffusion

◂ 4. Lack of grittiness of solid particles in dermal

ointments, creams, and ophthalmic preparations.

11
Powder mixing
techniques

12
Comminution
1. Trituration
2.Levigation
3.Pulverization by Intervention

13
Small Scale

14
 Trituration

◂ Grinding a drug in a mortar to reduce its particle

size

15
 Three Kinds of Mortar and Pestle

◂ Porcelain – used in soft, aggregate

crystals

◂ Wedgewood – used in crystals

◂ Glass – suitable for solutions,

suspensions, ad ointments

16
 Levigation

◂ The formation of paste by the addition of a non-

solvent (levigating agent).

◂ Common Levigating agent:

◂ Mineral Oil
◂ Glycerin

17
 Levigation

◂ A mortar and pestle or an ointment tile may be

used.

18
 Pulverization by Intervention

◂ is used with hard crystalline powders that do not

crush or triturate easily, or gummy-type substances.
◂ The first step is to use an "intervening" solvent (such
as alcohol or acetone) that will dissolve the
compound.

19
Large Scale
1. Mills and Pulverizers

20
Blending
1. Tumbling
2.Spatulation
3.Sifting
4.Geometric dilution

21
 Tumbling

◂ Use of rotating chamber

◂ Mixing by this process is thorough but time

consuming. Such blenders are widely employed in
industry, as are mixers that use motorized blades to
blend powders in a large vessel.

22
 Spatulation

◂ mixing of powders is done by the movement of a

spatula throughout the powders on a sheet of a paper
or on a porcelain tile.

23
 Sifting
◂ relates to putting through a sieve or straining device to
separate fine particles from coarse ones.

◂ Sifting results in a light, fluffy product.

24
 Geometric dilution
◂ the potent drug is placed with an approximately
equal volume of the diluent in a mortar and is mixed
thoroughly by trituration.
◂ Then, a second portion of diluent equal in volume to
the mixture is added and the trituration repeated.
◂ This process is continued by adding an equal volume
of diluent to the powder mixture and repeating this
until all of the diluent is incorporated.

25
Types of Powder

◂ Bulk Powders – dispensed in large

quantities

◂ Divided Powders - individualized

powder; paper tabs

26
 Topical Powders

◂ Topical powders should have a uniform, small particle

size that will not irritate the skin when applied.
◂ should be impalpable and free flowing
◂ should easily adhere to the skin
◂ should be passed through at least a No. 100-mesh
sieve to minimize skin irritation

27
 Insufflated Powders

◂ Insufflated powders are finely divided powders that

are intended to be applied in a body cavity, such as
the ears, nose, vagina, tooth socket, or throat.

28
Type of Paper used in Divided Powders
◂ Bond Paper – has no moisture; resistive
property
◂ Glassine – glazed, transparent; has
moisture resistive property
◂ Vegetable parchment – thin, light, semi-
opaque, suitable for light-sensitive drugs/
powders.
◂ Wax paper – waterproof, for hygroscopic/
deliquescent powders
29
30
31
32
 Standards for Vegetable and Animal
Drugs:
DESCRIPTIVE TERM SIEVE # LIMIT

Very Coarse No. 8 NMT 20% pass through #60

Coarse No. 20 NMT 40% pass through #60

Moderately Coarse No. 40 NMT 40% pass through #80

Fine No. 60 NMT 40% pass through #100

No unit or limit to greater

Very Fine No. 80
fineness

33
34
 Standards for Chemical Drugs:
DESCRIPTIVE TERM SIEVE # LIMIT

Coarse No. 80
NMT 60% pass through #40
Moderately Coarse No. 40

Fine No. 80
No Limit
Very Fine No. 120

35
Granules

36
 Granules

◂ Are aggregations of fine particles of powders in a

mass of about spherical shape.

◂ Granules typically fall within the range of 4- to 12-sieve

size, although granulations of powders prepared in
the 12- to 20-sieve range are sometimes used in tablet
making.

37
38
Methods

39
 1. Wet Granulation

◂ Method in which the powder particles mix can be

done by the use of granulating liquid.

40
 Granulating Fluids

◂ Water
◂ Ethanol
◂ Isopropanol

41
 2. Dry Granulation

◂ Dry granulation may be used if the materials

have sufficient inherent binding or cohesive
properties to form granules.

◂ Dry granulation refers to the process of

granulating without the use of liquids.

42
 Two Types of Dry Granulation

◂ A. Slugging (Old Method)

◂ material to be granulized is
first made into a large
compressed mass or "slug"
typically by way of a tablet
press using large flat-faced
tooling.

43
 Two Types of Dry Granulation

◂ B. Roller Compactor / Chilsonator

material particles are consolidated and
densified by passing the material
between two high-pressure rollers

◂ densified material from a roller

compactor is then reduced to a
uniform granule size by milling

44
 Advantages of Granules:

◂ Flows well compared to powders (facilitates the

transfer of the material from the hopper to the tablet
press)
◂ Less surface area compared to powders (more stable
from humidity; less tendency to cake or harden)
◂ Easily wetted compared to powders (suitable for
drugs that needs to be reconstituted prior to use)

45
Tablets

46
 Tablet

◂ Solid dosage form that contains Active Ingredient and

additives and usually prepared by either molding or
compression.

47
 Types of Tablets

1. Molded Tablets 7. Chewable Tablets

2. Compressed Tablets 8. Effervescent Tablets
3. Multi-compressed 9. Buccal Tablets
Tablets 10. Sublingual Tablets
4. Sugar-coated Tablets 11. RTD tablets (Ready-to-
5. Film-coated Tablets disintegrate)
6. Enteric-coated Tablets 12. Vaginal Tablets

48
 Molded Tablets

◂ “soft tablets”
◂ e.g. Tablet triturate

49
 Compressed Tablets
◂ “hard tablets”
◂ e.g. simple compressed
tablets

50
 Multi-compressed
tablets
◂ Appears to be layered
◂ More than 1 component

51
 Sugar-coated tablets
◂ Masks the offensive taste of the medicament
◂ Offers protection of the Active Ingredient

Disadvantage:
- adds bulk to the tablet formulation (50%)
- Time consuming
- Needs expertise

52
 Film-coated tablets
◂ Apply a thin layer of polymer or plastic material to
make the tablet durable.

ADVANTAGES:
- Less time consuming
- Does not add bulk to the formulation

53
 Enteric-coated tablets
◂ Meant to disintegrate in the small intestine to prevent
mucosal irritation

◂ For the delivery of drugs that are optimally absorbed in

the small intestine to their primary absorption site in
their most concentrated form.

54
 Chewable tablets
◂ For individuals which have difficulty in
swallowing

Excipient: Mannitol, Xylitol (sugar-free)

55
 Effervescent Tablets
◂ When in contact with water, they release Carbon
Dioxide

56
 Buccal tablets
◂ Meant to be disintegrated in the buccal cavity or
cheeks

Advantages:
- Rapid effect
- Avoid First Pass
- Can be self-administered

57
 Sublingual tablets
◂ Are placed under the tongue
◂ Mostly are emergency drugs
◂ e.g. Catapres

Advantages:
- Rapid effect
- Avoid First Pass
- Can be self-administered
58
 RDT or Ready to Disintegrate Tablets
◂ Upon introduction into the mouth, these tablets
dissolve or disintegrate in the mouth.
◂ Antipsychotics
◂ e.g. Risperdal

59
 RDT or Ready to Disintegrate Tablets
Advantages:
- No requirement of water or other liquid to swallow
- Can be easily administered to children, old and
mentally disabled patients.
- Accurate dosing as compared to liquids.
- Dissolution and absorption of drug is fast, offering
rapid onset of action
- Higher bioavailability
- Suitable for sustained/controlled release actives
60
 Vaginal tablets
◂ AKA Vaginal Inserts, needs a
device called plastic inserter

Advantages:
-Avoidance of the first pass effect
and enzymatic deactivation in GIT
-non-invasive
-large permeation area
61
 Types of Tablets

1. Molded Tablets 7. Chewable Tablets

2. Compressed Tablets 8. Effervescent Tablets
3. Multi-compressed 9. Buccal Tablets
Tablets 10. Sublingual Tablets
4. Sugar-coated Tablets 11. RTD tablets (Ready-to-
5. Film-coated Tablets disintegrate)
6. Enteric-coated Tablets 12. Vaginal Tablets

62
Manufacture of Tablets

1. Dry Granulation
2. Wet Granulation
3. Direct Compression (most common)

63
Capsules

64
 Capsules
Solid dosage forms which contains the active ingredient +
excipient in a small shell of gelatin.

Gelatin – result of the partial hydrolysis of collagen,

obtained from the skin, white connective tissues and bones
of animals.

65
 Two Types of Gelatin
1. Type A – produced by acid hydrolysis

2. Type B – produced by basic/ alkaline hydrolysis

66
Two Types of Capsule

67
 Hard Gelatin Capsules (HGC)
-“two piece” capsule
-it can contain about 65 mg to 1 g powder material.
Components: Gelatin, Sugar, Water
Capsule Size: the larger the capsule no., the smaller the capsule size.
000 – Veterinary Purposes
0 – Biggest for humans
5 – Smallest
Moisture Level: 13-16%; does not require the presence of
preservative.
Method of Manufacturing: Punch Method
68
69
 Soft Gelatin Capsules (SGC)
-“one piece” capsule
Components: Gelatin, Polyhydric alcohol (sorbitol, glycerol)
Capsule Size: the larger the capsule no., the smaller the capsule size.
Moisture Level: 6-10%; >10% - require addition of preservatives
(parabens: methyl/ propylparaben)
Method of Manufacturing: Rotary Die Process

70
71
Other solid dosage
forms for oral
administration

72
Lozenges or troches
are disc-shaped solid dosage forms containing a medicinal agent
and generally a flavoring substance in a hard candy or sugar base.

They are intended to be slowly dissolved in the oral cavity, usually

for local effects, although some are formulated for systemic
absorption. An example would be Mycelex troches (Bayer
Consumer Care).

73
Lollipops
Fentanyl Actiq (Cephalon) is a raspberry lollipop that is a sugar-
based lozenge on a stick and contains fentanyl citrate. It has an
off-white color, and the stick bears a large Rx mark.

Actiq is the first product specifically designed to aid in controlling

breakthrough pain in cancer patients.

74
Pellets
Pellets are dosage forms that are composed of small, solid
particles of uniform shape sometimes called beads.

They can be used to provide physical separation for chemically or

physically incompatible materials, extended release of an active
pharmaceutical ingredient (API), or delayed release to protect an
acid labile API from degradation in the stomach or to protect
stomach tissues from irritation.

75
Pills
are small, round solid dosage forms containing a medicinal agent
and intended to be administered orally.

Excipients are selected for pills based on their ability to produce a

firm and plastic mass.

76
Bolus Tablets
re large, usually elongated tablets intended for administration to
large animals

77
Video Project on Compounding Powders
DUE: July 25, 2019 (Thursday)

78