SCHOOL OF ALLIED HEALTH SCIENCE

DEPARTMENT OF PHARMACY

COURSE: INTRODUCTION TO PHARMACY

GROUP ASSIGNMENT 2

GROUP 4

CLINTON TINARWO H220245X

ANESU BIZABANI H220245X
NYASHADZASHE MUSIYIWA H220636Y
LAZARUS ALOIS JENYURA H220209G
RUMBIDZAI TENDERERE H220354Z
BRENDA JIMU H220594X
SUCCESS MUZONDI H220501G
TERRENCE NKIWANE H220474X
CHIBUNDU SHUPIKAI H220108X
NATASHA TAMBAMA H220369T
YVONNE MHAKAYAKORA H220685A
1) EXCIPIENTS

Pharmaceutical excipients are substances that are included in a pharmaceutical dosage form not
for their direct therapeutic action but to aid the manufacturing processes, to protect, support or
enhance stability, or for bioavailability or patient acceptibility. The term comes from a latin word
"excipiens" to receive or to take out. According to International pharmaceutical excipient council
(IPEC), excipients are the process aids or any substances other than the Active Pharmaceutical
ingredients (API) that is included in Pharmaceutical dosage forms. API are bulk drugs that are
pharmaceutically active and generate a desired pharmacological effect whereas excipients are
pharmacologically inactive substances that are generally used as a carrier of the API in the drug.

Characteristics of excipients

1. They must be nontoxic and acceptable to the regulatory agencies in all countries where the
product is to be marketed.

2. They must be commercially available in an acceptable grade in all countries where the product
is to be manufactured.

3. Their cost must be acceptably low.

4. They must not be contraindicated by themselves (e.g., sucrose) or because of a component

(e.g., sodium) in any segment of the population.

5. They must be physiologically inert.

6. They must be physically and chemically stable by themselves and in combination with the
drug(s) and other tablet components.

7. They must be free of any unacceptable microbiologic load.

8. They must be color-compatible (not produce any off-color appearance).

9. If the drug product is also classified as a food, (certain vitamin products), the diluent and
excipients must be approved direct food additives.

10. They must have no deleterious effect on the bioavailability of the drug(s) in the product.

Classification of excipients

1. Excipients for use in oral Medicines.

a. Excipients used in solid dosages form.

b. Excipients used in liquid dosage forms.

c. Excipients used in semi-solid forms.

2. Excipients used for parenteral (injection).

3. Excipients used in topical (application to the skin) drug delivery systems.

4. Excipients used in intranasal delivery systems.

Primary excipients

1) Diluents (filler)

They act as bulking agents to make the tablet weight practical (minimum weight 50mg) for the
patient. The dosage can be as low as 20 micrograms for oral steroids. They aid compression that
is deforms and fragments readily to facilitate robust bonding in tablet compacts. They also
function to enhance flow by reducing viscosity, to archive targeted content uniformity, and to
facilitate tablet handling during manufacture. Examples of diluents include sugar compounds
(lactose, dextrin, glucose, sucrose, sorbitol), inorganic compounds (silicates, calcium and
magnesium salts, sodium chloride).

2) Binders (adhesives)

Binder are used to hold active pharmaceutical ingredient and inactive ingredients together,
ensuring mechanical strength and exhibiting cohesive and adhesive force. Binders can be soluble
(HPMC) or insoluble (starch) in water or in both water and ethanol such as providone. They can
be classified according to their application, for example dry binders find use in direct powder
compression and dry granulating and as a solution or paste in wet granulation. Most binders are
either polysaccharide, disaccharides, protein, natural gums or synthetic polymers. Examples of
binders include starches, modified cellulose, sugar alcohols, etc.

3) Disintegrants and super-disintegrants

They disintegrate and cause rapid breakup of the tablet compact upon exposure to moisture.
They aid dispersion of the tablet in the GIT releasing the active ingredients and increasing the
surface area for dissolution.

Modes of action and examples:

Swelling (cellulose and its derivatives)

Porosity and capillary action (microcrystalline cellulose)

Deformation by enzymatic reaction: enzymes destroy the binding action of the binder. For
example amylase acts on starch binder and protease acts on gelatin.

4) Lubricants
They are used in formulations to smooth ejection of the tablet from cavity, reduce friction
between particles during compression, improve flow of powder blend and granules into the die
cavity, and prevent sticking of the powder on punch faces.

5) Glidant

They enhance flow property of powder blend by overcoming powder cohesiveness

6) Antiadherent: prevent sticking to the punch

Secondary excipients

1) Flavours

They are used to impart a pleasant flavour and odour to pharmaceutical formulations. They
ensure patient compliance especially in pediatric formulations. They can be natural (pepper mint,
and lemon oil) or artificial (butterscotch).

Bitter product-mint, cherry may be used

Salty product-peach, apricot may be used

Sour product-raspberry or liquorice may be used

Excessively weet product-vanilla may be used

2) Sweeteners

They are incorporated in tablets to impart sweetness to the product and hence the acceptability
of tablets. They are of particular importance if the tablet has a bitter drug substance. Can be
artificial such as saccharine and its salt, aspartame, and acesulfame-K or natural such as sorbitol
and sucrose

3) Coating agents

These excipients are added to tablets to help make large, difficult to swallow pill easier to
swallow. They prevent deterioration from water and moisture. Enteric coating allow for
breakdown in the small intestine, preventing breakdown in the acidic environment of the
stomach. A Hydroxypropyl methylcellulose (HPMC) film coating is used in most coated tablets
because it is sugar free and free of potential allergens. Other coating materials include synthetic
polymers, Cellulose acetate, phthalate, ethlycellulose, and methlycellulose

4) Plasticizers
They are substances that are added to drugs to make them softer and more flexible and to
decrease their viscosity. They are used for physical modification of coating polymer. Examples,
Glycerin monosterate, Polysobate80, Triethyl citrate, Triacetin

5) Wetting agents (surfactant)

They are chemical substance that increase the spreading and penetrating properties of a liquid
by lowering its surface tension. Not all are suitable for oral administration. Examples include
polysorbates and sodium louryl sulphate but these can cause excessive foaming if levels are too
high

6) Colourants

They are generally employed in tablet manufacture either for aesthetics or to uniquely identify
finished tablets. They minimize the possibility of mix ups. A distinction should be made between
excipients which have inherent colour and those that are used as colorants. Colorants can either
be water soluble dyes or water insoluble pigments. Each country has its own list of approved
colorants. Any of the approved, certified, water soluble FD&C dyes, mixtures of the same, or
their corresponding lakes may be used to colour tablets. The colour should be uniformly
distributed throughout the tablets. Examples include iron oxides, titanium dioxide, and
aluminium lakes.

Miscellaneous excipients

1) Buffers

Buffers can be necessary to maintain pH of the formulation in order to ensure physical

compatibility, and optimize solubility. Sodium phosphate, citric acid and acetic acid and
tromethamine.

2) Adsorbents

They are agents that will either allow substances to stick or adhere to them. Adsorbents are used
whenever they is need to include a liquid or semi-solid drug substance or excipient within the
tablet formulation. They adsorb moisture that may attack tablets or cause cohesiveness of tablet
power/granules from these liquid or semi-solid components thus allow proper tablet compression
during tablet formulation. The liquid or semi-solid constituents is adsorbed onto a solid
component which in many cases may be one of the other components in the tablet formulation
(eg diluents during mixing). If this approach is not possible then an adsorbent is specifically
included in the formulation. Examples Silicon dioxide, bentonite, caolin, magnesium silicate,
tricalcium phosphate, magnesium carbonate and magnesium .

Some excipients may cause adverse reactions in patients as shown by the table below
Table adopted from www.australianprescriber.com

2) WILLOW BARK

Willow bark is the common name for the dried bark of variouse species of the plant salix. The
willow family includes a number of different species of trees and shrubs native to Europe, Asia,
and some parts of North America. Some of the more commonly known species are white
willow/European willow (Salix alba), black willow/pussy willow (Salix nigra), crack willow
(Salix fragilis), purple willow (Salix purpurea), and weeping willow (Salix babylonica). The
willow bark sold in Europe and the United States usually includes a combination of the bark
from white, purple, and crack willows. Willow bark preparations are obtained by comminuting
(reducing into tiny pieces) or powdering the bark and as dry or liquid extracts. Extracts are
obtained by putting the plant material in a solvent (such as ethanol or water) to dissolve
compounds and form a liquid extract. The solvent is then evaporated to obtain a dry extract.
Herbal medicines containing these willow bark preparations are usually available as herbal tea to
be drunk and in solid or liquid forms to be taken by mouth.
Willow bark preparations may also be found in combination with other herbal substances in
some herbal medicines.

History of willow bark

The use of willow bark dates to the time of Hippocrates (400 BC) when people were advised to
chew on the bark to reduce fever and inflammation. Hippocrates burned willow leaves to make
smoke for “fumigating” the uterus to get rid of a miscarried pregnancy. Willow bark has been
used throughout the centuries in China and Europe, and continues to be used today for the
treatment of pain (particularly low back pain and osteoarthritis), headache, and inflammatory
conditions, such as bursitis and tendinitis.

Medicinal Uses and Indications

Willow bark is used to ease pain and reduce inflammation. Researchers believe that the chemical
salicin, found in willow bark, is responsible for these effects. However, studies show several
other components of willow bark, including plant chemicals called polyphenols and flavonoids,
have antioxidant, fever-reducing, antiseptic, and immune-boosting properties. Some studies
show willow is as effective as aspirin for reducing pain and inflammation (but not fever), and at
a much lower dose. Scientists think that may be due to other compounds in the herb. More
research is needed.

Treatment

Studies suggest that willow bark may be useful for the following conditions:
Headache
Willow bark has been shown to relieve headaches. There is some evidence that it is less likely to
cause gastrointestinal side effects than other pain relievers, such as ibuprofen (Advil) and other
nonsteroidal anti-inflammatory drugs, do. However, studies have not shown this beyond all
doubt, and people who are prone to stomach upset may want to avoid willow bark. Large-scale
studies are needed to fully determine how safe and effective willow bark is for chronic or
recurring headaches.

Low back pain

Willow bark appears to be effective for back pain. In a well-designed study of nearly 200 people
with low back pain, those who received willow bark experienced a significant improvement in
pain compared to those who received placebo. People who received higher doses of willow bark
(240 mg salicin) had more significant pain relief than those who received low doses (120 mg
salicin).

Osteoarthritis
Several studies show that willow is more effective at reducing pain from osteoarthritis than
placebo. In a small study of people with osteoarthritis of the neck or lower back, those who
received willow bark experienced significant improvement in symptoms compared to those who
received placebo. A similar study of 78 people hospitalized with osteoarthritis of the knee or hip
joint found that people who received willow bark had significant pain relief compared to those
who received placebo.

Other uses
Professional herbalists may recommend willow bark for the following conditions, however, more
research is needed.
• Menstrual cramps
• Fever
• Flu
• Tendonitis
• Bursitis
• Cancer

Dosage and Administration

Pediatric
Because of the danger of developing Reye syndrome (a rare but serious illness associated with
the use of aspirin in children), children under the age of 18 should not take willow bark.
Adult
Speak to your doctor to determine the appropriate dose for you.
Precautions
Because willow bark contains salicin, people who are allergic or sensitive to salicylates (such as
aspirin) should not use willow bark. Some researchers suggest that people with asthma, diabetes,
gout, gastritis, hemophilia, stomach ulcers, or with kidney or liver issues should also avoid
willow bark. If you have any of these conditions, or if you take nonsteroidal anti-inflammatory
drugs (NSAIDs) or blood-thinning medication, ask your health care provider before taking
willow bark. Children under the age of 16 should not take willow bark.

Side Effects
Side effects tend to be mild. However, stomach upset, ulcers, nausea, vomiting, and stomach
bleeding are potential side effects of all compounds containing salicylates. Overdoses of willow
bark may cause skin rash, stomach inflammation/irritation, nausea, vomiting, kidney
inflammation, and tinnitus (ringing in the ears).

Pregnancy and Breastfeeding

Salicylates are not recommended during pregnancy, so pregnant and breastfeeding women
should not take willow bark.

Interactions and Depletions

Because willow bark contains salicylates, it might interact with a number of drugs and herbs.
Talk to your doctor before taking willow bark if you take any other medications, herbs, or
supplements.

Willow bark may interact with any of the following:

Anticoagulants (blood-thinning medications): Willow bark may strengthen the effects of drugs
and herbs with blood-thinning properties, and increase the risk of bleeding.
Beta blockers: including Atenolol (Tenormin), Metoprolol (Lopressor, Toprol-XL), Propranolol
(Inderal, Inderal LA). Willow bark may make these drugs less effective.
Diuretics (water pills): Willow bark may make these drugs less effective.
Nonsteroidal anti-inflammatory drugs: including ibuprofen (Advil, Motrin) and naproxen
(Aleve). Taking willow bark with these drugs may increase risk of stomach bleeding.
Methotrexate and phenytoin (Dilantin): Willow bark may increase levels of these drugs in the
body, resulting in toxic levels.
References

1. Willow bark | University of Maryland Medical Center (archive.org)

2. https://www.versusarthritis.org/about-arthritis/complementary-and-alternative-treatments/types-of-
complementary-treatments/willow-bark/

3. Hippocrates and Willow Bark? What You Know About the History of Aspirin is Probably Wrong
(greekreporter.com)

4. https://pharmaceutical-journal.com/article/infographics/a-history-of-aspirin

5. History of Aspirin- Willow Bark Extract - Good News! (goodnewsplanet.com)

6. Coating Systems Excipients | American Pharmaceutical Review

7. https://www.pharmapproach.com/excipients-used-manufacture-tablets/2/#:~:text=Examples%20of
%20adsorbents%20used%20in%20the%20manufacture,of%20tablets%20include%20magnesium
%20oxide%2Fcarbonate%2C%20kaolin%2Fbentonite%20etc.