PHARMACEUTICAL EXCIPIENTS

Elizabeth Y. Tan, RPh, MSc

Gerard Lee L. See, RPh, MSc

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal

Chemistry. Cebu City: SoLine Publishing Company Inc., 2017.
Print.
 OVERVIEW
▪ Non-drug adjuncts in a formulation to aid stability, concentration, and protectivity
to final dosage forms

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 SURFACE ACTIVE AGENTS
▪ Reduce the interfacial tension between the dispersed phase and dispersion
medium
▪ Anionic agents
▪ Soap
▪ Sulfated compounds
▪ Sulfonated compounds
▪ Cationic agents
▪ Nonionic surfactants
▪ Amphoteric agents

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 EMULSIFYING AGENTS
▪ Excipients that maintain the stability of the dispersed phase and the dispersion
medium in emulsion are defined as emulsifying agents, normally classified as
anionic, cationic, ampholytic, and nonionic surfactants and have high molecular
weight

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 SUSPENDING AGENTS
▪ Increase the viscosity of the continuous phase are known as suspending agents
▪ Examples:
▪ Methylcellulose
▪ Carboxymethylcellulose
▪ Gelatin
▪ hydroxypropylmethyl cellulose
▪ Sodium carboxymethylcellulose
▪ Carbopol
▪ Clays (veegum and bentonite)

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 FLOCCULATING AGENTS
▪ Employed in pharmaceutical formulation can be electrolytes, polymers, or
surfactants.
▪ The efficiency of electrolytes in flocculate particles normally depends on the
valence of the ion.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 WETTING AGENTS
▪ Excipients normally reduce the interfacial tension and increase the interaction
between the solid particles of the dispersed phase and the dispersion medium

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 ANTIOXIDANTS
▪ Protect the formulation from oxidative degradation
▪ Water-soluble antioxidants
▪ sodium bisulfate USP38/NF33
▪ sodium metabisul te USP38/NF33
▪ sodium thiosulfate USP38/NF33
▪ thiourea USP38/NF33

▪ Oil-soluble antioxidants are used in parenteral solutions whose solvents are xed oils.
▪ tocopherol USP38/NF33
▪ ascorbylpalmitate USP38/NF33
▪ butylatedhydroxyanisole (BHA) USP38/NF33
▪ butylatedhydroxytoluene (BHT) USP38/NF33

▪ Synergists
▪ citric acid USP38/NF33
▪ lecithin USP38/NF33
▪ glycerin USP38/NF33
▪ phosphoric acid USP38/NF33
▪ PEG USP38/NF33
▪ propylene glycol USP38/NF33

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 PRESERVATIVES
▪ excipients that prevent microbial growth and prohibit large-scale chemical
changes in formulation
▪ The parabens also protect products against molds.
▪ Formic acid exhibits antibacterial properties as a preservative

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ inactive solid ingredients that can be mixed with medication to bring up the weight
of a tablet for it to be easily compressed.
▪ Lactose as a diluent is available in different grades such as lactose, anhydrous
lactose, and spray dried lactose.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Dextrose
▪ occurs as odorless, sweet-tasting, colorless crystals or as a white crystalline or granular
powder
▪ good stability under dry storage conditions but excessive heating can cause a reduction in
pH and caramelization of solutions
▪ used in solutions to adjust tonicity, and as a sweetening agent
▪ wet granulation diluent and binder, and a direct-compression tablet diluent and binder in
chewable tablets.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Lactose
▪ Occurring as white to off-white crystalline particles or powder
▪ anhydrous lactose is widely used in direct compression tableting applications as a tablet-
and-capsule diluent, filler, and binder.
▪ Due to its low moisture content, it can be combined with moisture-sensitive drugs, and
may be utilized in intravenous injections.
▪ anhydrous lactose may develop a brown coloration on storage, and may promote mold
growth under humid conditions (80% relative humidity and above)

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Sucrose
▪ obtained from sugar cane, sugar beet, and other sources
▪ occurs either as colorless crystals, as crystalline masses or blocks, or as a white
crystalline powder
▪ odorless, has a sweet taste and good stability at room temperature and at moderate
humidity.
▪ Sucrose syrup is a versatile additive with multiple uses:
▪ at concentrations of 50%-67%, as a tablet-coating agent, and as a binding agent for wet granulation
in tableting
▪ as vehicles in oral liquid-dosage forms to enhance palatability or to increase viscosity
▪ as a diluent in freezer-dried protein
▪ as additives in foods and confectionery

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Mannitol
▪ is D-mannitol, a white, odorless, crystalline powder, or free- owing granules, almost as
sweet as glucose, and half as sweet as sucrose
▪ imparts a cooling sensation in the mouth
▪ in pharmaceutical preparations, it is primarily a diluent (10-90% w/w) in tablet
formulations as it is not hygroscopic, and can mix with moisture-sensitive active
ingredients

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Sorbitol
▪ odorless, white or almost colorless, crystalline, hygroscopic powder
▪ available in a wide range of grades and polymorphic forms, such as granules,
flakes, or pellets that tend to cake less than the powdered form and have more
desirable compression characteristics
▪ pleasant, cooling, sweet taste (with approximately 50-60% of the sweetness of
sucrose)
▪ Extensively used in cosmetics and food products, and in pharmaceutical
formulations as an excipient, sorbitol possesses chemical inertness and
compatibility with other excipients.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Polysaccharides
▪ Starch
▪ Modified starch
▪ Microcrystalline cellulose

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DILUENTS
▪ Inorganic compounds
▪ Dibasic anhydrous calcium phosphate
▪ Dibasic dihydrate calcium phosphate
▪ Tribasic calcium phosphate
▪ Calcium phosphate
▪ Calcium carbonate

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 BINDER
▪ additive that holds together a tablet’s ingredients before compression
▪ List of commonly-used binders:
▪ acacia
▪ tragacanth
▪ starch
▪ gelatin
▪ polyvinylpyrrolidone
▪ Polyacrylamide
▪ Sugar
▪ Hydroxypropylcellulose
▪ sodium carboxymethlycellulose

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 DISINTEGRANTS
▪ excipients that break down compressed tablets into finer particles in the presence
of G.I. media
▪ To provide optimum disintegration effects, a large portion of the disintegrant is
mixed with other ingredients before granulation to provide rapid disintegration of
particles.
▪ Alginic acid (Na alginate) has a good disintegrating property due to its good
capacity to absorb fluid; consequently, it is frequently patronized as a
disintegrating agent.
▪ Starches including wheat, potato, and rice have excellent disintegrating property,
with cornstarch as the most saleable due to its varying moisture content (3%-20%)

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 SWEETENING AGENTS
▪ excipients to make products sweet are sweetening agents that help mask bitter or
unpalatable tastes in medications
▪ glucose USP38/NF33
▪ cane sugar (sucrose)
▪ Although easily available and is inexpensive, it can promote microbial growth and requires a large
quantity to produce sweetness.
▪ sorbitol
▪ glycerine
▪ saccharin sodium.
▪ This is ideal for diabetic patients, has less calories per serving, and requires less quantity to
produce sweetness. However, it is expensive and may cause cancer.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 GLIDANTS
▪ excipients that improve the ow property of granules from hopper into the die cavity
▪ List of commonly-used glidants:
▪ talc
▪ cornstarch
▪ colloidal silica
▪ Zn, Mg, and Ca stearate
▪ calcium silicate
▪ calcium phosphate

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 LUBRICANTS
▪ excipients that reduce interaction between particles and dye during compression
and ejection cycles
▪ List of commonly-employed lubricants:
▪ boric acid
▪ sodium, magnesium, zinc, and calcium salts of stearates
▪ sodium lauryl sulfate
▪ stearic acid
▪ PEG 4000
▪ PEG 6000
▪ waxes
▪ vegetable oils

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 ANTI-ADHESIVES
▪ inert excipients that prevent the adhesion of the tablet surface to the die walls and
punches, thereby eliminating the “picking” or “sticking” of the tablets
▪ List of commonly-used anti-adhesives:
▪ colloidal silica
▪ cornstarch
▪ sodium lauryl sulfate
▪ magnesium (stearate)

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 ADSORBENTS
▪ excipients that adsorb fluids and moisture and keep pharmaceutical products dry
are the adsorbents.
▪ They are normally used in formulations containing large amounts of liquid, eutectic
mixtures, oil soluble drugs, or essential oils.
▪ Silica is the most preferred adsorbent agent since it can hold water up to 80% its
own height and weight

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.
 ADSORBENTS
▪ List of commonly-employed adsorbents in the pharmaceutical industry:
▪ Silica USP38/NF33.
▪ submicroscopic fumed silica with a particle size of about 15 nm, is a light, loose, bluish-white, odorless, tasteless,
amorphous powder.
▪ Magnesium oxide USP38/NF33.
▪ It occurs as a fine, white, odorless powder; and comes in cubic crystal structure.
▪ Magnesium aluminum silicate USP38/NF33 .
▪ Occurring as an off -white to creamy white, odorless, tasteless, soft, slippery small flakes, or as a fine, micronized
powder, it is added in 10-50% concentrations.
▪ Kaolin USP38/NF33.
▪ It is a graying-white, unctuous powder, free from gritty particles, with an earthy or claylike taste. When
moistened with water, it becomes darker in color and develops a claylike odor.
▪ Magnesium carbonate USP38/NF33.
▪ Similar to kaolin, it has a slightly earthy taste, and occurs as light, white friable masses or as a bulky, white
powder. Though odorless, it can absorb odors due to its high absorptive ability. As an adsorbent, it is added in
concentrations of 0.5-1%.

Tan, Elizabeth and See, Gerard. Essentials of Inorganic Medicinal Chemistry. Cebu City: SoLine Publishing
Company Inc., 2017. Print.