Presented By-

Asha M .Jagtap.

Rajarambapu college of

pharmacy ,kasegaon.

M.Pharm 1st year

(Pharmaceutics) 11/17/2017 1

INTRODUCTION

• Excipients play an important role in formulating a dosage

form. These are ingredients which along with active

pharmaceutical ingredients make up the dosage forms.

Excipients act as protective agents, bulking agents and can

also be used to improve bioavailability of drug.

• Excipients as like other active pharmaceutical ingredients

need to be stabilized and standardized.

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Excipient

“An excipient is an inactive substance formulated

alongside the active ingredient of a medication, for the

purpose of bulking-up formulations that contain potent active

ingredients”.

The resultant biological, chemical and physical properties of

the drug product are directly affected by the excipient chosen,

their concentration and interactions with the API:

Consistency of drug release and bioavailability

Stability including protection from degradation

Ease of administration to the target patient population(s) by

the intended route

“An excipient is an inactive substance formulated

alongside the active ingredient of a medication, for the

purpose of bulking-up formulations that contain potent active

ingredients”.

The resultant biological, chemical and physical properties of

the drug product are directly affected by the excipient chosen,

their concentration and interactions with the API:

Consistency of drug release and bioavailability

Stability including protection from degradation

Ease of administration to the target patient population

the intended route

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Ideal properties of Excipient

• No interaction with drug

• Cost effective

• Pharmacologically inert

• Stable for handling

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Excipient are inactive ingredients used as carriers for

the active ingredients in a pharmaceutical product.

These may be classified into the following categories:

Anti adherents

Binders

Disintegrants

Preservatives

Sweeteners

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Drug excipient interaction

In pharmaceutical dosage forms the active

pharmaceutical ingredients are in intimate contact

with the excipient which are greater quantity excipient

and drugs may have certain incompatibility which

lead to drug excipient interaction.

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Types of drug excipient Interactions

1.Physical interactions.

2.Chemical interactions.

3.Biopharmceutical interactions.

4. Excipient –Excipient interactions.

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1. Physical interactions.

physical interactions alter the rate of

dissolution , dosage uniformity ,etc. physical

interactions do not involve chemical changes thus

permitting the components in the formulation to retain

their molecular structure .physical interactions are

difficult to detect .

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Interaction Beneficial effect examples Detrimental effect

examples

Complexation:-

Usually binds reversibly

with drugs to form

complex, sometimes

insoluble complexes

are formed which lead to

slower

dissolution and decreased

absorption of

drug.

Cyclodextrin is often used to

improve bioavailability of

poorly water soluble drugs.

This increases

bioavailability and increases

rate and extent of drug

dissolution by

increasing mucosal

permeability or

increasing stability of drug.

Tetracycline formed

insoluble complex with

calcium carbonate

leading to slower

dissolution and

decreased absorption.

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2. Chemical interactions

Active pharmaceutical ingredients and

exciepients react with each other to form unstable

compounds.

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Chemical interactionsInteraction Fact observed Examples of drugs

undergoing such

interactions

Hydrolysis Drugs with functional

groups like esters,

amides, lactones,

undergo hydrolysis, in

presence of water, low or

high pH, in presence of

alkaline metals, acids,

acids i.e. anion and

hydrogen ion, alkali etc.

Anesthetics , antibiotics,

vitamins, and

barbiturates,

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Oxidation Oxidative reactions are

catalyzed by oxygen, light,

heavy metal ions, fumed

metal oxides, fumed silica,

fumed, zirconia etc.

Steroids, Vitamins,

Antibiotics, Epinephrine,

Aldehydes, Alcohols,

Phenols.

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3. Biopharmaceutical interactions

These are the interaction observed after

administration of the medication. Interaction within the body

is between medicine and body fluids which influence the

rate of absorption . All excipient physiological way when

they are administered along with active pharmaceutical

ingredients.

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Examples

1. Premature breakdown of enteric coat-

The enteric coating polymers like cellulose

acetate phthalate and hydroxyl propyl cellulose acetate

phthalate. Are soluble more at basic pH, but antacids raise

pH of stomach resulting in breakdown of the enteric coat in

stomach and release of active pharmaceutical ingredient in

stomach itself , which results in degradation of drug in

stomach. In case of NSAID’s premature breakdown of

enteric coat may cause side effects like gastric bleeding.

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2. Increase in gastrointestinal motility-

Many of the excipients like Sorbitol

,xylitol have tendency to increase the gastrointestinal

motility thus reducing the time available for absorption of

drugs like metoprolol.

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4. Excipient –Excipient interactions.

Excipient –excipient interaction though observed

very rarely. These are prime importance in determining the

stability of the dosage forms excipient –excipient

interactions can be undesirable as well as some

interactions are used in the formulations to get the desired

product attributes.

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