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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 acti...
Excipient
“An excipient is an inactive substance formulated
alongside the active ingredient of a medication, for the
purpo...
Ideal properties of Excipient
• No interaction with drug
• Cost effective
• Pharmacologically inert
• Stable for handling
...
Excipient are inactive ingredients used as carriers for
the active ingredients in a pharmaceutical product.
These may be c...
Drug excipient interaction
In pharmaceutical dosage forms the active
pharmaceutical ingredients are in intimate contact
wi...
Types of drug excipient Interactions
1.Physical interactions.
2.Chemical interactions.
3.Biopharmceutical interactions.
4....
1. Physical interactions.
physical interactions alter the rate of
dissolution , dosage uniformity ,etc. physical
interacti...
Interaction Beneficial effect examples Detrimental effect
examples
Complexation:-
Usually binds reversibly
with drugs to f...
2. Chemical interactions
Active pharmaceutical ingredients and
exciepients react with each other to form unstable
compound...
Chemical interactions
Interaction Fact observed Examples of drugs
undergoing such
interactions
Hydrolysis Drugs with funct...
Oxidation Oxidative reactions are
catalyzed by oxygen, light,
heavy metal ions, fumed
metal oxides, fumed silica,
fumed, z...
3. Biopharmaceutical interactions
These are the interaction observed after
administration of the medication. Interaction w...
Examples
1. Premature breakdown of enteric coat-
The enteric coating polymers like cellulose
acetate phthalate and hydroxy...
2. Increase in gastrointestinal motility-
Many of the excipients like Sorbitol
,xylitol have tendency to increase the gast...
4. Excipient –Excipient interactions.
Excipient –excipient interaction though observed
very rarely. These are prime import...
11/17/2017 17
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Drug excipient interaction

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Drug excipient interaction

  1. 1. Presented By- Asha M .Jagtap. Rajarambapu college of pharmacy ,kasegaon. M.Pharm 1st year (Pharmaceutics)11/17/2017 1
  2. 2. 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. 11/17/2017 2
  3. 3. 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 11/17/2017 3
  4. 4. Ideal properties of Excipient • No interaction with drug • Cost effective • Pharmacologically inert • Stable for handling 11/17/2017 4
  5. 5. 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 11/17/2017 5
  6. 6. 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. 11/17/2017 6
  7. 7. Types of drug excipient Interactions 1.Physical interactions. 2.Chemical interactions. 3.Biopharmceutical interactions. 4. Excipient –Excipient interactions. 11/17/2017 7
  8. 8. 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 . 11/17/2017 8
  9. 9. 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. 11/17/2017 9
  10. 10. 2. Chemical interactions Active pharmaceutical ingredients and exciepients react with each other to form unstable compounds. 11/17/2017 10
  11. 11. Chemical interactions Interaction 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, 11/17/2017 11
  12. 12. 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. 11/17/2017 12
  13. 13. 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. 11/17/2017 13
  14. 14. 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. 11/17/2017 14
  15. 15. 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. 11/17/2017 15
  16. 16. 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. 11/17/2017 16
  17. 17. 11/17/2017 17

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