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Drug excipient interaction

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This document discusses excipients and their interactions with active pharmaceutical ingredients. It begins by defining excipients as inactive substances that are formulated alongside active ingredients for purposes such as bulking up medications. Excipients can affect properties like drug release, bioavailability, stability, and ease of administration. The document then examines ideal excipient properties and classifications. It proceeds to discuss four types of drug-excipient interactions: physical interactions which do not involve chemical changes; chemical interactions where ingredients react to form new compounds; biopharmaceutical interactions affecting absorption; and excipient-excipient interactions which can be undesirable or advantageous. Specific examples are provided to illustrate each type of interaction.

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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 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
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
Ideal properties of Excipient ? No interaction with drug ? Cost effective ? Pharmacologically inert ? Stable for handling 11/17/2017 4
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
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
Types of drug excipient Interactions 1.Physical interactions. 2.Chemical interactions. 3.Biopharmceutical interactions. 4. Excipient ¨CExcipient interactions. 11/17/2017 7
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
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
2. Chemical interactions Active pharmaceutical ingredients and exciepients react with each other to form unstable compounds. 11/17/2017 10
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
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
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
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
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
4. Excipient ¨CExcipient interactions. Excipient ¨Cexcipient interaction though observed very rarely. These are prime importance in determining the stability of the dosage forms excipient ¨Cexcipient interactions can be undesirable as well as some interactions are used in the formulations to get the desired product attributes. 11/17/2017 16
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Drug excipient interaction

  • 1. Presented By- Asha M .Jagtap. Rajarambapu college of pharmacy ,kasegaon. M.Pharm 1st year (Pharmaceutics)11/17/2017 1
  • 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. 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. Ideal properties of Excipient ? No interaction with drug ? Cost effective ? Pharmacologically inert ? Stable for handling 11/17/2017 4
  • 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. 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. Types of drug excipient Interactions 1.Physical interactions. 2.Chemical interactions. 3.Biopharmceutical interactions. 4. Excipient ¨CExcipient interactions. 11/17/2017 7
  • 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. 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. 2. Chemical interactions Active pharmaceutical ingredients and exciepients react with each other to form unstable compounds. 11/17/2017 10
  • 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. 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. 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. 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. 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. 4. Excipient ¨CExcipient interactions. Excipient ¨Cexcipient interaction though observed very rarely. These are prime importance in determining the stability of the dosage forms excipient ¨Cexcipient interactions can be undesirable as well as some interactions are used in the formulations to get the desired product attributes. 11/17/2017 16