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Questions and Answers
What is the primary purpose of adding excipients to pharmaceutical formulations?
What can occur when excipients interact with active pharmaceutical ingredients?
Which type of interaction between API and excipients does not involve the formation or breakage of chemical bonds?
What is a potential consequence of physical interactions between API and excipients?
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What is the term for the ability of excipients to modulate the bioavailability of active pharmaceutical ingredients?
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Which of the following is NOT a function of excipients in pharmaceutical formulations?
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What can excipients contain that may interact with active pharmaceutical ingredients?
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What is the term for the ability of excipients to improve the solubility of active pharmaceutical ingredients?
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What is the primary function of cyclodextrins in drug-excipient interactions?
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What is the purpose of adding lubricants like magnesium stearate during tablet formulation?
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Which type of interaction between a drug and an excipient can help control the polymorphic form of the drug?
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What is the potential detrimental effect of certain excipients on drug absorption in the gastrointestinal tract?
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What is the role of surfactants like polysorbate 80 in drug-excipient interactions?
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What is the purpose of using cyclodextrins in drug formulation?
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What is the potential beneficial effect of the interaction between a drug and an excipient like polyethylene glycol?
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What is the primary purpose of tablet formulation in pharmaceutical compression?
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What can excessive use of certain excipients or lubricants, such as magnesium stearate, lead to during tablet formulation?
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What type of interaction involves a chemical reaction between drugs and excipients or drugs and impurities/residues present in the excipients?
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What is an example of a chemical interaction between a drug and an excipient?
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What can residues in excipients, such as povidone and crospovidone, lead to?
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What is an example of an interaction between a drug and an excipient residue/impurity?
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What type of interaction occurs between two or more excipients in a drug molecule?
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What can poor tablet disintegration and dissolution lead to during tablet formulation?
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What is a consequence of chemical interactions between drugs and excipients?
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Study Notes
Mechanism of Drug Excipient Interaction
- Excipients are inactive substances added to pharmaceutical formulations to serve various purposes, including improvement of API stability, modulation of bioavailability, and maintenance of pH and rheology.
Beneficial Effects of Drug Excipient Interaction
- Complexation with cyclodextrins (e.g., hydroxypropyl beta-cyclodextrin) can improve drug solubility by encapsulating the hydrophobic drug molecule within the hydrophobic cavity of the cyclodextrin.
- Solid-state interactions with stabilizing polymers or crystallization inhibitors (e.g., PEG) can help control the polymorphic form of the drug, ensuring physical stability and preventing unwanted crystal transformations.
- Micellar solubilization with surfactants (e.g., polysorbate 80) can enhance the dispersion and absorption of lipophilic drugs.
- Tableting interactions with lubricants (e.g., magnesium stearate) can reduce friction between particles, improving tablet flow properties and preventing sticking to the tablet punches.
Detrimental Effects of Drug Excipient Interaction
- Interference with drug absorption can occur when certain excipients in oral formulations form insoluble complexes with the drug, reducing drug dissolution and absorption.
Classification of Drug Excipient Interactions
- Physical interactions: do not involve formation or breakage of chemical bonds in the drug molecular structure, but can affect dissolution rate, dosage uniformity, organoleptic properties, polymorphic forms, crystallization behavior, or drug-release and stability.
- Chemical interactions: involve chemical reactions between drugs and excipients or impurities/residues present in the excipients, leading to the formation of degradation products and changes in the integrity of the substance.
Examples of Chemical Interactions
- Maillard reaction between primary amine groups of chlorpromazine and glycosidic hydroxyl groups of reducing sugar dextrose, leading to the formation of imine and finally Amidori compounds.
- Precipitation of drugs such as neomycin and polymixin due to interaction with suspending agents like sodium alginate.
- Enhanced formation of N-oxide degradation product of raloxifene due to peroxide residues in povidone and crospovidone.
Excipients-Excipients Interaction
- Interaction between two or more excipients in a drug molecule, which can affect the overall stability, efficacy, or safety of the pharmaceutical product.
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Description
Explore the mechanisms of drug-exipient interactions, including complexation for enhanced solubility and solid-state interactions for polymorphic control. Learn about the beneficial effects of these interactions.
