Podcast
Questions and Answers
What role do co-solvents play in the solubility of orally administered drugs?
What role do co-solvents play in the solubility of orally administered drugs?
- They improve the aqueous solubility of the drug. (correct)
- They increase the stability of acidic drugs.
- They help drugs ionize in the gastrointestinal tract.
- They decrease the drug's partition coefficient.
In terms of drug absorption, what is the significance of pKa?
In terms of drug absorption, what is the significance of pKa?
- It indicates the degree of non-ionization at physiological pH. (correct)
- It determines the drug's water solubility.
- It measures the stability of drugs in solution.
- It defines the effectiveness of co-solvents.
What does hygroscopicity refer to?
What does hygroscopicity refer to?
- The tendency of a solid to take up water from the atmosphere. (correct)
- The ability of a drug to dissolve in lipid materials.
- The concentration ratio of a drug in oil and aqueous phases.
- The stability of a drug in aqueous solutions.
What does the partition coefficient represent?
What does the partition coefficient represent?
Which factor does NOT affect solid phase stability of drugs?
Which factor does NOT affect solid phase stability of drugs?
Why is the rotation disc method used in drug formulation?
Why is the rotation disc method used in drug formulation?
What is a major concern when formulating new drug substances?
What is a major concern when formulating new drug substances?
What characteristic must an orally administered drug have to ensure absorption?
What characteristic must an orally administered drug have to ensure absorption?
What is the primary purpose of preformulation testing in drug development?
What is the primary purpose of preformulation testing in drug development?
Which of the following is NOT a reason for performing preformulation testing?
Which of the following is NOT a reason for performing preformulation testing?
What defines polymorphism in a drug compound?
What defines polymorphism in a drug compound?
How does particle size affect drug formulation?
How does particle size affect drug formulation?
Which property primarily impacts the ability of a powder to be processed through tablet machines?
Which property primarily impacts the ability of a powder to be processed through tablet machines?
What role does crystallinity play in bulk properties of a drug?
What role does crystallinity play in bulk properties of a drug?
What is indicated by a relationship between particle size and surface area?
What is indicated by a relationship between particle size and surface area?
Which factor can influence polymorphic transitions in a drug substance?
Which factor can influence polymorphic transitions in a drug substance?
Study Notes
Preformulation Testing
- First step in dosage form development
- Investigates physical and chemical properties of drug substance alone and combined with excipients
- Physiochemical properties determined by in vitro experiments
Importance of Preformulation
- Prepare dosage forms with desired quality
- Achieve high physiological availability and therapeutic qualities
- Develop optimal dosage forms
- Targeted drug delivery systems
- Patient compliance
- Minimize cost of finished product
- Minimize errors in formulation
Bulk Properties
- Crystallinity: Appearance and internal structure of crystals
- Polymorphism: Ability of compounds to crystallize as different crystalline species with different internal structure
- Particle size: Affects solubility, dissolution rate, and absorption
- Powder flow property: Determines which excipients are needed for compressed dosage forms
- Surface Characteristics: Hygroscopicity - tendency of solid to absorb water from the atmosphere
Solubility Analysis
- Aqueous solubility: Orally administered drugs must dissolve in gastrointestinal fluids for absorption
- Drug pKa/ Ionization at physiological pH: Non-ionized substances are lipid-soluble and transported passively by diffusion, ionized substances are lipid insoluble and have slow permeation
- Partition coefficient: Concentration of drug in oil phase to concentration of drug in aqueous phase, important for membrane penetration
Dissolution
- Important for gastrointestinal absorption
- Determined by the rotating disc method
Stability Analysis
- Solution phase stability: Effect of pH on stability, acid-sensitive drugs need protection from gastric acidity
- Solid phase stability: Depends on temperature, pH, humidity, hydrolysis, and oxidation
Compatibility
- Interaction of drugs with preservatives, stabilizers, dyes, and flavors
- Formulators need to identify compatible excipients
Answers
- Dissolution rate: Rotating disc method
- Crystal habit: Outer appearance and internal structure
- Hygroscopicity: Tendency of a solid to absorb water
- Preformulation testing: The first step in the development of dosage forms
- Partition coefficient: Concentration of drug in oil phase to concentration of drug in aqueous phase
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Description
Explore the critical first steps in drug development through preformulation testing. This quiz covers the importance of evaluating the physical and chemical properties of drug substances, as well as the effects of excipients on dosage forms. Understand how these assessments impact the development of effective and patient-compliant medications.
