Drug Delivery: Solubility & Dissolution Rate Enhancement
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Questions and Answers

Which class of drugs in the Biopharmaceutics Classification System has significant problems for oral drug delivery?

  • Class IV (correct)
  • Class III
  • Class I
  • Class II
  • Which BCS class is defined as not being soluble in ≤ 250 mL of aqueous media over the range pH1 – pH7.5?

  • Class III
  • Class I
  • Class IV
  • Class II (correct)
  • Which drug is an example of a Class III drug in the Biopharmaceutics Classification System?

  • Propanolol
  • Atenolol (correct)
  • Ketoprofen
  • Flurbiprofen
  • Which drug is an example of a Class IV drug in the Biopharmaceutics Classification System?

    <p>Hydrochlorothiazide</p> Signup and view all the answers

    Which of the following drugs is classified as poorly soluble according to the Biopharmaceutics Classification System?

    <p>Carbamazepine</p> Signup and view all the answers

    Which drug had its oral bioavailability (BA) studied in rats using a solution and suspension in sesame oil?

    <p>Steroid</p> Signup and view all the answers

    Which drug had its lipophilic prodrugs studied in rats, with a solution in short chain fatty acid resulting in 4-fold greater BA than a solution of phenytoin sodium?

    <p>Phenytoin</p> Signup and view all the answers

    Which drug had its oral BA studied in beagle dogs using an oleic acid solution, resulting in 1-fold greater BA than a standard capsule?

    <p>Antimalarial amine</p> Signup and view all the answers

    Which drug had its oral BA studied in beagle dogs using an oleic acid solution, resulting in 4-fold greater BA than a standard tablet?

    <p>Cinnarizine</p> Signup and view all the answers

    What are lipid nanoparticles, and how are they prepared?

    <p>Particles prepared by high pressure homogenization techniques, solvent emulsification-evaporation, and sonoprocessing.</p> Signup and view all the answers

    What is the BCS classification for drugs with high solubility but low permeability?

    <p>Class I</p> Signup and view all the answers

    Which drug would most likely be classified as a Class II drug based on its characteristics?

    <p>Diclofenac</p> Signup and view all the answers

    In the BCS, drugs that are poorly soluble are defined as not being soluble in how much aqueous media?

    <p>≤ 250 mL</p> Signup and view all the answers

    Which therapeutic area would most likely have a higher percentage of new drugs classified as poorly soluble?

    <p>Oncology</p> Signup and view all the answers

    Which drug from the list is an example of a Class IV drug according to the Biopharmaceutics Classification System?

    <p>Furosemide</p> Signup and view all the answers

    Which drug's bioavailability was found to be 3-fold greater from a lipid solution in sesame oil compared to an aqueous suspension?

    <p>Steroid</p> Signup and view all the answers

    In which study was the bioavailability found to be 4-fold greater from a solution in short chain fatty acid compared to a solution of phenytoin sodium?

    <p>Phenytoin lipophilic prodrugs study in rats</p> Signup and view all the answers

    Which drug had its bioavailability studied in rats using both a solution and suspension in sesame oil?

    <p>Steroid</p> Signup and view all the answers

    Which drug had its bioavailability found to be 1-fold greater from an oleic acid solution compared to a standard capsule in a study with beagle dogs?

    <p>Antimalarial amine</p> Signup and view all the answers

    Which drug had its bioavailability found to be 4-fold greater from an oleic acid solution compared to a standard tablet in a study with beagle dogs?

    <p>Cinnarizine</p> Signup and view all the answers

    Study Notes

    Biopharmaceutics Classification System (BCS) Overview

    • Class II drugs have significant problems for oral drug delivery due to low solubility combined with high permeability.
    • Class IV drugs are characterized as not being soluble in ≤ 250 mL of aqueous media across a pH range of 1 to 7.5, indicating poor solubility and permeability.

    Class Examples

    • Class III drug example: the specific drug mentioned is not included.
    • Class IV drug example: the specific drug mentioned is not included, but this class generally includes drugs that demonstrate poor solubility and permeability.

    Drug Solubility and Bioavailability Studies

    • Poorly soluble drugs, according to BCS, are defined as those not dissolving in ≤ 250 mL of aqueous media.
    • A drug studied for oral bioavailability (BA) in rats, utilizing a solution and suspension in sesame oil, is unspecified.
    • Lipophilic prodrugs studied in rats showed a 4-fold greater BA when administered in a short chain fatty acid solution compared to phenytoin sodium solution.
    • A specific drug assessed in beagle dogs exhibited 1-fold greater BA from an oleic acid solution relative to a standard capsule.
    • Another drug also studied in beagle dogs showed a 4-fold greater BA when given in an oleic acid solution compared to a standard tablet.

    Lipid Nanoparticles

    • Lipid nanoparticles are advanced delivery systems for enhancing drug bioavailability and are prepared through methods such as emulsification, solvent injection, or high-pressure homogenization.

    BCS Classification Insights

    • Drugs with high solubility but low permeability fall under Class III in the BCS.
    • Therapeutic areas likely to have a higher percentage of newly developed drugs classified as poorly soluble include oncology and central nervous system disorders, where lipophilicity may be a desirable property for drug absorption.

    Specific Drug Studies and Findings

    • Example of a drug with bioavailability found to be 3-fold greater from a lipid solution in sesame oil compared to an aqueous suspension is unspecified.
    • A study demonstrating 4-fold greater BA from a solution in short chain fatty acid, compared to phenytoin sodium, is unspecified.
    • The drug achieving 1-fold greater BA from oleic acid solution in beagle dogs relative to a standard capsule is unspecified.
    • The drug demonstrating 4-fold greater BA from oleic acid solution compared to a standard tablet in beagle dogs is also unspecified.

    Conclusion

    • Understanding the BCS helps to predict absorption profiles and improve formulations for oral delivery of drugs. Key classes (Class II and Class IV) highlight challenges faced due to solubility and permeability. Bioavailability studies using various formulations aid in optimizing drug delivery systems.

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    Description

    Explore advanced topics in drug delivery including BCS classification, dissolution models, and formulation methods for enhancing solubility and dissolution rates. Learn about the relationships between drug solubility, permeability, and absorption for different drug classes.

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