Pharmaceuticals: pH-Dependent Colonic Drug Delivery Systems
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Questions and Answers

What is the primary advantage of colon mucosa in terms of proteolytic activity?

  • Complete absence of proteolytic activity
  • Equal proteolytic activity to small intestine
  • Higher proteolytic activity than small intestine
  • Lower proteolytic activity than small intestine (correct)
  • What is the primary criteria for selecting a drug for Colon-Targeted Drug Delivery Systems (CDDS)?

  • Drugs that are poorly absorbed from the upper GIT (correct)
  • Drugs that undergo minimal first-pass metabolism
  • Drugs that are highly stable in small intestine
  • Drugs that are highly soluble in stomach acid
  • Which type of CDDS is dependent on the pH of the gastrointestinal tract?

  • Bacterial enzyme-dependent CDDS
  • pH-dependent CDDS (correct)
  • Time-dependent CDDS
  • Pressure-controlled CDDS
  • What is the primary mechanism of Transit Time Dependent CDDS?

    <p>Prolonging the lag time of about 5 to 6 h</p> Signup and view all the answers

    What is the primary advantage of using enteric materials in CDDS?

    <p>Protection of the drug from acidic stomach pH</p> Signup and view all the answers

    Which type of CDDS is dependent on the enzymatic activity of bacterial enzymes in the colon?

    <p>Bacterial enzyme-dependent CDDS</p> Signup and view all the answers

    What is the primary mechanism of Osmotic Pressure-Controlled CDDS?

    <p>Osmotic pressure driven release of the drug</p> Signup and view all the answers

    What is the primary advantage of using polymeric coatings in CDDS?

    <p>Targeted release of the drug in the colon</p> Signup and view all the answers

    What is the primary disadvantage of Transit Time Dependent CDDS?

    <p>Unpredictable release of the drug</p> Signup and view all the answers

    What is the primary criteria for selecting a drug for CDDS in terms of first-pass metabolism?

    <p>Drugs that undergo extensive first-pass metabolism</p> Signup and view all the answers

    Study Notes

    Colon Targeted Drug Delivery Systems (CDDS)

    • CDDS are gaining importance for systemic and local effects, especially for delivering proteins and peptides.

    Anatomy of the Colon

    • The colon is the final part of the digestive system, responsible for reabsorbing fluids and processing waste products.
    • It consists of four parts: descending colon, ascending colon, transverse colon, and sigmoid colon.

    Diseases of the Colon

    • Ulcerative colitis
    • Crohn's disease
    • Colon cancer
    • Amoebiasis

    Importance of CDDS

    • Reduced adverse side effects
    • Useful for intentional delayed drug absorption
    • Delivery of drug in its intact form close to the target site

    Criteria for Selecting Drugs for CDDS

    • Drugs poorly absorbed from the upper GIT
    • Drugs that degrade in the stomach and small intestine
    • Drugs that undergo extensive first-pass metabolism
    • Drugs for colon cancer

    Approaches to CDDS

    1. pH- and Time-Dependent Colonic DDS

    • The outer layer dissolves at pH > 5, then the intermediate swellable layer made of an enteric material.
    • In another method, succinic acid is used as a pH-adjusting agent with the drug substance in a hard gelatin capsule.

    2. pH- and Time-Dependent Colonic DDS

    • The outermost enteric layer prevents drug release in the stomach, and the hydrophilic layer dissolves quickly after gastric emptying.
    • The onset time of drug release in the intestine can be controlled by the thickness of the acid-soluble layer.

    3. Bacterial Enzyme-Dependent Colonic DDS

    • The microflora of the colon (10^11-10^12 CFU/ml) produces enzymes that enhance the use of biodegradable polymers for CDDS.
    • These polymers shield the drug from the stomach and small intestine and deliver it to the colon, where they undergo assimilation or degradation.

    4. pH and Bacterial Enzyme-Dependent Colonic DDS (CODES System)

    • The CODES system is a unique CDDS technology that avoids problems associated with pH or time-dependent systems.

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    Description

    This quiz covers the design and functionality of pH-dependent colonic drug delivery systems, including the use of enteric materials and acid-soluble polymers. It explores the release of drug substances in the colon and the role of pH-adjusting agents.

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