Fourth B. Pharmacy

402. Biopharmaceutics & Dosage Form Design (Theory) 
  1. Introduction to biopharmaceutics and pharmacokinetics [ 1 ]
    History and their role in formulation development & therapeutics and clinical setting. 

  2. Biopharmaceutics : [ 8 ]

    1. Definition, absorption, distribution, metabolism(biotransformation) and excretion (elimination) of drugs, physicochemical, biological and pharmaceutical factors altering biopharmaceutical performance of drugs. Passage of drugs across biological barrier (passive diffusion, active transport, facilitated diffusion and pinocytosis). Factors influencing absorption- physiochemical, physiological and pharmaceutical. Drug distribution in the body, plasma protein binding. 

    2. Bioavailability and equivalance, federal requirements, methods of determinition of bioavailability using blood level and urinary excretion data. Design and evaluation of bioavailability assessment. 

  3. Pharmacokinetics: [ 10 ] 

    1. Definition and scope, significance of plasma drug concentration measurement. 

    2. Compartment model:

    3. Phamacokinetics of drug absorption, zero order and first order absorption rate constant using Wagner- Nelson and Loo-Riegelman method. 

    4. Volume of distribution and distribution coefficient. 

    5. Compartment kinetics-one compartment and two compartment models. Determination of pharmaccokinetics parameters from plasma and urine data after drug administration by intravascular and oral route. 

    6. Curve fitting (Method of Residuals),regression procedures. 

    7. Clearance concept, mechanism of renal clearance, clearance ratio, determination of renal clearance. 

    8. Hepatic elimination of drugs, first pass effect ,extraction ratio, hepatic clearance, biliary excretion, extrahepatic circulation.

    9. Non-linear pharmacokinetics with special reference to one compartment model after I.V. drug administration, Michals Menten Equation, detection of non-linearity (Saturation mechanism). 

    10. In-vitro, in-vivo correlation

    11. Numericals related to pharmacokinetic parameters using one compartmental models

  4. Non-Compartmental Models: [ 2 ]
    Statistical Moments, Application, bioavailability determination, Linear system pharmacokinetics. Unit impulse response, Deconvolution, application in bioavailability determination etc. 

  5. Clinical pharmacokinetics : [ 4 ]

    1. Definition and scope. 

    2. Dosage adjustment in patients with renal and hepatic failure. 

    3. Dosage regimen adjustment for ref. 

    4. Pharmacokinetic drug interaction significance in combination therapy. 

  6. Bioavailability and bioequivalence : [ 10 ]

    1. Measures of biovailability, Cmax, tmax, AUC

    2. Design of single dose bio-equivalent statistics, study designs, crossover designs, study protocol, log transformation of pharmacokinetic data, sequence effect, outliers

    3. Overview of regulatory requirement of bio-equivalence study. 

  7. Preformulation studies : [ 6 ]

    1.  Study of physical properties of drug like physical form, particle size, density, wetting, dielectric constant, solubility, dissolution and organoleptic property and their effect on formulation, stability and bioavailability. 

    2.  Study of chemical properties of drugs like hydrolysis, oxidation, reduction, racemization, polymerization etc., and their influence on formulation and stability of products. 

    3.  Study of prodrugs in solving problems related to stability, bioavailability and elegance of formulations.

  8. Design, development and process validation [ 8 ]
    methods for pharmaceutical operations involved in the production of pharmaceutical products with special reference to tablets, suspensions. Prospective, retrospective validation, organizing of validation, validation for dry heat, moist heat, filtration, ethylene oxide, radiation sterilization, Validation of parentrals, Solid dosage forms: validation of raw materials, Definition and control of process variables, guidelines, validation protocols

  9. Stabilization and stability testing [ 5 ]
    Protocol for various pharmaceutical products, ICH guidelines for stability testing

  10. Performance evaluation methods: [ 2 ]

    1. Invitro dissolution studies for solid dosage forms, methods, interpretation of dissolution data. 

    2. Bioavailability studies and bioavailability testing protocol and procedures. 

  11. Design, development, production and evaluation of controlled [ 16 ] 
    release formulations. 

    Introduction, design of Control release Drug Delivery Systems (Biopharmaceutic pharmacokinetic, pharmacodynamic, characteristics of drug) Pharmacokinetic principles in design , development of CDDS, drug release models, oral , parentral, ophthalmic, transdermal CDDS. Drug targeting, Evaluation of CDDS, Bioavailabilty testing

Biopharmaceutics & Dosage Form Design [Practical] 
  1. Experiments to illustrate absorption of drugs in various models. 

  2. Experiments to illustrate protein binding of drugs, K and N values of binding process. 

  3. Determination of plasma half life, elimination constant using plasma drug profile. 

  4. Determination of pharmacokinetics of single compartmental analysis. 

  5. Experiments to illustrate curve fitting, area under the blood level curves, binding, bioequivalence determinations. 

  6. Preformulation studies including drug-excipients compatibility studies, effect of stabilizers, preservatives etc. in dosage form design. 

  7. Experiments demonstrating improvement in bioavailability through prodrug concept. 

  8. Stability evaluation of various dosage and their expiration dating. 

  9. Dissolution testing and date evaluation for oral solid dosage forms. 

  10. Evaluation of Bioequivalence of some marketed products.

  11. In vivo bioavailability evaluation from plasma drug concentration and urinary excretion curves. 

  12. Design, development and evaluation of controlled relase formulations. 

Books Recommended: 
    1. Physical Pharmacy by Martin
    2. Theory and Practice of Industrial Pharmacy by Lachman.
    3. Remington’s Pharmaceutical Sciences.
    4. Textbook of Pharmaceutical Formulation by Mithal.
    5. Pharmaceutical Dosage Forms: Tablets by Lachman and others.
    6. Pharmaceutical Dosage Forms: Disperse Systems by Lieberman and others.
    7. Pharmaceutical Dosage Forms: Parenteral Medication by Lieberman and others.
    8. Microencapsulation by Benita.
    9. Pharmaceutical Dosage Forms and Drug Delivery Systems by Ansel & others.
   10. Controlled and Novel Drug Delivery by N.K. Jain.
   11. Drug Stability by Carstenen.