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1. Biopharmaceutics & pharmacokinetics Adapted by ABDUL BASIT ( SENIOR LECTURER) Pharm-D , M.Phil. (Pharmaceutics )

2. Biopharmaceutics & pharmacokinetics House rules Students are expected to prepare before class Switch off mobile phones in class 75% class attendance is a requirement to qualify for exam Group work & participation compulsory Assignment must be completed in time Unfinished work, cheating, poor participation in group, poor class attendance & undermining of any rules set here forth subject to penalty according to department rules

3. Chapter 1 DEFINITIONS AND TERMINOLOGY Biopharmaceutics Generic equivalence Therapeutic equivalents Bioavailability Bioequivalence Drug disposition Pharmacokinetics (LADMER)

4. Biopharmaceutics Definition Biopharmaceutics examines the interrelationship of the physical/chemical properties of the drug, the dosage form (drug product) in which the drug is given, the route of administration on the rate and extent of systemic drug absorption , the importance of the drug substance and the drug formulation on absorption, and   in-vivo  distribution of the drug to the site of action, is described as a sequence of events that precede elicitation of a drug's therapeutic effect. 

5. The dynamic relationship between the drug, the drug product and the pharmacological effects Drug product Drug release and dissolution Excretion and metabolism Pharmacologic or c linical effect Drug in tissues Drug in systemic circulation Absorption Elimination Distribution Drug

6. Scope of Biopharmaceutics Biopharmaceutics is a field that combines principles of biology, pharmacology, and pharmaceutical science to study the behavior of drugs within the body . Some applications of biopharmaceutics include: Design of Drug Delivery System Formulation Development Bioavailability Enhancement Pharmacokinetics Studies Bioequivalence Studies Drug Interactions Personalized Medicine Drug Safety and Efficacy

7. Overall, biopharmaceutics plays a fundamental role in the development, optimization , and safe use of pharmaceutical products, contributing to advancements in drug therapy and patient care . Biopharmaceutics provides the scientific basis for drug product design and drug product development.

8. Biopharmaceutics involves factors that influence The design of the drug product Stability of the drug within the drug product The manufacture of the drug product The release of the drug from the drug product The rate of dissolution/release of the drug at absorption site Delivery of drug to site of action

9. Drug, Drug products and Drug product performance Drug Use in diagnosis, cure, mitigation, treatment or prevention of disease Drug products/dosage form/drug delivery system That release and deliver drug to site of action and produce desire therapeutic effect Also meet patient’s needs e.g. palatability, convenience and safety Drug product performance The release of drug form drug product either for local or systemic effect

10. Biopharmaceutics consideration in drug product design

11. Pharmacokinetics Pharmacokinetics literally means the 'movement of drugs' ( from Pharmaco – drug, and Kinetic – movement ). PK is the science of the kinetics of drug absorption, distribution and elimination (metabolism and execration) It involves both Experimental Development of biologic sampling techniques Analytical methods to measure drugs and metabolites Procedures that facilitate data collection and manipulation theoretical approaches Development of pharmacokinetic models that predict drug disposition after drug administration

12. Biologic sampling techniques Main sample preparation techniques Protein precipitation Liquid-liquid extraction Solid phase extraction Dilution and shoot technique Alternative techniques Dialysis Ultrafiltration Affinity solvent extraction

13. Analytical techniques Spectroscopic techniques UV-visible IR NMR MASS Chromatographic techniques HPLC GC TLC HPTLC UPLC Hyphenated techniques LC-MS GC-MS ICP-MS

14. Theoretical approach

15. Pharmacokinetic curve

16. L ADME R Liberation Liberation is the first step in the process by which a drug product enters into the body and liberates the active ingredient that has been administered. The pharmaceutical drug must separate from the vehicle or the excipient that it was mixed with during manufacture Absorption Drug absorption is the transfer of a drug from the site of administration to the bloodstream. The rate and extent of absorption depend on the environment where the drug is absorbed, chemical characteristics of the drug and the route of administration (which influences the bioavailability). Route of administration other than intravenous may result in partial absorption and lower bioavailability .

17. Distribution Drug distribution is the process by which a drug reversibly leaves the bloodstream and enters the extracellular fluid and tissues. Following factors affect the distribution of drug : Blood flow Capillary permeability Plasma protein binding Charge on drug Volume of distribution

18. Elimination Metabolism and excretion is collectively called elimination. Metabolism Chemical alteration of the drug is called metabolism in which a non-polar (lipid soluble) compounds are converted to polar (lipid insoluble) form so that the drug are not reabsorbed in the renal tubule and are excreted . Excretion Passage out (removal) of systemically absorbed drug is called excretion. The drugs and their metabolites are excreted in urine, feces, saliva, milk etc. Net excretion = glomerulus filtration + active tubular secretion – tubular reabsorption

19. Response: Drug response refers to a direct measure of the pharmacologic effect of the drug Polygraph is used to measure response

20. Bioavailability Bioavailability Bio means biological system Availability means to become available Literally means availability of drug in biological system According to FDA It is the measurement of rate and extent of biologically active drug that is absorbed form drug product and become available at its site of action

21. Bioavailability is practically 100% (F = 1) following an intravenous administration. Bioavailability could be lower (F ≤ 1) and in some cases almost negligible for other routes (e.g., oral and dermal), depending on how efficiently a xenobiotic crosses various barriers

22. Types of bioavailability Absolute It compares the bioavailability of the active drug in systemic circulation following non-intravenous administration (i.e., after oral, rectal, transdermal , subcutaneous, or sublingual administration ), with the bioavailability of the same drug following intravenous administration. Relative Relative bioavailability refers to the extent and rate at which a drug or substance is absorbed and becomes available at the site of action, compared to a reference standard.

23. Significance of bioavailability study Optimizing Drug Formulations Determining Dosage Regimens Assessing Generic Equivalence Predicting Drug Interactions Developing Controlled Release Formulations Improving Pharmacokinetic Models Optimizing Nutrient Absorption

24. Bioequivalence Bioequivalence studies According to FDA The absence of significant difference in rate and extent of drug., absorbed from two drug products, when these drug product are administered in same molar concentration through same route of administration under similar experimental condition in an appropriate design study. where two drugs or two sets of formulation of the same drug are compared to show that they have nearly equal bioavailability and PK/PD parameters. These studies are often done for generic drugs or when a formulation of a drug is changed during development.