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Bio=Pharmaceutics
Life
general area of study concerned with the formulation, manufacture, stability and effectiveness of pharmaceutical dosage forms
Biopharmaceutics
study of the factors influencing the bioavailability of a drug in man and animals and the use of this information to optimize pharmacological or therapeutic activity of drug products in clinical application
Biopharmaceutics
Interrelationship of the physicochemical properties of the drug, the dosage form in which the drug is given, and the route of administration on the rate and extent of drug absorption
Biopharmaceutics
Study of the relationship of the physicochemical properties and in vitro behavior of the drug & drug product on the delivery of the drug to the body under normal or pathologic conditions
PHARMACOKINETICS a process of how the body deals with the drug, what your body does to your drug
PHARMACODYNAMICS a process of how your drug deals with the body, what your drug does to your body
Pharmacokinetics
Deals with the changes of drug concentration in a drug product inside the human or animal body following administration
Pharmacokinetics
Involves the kinetics of drug absorption, distribution, metabolism and elimination
Pharmacodynamics
Relationship between the drug concentration at the site of action (receptor) and pharmacologic response
Drug Product
Finished dosage form that contains an active drug ingredient generally, but not necessarily, in association with inactive ingredient (vehicle) Formulation or matrix in which the drug is contained Term may also include a dosage form that does not contain an active ingredient intended to be used = placebo
Pharmacologic/clinical effect
Rationale
Apply biopharmaceutic principles in developing a rational design of a drug product which would enhance the delivery of active drug and provide optimal therapeutic efficacy of the drug in the patient
AIM:
To deliver the right amount of drug that is EFFECTIVE and SAFE at the right place (site of action) and at the right time (oral, SL or IV/ fast or slow-release)
Mometasone cream AND Mometasone (Nasonex) nasal spray Methylprednisolone tablet AND Fluticasone spray Salbutamol nebules, Salbutamol MDI and Salbutamol syrup Nitroglycerin patch AND Nitroglycerin spray Lactacyd facial wash AND Lactacyd feminine wash Atropine eyedrops AND Atropine ampule Lidocaine spray, Epinephrine ampule and Lidocaine:Epinephrine carpule
Bioavailability of the drug (active ingredient) is the primary concern of biopharmaceutics - Remember you AIM
Time (mins.)
Identify.
Peak plasma level (cmax) max drug concentration related to the dose & the rate constants for absorption & elimination of the drug AUC (Area Under the Curve)- related to the amount of drug absorbed systemically Time of peak plasma level (tmax) time of max drug conc. in plasma roughly proportional to the average rate of drug absorption
Establish
Minimum effective concentration (MEC) Minimum toxic concentration (MTC)
Pharmacodynamic Response
Digoxin = ECG tracings Warfarin = Prothrombin time Insulin = Blood glucose levels Simvastatin = Blood cholesterol levels Nifedipine (anti-hypertensive) = ___________________ Paracetamol = ___________________
Will the intensity of the activity of Warfarin in a hemophiliac be the same with a normal person?
IQ
A 64 year-old male, diabetic patient with a poor creatinine clearance is being given Gentamycin 80mg (aminoglyocside) IV once daily as a treatment for sepsis. Which is important: a.Blood culture and sensitivity to determine his response to treatment b.Plasma level concentration to determine the blood level of the drug c.A and B Why?
Pharmacokinetic Models
Drugs are in a dynamic state within the body It is a hypothesis conceived using mathematical terms Describe drug concentrations in the body as a function of unit time
Pharmacokinetic Models
Concentration of drug in the tank would be governed by two parameters which are CONSTANT: 1.Fluid volume of the tank 2.Elimination of drug per unit of time
Pharmacokinetic Models
If a known set of drug concentrations in the tank were determined at various intervals volume of fluid in the tank & rate of drug elimination would be established
Pharmacokinetic Models
A compartment is a tank containing a volume of fluid In the human body, a fraction of drug is continually eliminated as a function of time
Pharmacokinetic Models
Concentration of drug in the tank (compartment) after a given dose (Ab) is governed by two parameters: 1. Fluid volume of the tank (Vd) 2. Elimination of drug per unit of time (kel, CL) this could be established by knowing a set of drug concentrations in the tank (Cp) at various time intervals
Pharmacokinetic Models
The number of parameters needed to describe the model depends on: 1. Complexity of the process (ADME) 2. route of drug administration
Pharmacokinetic Models
A.Compartment Model (Mammillary Model) B.Physiologic Pharmacokinetic Model (Flow Model)
Compartment Models
Rate constants (ka & ke) represents the overall rate processes of drug entry into and exit from the compartments
Compartment Model
FUNCTIONS: Enables the pharmacokineticist to write different equations to drug concentration changes inside each compartment Visual representation of rate processes Shows how many pharmacokinetic constants are necessary to describe the process adequately
Compartment Models
Open-one compartment model Open-two compartment model Compartment model for IV and oral
Compartment Model
Can a drug concentration data be obtained directly from each compartment??? In open two compartment data in the peripheral compartment cannot be obtained tissues are not easily sampled & may not contain homogenous concentration of the drug only estimated mathematically (from amount of drug absorbed & eliminated per unit time)
Compartment Model
DISADVANTAGES: NOT REALISTIC because everything is based on presumption and mathematical concept Cannot be extrapolated to humans
Application of Biopharmaceutics
Generic equivalency Drug availability Therapeutic efficacy Drug substitution