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Lecture 1

“ Biopharmaceutics as a theoretical base of medicines FOR pharmaceutical technology. The basic terms of biopharmaceutics ”. Lecture 1. Biopharmaceutics is a science which studies dependence of therapeutic action of edicines on the organism from the different variable factors.

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Lecture 1

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  1. “Biopharmaceutics as a theoretical base of medicines FOR pharmaceutical technology. The basic terms of biopharmaceutics” • Lecture 1

  2. Biopharmaceutics is a science which studies dependence of therapeutic action of edicines on the organism from the different variable factors. The term “biopharmaceutics” appeared at first in scientific pharmacy of the USA in the beginning of the 60th years of the 20th century and soon got worldwide acknowledgement.

  3. Founders of biopharmaceutics American scientists Levy and Wagner (1961) IBN-Sina of Х century Scientists ХIХ century Empiric supervisions about influence of honey additions and some vegetable medicines on the degree of medicinal substances action The influence of auxiliary substances on the processes of absorption of medicines was proved The dependence of absorption speed and efficiency of medicines on the way of introduction was defined experimentally Development of biophafraceutics

  4. Factors Constant Variable Medicinal substance Dose or concentration of medicinal substance Pharmaceutical Physiological Biochemical Clinical Factors are simultaneously working forces, conditions or other circumstances influencing on the result of researches, data or parameters

  5. sex a physical state of the medicinal substance age Physiological factors Pharmaceutical factors a simple chemical updating of the medicinal substance state of organism an auxiliary substances (their nature, physical state and quantity) a medicinal form and ways of application in the organism a technological process Classification of variable factors

  6. time of drug application Clinical factors interaction simultaneously or consistently entered drugs peculiarities of biochemical processes in the organism and metabolism of medicinal substances for the given patient • Biochemical factors infringements of functions: stomach, kidneys, intimate activity, nervous system etc. physical activity of the patient Classification of variable factors

  7. Factors Constant Variable Medicinal substance Dose or concentration of medicinal substance Pharmaceutical Physiological Biochemical Clinical Classification of variable factors

  8. Equivalence Is the quantitative study of the course of drug absorption, distribution, metabolism and elimination (ADME) Pharmacokinetic data is very usefull in optimization of the disage form design and establishing the dosage interval Pharmaceutical equivalent (chemical) Pharmacokinetics (PK) Pharmacodynamics(PD) Clinical equivalent Identity of therapeutic effect of the medicine to comparison standard medicine The state or property of being equivalent Describes the relationship between the dose and the pharmacological effect at the site of action The medicine which containing identical quantity of the substance in the same medicinal form and meeting the requirements which are defined by the technological norms Medicine which after application in the same dozes gives the identical therapeutic effectwhich has been checked up on any symptom or on treatment of illness Glossary of BiopharmaceIdutic terms

  9. Equivalence Non-equivalence Effective substance Efficiency Activeingredient Non equality of therapeutic action of the same medicines in identical dozes and medicinal forms prepared by different manufacturers or the same factory, but different series Biologically active part of medicine taking responsibility for its therapeutic effect That which enters into a compound, or is a component part of any combination or mixture; an element; a constituent is a term in pharmacokinetics used to assess the expected in vivo biological equivalence of two proprietary preparations of a drug. If two products are said to be bioequivalent it means that theywould be expected to be, for all intents and purposes, the same The production of the desired effects or results with minimum waste of time, effort, or skill

  10. The quantity of medicinal substances in the biological liquid, which is released from the researched medicinal form, expressed as a Percentage, in comparison with Absolute bioavailability or withthe standard medicinal form. Absolute availability Relative availability Dosage Absorption Absorption rate constant ( ka) The determination and regulation of the size, frequency and number of doses The movement of a substance, such as a liquid or solute, across a cell membrane by means of diffusion or osmosis The quantity of the medicinal substance entered in the medicinal form intravenously, which acts in blood circulation without influence on the effect of the first passage through the liver (effect «first pass»), and the course of speed this process. • The constant for a drug administered by a route other than the intravenous. The rate of absorption of a drug absorbed from its site of application according to first-order kinetics. • A value describing how much drug is absorbed per unit of time

  11. Is a function of the blood flow rate (Q) to these organs. It depends on the intrinsic ability of the organs such as the liver and kidneys to metabolize or excrete Clearance (Cl) Distribution coefficient Distribution Reabsorption Area under curve (AUC) The process during which the medicinal substance is distributed from blood to the tissues and body organs The ratio of concentrations of a substance in two immiscible phases at equilibrium Process of the opposite absorption of the medicinal substance Is the area under a plot of drug concentration vs. time.The most common method of estimating AUC is to use the trapezoidal rule where the concentration-time curve is considered as a series of trapezoids and estimate the total area of all the trapezoids

  12. The quantity of medicinal substances in the biological liquid, which is released from the researched medicinal form, expressed as a Percentage, in comparison with Absolute bioavailability or withthe standard medicinal form. Absolute availability Relative availability Dosage Absorption Absorption rate constant ( ka) The determination and regulation of the size, frequency and number of doses The movement of a substance, such as a liquid or solute, across a cell membrane by means of diffusion or osmosis The quantity of the medicinal substance entered in the medicinal form intravenously, which acts in blood circulation without influence on the effect of the first passage through the liver (effect «first pass»), and the course of speed this process. • The constant for a drug administered by a route other than the intravenous. The rate of absorption of a drug absorbed from its site of application according to first-order kinetics. • A value describing how much drug is absorbed per unit of time

  13. Is a function of the blood flow rate (Q) to these organs. It depends on the intrinsic ability of the organs such as the liver and kidneys to metabolize or excrete Distribution coefficient Distribution Reabsorption Area under curve (AUC) Clearance (Cl) The process during which the medicinal substance is distributed from blood to the tissues and body organs The ratio of concentrations of a substance in two immiscible phases at equilibrium Process of the opposite absorption of the medicinal substance Is the area under a plot of drug concentration vs. time.The most common method of estimating AUC is to use the trapezoidal rule where the concentration-time curve is considered as a series of trapezoids and estimate the total area of all the trapezoids

  14. Elimination Elimination constant Tolerance Antagonism Systemic clearance Is the sum of all individual organ clearances that contribute to the overall elimination of the drug. It is evaluated from the PK data as shown in following:Cl = Dose/AUC Is the sum of all individual organ clearances that contribute to the overall elimination of the drug. It is evaluated from the PK data as shown in following: Cl = Dose/AUC The constant rate is the process during which the effective substance is deduced from the body by the process of biotransformation Tolerance to a drug develops when the response to the same dose of the drug decreases with repeated use Antagonism is action in which two drugs given together will have an opposite effect on the body

  15. Therapeutic efficiency of medicines determined by processes: • absorption (suction) • distribution • elimination Influensing of variable factors on the medical effect of medicines LADMER General term characterizing the separate areas of co-operation of medicine with an organism (Liberation, Absorption, Distribution, Metabolism, Elimination, Response), i.e. includes biopharmaceutics, pharmaсokinetics and pharmaсodynamiсs

  16. Many factors are responsible for the entry of a drug into the body and then into biophase. These factors include the route of administration; the dosage form; the liberation rate of the drug from the dosage form; dissolution; penetration and permeation of the drug through biomembranes; its distribution within the body fluids and tissues; the type, amount and rate of biotransformation; and recycling processes and elimination. In addition to these factors, pharmacogenetics and certain pathophysiological conditions also affect the above process. The entire process can be described as the LADMER (liberation, absorption, distribution, metabolism, elimination and response) system showing that liberation, absorption, distribution, metabolism and elimination are involved to elicit the response. One can subdivided this approach according to the scheme shown in fig.

  17. . Interdisciplinary scheme of LADMER system

  18. LADMER Biopharmaceutic hurdle Biopharmaceutic class Approaches to overcome the hurdle Drug Formulation approaches Class II Poor Solubility Class IV Chemical modifications Liberation Formulation approaches Chemical degradation All Classes Chemical modifications Enzymatic degradation Enzyme inhibitors All Classes Chemical modifications Sorption promoters Poor Permeability Class III Class IV Chemical modifications Absorption First pass metabolism Distribution Alternative route All Classes Prodrug approach Metabolism Excretion Response LADMER system, biopharmaceutics hurdles in drug development, approaches to overcome them

  19. Biopharmaceutic factors affecting dissolution and/or absorption

  20. The quantitative side of medicinal substances absorption is limited, foremost, by efficiency (by kinetics) of their releasing on the initial stage of absorption. Efficiency of medicinal substances releasing is in direct dependence on pharmaceutical factors and their successive use for advancement of active substances by following chart:- choice of the chemical state;- choice of bodily condition;- influencing of auxiliary substances;- influencing of the simultaneously accepted medicines;- choice of medicinal form;- choice of way of introduction;- establishment of exact dosage;- influencing of pharmaceutical factors;- determination of role of physiological factors enorganic this.

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