For better view, kindly download the presentation. The presentation contains information about absorption of drug and various mechanisms which plays role in drug absorption. Additionally it includes factors affecting drug absorption.
PHYSIOLOGIC FACTORS RELATED TO DRUG ABSORPTIONN Anusha
ROUTES OF DRUG ADMINISTRATION
The route of administration (ROA) that is chosen has a large impact on how fast the drug is taken up and how much of it arrives at its destination in an active form.
MEMBRANE PHYSIOLOGY
The cell membrane also known as the plasma membrane or cytoplasmic membrane is a biological membrane that separates the interior of all cells from the outside environment.
GSTERO-INTESTINAL PHYSIOLOGY
AGE
INTRODUCTION OF ABSORPTION
TRANSPORT PROCESS
FACTORS AFFECTING DRUG ABSORPTION WITH EXAMPLES:
1) Physiological factors
2) physiochemical factors
3) pharmaceutical factors
The Importance of Product Design
It may seem obvious to state that a new product should be adequately defined before any serious product development is undertaken.
In many cases, the value of the design phase is often underestimated in the rush to start development and get products to the market quickly.
This can result in much wasted time and valuable resources. It can also lead to reduced staff motivation if a product is developed that is not wanted or if the product definition is constantly changing during development.
The quality of the design activities can strongly influence the success of the development of the right product to the market and ultimate return on investment (ROI).
Gastroretentive Drug Delivery System -> by Mohit kumarMohit Kumar
Contents
INTRODUCTION
WHAT IS GRDDS ?
NEED FOR GRDDS…?
POTENTIAL DRUG CANDIDATES
DRUGS THAT ARE UNSUITABLE FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
FACTORS AFFECTING THE GASTRORETENTIVE SYSTEM.
ADVANTAGES OF GRDDS
DISADVANTAGES OF GRDDS
APPROACHES TO EXTEND GI TRANSIT
INTRODUCTION
Oral route has been the most convenient and accepted route of drug delivery.
Gastroretentive drug delivery system is novel drug delivery systems which has an upper hand owing to its ability of prolonged retaining ability in the stomach and thereby increase gastric residence time of drugs and also improves bioavailability of drugs.
WHAT IS GRDDS ?
Gastroretentive drug delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects.
NEED FOR GRDDS…?
Oral drug delivery system, sustained drug delivery systems, these drug delivery systems suffer from mainly two adversities:
Short gastric retention time(GRT) and
Unpredictable short gastric emptying time (GET)
which can result in incomplete drug release from the dosage form in the absorption zone (stomach or upper part of small intestine) leading to diminished efficacy of administered dose.
To formulate a site-specific orally administered controlled release dosage form, it is desirable to achieve a prolong gastric residence time by the drug delivery.
Prolonged gastric retention time (GRT) in the stomach could be advantageous for local action e.g. treatment of peptic ulcer, etc.
POTENTIAL DRUG CANDIDATES FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
Drugs that disturb normal colonic microbes e.g. antibiotics against Helicobacter pylori.
Drugs that degrade in the colon. e.g. Ranitidine, Metformin HCl.
Drugs which are absorbed rapidly from the GI tract. e.g. Metronidazole, tetracycline.
Drugs with a narrow window of absorption e.g. Cyclosporine, Methotrexate, Levodopa, etc.
Drugs that are poorly soluble at alkaline pH e.g. Furosemide, Diazepam, Verapamil, etc.
Drugs that are primarily absorbed in the stomach e.g. Amoxicillin.
Drugs acting locally in the stomach(active in stomach) e.g. Antacids and drugs for H. Pylori viz., Misoprostol
DRUGS THAT ARE UNSUITABLE FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
Drugs that have very limited acid solubility phenytoin etc.
Drugs that suffer instability in the gastric environment e.g. erythromycin etc.
Drugs intended for selective release in the colon e.g. 5-amino salicylic acid and corticosteroids etc.
FACTORS AFFECTING THE GASTRORETENTIVE SYSTEM.
Density
Size
Shape of dosage form
Single or multiple unit formulation
Fed or unfed state.
Advantages of GRDDS
Increase in bioavailability and curative efficiency of drugs and economic usage of dosage.
Minimised factor of risk in resistance in antibiotics owing to stabilised therapeutic levels over prolonged periods removing fluctuations.
General pharmacology Diploma in pharmacy second year YogeshShelake
The General pharmacology ,Toxicology & Pharmacotherapeutics
To Undastanding the general pharmacology & Definitions of PHARMACODYNAMECIS ,PHARMACOKINITICS (Absorbation,Distribution,Metabolism,Excreation )Pharmacology ,Toxicology ,Pharmacotherapeutic ,
Advantages of Routs of Administration & Their Disadvantages
Factors affecting of absorpation ,excreation of drug,factor modifing deug action
First pass effect
Gastric emptying time
Gastrointestinal motility
Short note on Gastric emptying and motility
Physicochemical factors affecting drug absorption
A. Drug solubility and dissolution rate
B. Particle size and surface area of drugs
C. Polymorphism and amorphism
D. Hydrate or solvates
Biopharmaceutical classification system of drug
Absorption is the movement of the drug from its site
of administration into circulation. Not only
the fraction of the administered dose that gets
absorbed but also the rate of absorption is
important. Except when given i.v., the drug has
to cross biological membranes; absorption is
governed by the above-described principles.
PHYSIOLOGIC FACTORS RELATED TO DRUG ABSORPTIONN Anusha
ROUTES OF DRUG ADMINISTRATION
The route of administration (ROA) that is chosen has a large impact on how fast the drug is taken up and how much of it arrives at its destination in an active form.
MEMBRANE PHYSIOLOGY
The cell membrane also known as the plasma membrane or cytoplasmic membrane is a biological membrane that separates the interior of all cells from the outside environment.
GSTERO-INTESTINAL PHYSIOLOGY
AGE
INTRODUCTION OF ABSORPTION
TRANSPORT PROCESS
FACTORS AFFECTING DRUG ABSORPTION WITH EXAMPLES:
1) Physiological factors
2) physiochemical factors
3) pharmaceutical factors
The Importance of Product Design
It may seem obvious to state that a new product should be adequately defined before any serious product development is undertaken.
In many cases, the value of the design phase is often underestimated in the rush to start development and get products to the market quickly.
This can result in much wasted time and valuable resources. It can also lead to reduced staff motivation if a product is developed that is not wanted or if the product definition is constantly changing during development.
The quality of the design activities can strongly influence the success of the development of the right product to the market and ultimate return on investment (ROI).
Gastroretentive Drug Delivery System -> by Mohit kumarMohit Kumar
Contents
INTRODUCTION
WHAT IS GRDDS ?
NEED FOR GRDDS…?
POTENTIAL DRUG CANDIDATES
DRUGS THAT ARE UNSUITABLE FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
FACTORS AFFECTING THE GASTRORETENTIVE SYSTEM.
ADVANTAGES OF GRDDS
DISADVANTAGES OF GRDDS
APPROACHES TO EXTEND GI TRANSIT
INTRODUCTION
Oral route has been the most convenient and accepted route of drug delivery.
Gastroretentive drug delivery system is novel drug delivery systems which has an upper hand owing to its ability of prolonged retaining ability in the stomach and thereby increase gastric residence time of drugs and also improves bioavailability of drugs.
WHAT IS GRDDS ?
Gastroretentive drug delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects.
NEED FOR GRDDS…?
Oral drug delivery system, sustained drug delivery systems, these drug delivery systems suffer from mainly two adversities:
Short gastric retention time(GRT) and
Unpredictable short gastric emptying time (GET)
which can result in incomplete drug release from the dosage form in the absorption zone (stomach or upper part of small intestine) leading to diminished efficacy of administered dose.
To formulate a site-specific orally administered controlled release dosage form, it is desirable to achieve a prolong gastric residence time by the drug delivery.
Prolonged gastric retention time (GRT) in the stomach could be advantageous for local action e.g. treatment of peptic ulcer, etc.
POTENTIAL DRUG CANDIDATES FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
Drugs that disturb normal colonic microbes e.g. antibiotics against Helicobacter pylori.
Drugs that degrade in the colon. e.g. Ranitidine, Metformin HCl.
Drugs which are absorbed rapidly from the GI tract. e.g. Metronidazole, tetracycline.
Drugs with a narrow window of absorption e.g. Cyclosporine, Methotrexate, Levodopa, etc.
Drugs that are poorly soluble at alkaline pH e.g. Furosemide, Diazepam, Verapamil, etc.
Drugs that are primarily absorbed in the stomach e.g. Amoxicillin.
Drugs acting locally in the stomach(active in stomach) e.g. Antacids and drugs for H. Pylori viz., Misoprostol
DRUGS THAT ARE UNSUITABLE FOR GASTRORETENTIVE DRUG DELIVERY SYSTEMS
Drugs that have very limited acid solubility phenytoin etc.
Drugs that suffer instability in the gastric environment e.g. erythromycin etc.
Drugs intended for selective release in the colon e.g. 5-amino salicylic acid and corticosteroids etc.
FACTORS AFFECTING THE GASTRORETENTIVE SYSTEM.
Density
Size
Shape of dosage form
Single or multiple unit formulation
Fed or unfed state.
Advantages of GRDDS
Increase in bioavailability and curative efficiency of drugs and economic usage of dosage.
Minimised factor of risk in resistance in antibiotics owing to stabilised therapeutic levels over prolonged periods removing fluctuations.
General pharmacology Diploma in pharmacy second year YogeshShelake
The General pharmacology ,Toxicology & Pharmacotherapeutics
To Undastanding the general pharmacology & Definitions of PHARMACODYNAMECIS ,PHARMACOKINITICS (Absorbation,Distribution,Metabolism,Excreation )Pharmacology ,Toxicology ,Pharmacotherapeutic ,
Advantages of Routs of Administration & Their Disadvantages
Factors affecting of absorpation ,excreation of drug,factor modifing deug action
First pass effect
Gastric emptying time
Gastrointestinal motility
Short note on Gastric emptying and motility
Physicochemical factors affecting drug absorption
A. Drug solubility and dissolution rate
B. Particle size and surface area of drugs
C. Polymorphism and amorphism
D. Hydrate or solvates
Biopharmaceutical classification system of drug
Absorption is the movement of the drug from its site
of administration into circulation. Not only
the fraction of the administered dose that gets
absorbed but also the rate of absorption is
important. Except when given i.v., the drug has
to cross biological membranes; absorption is
governed by the above-described principles.
Absorption, Bioavailability and Bioequivalance.pdfShaikh Abusufyan
At the end of this e-learning session you are able to…
A. Explain factor affecting drug absorption, bioavailability and bioequivalence.
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Presentation covers the basics of pharmacokinetic. Mechanism for the transport of drug molecule. Absorption, factors affecting on absorption of drugs. Concept of bioavailability. Distribution, plasma protein binding, tissue binding, barriers.
Pharmacokinetics, sometimes described as what the body does to a drug, refers to the movement of drug into, through, and out of the body—the time course of its absorption, bioavailability, distribution, metabolism, and excretion.
This file contains the rout of absorption of the drug. the events drug pass through before reaching the systemic circulation. Also contains a little introduction of First Pass Mechanism.
Dosage form design - Biopharmaceutical considerationAniruddha Roy
Dosage form design - Biopharmaceutical consideration: Understanding how physicochemical characteristics of a drug and formulation component affect bioactivity
Pharmacokinetics is the study of the movement of drug molecules in the body. It includes absorption, distribution, metabolism, and excretion of drugs. Pharmacokinetics is the study of what happens to drugs once they enter the body (the movement of the drugs into, within, and out of the body). For a drug to produce its specific response, it should be present in adequate concentrations at the site of action. This depends on various factors apart from the dose.
Four pharmacokinetic properties determine the onset, intensity, and the duration of drug action (Figure 1.6.1):
• Absorption: First, absorption from the site of administration permits entry of the drug (either directly or indirectly) into plasma.
• Distribution: Second, the drug may then reversibly leave the bloodstream and distribute it into the interstitial and intracellular fluids.
• Metabolism: Third, the drug may be biotransformed by metabolism by the liver or other tissues.
• Elimination: Finally, the drug and its metabolites are eliminated from the body in urine, bile, or feces.
In short, pharmacokinetics means what the body does to the drug.
To have complete understanding kindly use my other presentations on distribution
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed distribution of drug through BBB, Placenta and Plasma Protein Binding, and redistribution
Pharmacology of Semi synthetic Penicillins Vijay Kevlani
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed various penicillins like acid resistant, beta lactamase resistant penicillins, Beta lactamase inhibitor penicillins, broad spectrum penicillins
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed pharmacology of penicillin G.
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed mecahnism of action of penicillin (all beta lactam antibiotics)
To enjoy the presentation kindly download it.
For Original view, download "Poetsen One" font style from dafont website.
Here I have discussed all the first to fifth generation cephalosporins.
Histamine: Turnover, Release and Receptor Vijay Kevlani
For better view of content, kindly download the presentation.
Histamine, means 'tissue amine'. It is almost present in all animal tissues and in certain plants e.g. stinging nettle.
Drug Distribution & Factors Affecting DistributionVijay Kevlani
To have the full content of slide, kindly download it and convert it to ppt form.
Drug distribution is the process by which a drug reversibly leaves the bloodstream and enters the interstitium (extracellular fluid) and/or the cells of the tissues.
Once a drug has gained access to the blood stream,
it gets distributed to other tissues that initially had no drug, concentration gradient being in the direction of plasma to tissues.
Autacoids: Introduction and classificationVijay Kevlani
Autacoids are diverse substances produced by a wide variety of cells in the body, having intense biological activity,
but generally act locally (e.g. within inflammatory pockets)
at the site of synthesis and release
These are synthetic antimicrobials having a quinolone structure.
They are active primarily against gram-negative bacteria, though the newer fluorinated compounds also inhibit gram positive ones.
The first member Nalidixic acid introduced in mid- l 960s
A breakthrough was achieved in the early 1980s by fluorination of the quinolone structure at position 6 and introduction of a piperazine substitution at position 7 resulting in derivatives called fluoroquinolones (FQs)
In the 1990s, compounds with additional fluoro an other substitutions have been developed, Further extending antimicrobial activity to gram-positive bacteria and anaerobes, and/or conferring metabolic stability (longer t½).
The fixed dose combination of trimethoprim and sulfamethoxazole is called cotrimoxazole.
Adverse Drug Reaction, Spectrum, Resistance and Use of Cotrimoxazole.
Here is anatomy and physiology of brain stem. Where we will discuss all three parts of brain stem. Starting from medulla, second is pons and third is mid brain. In this video I am presenting anatomy and physiology of medulla. Anatomy of medulla: Medulla Oblongata or more simply medulla is part of brain stem which forms base of the brain stem. Location of medulla oblongata is superior to spinal cord and inferior to Pons. It contains pyramid, olive and above pyramidal structure, there is decussation of pyramids which explains why each part of brain controls opposite part of body. Adding to that medulla also has several nuclei which controls activity of cardiovascular system and respiratory system. Medulla also has nuclei for controlling reflexes of vomiting, swallowing, hiccuping, coughing and sneezing. It has also nuclei for test, hearing and balance. Medulla also contains nuclei of cranial nerve number VIII, IX, X, XI and XII. Functions of medulla or what dose medulla do? So medulla controls blood pressure, diameter of wall of arteries, heart rate, basal respiration rate and also vomiting, swallowing, hiccuping, coughing and sneezing.
In this video, we explain you about anatomy and physiology of Pons. The reference material used to make video is: Principles of Anatomy and Physiology Gerard J. Tortora, Bryan H. Derrickson. Pons is part of brain stem, present superior to medulla, inferior to mid brain and anterior to cerebellum. Pons means a bridge. As the name denotes, it connects other areas of brain. Neurons extending from cerebral cortex to pons makes corticopontine tract. Pons is connected to cerebellum by middle cerebral peduncle. Pons has vestibular nuclei, which is part of equilibrium pathways from inner ear to brain. Pons has also respiratory nuclei. Along with rhythmicity area of medulla, pons controls basal respiratory rhythm. Pons also contains nuclei for cranial nerve number V, VI,VII, and VIII.
The midbrain or mesencephalon extends from the pons to the diencephalon and is about 2.5 cm (1 in.)long.
The cerebral aqueduct passes through the midbrain, connecting the third ventricle above with the fourth ventricle below.
The anterior part of the midbrain contains paired bundles of
axons known as the cerebral peduncles.
The cerebral peduncles consist of axons of Corticospinal, Corticopontine, and Corticobulbar tracts, which conduct nerve impulses from motor areas in the cerebral cortex to the spinal cord, pons, and medulla, respectively.
The posterior part of the midbrain, called the tectum, contains four rounded elevations.
Two superior elevations: Superior Colliculi
Two inferior elevations: Inferior Colliculi
The superior colliculi serves as reflex centers for certain visual activities.
Visual activities like, eye movements for tracking moving images (such as a moving car) and scanning stationary images (as you are watching this slide).
The superior colliculi are also responsible for reflexes that govern movements of the head, eyes, and trunk in response to visual stimuli.
The inferior colliculi are part of the auditory pathway, relaying impulses from the receptors for hearing in the inner ear to the brain.
These two nuclei are also reflex centers for the startle reflex, sudden movements of the head, eyes, and trunk that occur when you are surprised by a loud noise such as a gunshot.
The midbrain contains several other nuclei, which includes the left and right substantia nigra.
Neurons that release dopamine, extending from the substantia nigra to the basal ganglia, help control subconscious muscle activities.
Loss of these neurons is associated with Parkinson disease.
Parkinson's disease is a brain disorder that leads to Shaking,
Stiffness, Difficulty with walking, Difficulty with balance, Difficulty with coordination.
Also present are the left and right red nuclei, which look reddish due to their rich blood supply and an iron-containing pigment in their neuronal cell bodies.
Axons from the cerebellum and cerebral cortex form synapses in the red nuclei, which help control some voluntary movements of the limbs.
The reference material used to make video is: Principles of Anatomy and Physiology Gerard J. Tortora, Bryan H. Derrickson.
Pons is part of brain stem, present superior to medulla, inferior to mid brain and anterior to cerebellum.
Pons means a bridge. As the name denotes, it connects other areas of brain.
Neurons extending from cerebral cortex to pons makes corticopontine tract.
Pons is connected to cerebellum by middle cerebral peduncle.
Pons has vestibular nuclei, which is part of equilibrium pathways from inner ear to brain.
Pons has also respiratory nuclei. Along with rhythmicity area of medulla, pons controls basal respiratory rhythm.
Pons also contains nuclei for cranial nerve number V, VI,VII, and VIII.
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Medulla oblongata or more simply medulla is part of brain stem which forms base of the brain stem. It contains pyramid, olive and above pyramidal structure, there is decussation of pyramids which explains why each part of brain controls opposite part of body. Adding to that medulla also has several nuclei which controls activity of cardiovascular system and respiratory system. Medulla also has nuclei for controlling reflexes of vomiting, swallowing, hiccuping, coughing and sneezing. It has also nuclei for test, hearing and balance. Medulla also contains nuclei of cranial nerve number VIII, IX, X, XI and XII.
What is Alzheimer's disease? pathophysiology of disease, treatment of disease. If there is any update regarding the information provided, your comments are welcomed
You will find Dopamine, Parkinson, Mental Disorders, Antipsychotics, Antidepressants and Antimaniac drugs here with mechanism of drugs, uses, adverse drug reaction and diagrams explaining the mechanisms. In case, if there is any query or update regarding the information provided, your comments are welcomed.
How to Split Bills in the Odoo 17 POS ModuleCeline George
Bills have a main role in point of sale procedure. It will help to track sales, handling payments and giving receipts to customers. Bill splitting also has an important role in POS. For example, If some friends come together for dinner and if they want to divide the bill then it is possible by POS bill splitting. This slide will show how to split bills in odoo 17 POS.
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
We all have good and bad thoughts from time to time and situation to situation. We are bombarded daily with spiraling thoughts(both negative and positive) creating all-consuming feel , making us difficult to manage with associated suffering. Good thoughts are like our Mob Signal (Positive thought) amidst noise(negative thought) in the atmosphere. Negative thoughts like noise outweigh positive thoughts. These thoughts often create unwanted confusion, trouble, stress and frustration in our mind as well as chaos in our physical world. Negative thoughts are also known as “distorted thinking”.
Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
Students, digital devices and success - Andreas Schleicher - 27 May 2024..pptxEduSkills OECD
Andreas Schleicher presents at the OECD webinar ‘Digital devices in schools: detrimental distraction or secret to success?’ on 27 May 2024. The presentation was based on findings from PISA 2022 results and the webinar helped launch the PISA in Focus ‘Managing screen time: How to protect and equip students against distraction’ https://www.oecd-ilibrary.org/education/managing-screen-time_7c225af4-en and the OECD Education Policy Perspective ‘Students, digital devices and success’ can be found here - https://oe.cd/il/5yV
Operation “Blue Star” is the only event in the history of Independent India where the state went into war with its own people. Even after about 40 years it is not clear if it was culmination of states anger over people of the region, a political game of power or start of dictatorial chapter in the democratic setup.
The people of Punjab felt alienated from main stream due to denial of their just demands during a long democratic struggle since independence. As it happen all over the word, it led to militant struggle with great loss of lives of military, police and civilian personnel. Killing of Indira Gandhi and massacre of innocent Sikhs in Delhi and other India cities was also associated with this movement.
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
The Indian economy is classified into different sectors to simplify the analysis and understanding of economic activities. For Class 10, it's essential to grasp the sectors of the Indian economy, understand their characteristics, and recognize their importance. This guide will provide detailed notes on the Sectors of the Indian Economy Class 10, using specific long-tail keywords to enhance comprehension.
For more information, visit-www.vavaclasses.com
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Unit 8 - Information and Communication Technology (Paper I).pdfThiyagu K
This slides describes the basic concepts of ICT, basics of Email, Emerging Technology and Digital Initiatives in Education. This presentations aligns with the UGC Paper I syllabus.
2. Absorption is movement of the drug from its
site of administration into the circulation.
Not only the fraction of the administered dose that
gets absorbed, but also the rate of absorption
is important.
Except when given i.v., the drug
has to cross biological membranes
3. 1. Aqueous solubility
Drugs given in solid form
must dissolve in the aqueous bio-phase before
they are absorbed.
For poorly water soluble
drugs (aspirin, griseofulvin) rate of dissolution
governs rate of absorption.
Ketoconazole dissolves
at low pH: gastric acid is needed for its
absorption.
4. Obviously, a drug given as watery
solution is absorbed faster than when the same
is given in solid form or as oily solution.
2. Concentration
Passive diffusion dépends on
concentration gradient; drug given as concentrated
solution is absorbed faster than from
dilute solution.
5. 3. Area of absorbing surface
Larger is the surface area faster is the aborption.
4. Vascularity of the absorbing surface
Blood circulation removes the drug from the site of
absorption and maintains the concentration
gradient across the absorbing surface.
Increased blood flow hastens drug absorption just as wind
wind
hastens drying of clothes.
6. 5. Route of administration
This affects drug absorption, because each route has its own
7. A. Oral
The effective barrier to orally administered drugs
is the epithelial lining of the gastrointestinal tract,
which is lipoidal.
Nonionized lipid soluble drugs, e.g. ethanol are
readily absorbed from stomach as well as intestine
at rates proportional to their lipid : water partition
coefficient.
8. Acidic drugs, e.g. salicylates, barbiturates, etc.
are predominantly unionized in the acid gastric
juice and are absorbed from stomach,
while basic Drug e.g. morphine, quinine, etc. are
large
ionized and are absorbed only on reaching the
duodenum.
However, even for acidic drugs absorption from
stomach is s lower, because
the mucosa is thick,
covered with mucus and
9. Absorbing surface area is much larger in the small
intestine due to villi.
Thus, faster gastric emptying accelerates
drug absorption in general.
Dissolution is a surface phenomenon, therefore,
particle size of the drug in solid dosage form
of dissolution and in turn rate of absorption.
10. Presence of food
dilutes the drug and retards absorption.
Further, certain drugs form poorly absorbed
complexes with food constituents,
e.g. tctracyclines with calcium present in milk;
Moreover food delays gastric emptying.
Thus, most drugs are absorbed better if taken
in empty stomach.
11. However, there are some
exceptions , e.g. fatty food greatly enhances
lumefantrine absorption.
Highly ionized drugs, e.g. gentamicin, neostigmine are
poorly absorbed when given orally.
12. Certain drugs are degraded in the gastrointestinal
tract, e.g. penicillin G by acid,
Insulin by peptidases, and are inactive orally.
Enteric coated tablets
(having acid resistant coating)
and sustained release preparations
(drug particles coated with slowly dissolving material)
can be used to overcome
acid lability,
gastric irritancy and
brief duration of action.
13. The oral absorption of certain drugs is
low because a fraction of the absorbed drug
is extruded back into the intestinal lumen
by the efflux transporter P-gp located in
the gut epithelium.
The low oral bioavailability
of digoxin and cyclosporine is partly
accounted by this mechanism.
14. Inhibitors of P-gp like
quinidine, verapamil , erythromycin, etc. enhance,
while P-gp inducers like rifampin and phenobarbitone
reduce the oral bioavailability of these drugs.
15. Absorption of a drug can be affected by other
concurrently ingested drugs.
This may be a luminal effect:
formation of insoluble complexes,
e.g. tetracyclines and iron preparations with calcium
salts and antacids,
phenytoin with sucralfate.
Such interaction can be minimized by administering
the
two drugs at 2-3 hr intervals.
16. Alteration of gut
flora by antibiotics may disrupt the enterohepatic
cycling of oral contraceptives and digoxin.
Drugs can also alter absorption by
gut wall effects: altering motility
(anticholinergics, tricyclic antidepressants,
opioids retard motility while metoclopramide enhances
it)
or causing mucosaI damage
(neomycin, methotrexate, vinblatine).
17. Subcutaneous and Intramuscular
By these routes the drug is deposited directly
in the vicinity of the capillaries.
Lipid soluble
drugs pass readily across the whole surface
of the capillary endothelium.
Capillaries having large paracellular spaces do not
obstruct absorption of even large lipid insoluble
molecules
or ions.
18.
19. Very large molecules are
absorbed through lymphatics.
Thus, many drugs not absorbed orally are absorbed
parenterally.
Absorption from s.c. site is slower than that from
i.m. site, but both are generally faster and more
consistent/ predictable than oral absorption.
20. Application of heat and muscular
exercise accelerate drug absorption by increasing
blood flow,
while vasoconstrictors, e.g. adrenaline
injected with the drug (local anaesthetic)
retard absorption.
Incorporation of hyaluronidase
facilitates drug absorption from s.c. injection
by promoting spread.
21. Many depot preparations,
e.g. benzathine penicill in, protamine zinc
insulin, depot progestins, etc. can be given by
these routes.
22. Topical sites
(skin, cornea, mucous membranes)
Systemic absorption after topical application
depends primarily on lipid solubility of drugs.
However, only few drugs significantly penetrate
intact skin.
Hyoscine, fentanyl, GTN, nicotine,
testosterone, and estradiol have been
used in this manner.
23. Corticosteroids applied
over extensive areas of skin can produce systemic
effects and pituitary-adrenal suppression.
Absorption can be promoted by rubbing the drug
incorporated in an oleaginous base or by use
of occlusive dressing which increases hydration
of the skin.
Organophosphate insecticides coming
in contact with skin can produce systemic
toxicity.
24. Abraded surfaces readily absorb drugs
e.g. tannic acid applied over burnt skin has
produced hepatic necrosis.
Cornea is permeable to lipid soluble, unionized
physostigmine but not to highly ionized
neostigmine.
Drugs applied as eye drops may get absorbed
through the nasolacrimal duct,
e.g. timolol eye drops can produce bradycardia
and precipitate asthma.
26. Bioavailability
Bioavailability refers to the rate and extent
of absorption of a drug from a dosage form
administered by any route, as determined by
its concentration-time curve in blood or by its
excretion in urine.
It is a measure of the fraction (F) of administered
dose of a
drug that reaches the systemic circulation in
the unchanged form.
27. Bioavailability of drug
injected i.v. is I 00%, but is frequently lower
after oral ingestion because-
(a)the drug may be incompletely absorbed.
(b) the absorbed drug may undergo first pass
metabolism in the intestinal wall/liver or be
excreted in bile.
28.
29. Incomple te bioavailability after s.c. or i.m.
injection is less common, but may occur due
to local binding of the drug.
30. Bioequivalence
Oral formulations of a drug
from different manufacturers or different batches
from the same manufacturer may have the same
amount of the drug (chemically equivalent) but
may not yield the same blood levels- biologically
inequivalent.
Two preparations of a drug
are considered bioequivalent when the rate and
extent of bioavailability of the active drug
from them is not significantly different under
suitable test conditions.
31. Before a drug administered orally in solid
dosage form can be absorbed, it must break into
individual particles of the active drug (disintegration).
Tablets and capsules contain a number
of other materials-diluents, stabilizing agents,
binders, lubricants, etc.
The nature of these as well as details of the
manufacture process, e.g. force used in compressing
the tablet, may
affect disintegration.
32. The released drug must
then dissolve in the aqueous gastrointestinal
contents.
The rate of dissolution is governed
by the inherent solubility, particle size, crystal
form and other physical properties of the drug.
Differences in bioavailability may arise due to
variations in disintegration and dissolution rates.
33. Differences in bioavailability are seen mostly
with poorly soluble and slowly absorbed drugs.
Reduction in particle size increases the rate of
absorption of aspirin (microfine tablets).
The amount of griseofulvin and spironolactone in
the tablet can be reduced to half if the drug
particle is micro fined.
34. There is no need to
reduce the particle size of freely water soluble
drugs, e.g. paracetamol.
Bioavailability variation assumes practical
significance for drugs with low safety margin
(digoxin) or where dosage needs precise control
(oral hypoglycaemics, oral anticoagulants).
It may also be responsible for success or failure
of an antimicrobial regimen.
35. However, in the case of a large number of
drugs bioavailability differences are negligible and
the risks of changing from branded to generic
product or to another brand of the same drug
have often been exaggerated.