This document discusses modified release drug products, including extended release and delayed release dosage forms. It defines modified release as altering the timing and/or rate of drug release. Extended release aims for twice daily dosing by providing continuous drug levels while delayed release releases the drug at a time other than promptly after administration. The document discusses various extended release drug delivery technologies like coated beads, multilayer tablets, microencapsulation, embedding in eroding matrices, plastic matrices, complexation, and osmotic pumps. It emphasizes the importance of in vitro-in vivo correlations and bioequivalence studies in evaluating these modified release products.
This presentation involves the information about Modified-Release Drug Products, Targeted Drug Delivery Systems and Biotechnological Products in Pharmaceutics
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Computational modelling of drug disposition lalitajoshi9
computational modelling of drug disposition is the integral part of computer aided drug design. different kinds of tools being used in the prediction of drug disposition in human body. This topic in the CADD explains the details about the drug disposition, active transporters and tools.
This presentation involves the information about Modified-Release Drug Products, Targeted Drug Delivery Systems and Biotechnological Products in Pharmaceutics
Biopharmaceutic considerations in drug product design and In Vitro Drug Produ...PRAJAKTASAWANT33
Introduction, biopharmaceutic factors affecting drug bioavailability, rate–limiting steps in drug absorption, physicochemical nature of the drug formulation factors affecting drug product performance
This PPT includes what role does Dosage form impart on absorption. Why it is important in absorption. what should be its nature and type of dosage form.
Computational modelling of drug disposition lalitajoshi9
computational modelling of drug disposition is the integral part of computer aided drug design. different kinds of tools being used in the prediction of drug disposition in human body. This topic in the CADD explains the details about the drug disposition, active transporters and tools.
Myself Omkar Tipugade , M- Pharm ,Sem - II, Department of pharmaceutics , from Shree Santkrupa College Of Pharmacy , ghogaon . Today I upload presentation on Active Transport like P-gp , BCPR, Nucleoside transporters etc .
It includes Introductory part about what is Dissolution...then Mechanism of Dissolution is elaborated...Theories of Dissolution also given..It also includes Factors affecting Dissolution profile..Along with References given below for easily searching..
Special concerns in bioavaliblity and bioeqvivalencePradnya Shirude
you will get here special concerns about bioavailability and bioequivalance. it will also give regulations and criteria for bioavalablity and bioeuivalance
Introduction
Anatomy and physiology of lungs
Advantage and disadvantage of Pulmonary Drug Delivery system.
Aerosols , propellants & container types.
Current technologies for pulmonary drug delivery.
New technologies for pulmonary drug delivery.
Evaluation of Pharmaceutical Aerosols & PDDS.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of anti-asthmatic and other locally acting drugs directly to their site of action reduces the dose needed to produce a pharmacological effect, while the low concentrations in the systemic circulation may also reduce side-effects.
The drugs which are administered by pulmonary route are not only for lungs delivery but it goes to systemic circulation and produce the effect where it is desired through out the body. For Eg. A product containing ergotamine tartrate is available as an aerosolized dosage inhaler for the treatment of migraine & Volatile anesthetics, including, halothane, are also given via the pulmonary route.
Used for inhalation and topical aerosols .
Manufactured by impact extrusion process.
Light in weight, less fragile, Less incompatibility due to its seamless nature.
Greater resistance to corrosion .
Pure water and pure ethanol cause corrosion to Al containers.
Added resistance can be obtained by coating inside of the container with organic coating like phenolic , vinyl or epoxy and polyamide resins.
Myself Omkar Tipugade , M- Pharm ,Sem - II, Department of pharmaceutics , from Shree Santkrupa College Of Pharmacy , ghogaon . Today I upload presentation on Active Transport like P-gp , BCPR, Nucleoside transporters etc .
It includes Introductory part about what is Dissolution...then Mechanism of Dissolution is elaborated...Theories of Dissolution also given..It also includes Factors affecting Dissolution profile..Along with References given below for easily searching..
Special concerns in bioavaliblity and bioeqvivalencePradnya Shirude
you will get here special concerns about bioavailability and bioequivalance. it will also give regulations and criteria for bioavalablity and bioeuivalance
Introduction
Anatomy and physiology of lungs
Advantage and disadvantage of Pulmonary Drug Delivery system.
Aerosols , propellants & container types.
Current technologies for pulmonary drug delivery.
New technologies for pulmonary drug delivery.
Evaluation of Pharmaceutical Aerosols & PDDS.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of anti-asthmatic and other locally acting drugs directly to their site of action reduces the dose needed to produce a pharmacological effect, while the low concentrations in the systemic circulation may also reduce side-effects.
The drugs which are administered by pulmonary route are not only for lungs delivery but it goes to systemic circulation and produce the effect where it is desired through out the body. For Eg. A product containing ergotamine tartrate is available as an aerosolized dosage inhaler for the treatment of migraine & Volatile anesthetics, including, halothane, are also given via the pulmonary route.
Used for inhalation and topical aerosols .
Manufactured by impact extrusion process.
Light in weight, less fragile, Less incompatibility due to its seamless nature.
Greater resistance to corrosion .
Pure water and pure ethanol cause corrosion to Al containers.
Added resistance can be obtained by coating inside of the container with organic coating like phenolic , vinyl or epoxy and polyamide resins.
Sustained release drug delivery 130210234837-phpapp01pratik swarup das
SUSTAINED RELEASE DRUG DELIVERY: Any of the dosage form that maintains the therapeutic blood or tissue levels of drug by continuous release of medication for a prolonged period of time, after administration of a single dose. In case of injectable dosage forms it may vary from days to months.
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...Snehal Patel
ABSTRACT
Oral controlled release dosage forms face several physiological restriction like inability to retain
and position the controlled drug delivery system within the targeted region of the gastrointestinal
tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption
pattern, inadequate medication release and shorter residence time of the dosage form in the
stomach. As the fallout of this episode there is inadequate absorption of the drug having
absorption window predominantly, in the upper area of GIT. These contemplations have
provoked to the development of oral controlled release dosage forms with gastroretentive
properties. Microballoons (Hollow microspheres) hold certification as one of the potential
approaches for gastric retention. Microballoons are spherical empty particles without core and
can remain in the gastric region for delayed periods. They significantly increase the gastric
residence time of medication, thereby enhance bioavailability, improves patient compliance by
reducing dosing frequency, lessen the medication waste, enhance retention of medication which
solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH
environment. The present review preparation methods, characterization, advantages,
disadvantages, mechanism of drug release from microballoons, applications and list of the drugs
formulated as microballoons are discussed.
KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
Powerpoint presentation on controlled drug delivery system. Its introduction, terminologies, rationale, advantages, disadvantages, selection of drug, approaches for designing controlled release formulations and physicochemical and biological properties of drug
micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Anti ulcer drugs and their Advance pharmacology ||
Anti-ulcer drugs are medications used to prevent and treat ulcers in the stomach and upper part of the small intestine (duodenal ulcers). These ulcers are often caused by an imbalance between stomach acid and the mucosal lining, which protects the stomach lining.
||Scope: Overview of various classes of anti-ulcer drugs, their mechanisms of action, indications, side effects, and clinical considerations.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
2. INTRODUCTION
Modified release drug product are those that
alter the timing and/or the rate of release of
drug substance.
Types of modified release drug products are-
1. Delayed release
2. Extended release
3. Orally disintegrating tablet
3. Continued….
EXTENDED RELEASE DRUG PRODUCTS
Two fold release in dosage frequency, examples
include controlled release, sustained release and
long acting drug products.
DELAYED RELEASE DRUG PRODUCTS
Releases a discrete portion of drug at a time other
than promptly after administration. e.g – enterric
coated dosage forms like enterric coated aspirin,
other NSAIDS, etc.
4. ORALLY DISINTEGRATING TABLETS
Disintegrate rapidly in saliva after oral
administration.
Can be used without addition of water.
Drug dispersed in saliva and swallowed.
5. ADVANTAGES
Reduction in drug blood level fluctuation
Frequency reduction in dosing
Patient compliance
Reduced adverse side effect
Reduction in health care cost
6. Examples of modified release
dosage forms
Systems Examples of drugs
Oral drug products Diltiazem HCL (extended release)
Diclofenac sodium (delayed release)
Ondansetron (oral soluble film)
Transdermal drug delivery system Clonidine (transdermal therapeutic
system)
Opthalmic drug delivery Controlled release pilocarpine
Intravaginal drug delivery Dinoprostone vaginal insert
7. DOSAGE FORM SELECTION
Drug with low aqueous solubility generally should not
be formulated into a non-disintegrating tablet, because
risk of incomplete drug dissolution is high.
Drug with low solubility at neutral pH should be
formulated so that most of drug is released before it
reaches the colon.
A drug with high water solubility in acidic pH in
stomach but very insoluble at intestine pH may be
difficult to formulate into ER drug product.
With too much coating, bioavailabilty gets reduced.
8. KINETICS OF EXTENDED
RELEASE DOSAGE FORM
Dtotal = DI + DM
Here, Dtotal = total dose required
DI = initial dose released
DM = sum of maintainence dose
also , DM = k˚r td
so, [ Dtotal = DI + k˚r td ]
However maintainence dose is released after DI
has produced a blood level equal to the
therapeutic drug level.
9. Continued…
DMstarts to release at t = 0
For drug following one compartment model, rate of
elimination (R) needed to maintain the drug at a
therapeutic level (Cp) is:
R = k Vd Cp
also the equation can be written as :
R = Cp ClT
here, ClT = clearance of drug
10. Continued…
Thus to maintain the therapeutic dose level in
the body to Cp, the total dose needed will be
Dtotal = DI + Cp.ClT.Ԏ
here DI = loading dose
Ԏ = dosing interval
11. Continued…
Plasma drug release from a zero order
, extended release drug product
Cp = Ds (1-e-kt
)/ Vd.K
Here, Ds = maintainence dose
Cp = plasma drug conc.
K = elimination constant
Vd = volume of distribution
12. Extended-release oral dosage forms
The drugs best suited for incorporation into an extended-
release product have the following characteristics:
They exhibit neither very slow nor very fast rates of
absorption and excretion.
They are uniformly absorbed from the gastrointestinal
tract.
They are administered in relatively small doses.
They possess a good margin of safety.
They are used in the treatment of chronic rather than
acute conditions.
13. 1) Coated beads, granules, or
microspheres
- In these systems, the drug is
distributed onto beads, pellets,
granules, or other particulate
systems.
TYPES OF EXTENDED RELEASE PRODUCTS
14. - Using conventional pan coating or
air suspension coating, a solution
of the drug substance is placed on
small inert nonpareil seeds or
beads made of sugar and starch or
on microcrystalline cellulose
spheres.
15. 2) Multitablet system
Small spheroid compressed tablets
3 to 4 mm in diameter may be
prepared to have varying drug
release characteristics.
They may be placed in gelatin
capsule shells to provide the
desired pattern of drug release.
Each capsule may contain 8 to 10
minitablets, some uncoated for
immediate release and others
coated for extended drug release.
16. 3) Microencapsulated drug
Microencapsulation is a process by
which solids, liquids, or even gases
may be enclosed in microscopic
particles by formation of thin
coatings of wall material around the
substance.
17. The typical encapsulation process
usually begins with dissolving the
wall material, say gelatin, in water.
The material to be encapsulated is
added and the two-phase mixture
thoroughly stirred.
With the material to be
encapsulated broken up to the
desired particle size, a solution of a
second material, usually acacia, is
added.
18. This additive material concentrates the
gelatin into tiny liquid droplets.
One of the advantages of
microencapsulation is that the
administered dose of a drug is
subdivided into small units that are
spread over a large area of the
gastrointestinal tract, which may
enhance absorption by diminishing
localized drug concentration.
19. By this process, the drug
substance is combined and made
into granules with an excipient
material that slowly erodes in
body fluids, progressively
releasing the drug for absorption.
4) Embedding drug in slowly
eroding or hydrophilic matrix
system
20. When these granules are mixed with
granules of drug prepared without the
excipient, the uncombined granules provide
the immediate drug effect whereas the
drug-excipient granules provide extended
drug action.TYPE TRADE NAME RATIONALE
Erosion tablet Constant-T
Tenuate Dospan
Theophylline
Diethyl propion HCL
dispersed in hydrophilic
matrix
Waxy matrix tablet Kaon CI Slow reduce of potassium
chloride to reduce GI irritation
Pellets in tablet Theo-dur Theophylline
Coated ion exchange Tussionex Ion-exchange resin complex
of hydrocodone and
phenyltoloxamine
21. 5) Embedding drug in inert plastic
matrix
By this method, the drug is
granulated with an inert plastic
material such as polyethylene,
polyvinyl acetate, or
polymethacrylate, and the
granulation is compressed into
tablets.
The drug is slowly released from the
inert plastic matrix by diffusion.
The inert tablet matrix, expended of
22. 6) Complex formation
Certain drug substances when
chemically combined with certain
other chemical agents form chemical
complexes that may be only slowly
soluble in body fluids, depending
upon the pH of the environment.
This slow dissolution rate provides
the extended release of the drug.
23. 7) Ion-exchange resins
A solution of a cationic drug may be
passed through a column containing an
ion-exchange resin, forming a complex
by the replacement of hydrogen atoms.
The resin-drug complex is then washed
and may be tableted, encapsulated, or
suspended in an aqueous vehicle.
The release of the drug is dependent
upon the pH and the electrolyte
concentration in the gastrointestinal
tract.
24.
25. Release is greater in the acidity of the
stomach than in the less acidic environment
of the small intestine.
Examples of drug products of this type
include hydrocodone polistirex and
chlorpheniramine polistirex suspension and
phentermine resin capsules.
26. The mechanism of action of drug release
In the stomach:
1. Drug resinate+HClacidic resin+drug
hydrochloride
2. Resin salt+HClresin chloride+sodium salt of
drug
27. In the intestine
1. Drug resinate+NaClsodium
resinate+drug hydrochloride
2. Resin salt+NaClresin chloride+sodium
salt of drug
28. 8) Osmotic pump
The pioneer oral osmotic pump drug
delivery system is the Oros system,
developed by Alza.
The system is composed of a core
tablet surrounded by a semipermeable
membrane coating have a 0.4 mm
diameter hole produced by laser beam.
30. The system is designed such that only a
few drops of water are drawn into the
tablet each hour.
The rate of inflow of water and the
function of the tablet depends upon the
existence of an osmotic gradient between
the contents of the bi-layer core and the
fluid in the GI tract.
Drug delivery is essentially constant as
long as the osmotic gradient remains
constant.
31. The drug release rate may be altered by
Changing the surface area,
The thickness or composition of the
membrane,
Changing the diameter of the drug release
orifice.
The drug-release rate is not affected by
gastrointestinal acidity, alkalinity, fed
conditions, or GI motility.
32. Effect of coating membrane thickness on the rate and duration of
zero-order release of indomethacin from osmotic pressure-controlled
gastrointestinal delivery system
33. OROS OSMOTIC
THERAPEUTIC SYSTEMS
TRADE NAME MAUFACTURE GENERIC NAME
Acutrim Ciba Phenylpropanolamine
Covera-HS Searle verapamil
Dynacirc CR Sandoz Isradipine
Glucotrol XL Pfizer glipizide
34. In vitro/in vivo correlations
(IVIVCs)
IVIVCs is critical to the development of
oral extended-release products.
Assessing IVIVCs is important
throughout the periods of product
development, clinical evaluation,
submission of an application for FDA-
approval for marketing, and during
postapproval for any formulation or
manufacturing changes which are
EVALUATION OF MODIFIED-RELEASE DRUG
PRODUCTS
35. Three categories of IVIVCs are
included in the document
- Level A
A predictive mathematical model for the
relationship between the entire in vitro
dissolution/release time course, e.g.,
the time course of plasma drug
concentration or amount of drug
absorbed.
36. - Level B
A predictive mathematical model of the
relationship between summary
parameters that characterize the in vitro
and in vivo, time courses.
- Level C
A predictive mathematical model of the
relationship between the amount
dissolved in vitro at a particular time (or
T50%) and a summary parameter that
characterizes the in vivo time course
(e.g. Cmax or AUC).
37. DISSOLUTION STUDIES
Reproducibility of the method
Proper choice of the medium
Maintainence of sink condition
Control of solution hydrodynamics
Dissolution rate as function of pH, ranging
from 1-8
38. EVALUATION OF IN-VIVO
BIOAVAILABILITY DATA
1. PHARMACOKINETIC PROFILE
Plasma drug conc.-time curve should adequately
define bioavailabilty of drug from dosage form.
The bioavailability data should demonstrate the
extended release characteristics of the dosage
form compared to reference/immediate release
product.
39. 2. STEADY STATE PLASMA DRUG
CONCENTRATION
Fluctuation = C∞
max - C∞
min /C∞
av
where C∞
av is equal to [AUC]/T
40. 3. RATE OF DRUG ABSORPTION
For a extended release drug product to claim zero-
order absorption, wagner nelson method is used.
4. OCCUPANCY TIME
For drugs whose therapeutic window are known,
plasma drug conc. Maintained above the minimum
effective drug concentration.
The time required to obtain plasma drug levels within
therapeutic window is known as occupancy time.
41. 5. BIOEQUIVALENCE STUDIES
It includes the study of :
A fasting study
A food intervention study
A multiple dose study
42. REFERENCE
Shargel leon, WU Pong Susanna, B.C. YU
Andrew, Applied Biopharmaceutics and
Pharmacokinetics, 5th
edition,rights by
McGraw-hill, page no.-516-551