This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
TRANSDERMAL THERAPEUTIC DRUG DELIVERY SYSTEMS N Anusha
Transdermal drug delivery systems (TDDS) can be defined as self-contained discrete dosage forms which, when applied to the intact skin, delivers the drug(s) through the skin at a controlled rate to the systemic circulation.
For transdermal drug delivery, it is considered ideal if the drug penetrates through the skin to the underlying blood supply without drug buildup in the dermal layers.
They provide extended therapy with a single application, thereby improving patient compliance over other dosage forms requiring more frequent dose administration.
Delivery of drug through buccal mucosa of oral cavity is called BDDS. The buccal mucosa lines the inner cheek
It is placed between the upper gingivae and cheek.
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
This presentation includes introduction, physiology of GIT, factors affecting GRDDS, Advantages and disadvantages, approaches to GRDDS and their mechanism, some of the marketed products using GRDDS mechanism.
TRANSDERMAL THERAPEUTIC DRUG DELIVERY SYSTEMS N Anusha
Transdermal drug delivery systems (TDDS) can be defined as self-contained discrete dosage forms which, when applied to the intact skin, delivers the drug(s) through the skin at a controlled rate to the systemic circulation.
For transdermal drug delivery, it is considered ideal if the drug penetrates through the skin to the underlying blood supply without drug buildup in the dermal layers.
They provide extended therapy with a single application, thereby improving patient compliance over other dosage forms requiring more frequent dose administration.
Delivery of drug through buccal mucosa of oral cavity is called BDDS. The buccal mucosa lines the inner cheek
It is placed between the upper gingivae and cheek.
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
Physics of Tablet compression is very useful during study of the tablet. It contains the mechanism of tablet compression. It also contains the process of tablet compression.
SUSTAINED RELEASE (SR) & CONTROL RELEASE.pptxRAHUL PAL
Sustained-release medications are usually labeled with “SR” at the end of their name. These medications prolong the medication's release from a tablet or capsule so that you'll get the medication's benefits over a longer period of time.
CR = controlled release, SR = sustained release, ER = extended release, IR = immediate release. *
WHAT IS COMPRESSION ?
Compression means reduction of bulk volume of material as a result of the removal of gaseous phase (air) by applied pressure
WHAT IS CONSOLIDATION?
Consolidation is an increase in mechanical strength of material resulting from particle - particle interactions.
FORMULATION FACTORS EFFECTING BIOAVAILABILITY OF DRUGSN Anusha
Bioavailability means the rate and extent to which the active ingredient is absorbed from a drug product and becomes available at the site of action.
When the drug is given orally, only part of the administered dose appears in the plasma.
By plotting plasma concentrations of the drug versus time, one can measure the area under the curve (AUC).
This curve reflects the extent of absorption of the drug.
Physics of Tablet compression is very useful during study of the tablet. It contains the mechanism of tablet compression. It also contains the process of tablet compression.
SUSTAINED RELEASE (SR) & CONTROL RELEASE.pptxRAHUL PAL
Sustained-release medications are usually labeled with “SR” at the end of their name. These medications prolong the medication's release from a tablet or capsule so that you'll get the medication's benefits over a longer period of time.
CR = controlled release, SR = sustained release, ER = extended release, IR = immediate release. *
WHAT IS COMPRESSION ?
Compression means reduction of bulk volume of material as a result of the removal of gaseous phase (air) by applied pressure
WHAT IS CONSOLIDATION?
Consolidation is an increase in mechanical strength of material resulting from particle - particle interactions.
FORMULATION FACTORS EFFECTING BIOAVAILABILITY OF DRUGSN Anusha
Bioavailability means the rate and extent to which the active ingredient is absorbed from a drug product and becomes available at the site of action.
When the drug is given orally, only part of the administered dose appears in the plasma.
By plotting plasma concentrations of the drug versus time, one can measure the area under the curve (AUC).
This curve reflects the extent of absorption of the drug.
Controlled Release Oral Drug Delivery System
Controlled drug delivery is one which delivers the drug at a predetermined rate, for locally or systemically, for a specified period of time.
Formulation and evaluation of transdermal drug delivery system (TDDS)SanketPawar47
This is slide about formulation and evaluations of transdermal drugs delivery system . Introduction , general structure of TDDS , basic components of TDDS , approch for formulation of TDDS , manufacturing processes for TDDS ,and evaluations of TDDS
Among all diff. routes, oral has achieved more attention & quite successful.
This is due to fact that GI physiology provides more flexibility then other routes.
TDDS are topically administered medicaments in the form of patches that deliver drugs for systemic effects at predetermined and controlled rate.
Transdermal patch is an adhesive patch, that has a coating of medicine (drug), that is placed on the skin to deliver specific dose of the medicine, into the blood over a period of time.
ADVANTAGES
Avoidance of first-pass effect,
Long duration of action,
Comparable characteristics with IV infusion,
Ease of termination of drug action, if necessary,
No interference with gastric and intestinal fluids,
Suitable for administered of drug having- Very short half-life, e.g. nitroglycerine. Narrow therapeutic window.
DISADVANTAGES
Poor diffusion of large molecules,
Skin irritation,
Requires high drug load,
Unsuitable –If drug dose is large,
Absorption efficiency is vary with different sites of skin,
Skin has mainly 3 layers
Epidermis
Stratum Cornium
Stratum Granulosm
Stratum Spinosum
Stratum Basal
Dermis 3)Subcutaneous layer
EPIDERMIS
Stratum Cornium- consists of 25 to 30 layers of flattened dead keratinocytes. Which makes it water repellent.
Stratum Granulosm- consists of 3 to 5 layers and under goes Apoptosis. It contains granules known as Keratohyalin. These granules release Lipid rich secretion, which acts as the water repellent.
Stratum Spinosum- contains 8 to 10 layers of cells and it is closely arranged.
Stratum Basal- consists of single layer of cubical or columnar keratinocytes.
DERMIS
Composed of strong connective tissue containing collagen and elastic fibres, hence it can easily stretch and recoil easily.
Blood vessel, nerves gland and hair follicles are embedded in this layer.
SUBCUTANEOUS LAYER
It is also called as Hypodermis.
It is made up of loose connective tissue, including
Adipose tissue.
This helps to insulate the body by monitoring heat gain and heat loss.
The dermis is the layer of tissue that is Deeper and Thicker than epidermis.
CLASSIFICATION OF TDDS
Rate-Programmed Systems
Drug in Reservoir
Drug in Matrix
Drug in Adhesive
Drug in
Microreservoir
B. Physical Stimuli- Activated Systems
Structure-Based Systems
Electrically-Based Systems
Iontophoresis
Electroporation
Sonophoresis
Similar to ANDDS - GASTRO RETENTIVE DRUG DELIVERY SYSTEM (20)
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!
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ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
Title: Sense of Smell
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 primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
NVBDCP.pptx Nation vector borne disease control programSapna Thakur
NVBDCP was launched in 2003-2004 . Vector-Borne Disease: Disease that results from an infection transmitted to humans and other animals by blood-feeding arthropods, such as mosquitoes, ticks, and fleas. Examples of vector-borne diseases include Dengue fever, West Nile Virus, Lyme disease, and malaria.
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.
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
1. ADVANCES IN NOVEL DRUG
DELIVERY SYSTEM
DR. L.D. PATEL
DIRECTOR & PROFESSOR
C.U. SHAH COLLEGE OF PHARMACY & RESEARCH
WADHWAN-363030, DIST: SURENDRANAGAR
Email: lakshamandpatel@gmail.com
March 22, 2013 DrLDP 1
3. GASTRO RETENTIVE DRUG
DELIVERY SYSTEM (GRDDS)
Presentation
Outline:
Introduction
Merits
Stomach Physiology GRDDS
GR Technologies
Factors affecting
GRDDS
Evaluation of GRDDS
Demerits
March 22, 2013 DrLDP 3
4. . The Introduction
oral route is the
most
promising route of drug delivery.
Effective oral drug delivery may
depend upon
- gastric emptying process,
- GI transit & residence time,
- drug release from DF and
- site of absorption of drug.
. Conventional oral dosage forms
possess several physiological
limitations like
- variable gastric emptying,
- variable GI transit & shorter residence
time,
March 22, 2013 DrLDP 4
- incomplete drug release
5. Introduction….
• It may lead to incomplete & non
uniform absorption of the drugs
having absorption window in upper
part of GIT as once the DF passes
down the absorption site, the
remaining quantity goes
unabsorbed.
• Hence, a beneficial DDS would be
one which exhibits the ability to
control & prolong the gastric
emptying time and can deliver drug
in maximum conc. at the absorption
site (i.e. upper part of the small
intestine).
March 22, 2013 DrLDP 5
6. Introduction...
• Gastro Retentive Drug
Delivery System (GRDDS)
is one of the site specific
delivery for the delivery
of drugs either in
stomach or intestine .
This can be obtained by
retaining dosage form
into stomach and drug is
released in controlled
manner to specific site
either in stomach,
duodenum or/and
intestine. Absorption
March 22, 2013 DrLDP window 6
7. Different from SR…
Sustained Release Absorption GRDDS
March 22, 2013 window
DrLDP 7
8. Merits of GRDDS
• Deliver the drugs with narrow
absorption window in small
intestine. e.g Furosemide, L. Dopa.
• Efficient delivery for local action in
upper part of small intestine due to
longer residence time in stomach.
e.g. treatment of peptic ulcer.
• Improved bio-availability for
drugs that are absorbed readily upon
release in GIT.
• Better patient compliance by once
a day therapy.
March 22, 2013 DrLDP 8
9. Beneficiary Drugs by
GRDDS
• Drugs that act locally in stomach. e.g.
Antacids.
• Drugs that disturb colonic microbes . e.g.
against Helicobacter Pylori, Misoprostol.
• Drugs that are principally absorbed in the
stomach. e.g. amoxycillin.
• Drugs that are poorly soluble at alkaline pH.
e.g. diazepam, chlordiazepoxide, verapamil.
• Drugs absorbed readily throughout GIT.
e.g. metronidazole, tetracycline.
• Drugs that are unstable in the colon.
e.g. captopril, ranitidine, metformin.
• Drugs with a narrow absorption window in
GIT. e.g. L-DOPA, para aminobenzoic acid,
furosemide, riboflavin.
March 22, 2013 DrLDP 9
10. Drugs unsuitable for
GRDDS
- Drugs unstable in gastric environment.
e.g. erythromycin.
- Drugs intended for selective release in
colon. e.g. 5-aminosalicylic acid,
corticosteroids.
- Drugs having limited acid solubility.
e.g. phynytoin.
- Drugs in enteric coated systems.
March 22, 2013 DrLDP 10
11. Physiology of stomach
Under fasting conditions, stomach is like
a collapsed bag with a residual volume
of 50 ml.
The pH is 1-3 in fasted
state.
Normal GR time is
1.5-3 hrs.
Diameter of pyloric
sphincter is 12 ± 7
mm.
March 22, 2013 DrLDP 11
12. Cont…
GIT exhibits continuous motility of two
modes: Interdigestive &Digestive motility
pattern.
The interdigestive motility pattern is called as
“Migrating Motor Complex” (MMC) . It is
divided in four phases and repeated at every 2-
Phase I: Basal phase
3 hrs.
- Silent, no contractions
Phase II: Pre-burst phase
- Contraction increases
Phase III: Burst phase
- intense & large regular contractions
- efficient evacuation of contents
Phase IV: Transition phase
- Contraction dissipate betw the last part
of phase III & quiescence of phase I.
March 22, 2013 DrLDP 12
13. A) LOW
DENSITY
SYSTEMS
E) RAFT (FLOATING)
FORMING
SYSTEM B)
S EXPANDABLE/
SWELLABLE
GRDDS SYSTEMS
TECHNO
LOGIES
D) HIGH C)
DENSITY BIO/MUCO-
SYSTEM ADHESIVE
S SYSTEMS
March 22, 2013 DrLDP 13
14. E) RAFT A)LOW
FORMING DENSITY
SYSTEM SYSTEMS
S (FLOATING)
GRDDS
TECHNO B)
D) HIGH LOGIES EXPANDABL
DENSITY E/
SYSTEM SWELLABLE
S SYSTEMS
C)
BIO/MUCO
-
ADHESIVE
March 22, 2013 DrLDP 14
SYSTEMS
15. A)LOW DENSITY SYSTEMS
(FLOATING DRUG
DELIVERY)
Widely used approach.
Due to inherent low
density of dosage form,
it floats onto gastric
fluids.
It is known as “Hydro -
Dynamically Balanced
System (HBS)”
March 22, 2013 DrLDP 15
16. Floating systems
a) Non-effervescent b) Effervescent
Single Multiple units Single Multiple units
unit (i-ix) unit (i-ii)
(Monolithi (Monolithi
c c System)
system) (i-vii)
(i-x)
March 22, 2013 DrLDP 16
17. a) Floating Non-
effervescent Systems –
Monolithic (i-x)
HBSTM Capsule
It consists of Drug
+
Highly swellable gel
forming
Hydrocolloids (20-
75%) like HPMC,
HEC, Na-CMC, etc. DrLDP
March 22, 2013 17
18. Cont…
i) Matrix
Tablet
Single layer Tablet Bi-layer Tablet
Bilayer matrix tablet prepared using
polymers responsible for floating in
one layer + drug loaded in other layer.
Other type of bilayer tablet: prepared
by incorporating a loading dose of
drug in one layer + remaining drug in
other layer with hydrocolloid for its
sustained release effect.
Such tablets will float & remain in
March 22, 2013 stomach.
DrLDP 18
20. iii) Tablet with agar &
mineral oil
Drug + Mineral Oil
Mix Pour into Cool
tablet mould
Warm Agar gel solution
Air is entrapped in Agar gel.
Escape of air is prevented by oil.
The tablet contains approx 2% agar.
March 22, 2013 DrLDP 20
21. v) Tablet with
foam
• Polypropylene Foam
• Hydrophobic Powder
• Open-cell Structure
• Highly Porous
• Low Inherent Density
March 22, 2013 DrLDP 21
22. vi) Tablet with
lipid
Glyceryl Mono-oleate
• Swells in water
• Amphiphilic water insoluble lipid
• Converted to liquid crystals
(cubic shape)
It is usually melted & moulded
March 22, 2013 DrLDP 22
23. vii) Tablets in cylinder
viii) Coated
Hollow
globular shell
AIR AIR
March 22, 2013 DrLDP 23
24. ix) Multi-Layer Film
It Sealing at periphery films which are sealed
consists of two
together along their periphery in such a way as
to entrap some air between them & make air
pocket to impart floating.
One film is carrier film made up of water
insoluble polymer matrix having drug
dispersed/dissolved therein.
Other film is barrier film overlaying the carrier
film. Barrier film consists of copolymer of water
insoluble & water and drug permeable polymer.
Floating time & drug release rate can be
modulated by appropriate selection of polymer
March 22, 2013 DrLDP 24
25. x) Micro-porous
reservoir
Floating chamber
Drug reservoir
Microporous wall
It comprised of a drug reservoir encapsulated
in microporous compartment having pores on
its surface.
A floating chamber was attached at one
surface which gives buoyancy to entire device.
Drug slowly dissolves out via micro pores.
March 22, 2013 DrLDP 25
26. a) Floating Non-
effervescent system -
Multiple units (i-ix)
i) Calcium alginate / Pectinate /
chotosan beads
IONOTROPIC GELATION METHOD
Drug + CaCl2 solution
Na alginate solution
Separated & freeze dried Spherical gel beads
Freeze dried calcium alginate beads produced by
dropping Na alginate solution into CaCl 2 solution.
Due to chemical reaction named as Ionotropic
gelation, gelation take place and forms solid
spherical gel beads , which are separated from
solution and they are freeze dried at - 40oC for 24
hours. 2013
March 22, The resultant weight of beads is less
DrLDP 26
giving buoyancy up to 12 hours.
27. ii) Coated Alginate beads
with air compartment
Coating before drying
Alginate bead in
solution before
drying
Due to shrinkage of internal core bead during
drying, it produces the air compartment which
imparts buoyancy.
March 22, 2013 DrLDP 27
28. iii) Floating powder
Drug
+
Sodium/Potassium
Alginate
+
HPMC/HPC
+
Binder
Floating powder can be filled in capsule or
compressed to tablet
March 22, 2013 DrLDP 28
29. iv) Oil entrapped gel
beads
Vegetable oil is used as floating carrier as it is light weight &
hydrophobic. It is incorporated into gel matrix of beads. Oil
entrapped beads are prepared by both calcium alginate bead
and calcium pectinate bead.
March 22, 2013 DrLDP 29
31. vii) Foam containing Micro-
particles
Drug Polymer
Dissolved
Only foam
Organic
Aqueous PVA
Solvent
solution
Dispersed
Foam Micro-particle
Foam
Foam Micro-particles
March 22, 2013 DrLDP 31
32. viii) Calcium
Silicate as
floating
carrier
Highly porous ix) GELUCIRE ®
Large pore volume Granules
Low inherent
density
Granules Hydrophobic Lipid
containing Diff. Grades –39/01,
Drug, HPMC & Ca 43/01
Silicate. Low Inherent Density
March 22, 2013
Melt Granulation
DrLDP 32
SR of Highly Soluble
33. b) Floating effervescent
systems - Monolithic (i-vii)
i) Matrix Tablet ii) Matrix tablet
Bicarbonate + Polymer
with Carbopol
pH dependent Gelling
Single Layer Tablet
Bilayer Tablet Only Carbopol
Triple Layer Tablet - No gelling (at acidic
pH)
Triple layer tablet prepared having Bicarbonate + Carbopol
first swellable floating layer, second - Gelling due to Alkaline
sustained release layer of 2 drugs pH Carbopol gives swelling & gelling.
(Metronidazole & Tetracycline) and But this system do not remain intact
third rapid dissolving layer of for long time. Hence, it can be
bismuth salt. This tablet is used as coated with permeable elastic
single dosage form for Triple polymer like Eudragit to support
Therapy of H. Pylori.
March 22, 2013 integrity of core.
DrLDP 33
34. iii) Floating pills It consists drug pill
surrounded by double layers
Swellable polymer coat.
Inner layer, effervescent
Tartaric acid NaHCO 3
layer, contains two sub-
layers to avoid direct
contact of NaHCO3 &
tartaric acid.
Outer layer, swellable
permeable layer, is made up
DRUG
of PVA and shellac.
As CO2 gas can not go out from outer
membrane makes a balloon like system which
can float upto 5 hrs irrespective of pH &
viscosity22, 2013
March of medium. DrLDP 34
36. vi) Programmable drug delivery
CO2
Fluid in
Drug release
vii) Osmotically controlled DDS
March 22, 2013 DrLDP 36
37. b) Floating effervescent
systems - Multiple units
(i-ii)
i) Porous Alginate beads
CaCl 2
NaHCO 3 Na-Alginate Acetic
Solution
Solution Acid
Simultaneous generation of CO 2 and gelling of
beads.
Escape of CO 2 creates pores in beads.
March 22, 2013 DrLDP 37
38. ii) Ion exchange resin
beads
H+ Cl H+ Cl
HCO3
HCO3
Resin UG H+ Cl
DR
DR
HCO3 UG
H+ Cl H+ Cl
This system comprised of ion exchange resin beads loaded
with bicarbonate and a negatively charged drug tagged to
resin. The beads were encapsulated in a semi permeable
membrane. Upon contact with gastric fluid, Cl - ion of HCl is
exchanged with bicarbonate and produce CO 2 gas, which
can not escape due to semi permeable membrane. Hence,
March 22, 2013 DrLDP 38
it floats. Uncoated beads don’t show floating due to
39. B) EXPANDABLE
SYSTEMS
Also called ‘ PLUG
SYSTEM’
Size of the formulation
greater than Pyloric
sphincter
Smaller in size for oral
intake
Should expand/swell for
gastric retention
Should be collapsed after
March 22, 2013 DrLDP 39
40. EXPANDABLE
APPROACH
a)Swelling systems b) Unfolding systems
(i-ii) (i-iv)
Superporous hydrogel in its dry (a) & water-
swollen (b) state. On the right, schematic
illustration of the transit of superporous hydrogel.
March 22, 2013 DrLDP 40
41. a) Swelling
i) systems
Polymeric envelope reservoir (A)
It consist of drug in center
surrounded by swellable material (B) are placed
in elastic polymeric envelope type system (C).
The polymeric envelope is permeable to drug
and fluids.
This system gets swollen in gastric fluid and
integrity is retained by elastic polymeric
envelope and drug is released in controlled
manner.
March 22, 2013 DrLDP 41
42. Swelling systems
ii) Tiny pills in matrix
Tiny pills containing drug are incorporated into
hydrogel matrix and coated with wax to give
strength to wall. It works by plugging pylorus
sphincter. It keeps the stomach in fed state and
thus delays house keeper waves which comes in
fasted state.
After administration, it achieves high volume and
tiny pills are released slowly out from matrix and
gives GR to drug.
i) The dosage from side-view
ii) The cross-sectional view which
comprises of A) Waxy wall
B) Hydrogel Matrix
March 22, 2013 DrLDP 42
C) Tiny pills
43. b) Unfolding
systems a capsule
It is (A) containing 2
i) Obstructing means reservoirs (C) attached together
with hydrophilic/hydrophobic strips
(B). The flexible strips get enlarge
and get sufficient strength and
becomes rigid to achieve gastro
retention.
March 22, 2013 DrLDP 43
44. b) Unfolding
systems
ii) Multilayer films Gelatin band/Strip (C)
It consists of one erodible
polymeric film containing
drug (A) which is adhered
on another non-erodible
carrier polymeric film (B) .
This bilayer sheet is folded Before
and gelatin bands/strips (C)
are used to maintain
folded. The system is
placed in capsule. After
In stomach, capsule and
gelatin band dissolves to
give unfolded system.
Drug (A)
March 22, 2013 Drug Erodible Polymer film (B)
DrLDP 44
45. b) Unfolding
systems
ii) Multilayer films
Intec Pharma Drug Delivery
system produced by Virtual Point
March 22, 2013 DrLDP 45
47. C) BIO/MUCO-ADHESIVE
SYSTEMS
Drug is incorporated with
bio /muco adhesive agents,
enabling the device to
adhere to stomach wall,
thus resisting gastric
emptying.
The mucus on the walls of
stomach is in a state of
constant renewal, resulting
in unpredictable
adherence.
March 22, 2013 Hence, this approach is not
DrLDP 47
49. D) HIGH DENSITY
SYSTEMS- SEDIMENTATION
Density greater than stomach
content i.e. 1.004 g/cm3.
When the patient is upright,
small high-density pellets sink
to the bottom of stomach
where they are entrapped in
the folds of antrum & thus
withstand peristaltic motion of
stomach.
Prepared by coating or mixing
drug with heavy (>3g/cm3) inert
material like BaSO4, ZnO, iron
powder, TiO2.
March 22, 2013 DrLDP 49
50. E) RAFT FORMING
SYSTEMS
RAFT (Continuous viscous gel layer)
Raft forming system
contains alginates &
alkaline bicarbonates
or carbonates.
Upon reaction with the
gastric acid, causes
the bubbles to form &
thus enables floating.
Generally used for
antacids.
March 22, 2013 DrLDP 50
51. Factors affecting the
performance of
GRDDS
Formulation factors Idiosyncratic factors
• Density of DF • Food intake, nature
<1 for floating of food, caloric
• Size of DF content & frequency.
> size of DF, > • Effect of gender,
GR time posture, age, sleep &
disease state.
March 22, 2013 DrLDP 51
52. Evaluation of GRDDS
In-vitro evaluation
1) For floating systems
2) For swelling systems
3) Penetration rate
4) Dissolution
March 22, 2013 DrLDP 52
53. 1) For floating system
• Buoyancy lag time : Time taken by DF to float on top of
the dissolution medium.
• Floating time : Time for which DF continuously floats on
the dissolution medium.
• Specific gravity/ density
• Resultant weight : Density changes with change in
F resultant – Fgrav as Df.g.V – Ds.g.V = (Df – Ds).g.V = (Df –
= Fbuoy weight = a function of time.
M/V).g.V,
F=Resultant weight of object, Df=Density of Fluid, Ds=Density
of object, g=Gravitational force, M=Mass of dosage form,
V=Volume of DF
March 22, 2013 DrLDP 53
54. 2) For swelling system
i) Swelling Index: dimensional changes are
measured in terms of increase in tablet thickness /
diameter with time.
ii) Water uptake/Weight gain:
Water uptake= Wu= (Wt –
Wo).100/Wo,
Wt = weight of dosage form at
time t,
iii) Penetration
Wo = initial weight of dosage
form
rate:
March 22, 2013 DrLDP 54
57. In-vivo evaluation
• Radiology
∀ γ-Scintigraphy
• Gastroscopy
• Magnetic Marker Monitoring
• Ultrasonography
• 13C Octanoic Acid Breath
Test
March 22, 2013 DrLDP 57
58. Demerits…
- GRDDS is not preferred for drugs which are
unstable at acidic pH, insoluble drugs &
drugs causing gastric irritation.
- For floating, high level of fluid in stomach is
required. Sleeping condition is not favorable
for the better results as DF may swept
away.
- Food is an important factor . Presence of
food delays emptying time of DF. So
presence of food is preferable.
- Adhesive systems can not prevail longer due
to high turn-over rate of mucus layer and
presence of soluble mucin.
- For swelling systems, it is necessary that it
should not exit before appropriate swelling.
March 22, 2013 DrLDP 58
59. Conclusions
• In the field of GR, there are many
obstacles that need to be overcome in
order to able to claim true gastric
retention.
• Considering the advantages for improved
delivery of drugs, some mfgers have
undertaken the herculious task of
developing such devices, some with
success and some with failure ended due
to un-predictability of GIT.
• However, the scientists are as close as
ever been to seeing a greater transition
of GR devices from a developmental level
to the manufacturing & commercial.
March 22, 2013 DrLDP 59
60. Marketed
Products
Brand Drug (dose) Company
Name
Levodopa (100 mg),
Madopar® Roche, USA
Benserazide (25 mg)
Hoffman LaRoche,
Valrelease® Diazepam (15 mg)
USA
Liquid Al(OH)3 + MgCO3 GlaxoSmithKlein,
Gaviscon® India
Topalkan® Pierre Fabre Drug,
Al – Mg antacid
Liquid France
Conviron® Ferrous sulfate Ranbaxy, India
Cifran OD® Ciprofloxacin (1 g) Ranbaxy, India
Cytotec®
March 22, 2013 Misoprostal (100/200µg)
DrLDP Pharmacia, USA 60
61. References
• S. P. Vyas, Roop K. Khar, CONTROLLED DRUG DELIVERY – Concepts &
Advances, Vallabh Prakashan, page no. 196-217
• N. K. Jain, Progress in Controlled & Novel Drug Delivery Systems, 1st
edition 2004, CBS Publishers, page no.76-97
• G. Chawla, P. Gupta, V. Koradia, A. K. Bansal, Pharmaceutical
Technology, July 2003, 50-68
• Drs Jose Gutieerez-Rocca, Hossein Omedian, Khalid Shah, Progresses in
Gastro-retentive drug delivery system-A report. Business briefing,
Pharmtech 2003, 152-156.
• S.R.Parakh, A.V.Gothoskar, M.T.Karad, Pharmaceutical Technology, MAY
2003, 40-48
• M. C. Gohel, P. R. Mehta, R. K. Dave, N. H. Bariya, Dissolution
Technologies, November 2004.
• S. T. Prajapati, L. D. Patel, D. M. Patel, Formulation and In vitro Evaluation
of floating Matrix Tablets of domperidone: Influence of Combination of
Hydrophilic and Hydrophobic Matrix Formers, J. Pharmacy and Chemistry,
Vol. 2, Issue 1, 54-59, January-March 2008.
• S. T. Prajapati, L. D. Patel, D. M. Patel, Gastric floating matrix tablets:
Design and optimization using combination of polymers, Acta
Pharmaceutica, 58 (2), 221-229, 2008.
• Tejas B. Patel, L. D. Patel, Timir B. Patel, Kirit A. Patel, Tushar R. Patel,
Sunil H. Makwana, Design and Development of gastric Floating drug
delivery system Using Factorial Design, Pharma Buzz, Vol. 3, No. 6, 21-27,
June 2008.
March 22, 2013 DrLDP 61
62. THANK YOU
ALL
for your participation!
Dr. L. D. Patel
Sr. Lecturer, L.M. College of Pharmacy, Ahmedabad
March 22, 2013 DrLDP 62
(Gujarat)
63. BEST
WISHES…. L. D. Patel
Dr.
Principal & Professor
SAL Institute of
Pharmacy, Ahmedabad
(Gujarat)
Dr. L. D. Patel
Dean & Professor
Faculty of Pharmacy,
D.D. University, Nadiad –
387001 (Gujarat)
March 22, 2013 DrLDP 63
64. QUESTIONS - -
Lachoo College of
Pharmacy, Jodhpur on 7 th
June 2012
DR. L.D. PATEL
DIRECTOR & PROFESSOR
C.U. SHAH COLLEGE OF PHARMACY &
RESEARCH
March 22, 2013 DrLDP 64
WADHWAN-363030, DIST: SURENDRANAGAR