Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Gastro retentive drug delivery system (GRDDS)Shweta Nehate
Oral route is the most acceptable route for drug administration. Apart from conventional dosage forms several other forms were developed in order to enhance the drug delivery for prolonged time period and for delivering drug to a particular target site. Gastro-retentive drug delivery system (GRDDS) has gainned immense popularity in the field of oral drug delivery recently. it is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. different innovative approaches are being applied to fabricate GRDDS. Gastroretentive drug delivery is an approach to prolong gastric residence time, there by targeting site-specific drugs release in the upper gastrointestinal tract (GIT) for local or systemic effects. It is obtained by retaining dosage form into stomach and by releasing the in controlled manner.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Mucoadhesive drug delivery system interact with the mucus layer covering the mucosal epithelial surface, & mucin molecules & increase the residence time of the dosage form at the site of the absorption.
Mucoadhesive drug delivery system is a part of controlled delivery system.
Since the early 1980,the concept of Mucoadhesion has gained considerable interest in pharmaceutical technology.
combine mucoadhesive with enzyme inhibitory & penetration enhancer properties & improve the patient complaince.
MDDS have been devloped for buccal ,nasal,rectal &vaginal routes for both systemic & local effects.
Hydrophilic high mol. wt. such as peptides that cannot be administered & poor absorption ,then MDDS is best choice.
Mucoadhesiveinner layers called mucosa inner epithelial cell lining is covered with viscoelasticfluid
Composed of water and mucin.
Thickness varies from 40 μm to 300 μm
General composition of mucus
Water…………………………………..95%
Glycoproteinsand lipids……………..0.5-5%
Mineral salts……………………………1%
Free proteins…………………………..0.5-1%
The mechanism responsible in the formation of mucoadhesive bond
Step 1 : Wetting and swelling of the polymer(contact stage)
Step 2 : Interpenetration between the polymer chains and the mucosal membrane
Step 3 : Formation of bonds between the entangled chains (both known as consolidation stage)
Electronic theory
Wetting theory
Adsorption theory
Diffusion theory
Fracture theory
Advantages over other controlled oral controlled release systems by virtue of prolongation of residence of drug in GIT.
Targeting & localization of the dosage form at a specific site
-Painless administration.
-Low enzymatic activity & avoid of first pass metabolism
If MDDS are adhere too tightlgy because it is undesirable to exert too much force to remove the formulation after use,otherwise the mucosa could be injured.
-Some patient suffers unpleasent feeling.
-Unfortunately ,the lack of standardized techniques often leads to unclear results.
-costly drug delivery system
Approaches Of Gastro-Retentive Drug Delivery System or GRDDSAkshayPatane
Approaches Of Gastro-Retentive Drug Delivery System
Includes:
Floating and Non-Floating drug delivery system with their subtypes
Like Non-effervescent system, Effervescent system, Raft forming system,
High Density system, Expandable system, Muco-adhesive system,
Super porous hydrogel system and Magnetic Systems, etc.
Application Of Polymer In Controlled Release FormulationAnindya Jana
Polymers are becoming increasingly important in the field of drug delivery. The pharmaceutical applications of polymers range from their use as binders in tablets to viscosity and flow controlling agents in liquids, suspensions and emulsions. Polymers can be used as film coatings to disguise the unpleasant taste of a drug, to enhance drug stability and to modify drug release characteristics.
As a consequence, increasing attention has been focused on methods of giving drugs continually for a prolonged time periods and in a controlled fashion.
This technology now spans many fields and includes pharmaceutical, food and agricultural applications, pesticides, cosmetics, and household products.
Development and Characterisation of Fast Dissolving Oral FilmsPardeep Jangra
For My review article on Fast Dissolving Oral Films, click on this link http://www.ijupbs.com/Uploads/2.%20RPA13140283015.pdf or copy paste this link in browser.
Pardeep Kumar Jangra
In this ppt ,i have covered the introduction of microspheres,various preparation methods of microspheres, advantages and disadvantage of microspheres,types and evaluation parameters of the microspheres.
Bioavailability is defined as rate and extent of absorption of the unchanged drug from its dosage form and become available at the site of action. Solubility is the most important physical characteristic of a drug for its oral bioavailability, formulation, development of different dosage form of different drugs, therapeutic efficacy of the drug and for quantitative analysis. Proper selection of solubility enhancement method is the key to ensure the goals of a good formulation.
Drug excipient incompatibilities are major concerns in formulation development.
Selection of the proper excipient during preformulation studies is of prime importance.
Hydrogels,
introduction,
historical background,
properties,
classification,
difference between chemical and physical hydrogels,
common uses,
pharmaceutical applications,
preparation methods,
list of monomers used,
analytical machines,
advantages,
disadvantages,
conclusion
Buccal drug delivery system is part of mucoadhesive drug delivery system and their principal and formulation ,mechanisam of adhesion to mucosa ,use of polymers in BDDS and permiability enhancers and evaluation parameters of buccal tablets and patchs
Avoid first pass effect,
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
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
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!
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
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
Factory Supply Best Quality Pmk Oil CAS 28578–16–7 PMK Powder in Stockrebeccabio
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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.
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
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
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.
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.
1. Prepared by: Guided by:
Shivam Thakore Mrs Shital Acharya
Vishal Gajipara Mr Jaymin Patel
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 1
2. What is BDDS???
Delivery of drug through Buccal mucosa of oral
cavity is called BDDS. Buccal mucosa lines the
inner region of cheeks.
In biological term, the product is placed between
upper gingiva (gums) & cheek to treat local &
systemic conditions.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 2
3. Advantages
Avoids 1st pass metabolism
Avoids acid/Enzyme metabolism
Permeation is faster with respect to Skin & TDDS (4-
4000)
Large surface area with respect to sub-lingual mucosa
Good patient compliance with respect to parental
Easy administration & removal in case of toxicity.
For unconscious or comatose patients
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 3
4. Disadvantages
Drugs with bitter taste or irritant to mucosa or having
noxious smell
Not for children
Eating & drinking difficulty
Salivary erosion & it may enter GIT & choke esophagus
Less surface area than skin
Drugs unstable at Buccal pH(6.5 to 7)
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 4
6. Buccal Environment
It has four parts & is 500-800um thick & 150Cm^2
approx
Epithelium: 40-50 cell thick & is major barrier for
lipophilic drug. It has initially square shaped cells which
further grows in the elliptical cells which are permeable
for hydrophilic drugs. It may be Keratinized (having High
MW) or non-keratinized (Low MW).
Mostly, non-keratinized epithelium is permeable to drug
very easily due to absence of acylceramides & only
small amounts of ceramides. Also they contain small
amounts of neutral but polar lipids (Cholesterol
Sulfate& Glucosyl ceramides). Hence more permeable
to formulation
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 6
7. Cont…
Lamina propria: Barrier for hydrophilic drug
Hence highly hydrophilic & highly lipophilic drug
are not suitable for BDDS.
Salivary Secretions: It is secreted by Parotid,
Sub-maxillary & Sub-lingual glands
1% Solute
{Na, K, Ca, Mg,
99 % Aq liquid Mucin, Albumin,
Enzymes(Amylas
e, lipase) }
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 7
8. Mucin Biochemistry
The pH of saliva is due to Mucin (6.2-7.4).
Mucins are synthesized by the goblet cells and
special exocrine glands & secreted by sialic cells
& Mucus cells
It is gylcorylated glycoprotein having large peptide
backbone & oligosaccharides side chains & 14
side chains made up of oligosaccharide.
End part of side chains has negative charge due
to sialic acid, sulphonic grp & fructoic grp which
attract cationic polymers.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 8
9. Factors affecting…
FACTORS…
Polymer related factors MW of polymer
Flexibility
H-bond capacity
Cross-linking density
Charge
Concentration
Drug related factors Mw of Drug,
Lipophilicity
Patient Related factors Salivary secretion rate
pH of Buccal Cavity
Eating/Drinking habit
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 9
10. POLYMER RELATED FACTORS
MW of polymer MW increases, chain & ultimately
adhesion increases Eg PEG4000
Flexibility Should be high
H-bond Capacity HPMC, Carbopol, PVA, PMA
Cross-linking density Should be low as possible
Charge Charged molecule will be highly
adhere
Concentration 0.5-2 % optimum, because it will
directly increase the cross linking &
hence binding decreases
DRUG RELATED FACTORS
MW of Drug Mw of drug increases, the Absorption
decreases
Lipophilicity Should be high
PATIENT RELATED FACTORS
Salivary secretion rate
pH of Buccal Cavity
Eating/Drinking habit
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 10
11. Mechanism of Adhesion
The term bioadhesion is commonly defined as adhesion
between two materials where at least one of the
material is of biological origin.
When adhesion is restricted to mucus layer lining of the
mucosal surface, then it is known as Mucoadhesion.
Generally such adhesion occurs in four different steps…
Wetting & Swelling
Interpenetration of polymer chains in mucin chains
Formation of chemical bonds between Entangled
chains
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 11
12. 1. Wetting and swelling of polymer to permit
intimate contact with biological tissue.
2. Inter-penetration of bioadhesive polymer(BP)
chains and entanglement of polymer and
mucin chains.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 12
15. 3. Formation of chemical bonds between Entangled
chains.
Chemical bonds may be primary(covalent) or
secondary(ionic, van dervaals, H-bonds)
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 15
16. Theories of Adhesion
Adsorption theory: Polymer/groups form covalent/non-covalent
bonds which will bind very strongly (also H-bonds,
vanderwaal’s bonds).
Wetting theory: Polymer with positive spreading co-efficient will
have good binding.
Diffusion theory: Permeability is good in mucin due to chain
flexibility.
Fracture Theory: Irregular surface of polymer & mucin give
good physical entanglement.
Electronic theory: Electric bilayer between polymer & mucin is
responsible.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 16
17. Formulation of BDDS
• • Gels • Sprays
Semi-Solid Dasage forms
Liquid Dosage forms
Solid Dosage forms
Tablets
• Patches/films • Ointments
• Wafers
• Lozenges
• Powders
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 17
18. Basic Formulation components
Muco-adhesive Polymers Permeation enhancers
Preferred Drug
Candidate
Diluents Plasticizer
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 18
19. Selection of DRUG for BDDS
I. MW should be less than 1000da
II. It should be having both nature i.e. hydro-lipophilic type
III. Should be potent {low dose so that formulation is not
bulky}
IV. Non-irritant to mucosa
V. Drugs that degrades in GIT.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 19
20. List of API’s delivered via Buccal
route API
Acyclovir Metronidazole
Buprenorpine Metoprolol tartrate
Carbamazepine Morphine sulphate
Chlorpheniramine maleate Nifedipine
Danazol Omeprazole
Diclofenac sodium Pentazocine
Diltiazem Pindolol
Flurbiprofen Piroxicam
Hydrocortisone acetate Rh EFG
Insulin Testosterone
Lignocaine Terbutaline sulphate
LHRH Theophyline
Zinc sulphate Triamcinolone acetate
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 20
21. Mucoadhesive Polymers
These are the main component for adhesion.
They attract water from the biological surrounding, get
swells & adhere to the membrane.
Normally they should be having hydrophilicity, numerous
H-bonding groups, flexibility, interpenetration with
mucus & tissues
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 21
22. Ideal features…
Non-toxic, non-irritant & pure.
Good spreadibility, wetting, swelling, solubility &
biodegradable if possible.
Adhesion should be quick & with sufficient mechanical
strength.
Should have peel,tensile,shear strength.
Should easily incorporate drug in formulation & it should
not be obstacle in drug release.
Cost effective.
Department of Pharmaceutical Technology,
4/10/2013 LJ Institute of Pharmacy, Ahmedabad 22
23. Examples
Hydrogels:
Polyacrylates, carbopol, polycarbophils
PVA, Ethylene Vinyl alcohol, cellulose derivatives,
alginates
Thiolated Polymers
Hydrophilic macromolecules exhibiting free thiol groups
on the polymeric backbone.
Eg: Thiomers of chitosan and polyacrylic acid etc
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24. Permeation Enhancers
Permeation is very limiting factor in BDDS.
Substances that facilates permeation through Buccal
mucosa are called PE.
Epithelium & Lamina Propria are very effective barrier to
absorption.
They should be used with very care & in optimum
concentration(<1%), above this concentration toxicity
due to membrane damage may occur &
histopathological study should be done.
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25. Mechanisms of PE’s
Increasing fluidity & integrity of cell membrane.
Extracting inter/intra cellular lipids.
Altering cellular proteins.
Altering mucus rheology.
Acting at the tight junctions.
Increasing thermodynamic activity of drugs.
Surface tension decreasing.
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27. Important formulation
Tablets
Is small, flat, generally oval shape with 5-8mm diameter.
It is directly placed onto mucosal surface & adheres to
it.
DC/WG may be used to formulate.
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28. We can get
Unidirectional Release
Multidirectional release (as with conventional product)
Generally for unidirectional release, a backing
membrane is applied, which is impermeable to liquid,
to one side so that no drug release is observed form
that side & non-coated surface adheres to the Buccal
mucosa. Ethyl Cellulose is used as backing
membrane.
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29. Different marketed Buccal tablets…
Prochlorperazine maleate tab (BuccastemR M)
Glycerl trinitrite Buccal tab (Suscord)
Fentanyl Buccal tab (Fentora)
Miconazole Buccal tab (Oravig)
Testosterone (Striant) patented product
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31. Buccal Patches/films
They are long, flat, thin thickness, transparent with high
surface area.
They can be prepared by two methods
Solvent casting method
Direct milling method
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32. Solvent Casting Method
Here drug & all excipients are weighed and dispersed in
the suitable organic solvent & coated on the release
liner.
The organic solvent is allowed to evaporate & after
evaporation the thin layer of the backing material is
laminated on to the sheet of coated release liner to form
laminate.
After that the whole patch is ready to cut into required
size (almost 2*2 cm2 )
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33. Direct Milling Method
Here, drug & excipients are mixed mechanically
by milling or kneading.
After mixing the resultant material is rolled on
the release liner till desired thickness is
achieved.
Finally as the previous method, backing
material is laminated.
Though there is no difference in the patch
performance manufactured by either of the
method but with the SOLVENT method there
are chance of residual solvent.
Hence this Solvent free method is highly used
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34. What does backing layer does…
Control the direction of drug release
Also prevent drug losses
Minimize deformation during handling &
transportation
Reduces the disintegration of device during the
application
Examples
Nitroglycerin patches
Fentanyl patches (Onsolis)
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35. Evaluating the BDDS
Dosage forms Tablets Patches Semi-solids Sprays
In-vitro test
Weight Variation Y Y
Assay Y Y Y Y
Thickness Y Y
Friability Y
Disintegration time Y Y
Residence time Y Y Y
Tensile strength Y
Folding endurance Y
Viscosity Y
Droplets size Y
Dissolution Y Y Y
Mucoadhesion Y Y Y
Strength
Permeability test Y Y Y
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36. Some important in-vitro test
Disintegration time:
Slide frame method: film on slide + drop of water in it.
Note the time when hole is observed in the film.
Petri dish method: film in Petri plate + 2 ml of water in it.
Check time till film dissolves.
Residence time:
Take a slide, stick a mucosa on it with gum. Place
our dosage form on it with few droplets of PBS 6.8,
allow it to stick on it. Now make it inclined at 30 C
& at constant rate add PBS 6.8 drop wise on it
without moving the slide. Note the time till dosage
form detaches from mucosa.
Permeation Study: Franz diffusion cell
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37. Residence time
Locally modified USP disintegration apparatus
was used. DT media: 800 mL PBS pH 6.8 at 37
°C. The buccal tissue was glued to the surface of a
glass slab, vertically attached to the apparatus.
The buccal tablet was hydrated from one surface
using 0.5 mL of PBS pH 6.8, and then the
hydrated surface was brought into contact with the
mucosal membrane. The glass slab was vertically
fixed to the apparatus and allowed to run in such a
way that the tablet was completely immersed in
the buffer solution at the lowest point and was out
at the highest point. The time necessary for
complete erosion or detachment of the tablet from
the mucosal surface was recorded.
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39. Muco-adhesive strength
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40. Shear Force (for various
polymers)
The shear test measures the
force required to separate two
polymer-coated glass slides
joined by a thin film of natural
or synthetic mucus. The
results of this technique often
correlate well with in vivo test
results.
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41. Muco/bio adhesion test
Modified physical balance. Here lighter pan had replaced
the right pan and the left pan had been replaced by a
glass slide. The height of the total set-up was adjusted to
accommodate a glass container of 6.6 cm height. Buccal
tablet was stacked to the glass slide with the help of the
knob, which was situated at the base of the physical
balance. Five grams weight from the right pan was then
removed. This lowered the glass slide along with the
tablet over the membrane with a weight of 5.0 g. This was
kept undisturbed for 5 min. Then, the weights on the right-
hand side were slowly added in increments of 0.1 g till the
tablet just separated from the membrane surface. By
using this weight calculate the bio-adhesive force using
following equation
Bio adhesive force (N) = weight in grams × G/1000
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42. Modified Balance Method
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43. Block Diagram of Modified
Balance Method
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44. TEXTURE ANALYZER:
Here the force required to remove the formulation from
a model membrane is measured, which can be a disc
composed of mucin , a piece of animal mucous
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45. In-vivo test
Buccal Absorption study: Assay of drug solution,
after mouth gargles.
Perfusion study
Kinetic study
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46. Chien Diffusion Cell
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47. Recent Innovations
Gel Forming Liquids:
This type of a formulation is liquid upon instillation
and undergoes a phase transition to form a
viscoelastic gel in response to stimulus such as
temperature, ionic strength or ph
Carbomers become more viscous upon increased
pH.
Gellan gum and alginate both form gel in response
to increased ionic strength (particularly with Ca+2
ions).
Poloxamers and smart hydrogel®( Advanced
medical solution) gel at approximately body
temperature.
4/10/2013
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LJ Institute of Pharmacy, Ahmedabad 47
48. Slowly disintegrating buccal
mucoadhesive plain tablet (SDBMPT)
• Prepared by incorporating large amount of HPC.
e.g. tablet having 20mg drug, 20mg HPC, 20mg CMC &
60mg lactose – mixed & compressed with a flat faced
die that is 8mm in diameter.
• Limitation:
softens on extended period and
lose its shape which hinders the control of
disintegration over long time periods
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49. BCTS (Buccal Covered Tablet System)
• Sandwiched S-DBMP-T system between two
polyethylene sheets
• Upper sheet contains hole to absorb water and lower
sheet is made of adhesives
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50. OraVescent technology
• System which transports drug through across the mucosal
membrane.
• Based on effervescent technology and administered buccally
or sublingually by Cima labs Inc
• Principle:
pH < pKa of weak base –
ionization and solubilization
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51. Marketed products
Striant®, developed by Columbia Labs, is a testosterone
extended-release buccal tablet that delivers
testosterone systemically for hormone replacement in
hypogonadal men.
Asftach® is a buccal tablet containing triamcinolone
acetonide for treatment of apththous ulcers, and
contains a bioadhesive layer and a dissolvable lactose
nonadhesive backing layer
DentiPatch® has been developed by Noven, which is a
lidocaine extended-release buccal patch that adheres
to the gingival tissue to provide for local analgesia, and
was approved in the United States in May 1996.
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52. Cydot® is an example of a patch technology where the
patch adheres to the buccal mucosa for a period of up
to 24 hours to slowly release melatonin for normalizing
circadian rhythms.
Buccal Methyltestosterone
Brand name-Metandren, Ciba;
Avoids first-pass hepatic metabolism
Prochlorperazine
Brand name -Oreton ,Schering Buccastem,
Alternative to enteral tablet
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57. Administering the drug via membrane located below the
tongue is called Sublingual DDS(SLDDS) generally
called floor of mouth.
The SLDDS is almost similar to the BDDS having some
more advantages than Buccal drug delivery system.
Generally factors affecting the SLDDS are almost similar
to factors related with the BDDS.
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59. SLDDS vs BDDS
SLDDS BDDS
The absorption via sub lingual Here, in BDDS, the thickness of
route is faster than buccal mucosa buccal mucosa is 500um
due to the thickness of the approximately, hence permeation
sublingual mucosa. is slow in compare to sublingual
It is 100-200 µm thick route
Hence, in emergency conditions, like angina pectoris/asthmatic attack,
SLDDS in preferred than BDDS due to faster permeation of drug
Sub lingual mucosa has rapid It has less vascularization than
absorption and has higher blood sublingual mucosa.
levels due to very high
vascularization of the region than
Buccal mucosa
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60. Drug administered
Antianginal like nitrites and nitrates
Anti hypertensive like nifedipine
Analgesics like morphine
Bronchodilators like fenoterol
Certain steroids like estradiol
Peptides like Oxytocin can also be administered
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61. Various formulations
Sublingual tablets
Fast-disintegrating sublingual tablets
Bioadhesive sublingual tablet
Thin film drug delivery
Lipid matrix sublingual tablet
Sublingual immunotherapy
Sublingual vitamin tablet
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62. Evaluating SLDDS
Surface pH of the tablet
Uniformity of weight
Content uniformity
Hardness
Thickness
Diameter
Disintegration time
Wetting time
Friability
Dissolution test
Folding endurance
Bioadhesion strength
Permeation studies
% Elongation
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63. Marketed Products
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64. References
Katsumi Iga, “Modified-Release Drug Delivery Technology”,
Edited by Michael, J Rathbone , Jonathan Hadgraft and
Michael S . Roberts, Informa Healthcare 2002, New York, USA
Jaiswal S B, Brahmankar DM, “Biopharmaceutics &
Pharmacokinetics, A treatise” 2nd edition, Vallabh Prakashan,
New Delhi
Jain N K, “Controlled and Novel Drug Delivery Systems”, 1st edi,
2009 reprint, CBS publishers, New Delhi
Chien Yie W, “Novel Drug Delivery system”, 2nd edition, revised
& Expanded, volume 50, Informa healthcare, New York, USA
K. Patel Nibha1 and SS. Pancholi, “An Overview on: Sublingual
Route for Systemic Drug Delivery”, International Journal of
Research in Pharmaceutical and Biomedical Sciences, Vol. 3
(2) Apr – Jun2012
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65. Neha narang, Jyoti sharma, “Sublingual mucosa as a route
for systemic drug delivery”, International Journal of
Pharmacy and Pharmaceutical Sciences, Vol 3, Supply 2,
2011.
Pharmaquest.weebly.com/uploads/9/9/4/2/9942916/3.subling
ual_dds.pdf/accessed at 24/2/2013
Smart D John, “Drug delivery using buccal-adhesive
systems”, Advanced drug delivery reviews, Elsevier Science
Publishers, Volume 11, Issue 3, September 1993, Pages
253-270
Miller Nazila Salamat miller, Chittchang Montakarn, Johnston
Thomas P, “The use of mucoadhesive polymers in buccal
drug delivery
Advanced Drug Delivery Reviews, Elsevier Science
Publishers, Volume 57, Issue 11, 3 November 2005, Pages
1666-1691”
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66. Questions to CRAACK
GTU…
Discuss the merits and demerits of sublingual
dosage forms. How are they evaluated?
Discuss the in-vitro evaluation models for oral drug
delivery systems.
Explain evaluation methods for mucoadhesive
drug delivery.
Write applications of buccal & sublingual drug
delivery systems.
Explain the structure of buccal mucosa. Give a
brief account of mucoadhesive polymers for
buccal delivery.
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67. Discuss the merits and demerits of mucoadhesive
buccal drug delivery. How one can evaluate
mucoadhesive buccal formulation?
Describe methods to determine muco-adhesion
property of formulations.
Discuss in brief delivery systems for oral mucosa.
What are the objectives of sublingual drug delivery
system? Discuss evaluation parameters of
sublingual drug delivery system.
Enlist various method used for bio adhesive
property measurement. Discuss any one.
Explain significance of sublingual drug delivery
system. How they are evaluated?
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