The document discusses nasal drug delivery systems. It provides an overview of nasal drug delivery, including the advantages such as avoidance of first-pass metabolism and rapid onset of action. It also discusses some limitations, such as rapid removal of drugs from the nasal cavity. The document outlines the formulation development process for nasal delivery systems, including considerations for dosage forms, factors affecting drug absorption, and methods to enhance absorption.
Pulmonary route used to treat different respiratory diseases from last decade.
The inhalation therapies involved the use of leaves from plants, vapours from aromatic plants, balsams, and myhrr.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of drugs directly to their site of action reduces the dose needed to produce a pharmacological effect.
Pulmonary route used to treat different respiratory diseases from last decade.
The inhalation therapies involved the use of leaves from plants, vapours from aromatic plants, balsams, and myhrr.
Pulmonary drug delivery is primarily used to treat conditions of the airways, delivering locally acting drugs directly to their site of action.
Delivery of drugs directly to their site of action reduces the dose needed to produce a pharmacological effect.
Nose to brain a versatile mode of drug delivery systemSagar Savale
The Aim of present review highlights transport of drug in nose to brain via olfactory and trigeminal nerve pathway by passing blood brain barrier (BBB). Nose to brain drug delivery has received a great deal of attention as a non-invasive, convenient and reliable drug delivery system for the systemic and targeted administration of drugs.
Nasal Drug Delivery is Part of the Novel Drug Delivery System(NDDS) for effective drug delivery to the Brain, Lungs, and Local administartion. It has its own challenges and advantages.
Nose to brain a versatile mode of drug delivery systemSagar Savale
The Aim of present review highlights transport of drug in nose to brain via olfactory and trigeminal nerve pathway by passing blood brain barrier (BBB). Nose to brain drug delivery has received a great deal of attention as a non-invasive, convenient and reliable drug delivery system for the systemic and targeted administration of drugs.
Nasal Drug Delivery is Part of the Novel Drug Delivery System(NDDS) for effective drug delivery to the Brain, Lungs, and Local administartion. It has its own challenges and advantages.
THE CURRENT STATUS IN MUCOSAL DRUG DELIVERY SYSTEM (MDDS) AND FUTURE PROSPECT...RAHUL PAL
This systematic review aims to provide a comprehensive overview of the current status of
mucosal drug delivery systems (MDDS) and explore their future prospects in drug delivery.
MDDS have gained significant attention in recent years due to their potential to enhance drug
absorption, improve therapeutic efficacy, and minimize systemic side effects. This review
critically evaluates the existing literature on MDDS, including various mucosal routes such as
oral, nasal, ocular, pulmonary, and vaginal delivery. Additionally, it discusses the challenges
associated with MDDS, such as formulation development, stability, and regulatory
considerations. Furthermore, this review highlights emerging technologies and innovative
strategies that hold promise for the future of MDDS. Overall, this systematic review provides
valuable insights into the current landscape of MDDS and offers recommendations for future
research and development in this field.
ABSTRACT
Objective: The main objective of present investigation is to formulate the controlled release tablet of Lamivudine using 3² factorial design. Lamivudine, a basic molecule and antiretroviral drug belongs to BCS Class III, having low permeability and high solubility. Methods: The controlled release tablets of lamivudine were prepared employing different concentrations of Carboplol974P and Xanthan gum in different combinations as a rate retarding agent by Direct Compression technique using 32 factorial design. The quantity/ concentration of rate retarders, Carboplol974P and Xanthan gum required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution t10%, t50%, t75%,t90% were selected as dependent variables. Results: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, in-vitro drug release. From the results it was concluded that all the formulation were found to be with in the pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%,t90%. Conclusions: According to SUPAC guidelines the formulation (F5) containing combination of 10% Carboplol974P and 10% Xanthan gum, is the most similar formulation (similarity factor f2=85.04 & No significant difference, t= 0.20046) to Innovator product (Lamivir). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of drug release was found to be Case-II transport or typical Zero order release (Non-Fickian, n= 0.915).
Formulary and Insurance Lists of Medicines as a Means of Control of Quality o...QUESTJOURNAL
ABSTRACT: National pharmacological policy should be aimed at substantiated selection and rational use of medicinal drugs in order to ensure affordable, high-quality, efficient and safe pharmacotherapy. Primary openangle glaucoma (POAG) is still among the most common ophthalmic pathologies, characterized by steady increase in incidence. Therefore, the society is facing a challenge of optimizing costs for POAG pharmacotherapy, which should be addressed at the nation level. We have identified antiglaucoma medicines, recommended for inclusion in formulary and insurance lists, namely, Timolol, Latanoprost and Travoprost ophthalmic solutions for monotherapy, and combinations of antiglaucoma mono-drugs such as Arutimol 0.5% and Taflotan, Arutimol 0.5% and Lanotan, Azopt and Taflotan based on the results of complex marketing and pharmacoeconomic studies. The introduction of partial reimbursement of the cost of these medicines for patients with POAG will bring them more opportunities for using highly efficient and safe medicines from S01E Group "Antiglaucoma medicines and miotics" under conditions of limited funding of medical and pharmaceutical industries. Particular attention is drawn to the availability of domestic medicine Lanotan eye drops, 0.05 mg/ml, 2.5 ml number 1 produced by OJSC Farmak (Ukraine) among those recommended for inclusion in FL and IL as both a monotherapy for POAG and a part of treatment regimens that combine several AGMs.
To nurture the future pharmacist with focussed approach for academic excellence and complete overall development - krupanidhi college of pharmacy News letter 2016
visit us - http://www.krupanidhi.edu.in
- 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
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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
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
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.
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
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
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
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
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...
Nasal drugdeliverysystem
1. NASAL
Welcome!
DRUG DELIVERY
SYSTEM
Dr. Basavaraj K. Nanjwade M.Pharm., Ph.D
Associate Professor
[Company Name]
Department of Pharmaceutics
KLE University, Belgaum – 590010
Karnataka, INDIA
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 1
2. CONTENTS
Novel Drug Delivery System
Global trends in drug delivery systems
Nasal Drug Delivery System
Medical aspects
Formulation Development
Applications
Conclusion
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 2
3. NOVEL DRUG DELIVERY
SYSTEM
- an overview
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 3
4. Novel drug delivery is one of
the fastest growing healthcare
sectors, with sales of drugs
incorporating novel drug
delivery systems increasing @
an annual rate of 15%
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 4
5. By 2010, the US drug
delivery market alone will
be worth $30 billion
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 5
6. There are great opportunities for companies
investing in R&D for new, improved drug
delivery system, allowing for improved
therapeutic absorption and efficacy in
patients
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 6
7. Why Novel Drug
Delivery system?
To optimize drug’s therapeutic
effect, convenience and dose
To enhance a product’s life-cycle
To improve `patient compliance
To target drug delivery
To control overall healthcare costs
To facilitate biological drug delivery
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 7
8. The Novel Drug Delivery industry is comprised of
companies seeking to develop
Novel alternatives to existing delivery systems
Eg. implantable pumps
Enhancements to existing systems
Eg. sustained release oral dosage forms to
reduce dosing frequency
Commercially enabling delivery systems that provide
viable alternatives for therapeutics that are not fully
developed and marketed because there are
limited practical means of administration
Eg. polar organics and other poorly absorbed
therapeutics
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 8
9. Novel drug delivery companies have
existed since the late 1960s, when Alza
and Elan pioneered the oral methods of
enhanced drug delivery
The introduction of hypodermic devices
but especially metered dose inhalers &
nasal sprays, promoted the concept and
absolute need for specific drug delivery
systems for specific diseases
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 9
10. Today there are between 300 & 350 companies
worldwide with an interest in drug delivery, operating in a
fierce environment where the number of drug launches
using proven delivery technology is growing
More novel technologies such as pulmonary delivery
of insulin or needle-less human growth hormone
injections are under development and are yet to be
commercialized
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 10
11. Drug Delivery Systems
Inject- Trans- Vaginal/
Oral Mucosal Topical Ocular
able dermal Anal
Needle Nasal Active
Needle-
Buccal Passive
less
Pulmo-
nary
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 11
12. Global drug delivery market by administration mode
Nasal 2%
Ocular 2%
Injectable/ Oral 53%
Implant 3%
Transdermal
8%
Inhalation
32%
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 12
13. AS AL
N ST EM
SY
RY
EL IVE
D
R UG
D
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 13
14. Inhalation/pulmonary drug delivery system includes
² Metered dose inhalers
² Dry powder inhalers
² Inhalation solutions & suspensions (for nebulizers)
² Inhalation nasal sprays
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 14
15. Historically, nasal drug delivery system has
received interest since ancient times
Therapy through intranasal administration has been
an accepted form of treatment in the Ayurvedic
system of Indian medicine
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 15
16. Nasal Drug Delivery System
&
Opportunity
Annual market growth
Development time vis-a-vis new chemical entity
Development cost vis-a-vis new chemical entity
Merits
Limitations
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 16
17. 30%
11%
Annual growth of Annual growth of
locally acting systemically acting
products products
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 17
18. Drug development time
10 – 14 years New Chemical
Entity
2 – 5 years Nasal Drug Delivery
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 18
19. Drug development cost
$300-600 mio New Chemical
Entity
$50 mio
Nasal Drug Delivery
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 19
20. Merits
Avoidance of hepatic first-pass metabolism
Rate of absorption comparable to IV
medication
Rapid onset of pharmacological action
User-friendly, painless, non-invasive,
needle-free administration mode
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 20
21. Merits...
Lower dose & hence lower side effects
Useful for both local & systemic drug delivery
For CNS drugs, better site for rapid onset of
action
Eg. Inhalation anesthesia, Morphine etc.
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 21
22. Limitations
¢ Once administered, rapid removal of the
therapeutic agent from the site of absorption is
difficult
¢ Pathologic conditions such as cold or allergies
may alter significantly the nasal bioavailability
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 22
23. U TE
R O
ts
S AL sp ec
N A la
di ca
e
-m
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 23
24. The respiratory tract, which includes the
nasal mucosa
hypopharynx
large airways &
small airways
provides a relatively large mucosal surface area of
approx. 100 m2 (in normal adult) for drug
absorption
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 24
25. Cross-sectional view
Nasal site of drug spray & absorption
Pathways for nasal absorption
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 25
26. Cross-sectional view
a – nasal vestibule d – middle turbinate
b – palate e – superior turbinate (olfactory mucosa)
c – inferior turbinate f – nasopharynx
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 26
27. Site of drug
spray &
absorption
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 27
28. Pathways for nasal absorption
Absorption through the olfactory neurons
- transneuronal absorption. Olfactory epithelium is
considered as a portal for substances to enter CNS
Absorption through the supporting cells & the
surrounding capillary bed
- venous drainage
Absorption into the cerebrospinal fluid
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 28
29. Transneuronal absorption
Olfactory nerve – 1st cranial sensory nerve
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 29
31. Nasal enzymes
•Cytochrome P 450 dependent onooxygenases, Lactate
dehydrogenase, Oxidoreductase, Hydrolases, Esterase,
lactic dehydogenase, malic enzymes, lysosomal
proteinases, steroid hydroxylases., etc.,
•Cytochrome P450 dependent mono oxygenases has
been reported to catalyse the metabolism of xenobiotics,
nasal decongestants, nocotine, cocaine, phenacetin,
nitrosamine progesterone etc.,
•Insulin zinc free was hydrolysed slowly by leusine
aminopeptidase,
•PG of E series was inactivated 15 hydroxyprostaglandin
dehydrogenase
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 31
32. Nasal enzymes – contd.,
•Progesterone and testosterone were
metabolized by several steroid
hydroxylases in the nasal mucosa of rats
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 32
33. Nasal pH
•Nasal secretion of adult : 5.5-6.5
•Infants and children: 5-6.7
•It becomes alkaline in conditions such as
acute rhinitis, acute sinusitis.
•Lysozyme in the nasal secretion helps as
antibacterial and its activity is diminished in
alkaline pH
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 33
34. of
ss te
la u
c
ic l ro
ut sa
pe na
ra or
e f
Th gs
d ru
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 34
35. Therapeutic class of drugs
1. β2 adrenergic agonists
2. Corticosteroids
3. Antiviral
4. Antibiotics
5. Antifungal
6. More recently, vaccines
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 35
37. Formulation
Development
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 37
38. Formulation Development
Dosage form
Factors affecting drug
absorption
Formulation considerations
Physiological
Pharmaceutical
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 38
39. Dosage forms
Liquid drop
Liquid spray/nebulizers
Aerosol
Suspension spray/nebulizers
Gel
Sustained release
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 39
40. Drug concentration
Factors affecting
Vehicle of drug delivery
drug absorption
Mucosal contact time
Degree of drug’s ionization
pH of the absorption site
Size of the drug molecule
Relative lipid solubility
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 40
41. Physiological effects
- Drug metabolism in the respiratory tract &
reduction of systemic effect
- Protein binding
- Mucociliary transport causing increased or
decreased drug residence time
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 41
42. Physiological effects....
- Local toxic effects of the drug
Eg., edema, cell injury, or altered tissue defenses
- Local or systemic effects of propellants,
preservatives, or carriers
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 42
43. Pharmaceutical
- Physico-chemical properties of a drug candidate
- Methods to enhance drug absorption
- Spray pump devices
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 43
44. 1. Effect of particle size
2. Effect of molecular size
3. Effect of solution pH
4. Effect of drug lipophilicity
5. Effect of drug concentration
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 44
45. 1. Effect of particle size
(aerodynamic size distribution)
- Access to distal airways is a function of particle size
- Large particles (> 7 microns) will be lost in the
gastrointestinal tract
- Small particles (< 3 microns) will be lost in exhaled
breathe
- Intermediate particles (3 to 7 microns) reach the
actual site of action
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 45
46. 2. Effect of molecular size
- Higher the molecular size, lower the nasal absorption
- A good systemic bioavailability can be achieved for
molecules with a molecular weight of up to 1000
Daltons when no absorption enhancer is used
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 46
47. 2. Effect of molecular size.....
- With the assistance of absorption enhancer, a good
bioavailability can be extended to a molecular
weight of at least 6000 Daltons
Absorption enhancers: Polyacrylic acid
Sodium Glycocholate
Sodium Deoxycholate
Polysorbate 80 etc.
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 47
48. 3. Effect of solution pH
- Nasal absorption is pH dependent
- Absorption is higher at a pH lower than the
dissociation constant (pKa) of the molecule
- Absorption is lower as the pH increases beyond
the dissociation constant
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 48
49. 4. Effect of drug lipophilicity
- Polar (water soluble) drugs tend to remain on the
tissues of the upper airway
- Non-polar (lipid soluble) drugs are more likely to
reach distal airways
- Lipid soluble drugs are absorbed more rapidly
than water soluble drugs
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 49
50. 5. Effect of drug concentration
- Absorption depends on the initial concentration of
the drug
- The absorption follows first-order kinetics
03/10/2009 Sinhgad College of Pharmacy, Vadgaon, Pune-411041 50
51. Methods to enhance nasal absorption of drugs
Structural modification
Salt or ester formation
Formulation design
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52. SPRAY PUMP DEVICES
- Unidose
- Bidose
- Multidose
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53. Bidose
Unidose
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55. LEADING PUMP SUPPLIERS
Pfeiffer, Germany
Valois, France
Becton Dickinson, France
Nemo, Spain
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56. Applications
Delivery of non-peptide pharmaceuticals
Delivery of peptide-based pharmaceuticals
Delivery of diagnostic drugs
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57. 1. Delivery of non-peptide pharmaceuticals
Drugs with extensive pre-systemic metabolism, such as
- progesterone
- estradiol
- propranolol
- nitroglycerin
- sodium chromoglyate
can be rapidly absorbed through the nasal mucosa
with a systemic bioavailability of approximately 100%
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58. 2. Delivery of peptide-based pharmaceuticals
Peptides & proteins have a generally low oral
bioavailability because of their physico-chemical
instability and susceptibility to hepato-
gastrointestinal first-pass elimination
Eg. Insulin, Calcitonin, Pituitary hormones etc.
Nasal route is proving to be the best route for such
biotechnological products
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59. 3. Delivery of diagnostic drugs
Diagnostic agents such as
• Phenolsulfonphthalein – kidney function
• Secretin – pancreatic disorders
• Pentagastrin – secretory function of gastric acid
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60. IO N
LU S
O N C
C
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61. Nasal route is a part of drug delivery
strategy that is emerging to be a fastest
growing drug delivery system with an
annual growth of
11% for locally acting drugs
&
30% for systemically acting drugs
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62. Nasal drug delivery offers such benefits as
Rapid onset of action with lower dose &
minimal side effects
Has an advantage of site-specific delivery
with improved therapeutic effects
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63. Attractive for delicate molecules
allowing systemic administration
without significant degradation
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64. Nasal drug delivery system offers
flexibility for multiple formulations
ranging from nasal drop to
suspension spray
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65. Recent activities indicate a bright
prospect for site-specific delivery of
biotechnological products such as
Insulin & other hormones
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66. Cell No: 00919742431000; E-mail: bknanjwade@yahoo.co.in
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