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Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amoebiasis, colonic cancer, local treatment of colonic pathologies, and systemic delivery of protein and peptide drugs, NSAIDs, steroids.
The colon is believed to be a suitable absorption site for peptides and protein drugs for the following reasons; (i) less diversity, and intensity of digestive enzymes, (ii) less proteolytic activity of colon mucosa than that of small intestine.
CRITERIA: Drugs used for local effects in colon against GIT diseases.
Drugs poorly absorbed from upper GIT.
Drugs for colon cancer.
Drugs that degrade in stomach and small intestine.
Drugs that undergo extensive first pass metabolism.
Drugs for targeting.
Targeted drug delivery into the colon is highly desirable for local treatment of a variety of bowel diseases such as ulcerative colitis, Crohn’s disease, amoebiasis, colonic cancer, local treatment of colonic pathologies, and systemic delivery of protein and peptide drugs, NSAIDs, steroids.
The colon is believed to be a suitable absorption site for peptides and protein drugs for the following reasons; (i) less diversity, and intensity of digestive enzymes, (ii) less proteolytic activity of colon mucosa than that of small intestine.
CRITERIA: Drugs used for local effects in colon against GIT diseases.
Drugs poorly absorbed from upper GIT.
Drugs for colon cancer.
Drugs that degrade in stomach and small intestine.
Drugs that undergo extensive first pass metabolism.
Drugs for targeting.
Bioavailability and bioequivalence
Bioavailability-
Whenever a drug is given by oral route it has to go through certain pathway to reach the systemic circulation. Eg. If 100 mg drug is given orally, and if 80 mg is absorbed and 20 mg gets excreted then 80 mg absorbed drug reaches liver through portal system. In liver it gets metabolized, here if 30 mg gets metabolized by the liver 50 mg reaches the systemic circulation in the unchanged from. But Bioavailability is expressed in mg it has to be expressed in fraction. So Bioavailability is basically the fraction of unchanged from of the drug that reaches the systemic circulation following administration by any route.
As the drug given by intravenous route reaches directly into the systemic circulation. So the Bioavailability of drug given i.v is 100 %. % Bioavailability can be calculated as- Area under the curve (AUC oral)/ (AUC i.v) *100.
Bioavailability depends on both the rate and extent of absorption.
Rate of absorption depends on- site of adminstration and the drug formulation.
Extent (amount) of absorption depends on- route of drug administration
Factors affecting absorption and Bioavailability-
Pharmaceutical and pharmacological factors:
Pharmaceutical factors include- particle size, crystal from, salt form, water of hydration, Nature of excipients and adjuvants, degree of ionisation.
Pharmacological factors- gastric emptying & g.i mobility, g.i diseases, food and other substances, first-pass effect, Drug-drug interaction, pharmacogenetics, miscellaneous factors like route of administration, area of absorbing surface, state of circulation at site of absorption.
Various approaches to Targeted Drug Delivery Systems (TDDS) in its formuation and evaluation in a pharmaceutical industry and research is outlined in this presentation.
Colon-specific drug delivery systems (CDDS) are desirable for the treatment of a range of local diseases such as ulcerative colitis, amebiasis ,irritable bowel syndrome, Crohn’s disease, chronic pancreatitis and colon cancer.
Bioavailability and bioequivalence
Bioavailability-
Whenever a drug is given by oral route it has to go through certain pathway to reach the systemic circulation. Eg. If 100 mg drug is given orally, and if 80 mg is absorbed and 20 mg gets excreted then 80 mg absorbed drug reaches liver through portal system. In liver it gets metabolized, here if 30 mg gets metabolized by the liver 50 mg reaches the systemic circulation in the unchanged from. But Bioavailability is expressed in mg it has to be expressed in fraction. So Bioavailability is basically the fraction of unchanged from of the drug that reaches the systemic circulation following administration by any route.
As the drug given by intravenous route reaches directly into the systemic circulation. So the Bioavailability of drug given i.v is 100 %. % Bioavailability can be calculated as- Area under the curve (AUC oral)/ (AUC i.v) *100.
Bioavailability depends on both the rate and extent of absorption.
Rate of absorption depends on- site of adminstration and the drug formulation.
Extent (amount) of absorption depends on- route of drug administration
Factors affecting absorption and Bioavailability-
Pharmaceutical and pharmacological factors:
Pharmaceutical factors include- particle size, crystal from, salt form, water of hydration, Nature of excipients and adjuvants, degree of ionisation.
Pharmacological factors- gastric emptying & g.i mobility, g.i diseases, food and other substances, first-pass effect, Drug-drug interaction, pharmacogenetics, miscellaneous factors like route of administration, area of absorbing surface, state of circulation at site of absorption.
Various approaches to Targeted Drug Delivery Systems (TDDS) in its formuation and evaluation in a pharmaceutical industry and research is outlined in this presentation.
Colon-specific drug delivery systems (CDDS) are desirable for the treatment of a range of local diseases such as ulcerative colitis, amebiasis ,irritable bowel syndrome, Crohn’s disease, chronic pancreatitis and colon cancer.
PHARMACOSOME, METHODS OF PREPARATION OF PHARMACOSOME, APPLICATIONS, ADVANTAGES, DISADAVNTAGES OF PHARMACOSOME, FORMULATION OF PHARMACOSOME, COMPONENTS OF PHARMACOSOME, ACTION OF PHARMACOSOME
Gastroretentive Drug Delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects
GASTRO RETENTIVE DRUG DELIVERY SYSTEM , approaches grdds,
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Patient compliance with medical adviceRavish Yadav
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Infrared spectrum / infrared frequency and hydrocarbonsRavish Yadav
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Narcotic drugs and psychotropic substances act, 1985Ravish Yadav
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Medicinal and toilet preparations (excise duties) act, 1995 and rules, 1956Ravish Yadav
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Anti mycobacterial drugs (tuberculosis drugs)Ravish Yadav
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Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
Role of Ethnopharmacology in drug evaluation,
Reverse Pharmacology.
Instructions for Submissions thorugh G- Classroom.pptxJheel Barad
This presentation provides a briefing on how to upload submissions and documents in Google Classroom. It was prepared as part of an orientation for new Sainik School in-service teacher trainees. As a training officer, my goal is to ensure that you are comfortable and proficient with this essential tool for managing assignments and fostering student engagement.
Model Attribute Check Company Auto PropertyCeline George
In Odoo, the multi-company feature allows you to manage multiple companies within a single Odoo database instance. Each company can have its own configurations while still sharing common resources such as products, customers, and suppliers.
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
2024.06.01 Introducing a competency framework for languag learning materials ...Sandy Millin
http://sandymillin.wordpress.com/iateflwebinar2024
Published classroom materials form the basis of syllabuses, drive teacher professional development, and have a potentially huge influence on learners, teachers and education systems. All teachers also create their own materials, whether a few sentences on a blackboard, a highly-structured fully-realised online course, or anything in between. Despite this, the knowledge and skills needed to create effective language learning materials are rarely part of teacher training, and are mostly learnt by trial and error.
Knowledge and skills frameworks, generally called competency frameworks, for ELT teachers, trainers and managers have existed for a few years now. However, until I created one for my MA dissertation, there wasn’t one drawing together what we need to know and do to be able to effectively produce language learning materials.
This webinar will introduce you to my framework, highlighting the key competencies I identified from my research. It will also show how anybody involved in language teaching (any language, not just English!), teacher training, managing schools or developing language learning materials can benefit from using the framework.
How to Create Map Views in the Odoo 17 ERPCeline George
The map views are useful for providing a geographical representation of data. They allow users to visualize and analyze the data in a more intuitive manner.
How to Make a Field invisible in Odoo 17Celine George
It is possible to hide or invisible some fields in odoo. Commonly using “invisible” attribute in the field definition to invisible the fields. This slide will show how to make a field invisible in odoo 17.
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
The Art Pastor's Guide to Sabbath | Steve ThomasonSteve Thomason
What is the purpose of the Sabbath Law in the Torah. It is interesting to compare how the context of the law shifts from Exodus to Deuteronomy. Who gets to rest, and why?
Welcome to TechSoup New Member Orientation and Q&A (May 2024).pdfTechSoup
In this webinar you will learn how your organization can access TechSoup's wide variety of product discount and donation programs. From hardware to software, we'll give you a tour of the tools available to help your nonprofit with productivity, collaboration, financial management, donor tracking, security, and more.
We all have good and bad thoughts from time to time and situation to situation. We are bombarded daily with spiraling thoughts(both negative and positive) creating all-consuming feel , making us difficult to manage with associated suffering. Good thoughts are like our Mob Signal (Positive thought) amidst noise(negative thought) in the atmosphere. Negative thoughts like noise outweigh positive thoughts. These thoughts often create unwanted confusion, trouble, stress and frustration in our mind as well as chaos in our physical world. Negative thoughts are also known as “distorted thinking”.
3. Application
In local colonic pathologies
Systemic delivery of protein and peptide
Potential site for the treatment of diseases
liike asthma,arthritis & angina
For the drugs that are absorbed through
colon such as steroids
For the treatment of disorders like IBS,
colitis,crohn’s disease where it is necessary
to attain high concentration of drugs in colon
3
4. Limitation and Challenges
Dissolution in luminal fluid.
Stability of drugs.
Binding of drugs to dietary residues, intestinal
secretions, mucus or fecal matter.
Metabolic degradation by colonic microflora.
Wide range of pH values
4
5. Lower surface area and relative “tightness” of the
tight junctions in the colon restrict drug transport.
Longer residence time
Requires protection against variety of the gastric
enzymes.
Cytochrome P450 3A class of drug metabolizing
enzymes have lower activity in colon
5
6. Target sites Disease
conditions
Drugs used
Topical/local
action
Inflammatory
bowel disease,
Irritable bowel
syndrome
&crohn’disease
Hydrocortisone,
Budenoside,
Prednisolone,
Sulphasalazine,
Olsalazine,
Infliximab
Mesalazine,
Balsalazide, 6-
Mercaptopurine,
Azathiorprine,
Cyclosporine,etc
Introduction to colonic
drug delivery system
6
10. A. Gastric emptying
Fasted state 10 min. to 2 hrs
Fed state Higher than 2 hrs
Small intestinal transit 3-4 hours
Colonic transit 20-35 hours
10
11. DISEASE EFFECT ON COLONIC
ABSORPTION OF DRUGS
IBD (Crohn’s
disease &
Ulcerative
colitis)
Malabsorption lipophilic drugs
Mucosa & submucosa gets thick & so
reduces surface area, reduces
diffusion
Diarrhoea Retention time reduces.
Reduces drug absorption & release
from dosage form
B.Gastrointestinal disease state
11
12. Constipation Reduction in bowel movement &
decreases the avaibility of drug
at absorption site
Gastroenteritis Diarrhoea affects the
performance of formulations
12
13. 13
Stomach
Fasted state
Fed state
1.5 – 2
2 - 6
Small intestine 6.6 – 7.5
Ascending colon
Transverse colon
Descending colon
6.4
6.6
7.0
c.Gastric and intestinal pH
15. Approaches
1. Prodrug
2. Osmotically controlled drug delivery
3. Redox-sensitive polymers
4. pH dependent system
5. Time dependent system
6. Microflora activated system
7. Pressure controlled system
8. Bioadhesive systems
9. Micro particulate system
15
16. A. PRODRUG APPROACH (Drug is conjugated with
carrier)
I. Azo conjugate
eg. Sulphasalazine for 5-ASA
Drug is conjugated with an azo bond.
II. Glycoside conjugate
eg. Dexamithasone
Drug is conjugated with glycoside
III. Glucuronide conjugate Drug is conjugated with Glucuronide
IV. Cyclodextrin
conjugate(βCD)
Drug is conjugated with cyclodextrin
V. Dextran conjugate
eg. Naproxen-dextran
conjugation
Drug is conjugated with dextran
1. Prodrug approach
16
17. VI. Polymeric conjugate Drug is conjugated with polymer
VII. Amino acid conjugate
eg. Proteins.
Drug is conjugated with aminoacid
17
18. 1)Azo bond conjugate:-
Azoreductase enzyme produced in colon by
colonic bacteria which degrades azo bond.
This principle is utilized in preparation of
prodrug derivative of active drug for targeting in colon.
18
19. Sulphasalazine(SASP) is prodrug of 5-ASA. It is
conjugated with sulphapyridine through azo bond.
Sulphasalazine was introduced for the treatment
of rheumatoid arthritis and anti-inflammatory
disease.
19
20. Carrier moiety conjugated with
5-amino salicylic acid
Prodrug of 5-amino
salicylic acid
p-aminohippurate (4-amino
benzoyl glycine)
ipsalazine,
p- 4-amino benzoyl-β-alanine balsalazine
p-aminobenzoate HB-313
nonabsorbable sulphanilamide
ethylene polymer
poly-ASA
a dimer representing two
molecules of 5-ASA that are
linked via an azo bond
olsalazine (OSZ)
20
22. 2)Glycoside conjugation:-
Certain drugs can be conjugated to different
sugar moieties to form glycosides
Glycosides are bulky and hydrophilic
They do not penetrate the biological
membranes upon ingestion
They are poorly absorbed from the small
intestine
When it reaches the colon, it will be cleaved by
colonic bacterial glycosidase
22
24. 3)Glucuronide conjugations:-
• Same as that of glycoside conjugation.
•Here, glucuronide moiety is joined
•Example: Dexamethasone is tried for conjugation
and the results were evaluated in ulcerative colitis
induced in the rates.
Dexamethasone- b -D-glucuronide.
24
25. 4)Cyclodextrin conjugate:-
• Cyclodextrin metabolizing enzymes produced by
colonic bacteria degrades Cyclodextrin particularly β-
CD. This principle can be used for preparation of
prodrug with CD.
• The β-CD is practically resistant to gastric acid and
salivary and pancreatic amylases. But they are complete
degraded by the colonic microflora.
5)Dextran conjugate:-
NASIDS ware directly coupled to dextran by using
carboxylic groups of drugs
25
26. 6)Amino acid conjugation:-
In the amino acid, acid group
• increase hydrophilicity and chain length of carrier
amino acid,
•decrease the permeability of amino acids and proteins.
So the amino acid conjugate showed more enzymatic
specificity for hydrolysis by colonic enzyme.
Glycine and glutamic acid conjugates of salicylic acid.
26
27. 2)Osmotic controlled drug delivery
OROS-CT (Alza corporation)
Immediately after the OROS-CT is swallowed, the
gelatin capsule containing the push-pull units dissolve
Because of its enteric coating, each push-pull unit is
prevented from absorbing water in the acidic environment.
As the unit enter the small intestine, the coating
dissolve in this higher pH (pH >7), water enters the unit,
causing the osmotic push compartment to swell and
concomitantly creates a flowable gel in the drug
compartment.
Swelling of the osmotic push layer forces drug gel out
of the orifice.
27
29. 3)Redox-sensitive polymers
Novel polymers that are hydrolysed nonenzymatically by
enzymatically generated FLAVIN
For azo bond cleavage,mainly 2 approches
1. Intracellular enzymatic compartment,
2. Extracellular reduction by flavin.
Under anaerobic conditions, bacterial azo reduction by
enzymatically generated reduced flavins requires the
presence of NADPH as its electron source.
As NADPH oxidized, the electron mediator (reduced
flavins) acts as an electron shuttle from the NADPH
dependent flavoprotein to the azo compound.
29
35. 5.Time dependent
delivery
• Difficult to predict in advance.
• The strategy is to resist the drug release
in acidic & intestinal environment
• In this approch, specific lag time is
previously determined.
35
36. Pulsincap
• It consists of enteric coated capsule containing
water soluble cap and water insoluble body.
• The body is loaded with Hydrogel plug and drug
layer.
• Enteric coat dissolves in small intestine and the
water soluble cap also dissolves.
• The Hydrogel plug absorbs water and swell and
release drug at a predetermined lag time of 4
hours.
36
38. Time clock
The Time Clock system consists of a solid dosage
form coated with lipidic barriers containing
carnuba wax and bee’s wax along with surfactants,
such as polyoxyethylene sorbitan mono oleate.
This coat erodes or emulsifies in the aqueous
environment in a time proportional to the thickness
of the film, and the core is then available for
dispersion.
38
39. Technique
employed
Polymer used Drug used
Bacteria
dependent/Polysacchari
de based
Chitosan Diclofenac
Sodium
Pectin
Chondroitin salphate
Guar gum
Indomethacin
Indomethacin
Doxamithacin
Amylose
Alginate
5 – ASA
5 – ASA
6. Bacterial based approach
39
40. Microbial
flora
Enzymes
produced
Chiefly applied for:
Majority of
them
Azoreductase Release of 5- ASA from
variety of prodrugs
Lactobacilli Glycosidase,
Glucuronidase
Glycosides &
glucuronides
Bacteroides Glycosidase,
Glucuronidase
Glycosides &
glucuronides
40
41. 7. Pressure-controlled
drug-delivery systems
Muscular contraction of the gut wall generate
pressure
Colon has higher luminal pressure
System can be developed which withstand the
pressure in intestine and ruptures in response
to raised pressure in colon.
Ethyl cellulose capsules have been used for
this purpose.
41
42. 8. Bioadhesive systems:-
Oral administration of some drugs requires high
local concentration in the large intestine for
optimum therapeutic effects.
Bioadhesion is a process by which a dosage
form remains in contact with particular organ for an
augmented period of time.
This longer residence time of drug would
have high local concentration or improved absorption
Various polymers including polycarbophils,
polyurethanes and polyethylene oxide-polypropyline
oxide copolymers have been investigated for colon.
42
46. Evaluation
1. In vitro dissolution study
2. In vitro enzymatic degradation test
3. Relative colonic tissue exposure
4. Relative systemic exposure to drugs
5. -Scintigraphy
6. Magnetic moment imaging study
7. Drug delivery index
8. High frequency capsule
46
47. • Invitro test for intactness of coatings and
carriers in simulated conditions of stomach and
intestine
• Drug release study in 0.1 N HCl for 2 hours (mean
gastric emptying time)
• Drug release study in phosphate buffer for 3
hours (mean small intestine transit time PH 6.8)
47
48. Method 1
• Drug release in buffer medium containing enzymes
(e.g. pectinase, dextranase) or cecal contents
of rat or guinea pig or rabbit
Method 2
• Suitable medium containing colonic bacteria
(Streptococcus faecium or B. ovatus)
48
49. BioDis-III (Apparatus III)
• Ideal for the dissolution profiling of extended
release dosage forms.
• It is designed to meet or exceed current USP
specification.
• It used a reciprocating motion to dip the inner
tube into media.
• At the designated time, the entire row of inner
tubes raises and moves to the next row of
media.
49
50. Bio-Dis III
• Capable of running unattended upto 6 days and can
store upto 25 programms.
• 7 sample tubes which automatically traverse upto
6 rows of corresponding outer tubes filled with
different media.
• With accessories, the appropriate media volume
can vary from 100, 300 ml (USP) or 1000 ml.
50