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DESIGN AND DEVELOPMENT OF
ORAL DRUG DELIVERY SYSTEM
PRESENTER : PRABHAKAR MARUTI MADVALI
ROLL NO. PH06
DEPARTMENT : M. PHARMACY PHARMACEUTICS
GUIDE : Mrs. GANGOTRI YADAV
(Assistant Professor)
Shri. D. D. Vispute College of Pharmacy & Research Centre, Navi Mumbai
1
HISTORY
INTRODUCTION
FACTORS AFFECTING
IDEAL PROPERTIES
MECHANISMS
PATENTED FORMULATIONS
MARKETED FORMULATION
FUTURE ASPECTS
CONCLUSION
REFERENCE
CONTENT
2
HISTORY
The use of oral drug delivery systems can be traced back to ancient times, when plant extracts and other
natural substances were ingested to treat various ailments.
The modern era of oral drug delivery systems began in the late 19th and early 20th centuries with the
development of tablets and capsules, In 1884.
Compressed tablets were introduced as a convenient and standardized way to deliver medicine. This was
followed by the invention of gelatin capsules in 1833, which allowed for the administration of powders and
liquids in a more palatable and convenient form.
In the mid-20th century, sustained-release and enteric-coated formulations were developed to provide
prolonged or targeted drug delivery, respectively.
3
INTRODUCTION
Oral medication is the most common form of drug administration because of advantages such as convenience
of drug administration via the oral route, patient preference, cost-effectiveness.
Ease of large-scale manufacturing of oral dosage forms. Around 60% of established small-molecule drug
products available commercially are administered via the oral route.
Current estimates indicate that oral formulations represent about 90% of the global market share of all
pharmaceutical formulations intended for human use.
Around 84% of the best-selling pharmaceutical products are orally administered and are currently valued at
$35 billion, with an annual growth rate of 10%
4
5
oral
Digestive Tract
Solid
Tablet, Capsule, Lozenges,
Chewable Tablet, Powder,
Granules
Liquid
Solution, Suspension,
Emulsion
Buccal, Sublingual
Solid
Oral Disintegrating
Tablet(ODT), Oral Thin
Film(OTF), Sublingual Drug
Liquid
Mouth Wash, Throat Paints,
Gargles, Oral Spray
Respiratory Tract
Solid Dry Powder Inhaler(DPI)
Liquid
Anesthetic Vaporizer,
Nebulizer, Metered-dose
inhaler(MDI)
Gases
Oxygen Mask, Oxygen
Concentrator, Anesthetic
Machine
Oral Drug Delivery System
ADVANTAGES OF
ORAL DRUG
DELIVERY SYSTEM
Duration of
action may
extend into
post treatment
period.
Requires only
minimal
training.
Oral route less
objectionable
than
parenteral.
Drug reactions
are generally
less severe.
Drugs readily
available by
prescription.
Simple and
convenient to
use.
6
ADVANTAGES OF ORAL DRUG DELIVERY SYSTEM
DISADVENTAGES
OF ORAL DRUG
DELIVERY
SYSTEM
Patient
noncompliance.
Slow Absorption
delayed onset of
action Not
suitable for
emergencies
May cause
Nausea and
Vomiting
Not useful in
extremely
apprehensive
patients.
Level of sedation
cannot be
altered.
Erratic
absorption
makes response
unpredictable.
7
DISADVENTAGES OF ORAL DRUG DELIVERY SYSTEM
FACTORS AFFECTING ORAL DRUG DELIVERY SYSTEM
8
FACTORS
AFFECTING
ORAL DRUG
DELIVERY
SYSTEM
Physicoche
mical
properties
of the drug
pH and
digestive
enzymes
Drug-
drug
interactio
ns
Food and
beverage
intake
Dosage
form
Genetic
factors
Patient
complian
ce
Disease
state
IDEAL PROPERTIES OF ORAL DRUG DELIVERY
SYSTEM
9
IDEAL
PROPERTIES
OF ORAL
DRUG
DELIVERY
SYSTEM
Stability
Bioavailability
Permeability
Solubility
Targeting
Controlled
release
Non-toxicity
Ease of
administration
Cost-
effectiveness
The mechanism of oral drug delivery system involves several steps, Including disintegration of
the dosage form, dissolution of the drug in the gastrointestinal (GI) fluids, absorption across the
Gl membrane, and metabolism and elimination of the drug by the body.
Mechanism of oral drugs delivery system
10
Mechanism
of oral drugs
delivery
system
Disintegration
Dissolution
Absorption
Metabolism
and
elimination
Patented formulation of oral drugs delivery system
11
SR.NO Patent No. Contents
1 EP2001450 (2008) Orally disintegrating tablets dissolve very
fast, have optimal mechanical strength and
disintegrate within 60 sec
2 WO2006123364 (2006) Oral drug delivery system is in the form of a
coated tablet which includes after a
predetermined delay the coating is reliably
removed fully or partially from one or more
of the tablet surfaces and controlled drug
release
3 WO2007001448 (2007) Coated controlled release polymer particles
encapsulate the active agent and a
mucoadhesive coating disposed about the
core
4 WO2008075448 (2008) A chitosan coating solution is so safe that it
is capable of oral administration in the fields
of foods and medicine
5 US2008293787 (2008) Solid dispersions of poorly soluble
compounds formed by co-precipitation
resulted in improved stability
There are many marketed formulations of oral drug delivery systems available for various
therapeutic indications. Here are a few examples:
1. Extended-release tablets and capsules: Examples include OxyContin (oxycodone), Ritalin
LA(methylphenidate), and Glucophage XR (metformin).
2. Oral disintegrating tablets: Examples include Zofran ODT(ondansetron) and Claritin
Reditabs (loratadine).
3. Liquids and suspensions: Examples include Amoxicillin Oral Suspension and Dimetapp
Elixir.
4. Chewable tablets: Examples include Tums (calcium carbonate)and Children's Tylenol
Chewable(acetaminophen).
5. Orally disintegrating films: Examples include Suboxone Film(buprenorphine and naloxone)
and Zuplenz (ondansetron)
Marketed formulations of oral drug delivery systems
12
Solid dosage forms
• Capsules:Are a solid dosage form in which the drug is enclosed within a hard or soft gelatin shell
• Example : Feroglobin capsules (iron supplements)
• Lozenges: Are hard, oval, solid dosage forms with a drug contained in a flavored
sugar base. They are dissolved in the mouth and generally have local therapeutic
effects.
• Example: Sore Throat lozenges
• Powders: Are finely ground mixtures of dry drugs and inactive ingredients that can be used
topically or internally
13
Granules:
are larger than powders and are wetted, allowed to dry, and ground into coarse,
irregularly shaped pieces.
E-Z-GAS 11
Liquid dosage forms contain one or more active ingredients in a
liquid vehicle such as:
• Solution
• Suspension
• Emulsion
The drug may be dissolved in the vehicle or suspended as very fine particles. They
are often less stable than medications in solid dosage forms
Liquid dosage forms
14
• Solution:
is homogenous mixture of one or more dissolve medications in a liquid vehicle
• Example: Paracetamol syrup (fevadol)
• Suspension:
is a mixture of undissolved, very fine, solid particles distributed through a liquid.
Example: Amoxicillin suspension.
• Emulsion: Is a type of semi-solid dosage form. It is a mixture of two substances
that are unbendable.
• oil-in-water (O/W) emulsion contains a small amount of oil dispersed in water.
• water-in-oil (W/O) emulsion contains a small amount of water dispersed in oil
Example: castor oil emulsion as laxative
15
Sublingual (under the tongue) and Buccal (between the check and gum) routes of
administration are used when a rapid onset of action is needed. The medication is
absorbed directly by the blood vessels under the tongue or in the lining of the
mouth which provide fast action and Bypasses first-pass effect.
16
Sublingual/ Buccal Drug Delivery System
• Example of sublingual tablet: Nitroglycerine (Anti-AnginaI)
• Example of Buccal tablet : fentanyl buccal tablets (Narcotic)
17
1. Nanotechnology: The use of nanoparticles to deliver drugs orally could enhance drug
bioavailability and efficacy. Nanoparticles can protect drugs from degradation in the
gastrointestinal tract and improve their absorption.
2. Smart drug delivery systems: Smart drug delivery systems are designed to respond to
specific stimuli, such as changes in pH or temperature, to release drugs at the desired
location. These systems could improve drug targeting and reduce side effects.
3. 3D printing: 3D printing technology could revolutionize the manufacture of personalized
oral drug delivery systems. Patients could receive tailored dosages and formulations that are
specific to their individual needs.
4. Biodegradable materials: The use of biodegradable materials in oral drug delivery systems
could reduce environmental impact and improve safety.
5. Microbial-based delivery systems: Microbial-based delivery systems, such as probiotics,
could be used to deliver drugs orally. Probiotics can survive the harsh conditions of the
gastrointestinal tract and could potentially improve drug delivery to the gut microbiome.
Future aspects of oral drug Delivery system
18
CONCLUSION
In conclusion, oral drug delivery systems are an important part of modern medicine, allowing for
safe and effective delivery of drugs to patients.
They have several advantages over other routes of administration, including convenience, ease of
use, and improved patient compliance.
Over the years, there have been several advancements in the field of oral drug delivery systems,
including the development of novel drug formulations and the use of innovative drug delivery
technologies.
These developments could lead to further improvements in drug efficacy, safety, and patient
outcomes.
19
References :
20
1. Rowland, M., Tozer, T. N., Derendorf, H., Hochhaus, G. Chapter 1. Therapeutic
Relevance. Clinical pharmacokinetics and pharmacodynamics: concepts and applications.
4th ed. ed. Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins 2011, 3-15.
2. Grass, G.M.; Robinson, J.R. Mechanisms of sustained-release drug delivery. Nat Rev Drug
Discov.2016;15(9):581-598.
3. Vishwakarma, A.; Sharpe, P.; Shi, S.; Wang, X.-P. Stem Cell Biology and Tissue Engineering
in Dental Sciences; Elsevier Ltd.: London, 2015.
4. Park, K. Controlled Drug Delivery; Acs Professional Reference Boo, 1997.
5. Verma, S.; Verma, S. K. Advancements in Controlled Drug Delivery Systems; IGI Global,
2022.
6. Smith, E. W.; Maibach, H. I. Percutaneous Penetration Enhancers; Crc Press: Boca Raton,
1995.
7. Alexandru Mihai Grumezescu. Nano biomaterials in Drug Delivery; William Andrew, 2016.
8. Sabyasachi Maiti; Kalyan Kumar Sen. Advanced Technology for Delivering Therapeutics;
BoD – Books on Demand, 2017.
9. Kerns, E.; Di, L. Drug-like Properties : Concepts, Structure Design and Methods from ADME
to Toxicity Optimization; Elsevier: Burlington, 2008.
10. Kumar, S.; Priya Ranjan Sahoo; Violet Rajeshwari Macwan; Kaur, J.; Mukesh; Rachana
Sahney. Macrocyclic Receptors for Environmental and Biosensing Applications; CRC Press,
2022.
21

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Oral Drug Delivery System.pptx

  • 1. DESIGN AND DEVELOPMENT OF ORAL DRUG DELIVERY SYSTEM PRESENTER : PRABHAKAR MARUTI MADVALI ROLL NO. PH06 DEPARTMENT : M. PHARMACY PHARMACEUTICS GUIDE : Mrs. GANGOTRI YADAV (Assistant Professor) Shri. D. D. Vispute College of Pharmacy & Research Centre, Navi Mumbai 1
  • 2. HISTORY INTRODUCTION FACTORS AFFECTING IDEAL PROPERTIES MECHANISMS PATENTED FORMULATIONS MARKETED FORMULATION FUTURE ASPECTS CONCLUSION REFERENCE CONTENT 2
  • 3. HISTORY The use of oral drug delivery systems can be traced back to ancient times, when plant extracts and other natural substances were ingested to treat various ailments. The modern era of oral drug delivery systems began in the late 19th and early 20th centuries with the development of tablets and capsules, In 1884. Compressed tablets were introduced as a convenient and standardized way to deliver medicine. This was followed by the invention of gelatin capsules in 1833, which allowed for the administration of powders and liquids in a more palatable and convenient form. In the mid-20th century, sustained-release and enteric-coated formulations were developed to provide prolonged or targeted drug delivery, respectively. 3
  • 4. INTRODUCTION Oral medication is the most common form of drug administration because of advantages such as convenience of drug administration via the oral route, patient preference, cost-effectiveness. Ease of large-scale manufacturing of oral dosage forms. Around 60% of established small-molecule drug products available commercially are administered via the oral route. Current estimates indicate that oral formulations represent about 90% of the global market share of all pharmaceutical formulations intended for human use. Around 84% of the best-selling pharmaceutical products are orally administered and are currently valued at $35 billion, with an annual growth rate of 10% 4
  • 5. 5 oral Digestive Tract Solid Tablet, Capsule, Lozenges, Chewable Tablet, Powder, Granules Liquid Solution, Suspension, Emulsion Buccal, Sublingual Solid Oral Disintegrating Tablet(ODT), Oral Thin Film(OTF), Sublingual Drug Liquid Mouth Wash, Throat Paints, Gargles, Oral Spray Respiratory Tract Solid Dry Powder Inhaler(DPI) Liquid Anesthetic Vaporizer, Nebulizer, Metered-dose inhaler(MDI) Gases Oxygen Mask, Oxygen Concentrator, Anesthetic Machine Oral Drug Delivery System
  • 6. ADVANTAGES OF ORAL DRUG DELIVERY SYSTEM Duration of action may extend into post treatment period. Requires only minimal training. Oral route less objectionable than parenteral. Drug reactions are generally less severe. Drugs readily available by prescription. Simple and convenient to use. 6 ADVANTAGES OF ORAL DRUG DELIVERY SYSTEM
  • 7. DISADVENTAGES OF ORAL DRUG DELIVERY SYSTEM Patient noncompliance. Slow Absorption delayed onset of action Not suitable for emergencies May cause Nausea and Vomiting Not useful in extremely apprehensive patients. Level of sedation cannot be altered. Erratic absorption makes response unpredictable. 7 DISADVENTAGES OF ORAL DRUG DELIVERY SYSTEM
  • 8. FACTORS AFFECTING ORAL DRUG DELIVERY SYSTEM 8 FACTORS AFFECTING ORAL DRUG DELIVERY SYSTEM Physicoche mical properties of the drug pH and digestive enzymes Drug- drug interactio ns Food and beverage intake Dosage form Genetic factors Patient complian ce Disease state
  • 9. IDEAL PROPERTIES OF ORAL DRUG DELIVERY SYSTEM 9 IDEAL PROPERTIES OF ORAL DRUG DELIVERY SYSTEM Stability Bioavailability Permeability Solubility Targeting Controlled release Non-toxicity Ease of administration Cost- effectiveness
  • 10. The mechanism of oral drug delivery system involves several steps, Including disintegration of the dosage form, dissolution of the drug in the gastrointestinal (GI) fluids, absorption across the Gl membrane, and metabolism and elimination of the drug by the body. Mechanism of oral drugs delivery system 10 Mechanism of oral drugs delivery system Disintegration Dissolution Absorption Metabolism and elimination
  • 11. Patented formulation of oral drugs delivery system 11 SR.NO Patent No. Contents 1 EP2001450 (2008) Orally disintegrating tablets dissolve very fast, have optimal mechanical strength and disintegrate within 60 sec 2 WO2006123364 (2006) Oral drug delivery system is in the form of a coated tablet which includes after a predetermined delay the coating is reliably removed fully or partially from one or more of the tablet surfaces and controlled drug release 3 WO2007001448 (2007) Coated controlled release polymer particles encapsulate the active agent and a mucoadhesive coating disposed about the core 4 WO2008075448 (2008) A chitosan coating solution is so safe that it is capable of oral administration in the fields of foods and medicine 5 US2008293787 (2008) Solid dispersions of poorly soluble compounds formed by co-precipitation resulted in improved stability
  • 12. There are many marketed formulations of oral drug delivery systems available for various therapeutic indications. Here are a few examples: 1. Extended-release tablets and capsules: Examples include OxyContin (oxycodone), Ritalin LA(methylphenidate), and Glucophage XR (metformin). 2. Oral disintegrating tablets: Examples include Zofran ODT(ondansetron) and Claritin Reditabs (loratadine). 3. Liquids and suspensions: Examples include Amoxicillin Oral Suspension and Dimetapp Elixir. 4. Chewable tablets: Examples include Tums (calcium carbonate)and Children's Tylenol Chewable(acetaminophen). 5. Orally disintegrating films: Examples include Suboxone Film(buprenorphine and naloxone) and Zuplenz (ondansetron) Marketed formulations of oral drug delivery systems 12
  • 13. Solid dosage forms • Capsules:Are a solid dosage form in which the drug is enclosed within a hard or soft gelatin shell • Example : Feroglobin capsules (iron supplements) • Lozenges: Are hard, oval, solid dosage forms with a drug contained in a flavored sugar base. They are dissolved in the mouth and generally have local therapeutic effects. • Example: Sore Throat lozenges • Powders: Are finely ground mixtures of dry drugs and inactive ingredients that can be used topically or internally 13
  • 14. Granules: are larger than powders and are wetted, allowed to dry, and ground into coarse, irregularly shaped pieces. E-Z-GAS 11 Liquid dosage forms contain one or more active ingredients in a liquid vehicle such as: • Solution • Suspension • Emulsion The drug may be dissolved in the vehicle or suspended as very fine particles. They are often less stable than medications in solid dosage forms Liquid dosage forms 14
  • 15. • Solution: is homogenous mixture of one or more dissolve medications in a liquid vehicle • Example: Paracetamol syrup (fevadol) • Suspension: is a mixture of undissolved, very fine, solid particles distributed through a liquid. Example: Amoxicillin suspension. • Emulsion: Is a type of semi-solid dosage form. It is a mixture of two substances that are unbendable. • oil-in-water (O/W) emulsion contains a small amount of oil dispersed in water. • water-in-oil (W/O) emulsion contains a small amount of water dispersed in oil Example: castor oil emulsion as laxative 15
  • 16. Sublingual (under the tongue) and Buccal (between the check and gum) routes of administration are used when a rapid onset of action is needed. The medication is absorbed directly by the blood vessels under the tongue or in the lining of the mouth which provide fast action and Bypasses first-pass effect. 16 Sublingual/ Buccal Drug Delivery System
  • 17. • Example of sublingual tablet: Nitroglycerine (Anti-AnginaI) • Example of Buccal tablet : fentanyl buccal tablets (Narcotic) 17
  • 18. 1. Nanotechnology: The use of nanoparticles to deliver drugs orally could enhance drug bioavailability and efficacy. Nanoparticles can protect drugs from degradation in the gastrointestinal tract and improve their absorption. 2. Smart drug delivery systems: Smart drug delivery systems are designed to respond to specific stimuli, such as changes in pH or temperature, to release drugs at the desired location. These systems could improve drug targeting and reduce side effects. 3. 3D printing: 3D printing technology could revolutionize the manufacture of personalized oral drug delivery systems. Patients could receive tailored dosages and formulations that are specific to their individual needs. 4. Biodegradable materials: The use of biodegradable materials in oral drug delivery systems could reduce environmental impact and improve safety. 5. Microbial-based delivery systems: Microbial-based delivery systems, such as probiotics, could be used to deliver drugs orally. Probiotics can survive the harsh conditions of the gastrointestinal tract and could potentially improve drug delivery to the gut microbiome. Future aspects of oral drug Delivery system 18
  • 19. CONCLUSION In conclusion, oral drug delivery systems are an important part of modern medicine, allowing for safe and effective delivery of drugs to patients. They have several advantages over other routes of administration, including convenience, ease of use, and improved patient compliance. Over the years, there have been several advancements in the field of oral drug delivery systems, including the development of novel drug formulations and the use of innovative drug delivery technologies. These developments could lead to further improvements in drug efficacy, safety, and patient outcomes. 19
  • 20. References : 20 1. Rowland, M., Tozer, T. N., Derendorf, H., Hochhaus, G. Chapter 1. Therapeutic Relevance. Clinical pharmacokinetics and pharmacodynamics: concepts and applications. 4th ed. ed. Philadelphia: Wolters Kluwer/Lippincott Williams & Wilkins 2011, 3-15. 2. Grass, G.M.; Robinson, J.R. Mechanisms of sustained-release drug delivery. Nat Rev Drug Discov.2016;15(9):581-598. 3. Vishwakarma, A.; Sharpe, P.; Shi, S.; Wang, X.-P. Stem Cell Biology and Tissue Engineering in Dental Sciences; Elsevier Ltd.: London, 2015. 4. Park, K. Controlled Drug Delivery; Acs Professional Reference Boo, 1997. 5. Verma, S.; Verma, S. K. Advancements in Controlled Drug Delivery Systems; IGI Global, 2022. 6. Smith, E. W.; Maibach, H. I. Percutaneous Penetration Enhancers; Crc Press: Boca Raton, 1995. 7. Alexandru Mihai Grumezescu. Nano biomaterials in Drug Delivery; William Andrew, 2016. 8. Sabyasachi Maiti; Kalyan Kumar Sen. Advanced Technology for Delivering Therapeutics; BoD – Books on Demand, 2017. 9. Kerns, E.; Di, L. Drug-like Properties : Concepts, Structure Design and Methods from ADME to Toxicity Optimization; Elsevier: Burlington, 2008. 10. Kumar, S.; Priya Ranjan Sahoo; Violet Rajeshwari Macwan; Kaur, J.; Mukesh; Rachana Sahney. Macrocyclic Receptors for Environmental and Biosensing Applications; CRC Press, 2022.
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