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PH 1.3 Drug formulations & drug delivery systems_1.1 - Copy.pptx
1. Drug: Dosage Forms,
Formulations & Delivery
Systems
Dr. Vikram Sharma, MD
Senior Resident
Department of Pharmacology
ESIC Medical College & Hospital
Faridabad
2. âĸ Difference between
dosage form &
formulation
âĸ Various Dosage forms
âĸ What are various drug
delivery system â
3. ī§ Dosage form:
o Product suited for administration to patient by various routes for
diagnosis or treatment
o They provide accurate dosage of drugs for treatment of disease
o Eg: Tablet, Capsule etc
ī§ Formulations:
o Consist of name of drug, strength & its dosage form.
o Eg: PCM 500 mg as tablet; Amphotericin B 50mg/vial injection;
Baclofen 5mg/5ml syrup
o Essential Drug List includes formulations
Srivastava SK, Srivastava Rohan. Manual of practical pharmacology for MBBS, First Edition 2021.
4. īą Dosage form
ī Means (or the form) by which drug molecules are delivered to sites of
action within the body.
īą Drug (Active pharmaceutical ingredients )
ī Chemical compound intended for used in diagnosis, treatment
prevention, of disease.
ī Active Pharmaceutical Ingredient (API) is the part of any drug that
produces its therapeutic effect.
īą Excipients
ī Donât increase or affect the therapeutic action of the active ingredient
ī Inactive ingredients may also be referred to as inert ingredients or
excipients, and generally have no pharmacological effect.
ī Examples of inactive ingredients include binding materials, dyes,
preservatives, & flavoring agents,sweetening agents,coloring agents etc.
5. âĸDosage form= Drug (API) + Excipients
âĸFormulation = Dosage form (Drug + Excipients) + Drug
strength
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/
6. ī§ API handling andAccurate dosing can be difficult or
impossible (e.g., potent drugs: low mg and Âĩg doses).
ī§ API administration can be impractical/unfeasible because of
size, shape, smell/odour, taste and low activity.
ī§ SomeAPI are chemically unstable in light, moisture, O2
ī§ API can be degraded at the site of administration (e.g., low pH
in stomach).
ī§ API may cause local irritations or injury when they are present
at high concentrations at the site of administration.
ī§ Administration of active substance would mean to have no
chance for modification (improvement) of its PK profile.
7. o Accurate dose
o Protection e.g. coated tablets, sealed ampules
o Protection from gastric juice
o Masking taste and odour
o Placement of drugs within body tissues
o Sustained release medication
o Controlled release medication
o Optimal drug action
o Insertion of drugs into body cavities (rectal,
vaginal)
o Use of desired vehicle for insoluble drugs
11. ī§ Vary in size, shape, hardness, thickness, weight,
disintegration,dissolution characterisitics and in other aspect.
12. ī§ These are small, rounded solid dosage forms containing
medicaments intended for oral use.
ī§ The medicaments are mixed with excipients to forms a firms
plastic mass.
ī§ The mass is rolled to uniform pill pipe, which cut into numbers
of uniform pills. The pills are spherical in shape & produced
by rolling them under wooden pill rounder.
13. ī§ Solid preparation consisting of sugar
and gum & are intended to dissolve
or disintegrate slowly in the mouth.
ī§ Used to medicate the mouth and
throat for the slow administration of
indigestion or cough remedies.
14. ī§ Solid medicated preparations
designed to dissolve slowly
in the mouth.
ī§ Softer than lozenges & their
bases are either glycerol and
gelatin, or acacia and sugar.
15. ī§ Powders are solid dosage form of medicaments which are
meant for internal or external use.
ī§ They are available in amorphous & crystalline forms.
ī§ TYPES OF POWDERS
1. Bulk Powders for internal use e.g. fine powders or granules
2. Bulk Powders for external use e.g. snuff, dusting powders, tooth powder
3. Simple and compound powder for internal use
4.Powders in the form of compressed tablets and tablet triturates
5.Powders enclosed in cachets and capsules
16. ī§ These are meant for external application to the skin & are
generally in a very fine state of subdivision to avoid local
irritation.
ī§ These are mainly used for their antiseptic, astringent,
absorbent, antiperspirant and antipruritic action.
17. ī§ These are medicated dusting powders
meant for introduction into body cavities
(nose, throat, ear, vagina etc) with the
help of an apparatus known as a
insufflator.
ī§ It sprays the powders (in a state of fine
particles) on site of application.
18. finely divided solid
ī§ These are
dosage forms of medicaments
which are inhaled into nostrils.
mainly
ī§ They are
antiseptic, bronchodilator
used for their
and
decongestion action.
19. ī§ It may be defined as âA solution is a liquid-preparation that contains one or
more soluble chemical substances dissolved in a specified solventâ
ī§ Liquid dosage forms are intended for External, Internal or parenteral use.
ī§ They mainly classified into two category namely as â
I) Internal Liquid Preparations.
A) Monophasic liquid preparations
B) Biphasic liquid preparations
II) External Liquid Preparations
A) Applied on the skin
B) Instilled into body cavities
C) Used in mouth
20. ī Immediately available for absorption.
ī Administration convenient, particularly for infants, psychotic
patients.
ī Easy to color, flavor & sweeten.
ī Liquids are easier to swallow than solids and are therefore
particularly acceptable for pediatric patient.
ī A solution is an homogeneous system and therefore the drug
will be uniformly distributed throughout the preparation.
ī Some drugs like aspirin, KCl can irritate gastric mucosa if
used orally as a solid dosage forms. But this effect can be
reduce by solution system.
21. ī Less stable in aqueous system. Incompatibility is faster
in solution than solid dosage form.
ī Patients have no accurate measuring device
ī Accident breakage of container results in complete loss
ī Solution often provide suitable media for the growth of micro-
organisms
ī The taste of a drug, which is often unpleasant, is always
more pronounced when in solution than in a solid form
ī Bulky than tablets or capsule, so difficult to carry transport
22. âĸ It contain only one phase.
âĸ It is represented by true solution.
âĸ Atrue solution is a clear homogenous mixture that is prepared
by dissolving solute in a suitable solvent.
âĸ Monophasic liquid dosage forms are â a)Syrup b)Elixirs
c)Solutions d) Linctuses
23. ī§ It is a concentrated or saturated solutions of sucrose in purified
water.
ī§ The concentration of sucrose is 66.7% w/w & due to that it is a
viscous preparations.
ī§ The syrup which contains medical substance called as a
medicated syrup & those containing aromatic or flavored
substance known as a flavored syrup.
24. ī§ It is clear, sweetened, aromatic,
hydroalcholic preparations meant for
oral use.
ī§ Medicated elixirs are generally
contained potent drug like as
antibiotics, antihistamine or sedative ,
where as nonâmedicated elixirs
contained flavored.
ī§ The composition of elixirs contained
mainly as ethyl alcohol (active
ingredients),water, glycerin or
propylene glycol, coloring agent,
flavoring agent & preservative.
25. ī§ These are viscous liquid preparations
thatâs are used for the treatment of
cough.
ī§ They contain one or more
medicaments which have demulcent,
sedative, expectorant action on the
mucus membrane of throat.
ī§ They are taken in small doses without
diluting with water to have prolonged
effect of medicines.
ī§ Simple syrup is used as a vehicle for
most of the linctuses.
26. ī§ The liquid which consist of two phases are known as
a biphasic liquid dosage forms.
ī§ They are sub categorized into two different forms namely as â
I) Emulsion
II) Suspension
ī§ In emulsion both phases are available in liquid where as in
suspension, finely divided solid particles are suspended in
liquid medium.
27. ī§ Emulsion is a biphasic liquid preparations containing two
immiscible liquid (Continuous Phase & dispersed phase) made
miscible.
ī§ The liquid which is converted into minute globules is called as
dispersed phase & the liquid in which the globules are
dispersed is called the continuous phase.
dispersed phase
continuous phase
Two Immiscible Liquids
Dispersed Phase
(Internal phase)
Continuous Phase
(External phase)
28. Simple type
ī Water in oil (w/o)
īOil in water (o/w)
Depending on globule size
ī Micro emulsion
īFine emulsion
Special type
ī Multiple emulsion (w/o/w, o/w/o)
29. ī§ Suspensions are the biphasic liquid dosage forms of medicament in which
finely divided solid particles ranging from 0.5 to 5 micron are dispersed in a
liquid or semisolid vehicle, with aid of single or combination of suspending
agent.
ī§ In which solid particles acts as disperse phase where as liquid vehicle acts as
continuous phase
ī§ The external phase (suspending medium) is generally aqueous in some
instance, may be an organic or oily liquid for non oral use.
ī§ The particle size for non oral suspension is so important to avoid grittiness to
skin.
30. A) Applied on the skin
LOTIONS
ī§ Are usually aqueous, alcoholic or oily
liquid preparations.
ī§ They are intended for external
application without friction or
rubbing to the affected area
ī§ Usually applied with the help of some
absorbent material such as cotton
wool or gauze.
ī§ It is generally used to provide
cooling, soothing and protective &
antiseptic action.
31. ī§ Liniments are liquid or semi- liquid preparations
meant for external application to the skin.
ī§ They are usually applied to the skin with friction
& rubbing of the skin.
ī§ Are usually alcoholic and oily liquid preparations
(monophasic) or emulsion (biphasic).
ī§ Alcoholic liniments are used generally for their
rubefacient and counterirritant effects. Such
liniments penetrate the skin more readily than do
those with an oil base.
ī§ The oily liniments are milder in their action and
may function solely as protective coatings
ī§ Liniments should not be applied to skin that are
bruised or broken.
33. ī§ These are the solutions of drugs that are instilled into
ear cavity with the help of dropper.
ī§ These are generally used for cleaning the ear, softening
the wax & for treating the mild infections.
ī§ The solutions is generally prepared in water,
glycerin,
ī§ propylene glycol & dilute alcohol.
34. ī§ Nasal drops are aqueous or liquid
paraffin solutions meant for instillation
into nostrils.
ī§ Drugs in solution may be instilled into
the nose from a dropper or from a
plastic squeeze bottle.
ī§ The drug may have a local effect, e.g.
antihistamine, decongestant.
ī§ Alternatively the drug may be absorbed
through the nasal mucosa to exert a
systemic effect.
35. âĸ Adouche is a device used to introduce
a stream of water into the body for
medical or hygienic reasons, or the
stream of water itself.
âĸ Douche usually refers to vaginal
irrigation, the rinsing of the vagina, but
it can also refer to the rinsing of any
body cavity.
âĸ Adouche bag is a piece of equipment
for douchingâa bag for holding the
fluid used in douching.
36. Gargles
ī§ Gargles are aqueous solutions used
for treating throat infection by
forcing air from lungs through the
gargle that is held in the throat.
forms
with
ī§ dispensed in concentrated
with directions of dilution
water before use
ī§ They are used into intimate contact
with the mucous membrane of throat
for few seconds, before they are
thrown out of the mouth.
ī§ They are also used for their
antiseptics, antibiotics anesthetics,
astringent,alkalinizing antifungal
action.
37. ī§ These are aqueous solutions with
pleasant or acceptable taste & odour
ī§ These are used to make clean &
deodorise the buccal cavity or used
for oral hygiene and to treat
infections of the mouth.
ī§ They mainly contain antibacterial
agent, alcohol, glycerin, sweetening
agent, flavoring agent & colouring
agent.
38. ī§ Semisolid dosage forms meant for external application
ī§ They contain one or more active ingredients dissolved or
uniformly dispersed in a suitable base and any suitable
excipients such as emulsifiers, viscosity-increasing agents,
antimicrobial agents, antioxidants, or stabilizing agents
ī§ Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories
39. ī§ Ointments are homogeneous semisolid
preparation meant for application to skin or
mucous membrane.
ī§ Mainly used for their protective or emollient
properties
40. ī§ Creams are homogeneous, semi-solid preparations consisting
of opaque emulsion systems.
ī§ Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
ī§ In case of aqueous creams the emulsions are o/w type & it is
relatively non greasy.
ī§ In case of oily creams w/o type & it is relatively greasy
ī§ The cream should be store in collapsible tube & supplied in
well closed container to prevent evaporation & contamination.
41. ī§ Pastes are homogeneous, semi-solid
preparations containing high concentrations
of insoluble powdered substances (usually
not less than 20%) dispersed in a suitable
base.
ī§ Mainly used as antiseptic, protective,
soothing dressings.
ī§ Should be stored & supplied in containers
made of materials which do not allow
absorption or diffusion of content.
42. Gel
ī§ Usually transparent or translucent,non-
greasy semi-solid preparations.
ī§ Applied to the skin or certain mucous
membranes for protective, therapeutic, or
prophylactic purposes.
ī§ Used for lubricating catheters, surgical
gloves & rectal thermometer.
43. ī§ These are hypodermic tablets are placed under the skin by a
minor surgery in order to release drugs over prolonged periods
of time.
ī§ Now the magnetically controlled implants have been
developed.
ī§ These implants are useful in hormone therapy.
44. īļ Meant for topical application for slow release of drug over
predetermined period of time. They are sub categorized in to following
types namely as
īļ Zero order release films
īļ Buccal strips
īļ Spray bandages
45. ī§Method or a process of administering or
delivering a pharmaceutical compound in
systemic circulation to achieve its
therapeutic effect.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3465154/
46. ī§ Many drugs have unacceptable side effects due to the
drug interacting with healthy tissues that are not the
target of the drug.
ī§ Side effects limit ability to design optimal medications
for many diseases such as cancer, neurodegenerative
diseases, and infectious diseases.
https://www.nibib.nih.gov/science-education/science-topics/drug-delivery-systems-getting-drugs-their-targets-controlled-manner
47. System comprises of:
A. Drug formulation
B. Medical device or technology to carry the drug
inside the body
C. Mechanism for release
https://www.nibib.nih.gov/science-education/science-topics/drug-delivery-systems-getting-drugs-their-targets-controlled-manner
48. A. Conventional / Traditional
B. Novel / Targeted
https://www.pharmapproach.com/drug-delivery-systems-an-overview/
49. īŧ Increase the bioavailability of the drug
īŧ Transport the drug intact to the site of action while avoiding the
non-diseased host tissue
īŧ Stable and delivery should be maintained under various
physiological variables
īŧ High degree of drug dispersion
īŧ Applicable to a wide range of drugs
īŧ Easy to administer to the patient
īŧ Safe & reliable
īŧ Cost-effective
https://www.pharmapproach.com/drug-delivery-systems-an-overview/
50. CONVENTIONAL/TRADITIONAL
DRUG DELIVERY SYSTEM
ī§ Classical methods for delivery of a drug into the
body.
ī§ Goal is quickly absorption of a drug; therefore, a
quick release of the drug is required.
ī§ Example:- oral, topical, inhaled, or injection
methods.
https://www.pharmapproach.com/drug-delivery-systems-an-overview/
53. ī§ Defined as self contained, discrete dosage forms which,
when applied to the intact skin, deliver the drug,
through the skin at controlled rate to the systemic
circulation.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
54. īŧ Avoidance of first pass metabolism
īŧ Avoidance of gastro intestinal incompatibility
īŧ Predictable & extended duration of activity
īŧ Improving physiological & pharmacological response
īŧ Termination of therapy is easy at any point of time
īŧ Greater patient compliance due to elimination of
multiple dosing profile
īŧ Provide suitability for self administration
īŧ Enhance therapeutic efficacy
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
55.
56. SONOPHORESIS
ī§Process that exponentially increases the
absorption of topical compounds (transdermal
delivery) into the epidermis, dermis and skin
appendages by ultrasonic energy.
ī§Localized, nonâinvasive, convenient & rapid
method of delivering low molecular weight
drugs as well as macromolecules into the skin.
ī§Ultrasound at various frequencies in the range
of 20 kHzâ16 MHz with intensities of up to
3W/cm2 are being used for sonophoresis.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
57. ī§ Osmotic pressure is used as driving force for these
systems to release the drug in controlled manner .
Classification of Osmotic Drug Delivery System:
They can be divided in oral and implantable systems
Implantable:
âĸThe Rose and Nelson Pump
âĸHiguchi Leeper Pump
âĸHiguchi Theuwes pump
âĸImplantable Miniosmotic
pump
Oral osmotic Pump
âĸSingle chamber osmotic pump
âĸElementary osmotic pump
âĸMulti chamber osmotic pump
âĸPush pull osmotic pump
âĸOsmotic pump with non expanding
second chamber
âĸSpecific types:
âĸControlled porosity osmotic pump
âĸOsmotic bursting osmotic pump
âĸLiquid OROS
âĸDelayed Delivery Osmotic device
âĸTelescopic capsule
âĸOros ct (colon targeting)
âĸSandwiched oral therapeutic system
âĸOsmotic pump for insoluble drugs
âĸMonolithic osmotic system and OSMAT
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-
58. ī§ These are systems fabricated by encapsulating an
osmotic drug core containing an osmotically active drug
within a semi permeable membrane made from
biocompatible polymer eg- cellulose acetate
Osmotic pressure controlled drug delivery system (Elementary Osmotic Pump)
59. īŧ typically give a zero order release profile after an initial lag
īŧ deliveries may be delayed or pulsed if desired
īŧ drug release is independent of gastric pH and hydrodynamic condition
īŧ well characterized and understood
īŧ release mechanisms are not dependent on drug
īŧ rationale for this approach is that the presence of water in GIT is
relatively constant, at least in terms of the amount required for activation
and controlling osmotically base technologies
īŧ higher release rates are possible with osmotic systems compared with
conventional diffusion-controlled drug delivery systems
īŧ release from osmotic systems is minimally affected by the presence of food
in gastrointestinal tract
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
60. o Expensive
o If the coating process is not well controlled there is a risk of film
defects, which results in dose dumping
o Size hole is critical
o Dose dumping
o Retrieval therapy is not possible in the case of unexpected adverse
events.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
61.
62. MICROENCAPSULATION
ī§ Process in which small droplets or particles of liquid
or solid material are surrounded or coated by a
continuous film of polymeric materials.
ī§ Microencapsulation process helps for converting the
liquids to solids, changing the colloidal & surface
properties, providing environmental protection and
controlling the release characteristics of different
coated materials.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext
66. TARGETED DRUG
DELIVERY SYSTEMS
(TDDS)
ī§ Pharmacologically active agent or medicament is
selectively targeted or delivered only to its site of
action or absorption and not to the non-target
organs or tissues or cells.
ī§ Lead to efficient use of expensive drugs &
excipients, & reduce in production cost.
67. īŧ Biochemically inert (non-toxic)
īŧ Non-immunogenic
īŧ Physically and chemically stable in vivo and in vitro
conditions
īŧ Restricting drug distribution to target cells or tissues or
organs & should have uniform capillary distribution.
īŧ Controllable and predictable rate of drug release and also
drug release should not affect the drug action
68. īŧ Therapeutic amount of drug release
īŧ Minimal drug leakage during transit
īŧ Carriers used should be bio-degradable or readily eliminated
from the body without any problem
īŧ Preparation of delivery system should be easy or reasonably
simple, reproductive & cost effective
71. īą Active Moiety
ī To achieve the therapeutic effect
īą Carrier System
ī For favorable distribution of the drug
ī To protect drug from metabolism
ī To protect drug from early clearance
īą Ligands
ī To specifically target drug to target cells or target
tissue
72.
73.
74. LIPOSOMES MICELLES DENDRIMERS POLYMERIC NP NANOCRYSTALS
50-450 nm <100 nm 10-100 nm
Aqueous interior
Outer lipid bilayer
Hydrophobic
interior
Hydrophilic
exterior
Central core,
Interior dendritic
structure &
Exterior surface
with functional
groups
Matrix system Drug itself
formulated at
a nanoscale; its own
carrier
Encapsulate both
hydrophilic &
hydrophobic drugs
Encapsulate/solub
ilize hydrophobic
drugs into interior
Hyperbranched,
compartmentalized
structure- high
entrapment
efficiency
Nanocapsules
Nanospheres
Drugs with poor
water solubility
& dissolution
rate into readily
water-soluble
dispersions
75. Polymer-Drug Conjugates Protein NPs Nanogels
Covalent conjugation- sustained drug
release
Virus-like particles (VLP)
Caged proteins (CP)
non-fluid colloidal or polymeric
networks that swell when in
contact with
fluid
pH sensitive polymer-drug conjugate decreased untimely drug
leakage
For low molecular weight agents Vaccines development delivery of therapeutics such as
nucleic acids, vaccines,
cytokines, and nasal vaccines
are the most
widely studied
76. Carbon Nanotubes Nanodiamonds
(NDs)
Metallic NP Quantum dots Silica-based NP
Dia-1 nm
Length- 1-100nm
Carbon-based
<100 nm
cobalt, nickel, iron,
gold, and their
respective oxides
tiny particles of a
semiconducting
material
diameters 2-10
nm
Porous
Capacity for
functionalization
Single layer of
graphite wrapped
into cylinder
Different shapes
from different
methods
targeted to a
specific location by
using an external
magnetic field
semiconductor
inorganic core
aqueous organic
coated shell
large surface area
covered with polar
silanol groups-
water adsorption
Singled-walled
(SWNT)
Multi-walled
(MWNT)
C60 fullerenes
Detonation
Chemical vapour
deposition- thin
films in substrate
super-
paramagnetic iron
oxide nanoparticles
(SPIONs)
- large magnetic
susceptibility -
contrast agents for
MRI
core structure
determines the
color emitted,
while the outer
aqueous shell
used for
conjugation of
biomolecules
such as peptides,
protein, or DNA
ability to interact
with nucleic acids
nanopore size and
density can be
tailored to achieve
a constant
delivery rate
77. Carbon Nanotubes Nanodiamonds
(NDs)
Metallic NP Quantum dots Silica-based NP
Delivery of antibiotics,
antiviral and anti-
cancer agents
Targeting of
mitochondria
NDs coupled with
gadolinium as
contrast agent in
MRI
Contact lens
Drug delivery
Magnetic
Hyperthermia
Gold nanoparticles
(AuNP) - most
widely used
metallic
nanoparticles
Can be used for
tracking
therapeutic
agents within the
cells/tissues
Pores can be
capped with
various stimuli-
responsive
Molecules: capping
with β-cyclodextrin
were developed to
release the
encapsulated drug
at the acidic
tumor tissue
83. oHigh cost, which makes productivity more difficult.
oHighly sophisticated technology hence, technical
skill required.
oReduced ability to adjust the dosages.
oRapid clearance of targeted systems.
oInsufficient localization of targeted systems into
tumour cells.
oImmune reactions