2. Drug
Drug may be defined as an
agent or substance,
intended for use in the
diagnosis, mitigation,
treatment, cure or
prevention of disease in
human beings or animals.
Drugs are rarely
administered in their original
or crude forms. They are
administered in different
dosage forms by converting
them into suitable
formulations.
Crude Drugs
3. • Drug ?
• International nonproprietary names (INN, „generic“ names)
• Direct clinical use of the active drug substances is rare: Why??
• API handling and Accurate dosing can be difficult or impossible
(e.g., potent drugs: low mg and g doses)
• API administration can be impractical/unfeasible because of
size, shape, smell/odour, taste and low activity.
• Some API are chemically unstable in light, moisture, O2
• API can be degraded at the site of administration (e.g., low pH
in stomach).
• API may cause local irritations or injury when they are present
at high concentrations at the site of administration.
• Administration of active substance would mean to have no
chance for modification (improvement) of its PK
(Pharmacokinetic)profile
DRUG /ACTIVE DRUG SUBSTANCES/API
DRUG /ACTIVE DRUG SUBSTANCES /API
4. Drug:-(active pharmaceutical ingredient - API)
chemical compound intended for used in
diagnosis, treatment or prevention of diseases.
Excipients:-
(inactive pharmaceutical ingredients)
Technological, biopharmaceutical and/or
stability reasons.
Diluents/fillers, binders, lubricants,
disintegrants, coatings, preservants and
stabilizers, colorants and flavourings
dosage form:-
Drug+excipients
5. Dosage Forms
Definition: Dosage forms are the means by
which drug molecules are delivered to sites of
action within the body.
Every dosage forms is a combination of
the drug and different kinds of non – drug
components called as Excipients or
additives.
The additives are used to give a particular
shape to the formulation, to increase
stability, palatability & more elegance to
preparations.
8. 1. To provide for the safe and convenient delivery of accurate dosage
Examples: Tablets, Capsules, syrups
2. For the protection of a drug substance from the destructive influence of
atmospheric oxygen or moisture.
Examples: coated tablets, sealed ampules
3. For the protection of a drug substance from the destructive influence of
gastric acid after oral administration.
Example: enteric coated tablets
4. To conceal the bitter taste, salty obnoxious or odor of a drug substance.
Examples: Capsules, coated tablets, flavored syrups
Need of dosage forms: overcoming the
difficulties
9. The majority of drug substances are administered in manufacturing amounts,
much too small to be weighed on anything but a sensitive analytical balance.
Example: How can a layman accurately obtain 325 mg or 5 gr of aspirin found
in common aspirin tablets from bulk supply of aspirin?
Examples Of Drugs with Low Usual doses
Ferrous sulfate 300 mg Hematinic
Cimetidine 300 mg Antiulcer
Amoxicillin 250 mg Antibacterial
Propoxyphene HCl 65 mg Analgesic
Phenobarbital 30 mg Sedative
Diphenhydramine HCl 25 mg Antihistamine
Morphine sulfate 10 mg Narcotic
Analgesic
Cochicine 0.5 mg Gout suppressant
Nitroglycerin 0.4 mg Antianginal
Digoxin 0.25 mg Cardiotonic
Ethinyl Estradiol 0.05 mg Estrogen
Need of dosage forms: overcoming the
difficulties
10. 5. To provide liquid preparations of substances that are either
insoluble or unstable in the desired vehicle.
Example: suspension
6. To provide liquid dosage forms of substances soluble in desired
vehicle.
Example: solution
7. To provide extended drug action through controlled release
mechanisms
Examples: controlled release tablets, capsules, suspensions
8. To provide optional drug action from topical
administration sites
Examples: ointments, creams, ophthalmic, ear and nasal preparations
Need of dosage forms: overcoming the
difficulties
11. 9. To provide for insertion of a drug into one of the body’s
orifices
Examples: rectal and vaginal suppositories
10. To provide for the placement of drugs
within body tissues.
Examples: Implants
11. To provide for the optimal drug action through
inhalation therapy.
Examples: inhalants and inhalations
12. In addition, many dosage forms permit ease of drug
identification through distinctiveness of color, shape, or
identifying markings
Need of dosage forms: overcoming the
difficulties
12. They are classified according to:
2.Physical form
Solid
Semisolid
Liquid
Gases
1.Route of administration
Oral
Topical
Transdermal
Parenteral
Inhalation
Buccal & sublingual
Ophthalmic
Otic
Rectal
Vaginal
TYPES OF DOSAGE FORMS
13. Classification acc.to physical
form
Solid dosage
forms
Unit dosage
forms
Tablets
Capsule
Pills
Bulk
Internal
Fine powders &
granules
External
Dusting powders
Insufflations
Dentifrice
Snuffs
Ear powders
Liquid dosage
forms
Biphasic
Emulsion
Suspension
Monophasic
Internal External
Syrups
Elixirs
Linctus
Drops
Liniments
Lotions
Gargles
Throat paints
Mouth washes
Sprays
Eye lotions
Eye drops
Nasal drops
Semi solid dosage
forms
Internal External
Suppositories
Pessaries
Ointment
Creams
pastes
Jellies
Gaseous
dosage
form
Inhaler
aerosols
14. I) Oral dosage
forms:
1-Tablet:
A tablet is a hard, compressed medication in round, oval or square
shape.
The excipients include:
(flow aids) and lubricants to ensure efficient
-Binders, glidants
-Disintegrants to ensure that the tablet breaks up in the digestive tract.
-Sweeteners or flavours to mask the taste of
bad-tasting active ingredients.
-Pigments to make uncoated tablets visually attractive.
.
8
15. 1-Tablet (Cont.)
A coating may be applied to:
1- hide the taste of the tablet's components.
2- make the tablet smoother and easier to
swallow .
3- make it more resistant to the environment.
4- extending its shelf life.
9
16. 2-Buccal and
sublingual tablet:
- Sublingual and buccal medications are administered by placing
them in the mouth, either under the tongue (sublingual) or
between the gum and the cheek (buccal).
- The medications dissolve rapidly and are absorbed through the
mucous membranes of the mouth, where they enter into the
bloodstream.
- Avoid the acid and enzymatic environment of the stomach and
the drug metabolizing enzymes of the liver.
- Examples of drugs administered by this route: e.g. vasodilators,
steroidal hormones.
17. 3-Effervescent
tablet:
Effervescent tablets are uncoated tablets that generally
contain acid substances (citric and tartaric acids) and
carbonates or bicarbonates and which react rapidly
in the presence of water by releasing carbon dioxide.
-They are intended to be dissolved or dispersed in
water before use providing:
A- Very rapid tablet dispersion and dissolution.
B- pleasant tasting carbonated drink.
18. 4- Chewable
tablet:
-
-
They are tablets that chewed prior to swallowing.
They are designed for administration to children e.g.
vitamin products.
19. vinay gupta
Dosage forms (Tablet) for oral
administration
Generations of
dosage forms
– 1st gen.
conventional
(unmodified)
release of API
– 2nd gen.
controlled
release of API
(CR)
20. Conventional vs. controlled
release forms
I. Gen. – disintegration of the dosage form and
dissolution of API is spontaneous process;
– drug absorption and distribution is based only on
physico-chemical properties of API
21. II. Gen. The release of API is under control of the
drug delivery system (temporal control)
–
–
– Advantages:
Avoids fluctuations of plasma drug concentration better
safety and efficacy
Decreased frequency of drug administration (often once daily
admin) better compliance
Sustained release (SR) – release of the initial API dose
& further prolonged release
Controlled release (CR) – properly controlled (Zero
order) release of API
15
23. 5- Capsule:
A capsule is a medication in a gelatin container.
-Advantage: mask the unpleasant taste of its contents.
-The two main types of capsules are:
1.hard-shelled capsules, which are
normally used for dry, powdered ingredients,
2.soft-shelled capsules, primarily used for oils and for
active ingredients that are dissolved or suspended in
oil.
Soft gelatin capsule
Hard gelatin capsule
Spansules
17
24. 6-
Lozenge:
-It is a solid preparation consisting of sugar and gum,
the latter giving strength and cohesiveness to the
lozenge and facilitating slow release of the
medicament.
- It is used to medicate the mouth and throat for the
slow administration of indigestion or cough
remedies.
25. 7-Pastilles:
They are solid medicated preparations designed to
dissolve slowly in the mouth. They are softer than
lozenges and their bases are either glycerol and
gelatin, or acacia and sugar.
26. 8- Dental Cones:
- A tabletform intended to be
placed in the empty socket
following a tooth local, for multiplication of
bacteria associated with tooth
pathogenic
extractions.
may contain an antibiotic or
- The cones
antiseptic.
27. 9-Pills:
- Pills are oral dosage forms which consist of spherical
more medicaments
-
masses prepared from one or
incorporated with inert excipients.
Pills are now rarely used.
28. 10-
Granules:
- solid, dry aggregates of
supplied in single-dose
They are consisting of
powder particles often
sachets.
- Some granules are placed on the tongue and
swallowed with water, others are intended to be
dissolved in water before taking.
- Effervescent granules evolve carbon dioxide when
added to water.
29. 11- Powder
(Oral):
There are two kinds of powder intended for internal use.
1-Bulk Powders are multidose preparations consisting of solid,
loose, dry particles of varying degrees of fineness. They contain
one or more active ingredients, with or without excipients and, if
necessary, coloring matter and flavoring substances.
- usually contain non-potent medicaments such as antacids since
the patient measures a dose by volume using a 5ml medicine
spoon. The powder is then usually dispersed in water or, in the
case of effervescent powders, dissolved before taking.
2-Divided Powders are single-dose presentations of powder ( for
example, a small sachet) that are intended to be issued to the
patient as such, to be taken in or with water.
30. 12- Powders for mixtures:
- The mixed powders may be stored in dry form and
mixture prepared by the pharmacist when required
for dispensing , by suspending the powders in the
appropriate vehicle.
31. 13-Liquid preparations:
a. Oral solution:
Oral solutions are clear Liquid preparations for oral use containing
one or more active ingredients dissolved in a suitable vehicle.
b. Oral emulsion:
Oral emulsions are stabilized oil-in-water
dispersions, either or both phases of which may contain
dissolved solids.
c. Oral suspension:
- Oral suspensions are Liquid preparations for oral use containing
one or more active ingredients suspended in a suitable vehicle.
- Oral suspensions may show a sediment which is readily
dispersed on shaking to give a uniform suspension which
remains sufficiently stable to enable the correct dose to be
delivered.
32. 13-Liquid preparations
(Cont.):
d- Syrup:
-
-
It is a concentrated aqueous solution of a sugar, usually
sucrose.
Flavored syrups are a convenient form of masking
disagreeable tastes.
e- Elixir:
-It is pleasantly flavored clear liquid oral preparation of potent or
nauseous drugs.
- The vehicle may contain a high proportion of ethanol or sucrose
together with antimicrobial preservatives which confers the
stability of the preparation.
33. 13-Liquid preparations
(Cont.):
f- Linctuses:
-Linctuses are viscous, liquid oral preparations that are usually prescribed for
the relief of cough.
-They usually contain a high proportion of syrup and glycerol which have a
demulcent effect on the membranes of the throat.
-The dose volume is small (5ml) and, to prolong the demulcent action, they
should be taken undiluted.
g- Oral drops:
Oral drops are Liquid preparations for oral use that are intended to be
administered in small volumes with the aid of a suitable measuring device.
They may be solutions, suspensions or emulsions.
34. 13-Liquid preparations:
h- Gargles:
-
- They are aqueous solutions used in the
prevention or treatment of throat infections.
Usually they are prepared in a concentrated
solution with directions for the patient to
dilute with warm water before use.
i- Mouthwashes:
These are similar to gargles but are used for
oral hygiene and to treat infections of the
mouth.
35. II) Topical dosage forms:
1- Ointments:
-Ointments are semi-solid, greasy
preparations for application to the skin, rectum or
nasal mucosa.
-The base is usually anhydrous and immiscible with skin
secretions.
-Ointments may be used as emollients or to apply
suspended or dissolved medicaments to the skin.
36. Topical dosage forms
(Cont.):
2- Creams:
-
-
Creams are semi-solid emulsions, that is mixtures of oil and water.
They are divided into two types:
A- oil-in-water (O/W) creams: which are composed of small droplets of
oil dispersed in a continuous aqueous phase.
Oil-in-water creams are more comfortable and cosmetically acceptable as
they are less greasy and more easily washed off using water.
B- water-in-oil (W/O) creams: which are composed of small droplets of
water dispersed in a continuous oily phase.
Water-in-oil creams are more difficult to handle but many drugs which are
incorporated into creams are hydrophobic and will be released more
readily from a water-in-oil cream than an oil-in-water cream.
Water-in-oil creams are also more moisturising as they provide an oily
barrier which reduces water loss from the stratum corneum, the
outermost layer of the skin.
30
37. Topical dosage forms
(Cont.):
3- Gels (Jellies):
-Gels are semisolid system in which a liquid phase is constrained within a 3-
D polymeric matrix (consisting of natural or synthetic gum) having a high
degree of physical or chemical cross-linking.
-They are used for medication, lubrication and some miscellaneous
applications like carrier for spermicidal agents to be used intra vaginally .
4- Poultice:
It is soft, viscous, pasty preparation for external use. They are applied to skin
while they are hot. Poultice must retain heat for a considerable time because
they are intended to supply warmth to inflamed parts of body.
E.g. Kaolin poultice (B.P.C.)
38. Topical dosage forms (Cont.):
5- Pastes :
- Pastes are basically ointments into which a high percentage of insoluble solid
has been added
-The extraordinary amount of particulate matter stiffens the system.
-Pastes are less penetrating and less macerating
and less heating than ointment.
-Pastes make particularly good protective barrier when placed on the skin, the
solid they contain can absorb and thereby neutralize certain noxious chemicals
before they ever reach the skin.
- Like ointments, paste forms an unbroken relatively water – impermeable film
unlike ointments the film is opaque and therefore can be used as an effective
sun block accordingly.
-Pastes are less greasy because of the absorption of the fluid hydrocarbon
fraction to the particulates.
39. Topical dosage forms
(Cont.):
There are two types of paste:
a) Fatty pastes (e.g: leaser's paste) .
b) Non greasy pastes (e g: - bassorin paste).
6- Dusting powders:
- These are free flowing very fine powders for external
use.
- Not for use on open wounds unless the powders
are sterilized.
40. 40
Topical dosage forms
(Cont.):
7- Transdermal patch:
-A transdermal patch or skin patch is a medicated adhesive patch
that is placed on the skin to deliver a specific dose of medication
through the skin and into the bloodstream.
-An advantage of a transdermal drug delivery route over other types
such as oral, topical, etc is that it provides a controlled release of
the medicament into the patient.
- The first commercially available patch was scopolamine for motion
sickness.
41. 41
Topical dosage forms (Cont.):
8-Plasters:
- Plasters are solid or semisolid masses adhere to the
skin when spread upon cotton felt line or muslin as a
backing material and they are mainly used to,
A- Afford protection and mechanical support.
B- Furnish an occlusive and macerating action.
C- Bring medication into close contact with the surface
of the skin.
42. 42
Topical dosage forms (Cont.):
9- Liniments:
-Liniments are fluid, semi-fluid or, occasionally, semi-
solid preparations intended for application to the skin.
-They may be alcoholic or oily solutions or emulsions.
-Most are massaged into the skin (e.g. counter-
irritant).
-Liniments should not be applied to broken skin.
43. 43
Topical dosage forms (Cont.):
10-Lotions:
These are fluid preparations (aqueous)
for external application without friction.
They are either dabbed on the skin or applied
on a suitable dressing and covered with a
waterproof dressing to reduce evaporation.
44. Topical dosage forms (Cont.):
11- Collodion:
in ether or acetone,
Collodion is a solution of nitrocellulose
sometimes with the addition of alcohols.
-Its generic name is pyroxylin solution.
-It is highly flammable.
- As the solvent evaporates, it dries to a celluloid-like film.
- Compound Wart Remover consists of acetic acid and salicylic acid
in an acetone collodion base used in Treatment of warts by
keratolysis.
38
45. Topical dosage forms (Cont.):
application to the skin or
12- Paints:
- Paints are
liquids for mucous
membranes.
- Skin paints contain volatile solvent that evaporates
quickly to leave a dry resinous film of medicament.
- Throat paints are more viscous due to a high content
of glycerol, designed to prolong contact of the
medicament with the affected site.
39
46. Topical dosage forms (Cont.):
13- Pressurized dispensers (aerosol sprays):
- Several different types of pharmaceutical product may be
packaged in pressurized dispensers, known as aerosols.
- Surface sprays produce droplets of 100 um diameter or
greater.
- May be used as surface disinfectants, wound or burn dressing,
relieve irritation of bites.
- Spray-on dusting powders are also available from pressurized
containers.
47. 47
III) Rectal dosage
forms:
1- Suppository:
It is a small solid medicated mass, usually
cone-shaped ,that is inserted either into the
rectum (rectal suppository), vagina (vaginal
suppository or pessaries) where it melts at
body temperature .
48. Rectal dosage forms:
2- Enema:
An enema is the procedure of introducing liquids into the rectum
and colon via the anus.
Types of enema:
1- Evacuant enema: used as a bowel stimulant to treat
constipation. E.g. soft soap enema & Mgso4 enema
-The volume of evacuant enemas may reach up to 2 liters.
before
- They should be warmed to body temperature
administration.
49. Rectal dosage forms
(Cont.):
2- Retention enema:
-
-
Their volume does not exceed 100 ml.
No warming needed.
- May exert:
A- Local effect: e.g. a barium enema is used
as a contrast substance in the radiological imaging of the bowel.
B- Systemic effect:
e.g. the administration of substances into the bloodstream. This
may be done in situations where it is impossible to deliver a
medication by mouth, such as antiemetics.
e.g. nutrient enema which contains carbohydrates,
vitamins & minerals.
50. IV) Vaginal dosage
forms:
1- Pessary:
-
-
Pessaries are solid medicated preparations designed for
insertion into the vagina where they melt or dissolve.
There are three types:
A- Moulded pessaries: they are cone shaped and prepared in a
similar way to moulded suppositories.
B- Compressed pessaries: made in a variety of shapes and are
prepared by compression in a similar manner to oral tablets.
C- Vaginal capsules: are similar to soft gelatin oral Capsules
differing only in size and shape.
51. Vaginal dosage
forms:
2- Vaginal ring:
Vaginal rings are 'doughnut-shaped' polymeric
drug delivery devices
designed to provide controlled release of drugs to the vagina over
extended periods of time.
Several vaginal ring products are currently available, including:
Femring :
a low-dose estradiol-acetate releasing ring, manufactured from
silicone elastomer, for the relief of hot flashes and vaginal atrophy
associated with menopause.
NuvaRing:
a low-dose contraceptive vaginal ring, releasing progesterone and
estrogen.
45
52. 52
Vaginal dosage forms
(Cont.):
3- Douche:
A douche is a device used to introduce a stream
of water into the body cavity for medical or
hygienic reasons.
53. 53
Vaginal dosage forms
(Cont.):
4- Intrauterine device:
-It is a birth control device placed in the uterus, also known as an IUD or a
coil.
-The IUD is the world's most widely used method of reversible birth
control.
-The device has to be fitted inside or removed from the uterus by a doctor .
-It remains in place the entire time pregnancy is not desired. Depending on
the type, a single IUD is approved for 5 to 10 years use.
-There are two broad categories of intrauterine contraceptive devices: A-
inert and copper-based devices.
B- hormonally-based devices that work by releasing a progesterone.
54. 54
V) Parenteral dosage
forms:
An injection is an infusion method of putting liquid into
the body, usually with a hollow needle and a syringe
which is pierced through the skin to a sufficient depth
for the material to be forced into the body.
There are several methods of injection, including: 1-An
intravenous injection:
It is a liquid administered directly into the bloodstream
via a vein.
It is advantageous when a rapid onset of action is
needed.
55. 55
Parenteral dosage
forms :
2- Intramuscular injection:
-It is the injection of a substance directly into a muscle.
-Many vaccines are administered intramuscularly.
-Depending on the chemical properties of the drug, the
medication may either be absorbed fairly quickly or more
gradually.
-Intramuscular injections are often given in the deltoid, vastus
lateralis, ventrogluteal and dorsogluteal muscles.
56. 56
Parenteral dosage
forms:
3- Subcutaneous injection:
Subcutaneous injections are given by injecting
a fluid into the sub cutis, thelayer of skin directly
below the dermis and epidermis.
Subcutaneous injections are highly effective in
administering vaccines and such medications as
insulin.
58. VI) Inhaled dosage
forms
:
1- Inhaler :
-
-
-
-
Inhalers are solutions, suspensions or emulsion of drugs in
a mixture of inert propellants held under pressure in an
aerosol dispenser.
Release of a dose of the medicament in the form of
droplets of 50 um diameter or less from the container
through a spring-loaded valve incorporating a metering
device. The patient then inhales the released drug through
a mouthpiece.
In some types, the valve is actuated by finger pressure, in
other types the valve is actuated by the patient breathing in
through the mouthpiece.
It is commonly used to treat asthma and other respiratory
problems.
52
59. 59
Inhaled dosage forms
(Cont.):
2 Nebulizer or (atomizer):
A nebulizer is a device used to administer medication to people in forms of
a liquid mist to the airways.
-It is commonly used in treating asthma, and other respiratory diseases.
-It pumps air or oxygen through a liquid medicine to turn it into a vapor,
which is then inhaled by the patient.
-As a general rule, doctors generally prefer to prescribe inhalers for their
patients, because:
1-These are cheaper 2- more portable
3- carry less risk of side effects.
Nebulizers, for that reason, are usually reserved only for serious cases of
respiratory disease, or severe attacks.
60. 60
VII) Ophthalmic dosage
forms:
1- Eye drops:
Eye drops are saline-containing drops used as a
vehicle to administer medication in the eye.
may contain steroids,
in them and are only
Depending on the condition being treated, they
antihistamines or topical anesthetics.
Eye drops sometimes do not
have medications lubricating and
tear-replacing solutions.
2- Ophthalmic ointment & gel:
These are sterile semi-solid
Preparations intended for application
To the conjunctiva or eyelid margin.
61. 61
VIII) Otic dosage
forms:
- Ear drops are solutions, suspensions or emulsions of
drugs that are instilled into the ear with a dropper.
It is used to treat or prevent ear infections,
especially infections of the outer ear and ear
canal.
1- Ear drops:
-
62. IX) Nasal dosage
forms:
1- Nasal Drops and Sprays:
Drugs in solution may be instilled into the nose from a
dropper or from a plastic squeeze bottle.
The drug may have a local effect, e.g. antihistamine,
decongestant.
Alternatively the drug may be absorbed through the
nasal mucosa to exert a systemic effect.
The use of oily nasal drops should be avoided
because of possible damage to the cilia of the nasal
mucosa.
56
65. Solid dosage forms one of the oldest dosage forms and
most of the solid dosage forms are available in Unit
dose.
Unit dose may be defined as a exact quantity of the drug
administered at once. e.g. Tablets, Capsule, pills,
cachets, powders etc.
When drugs are to be administered orally in dry state,
then tablets, capsules are most convenient dosage
forms.
Some solids are supplied in bulk (Means quantity
available in large). Bulk powders can be supplied as
Internal (Granules, Fine powders) as well as External
(Dusting Powders, Insufflations etc)
66. Dusting Powders
Dusting powders are applied externally to skin,
so they should be applied in very fine state to
avoid local irritation. Hence dusting powders
should be passed through sieve no 80 to
obtained fined powders.
Dusting powders are prepared by mixing of
more than one ingredients in which either
starch, kaolin, or talc are used in their
formulation. Generally talc or kaolin are used
because they are inert in nature.
Dusting powders are used for antiseptic,
astringent, absorbent, antiperspirant etc.
Dusting powders are of two sub type they are
as
I) Medical dusting powder
67. Medical Dusting
Powders
Medical Dusting powders are used to
increase superficial condition of skin.
These are not applied on wounds, burns etc
Medical dusting powders must be free from
dangerous pathogenic micro- organism.
68. Surgical Dusting Powders
Surgical dusting powders are used in body
cavities and also on major wounds like as
burns etc.
They should be sterilized before use.
They are mainly used for their antiseptic,
absorbent action.
69. Insufflations
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.
It sprays the powders (in a state of fine particles)
on site of application.
Now a days insufflations are also available in
pressure aerosols. This pressure aerosols are
used for administration of potent drug.
They are used in the treatment of ear, nose, throat
infections with antibiotics to produce local effect of
drugs.
70. Snuffs
These are finely divided solid dosage forms of
medicaments which are inhaled into nostrils.
They are mainly used for their antiseptic,
bronchodilator and decongestion action.
71. Granules
Granulation is the process in which primary
powder particles are made to adhere to form
larger multiparticle or large particles entities
called granules.
The bitter, nauseous, unpleasant powders can
not be given tablets, capsule due to bulk
quantity are required to be taken, as well as
they are not given in liquid dosage forms due
to their stability such powders are given in the
granules forms.
These powders are mixed with suitable
exicipent along with granulating agent,
prepare a coherent mass then dried & passed
through the sieve to obtained desired size of
granules.
72. Effervescent Granules
Effervescent granules are meant for internal use.
They contained medicaments mixed with citric acid,
tartaric acid & sodium bi carbonates, sometime
saccharin or sucrose may be added for sweetening
taste.
Before, administration desired quantity of granules are
dissolved in water, the acid & bicarbonate reacts with
each other to produce effervescence.
Effervescent granules are prepared by two methods,
namely as, I) Heat method, II) Wet method
73. Heat method
A large porcelain or stainless steel evaporating dish is placed over
the boiling water bath.
The dish must be sufficiently hot (generally heating takes place for 1
– 5 min.) before transferring the powders into it, to ensure rapid
liberation of water of crystallization from citric acid.
If heating of the dish is delayed then the powder which is added to
it, will heat up slowly & liberated water of crystallization will also be
liberated simultaneously.
As a result, sufficient water will not be available to make a coherent
mass.
This coherent mass will pass through the sieve to obtained suitable
size of granules, dry it in oven at 600c then packed in air tight
container.
74. Wet method
In this methods all the ingredients are mixed thoroughly
This powders mixture make moistened with non –
aqueous vehicle (e.g. alcohol), to prepare a coherent
mass which is then passed through sieve no 8 to
obtained suitable granules.
Then dried in oven at 600c. The dried granules are again
passed through the sieve to break the lumps which may
be formed during drying.
The dried granules are packed in air tight container.
75. Tablets
These are solid dosage forms of medicaments which are
prepared by moulding or by compression with or without
Excipients.
The tablets can be prepared by two methods namely as
a
I) Dry granulation, II) Wet Granulation
76. Capsule
Capsules are solid unit dosage forms in which one or more
medicaments enclosed within a shell.
Capsules mainly divided in to two parts namely as –
I) Body (Longest part of capsule shell), II) Cap (Smallest part
of capsule shell)
The capsule are generally prepared by gelatin.
Depending on their formulation, two types of gelatin are used
namely as – I) Hard gelatin, II) Soft gelatin.
Body
Cap
77. Pills
These are small, rounded solid dosage forms containing
medicaments intended for oral use.
The medicaments are mixed with excipients to forms a
firms plastic mass.
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.
Sometimes pills are coated with varnish, gold leaf, etc to
improve finish, unpleasant taste & stability.
Now a days pills are outdated preparations because of
number of disadvantages such as -
78. Disintegration time of pill is uncertain means freshly
prepared pills are disintegrates readily rather than old
dried pills.
It is difficult to prepare pills of uniform size & weight.
81. It may be defined as “A solution is a liquid-preparation
that contains one or more soluble chemical substances
dissolved in a specified solvent”
Liquid dosage forms are intended for External, Internal
or parenteral use.
The component of the solution which is present in a
large quantity is known as “SOLVENT” where as the
component present in small quantity is termed as
“SOLUTE”
They mainly classified in to two category namely as –
I) Monophasic Liquid dosage forms.
II) Biphasic liquid dosage forms.
82. Advantage
Immediately available for absorption.
Administration convenient, particularly for infants,
psychotic patients.
Easy to color, flavor & sweeten.
Liquids are easier to swallow than solids and are
therefore particularly acceptable for pediatric patient.
A solution is an homogeneous system and therefore the
drug will be uniformly distributed throughout the
preparation.
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.
83. Disadvantage
Less stable in aqueous system. Incompatibility is faster in
solution than solid dosage form.
Patients have no accurate measuring device.
Accident breakage of container results in complete loss.
Solution often provide suitable media for the growth of micro
organisms.
The taste of a drug, which is often unpleasant, is always more
pronounced when in solution than in a solid form.
Bulky than tablets or capsule, so difficult to carry transport.
85. Monophasic liquid dosage forms are represent by true or
colloidal solution.
The component of the solution which is present in a large
quantity is known as “SOLVENT” where as the component
present in small quantity is termed as “SOLUTE”.
A solution is homogenous because the solute is an ionic or
molecular forms of subdivision.
In case of colloidal solutions, the solutes are present as
aggregates although they cannot be seen by necked eye or
ordinary microscope.
It is sub classified as –
I) Internal Use, II) External use
88. Syru
p
It is a concentrated or saturated solutions of sucrose in
purified water.
The concentration of sucrose is 66.7% w/w & due to that
it is a viscous preparations.
The syrup which contains medical substance called as a
medicated syrup & those containing aromatic or flavored
substance known as a flavored syrup.
89. Importance of syrup
It retards oxidation because its partly hydrolyzed into
reducing sugar.
It prevents decomposition of many vegetable substance
because its have high osmotic pressure which prevent
the growth of bacteria.
They are palatable due sweet taste.
90. It is clear, sweetened, aromatic,
hydroalcholic preparations meant
for oral use.
The medicated elixirs are generally
contained potent drug like as
antibiotics, antihistamine or
sedative , where as non –
medicated elixirs contained
flavoured.
The composition of elixirs
contained mainly as ethyl alcohol
(active ingredients),water, glycerin
or propylene glycol, colouring
Elixirs
91. Linctuse
s
These are viscous liquid preparations
that’s are used for the treatment of
cough.
They contain medicaments which
have demulcent, sedative,
expectorant action.
They are taken in small doses without
diluting with water to have prolonged
effect of medicines.
Simple syrup is used as a vehicle for
most of the linctuses.
Tolu syrup is preferred in certain
cases because of its aromatic odour &
92. Drop
s
These are liquid preparations meant for oral
administration.
The oil soluble vitamins, such as vitamin A & D
concentrates in fish – liver oil are presented as drops for
administration.
Since these preparations contain potent medicaments,
the dose must be measured accurately
The following two methods are commonly used for this
purpose.
Use of a dropper which is accurately graduated in
fractions of a milliliters.
Use of a pre – calibrated dropper.
94. Liniments
Liniments are liquid or semi- liquid
preparations meant for external application to
the skin.
They are usually applied to the skin with
friction & rubbing of the skin.
Are usually alcoholic and oily liquid
preparations (monophasic) or emulsion
(biphasic).
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.
The oily liniments are milder in their action
and may function solely as protective
coatings
95. Lotions
Are usually aqueous, alcoholic
or oily liquid preparations.
They are intended for external
application without friction or
rubbing to the affected area
Usually applied with the help of
some absorbent material such
as cotton wool or gauze.
It is generally used to provide
cooling, soothing and protective
& antiseptic action.
96. Gargles
Gargles are aqueous solutions used for treating throat infection
(pharynx and nasopharynx part)
Supplied in concentrated forms with directions of dilution with
warm water before use
They are used into intimate contact with the mucous membrane
of throat for few seconds, before they are thrown out of the
mouth.
They are used to relieve soreness in mild throat infection.
They are also used for their antiseptics, antibiotics and/or
anesthetics
97. Mouth wash
These are aqueous solutions with
pleasant or acceptable taste &
odour
These are used to make clean &
deodorise the buccal cavity or
used for oral hygiene and to treat
infections of the mouth.
They mainly contain antibacterial
agent, alcohol, glycerin,
sweetening agent, flavoring agent
& colouring agent.
98. Throat paints
Throat paints are viscous liquid
preparations used for mouth
and throat infections
Glycerin is commonly used as a
base because being viscous it
adheres to mucous membrane
for long period and it possess a
sweet taste.
99. Sprays
These are the preparations of drugs in
media which may be aqueous, alcoholic,
or glycerin.
They are applied to the mucous
membrane of throat or nose with an
atomizer.
The throat sprays must be sprayed from a
special type of atomizer known as a
nebulizer, which removes the large
droplets by baffling system. Only
precaution should be taken that the fine
droplet will used to easily reach the lungs.
Nebulizer
100. Inhalations
These are liquid preparations containing volatile substance & are
used to relieve decongestion & inflammations of respiratory tract.
The volatile substance in inhalations would be volatile at room
temperature so that they should be placed on some adsorbent pad
or handkerchief.
In some cases inhalations will added to hot water (650c) then
vapors will inhaled.
101. Nasal drops
Drugs in solution may be instilled into the nose from a dropper or
from a plastic squeeze bottle.
The drug may have a local effect, e.g. antihistamine, decongestant.
Alternatively the drug may be absorbed through the nasal mucosa
to exert a systemic effect.
The use of oily nasal drops should be avoided because of possible
damage to the cilia of the nasal mucosa & if it is used for long
period may reach the lungs & cause lipoid pneumonia.
To avoid that Nasal drops are prepared so that they are similar in
many respects to nasal secretions, so that normal ciliary action is
maintained thus aqueous nasal solutions usually are isotonic and
slightly buffered to maintain a pH of 5.5 to 6.5.
102. Eye drops
Sterile, aqueous/oily solutions or suspensions intended for
instillation in eye sac.
Eye drops may contain buffers, stabilizing agents, dispersing
agents, solubilising agents, anti-oxidants & agents required for
tonicity/ viscosity adjustment
Single dose container should not contain anti-microbial
preservative.
In case of multi dose container a dropper should be supplied with it
for administration. Maximum size of such containers is 10 ml.
103. Eye lotions
These are the aqueous solutions used for washing the eyes.
These are supplied in concentrated forms & are required to diluted
with warm water immediately before use.
They should be free from foreign particles to avoids irritation to the
eye.
They are required to prepared fresh & should not be stored for
more than two days to avoid microbial contaminations.
104. Ear drops
These are the solutions of drugs that are instilled into ear cavity with
the help of dropper.
These are generally used for cleaning the ear, softening the wax &
for treating the mild infections.
The solutions is generally prepared in water, glycerin, propylene
glycol & dilute alcohol.
106. Biphasic liquid dosage forms
The liquid which consist of two phases are known as a biphasic
liquid dosage forms.
They are sub categorized into two different forms namely as –
I) Emulsion
II) Suspension
In emulsion both phases are available in liquid where as in
suspension, finely divided solid particles are suspended in liquid
medium.
107. Emulsion
Emulsion is a biphasic liquid preparations containing two
immiscible liquid (Continuous Phase & dispersed phase) made
missicible.
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)
An emulsion is a thermodynamically unstable system consisting of
at least two immiscible liquid phases one of which is dispersed as
globules in the other liquid phase stabilized by a third substance
called emulsifying agent.
The globule size in emulsion varies from 0.25 to 25 µm.
108. Examples for emulsions:- milk, rubber latex, crude oil etc.
A.: Two immiscible liquids not emulsified
B. An emulsion of phase B dispersed in Phase A
C. Unstable emulsion slowly separates.
D. The emulsifying agent ( black film) places it self on the interface
between phase A and phase B and stabilizes the emulsion.
109. Types of emulsions
Simple type
Water in oil (w/o)
Oil in water (o/w)
Depending on globule size
Micro emulsion
Fine emulsion
Special type
Multiple emulsion (w/o/w, o/w/o)
110. Water in oil (w/o)
In this types of emulsion water is dispersed phase & oil is
continuous phase
w/o types of emulsion generally meant for External use.
Examples are butter, lotions, creams etc.
In rare case they are used internally.
Water is dispersed
phase
Oil is continuous phase
111. Oil in water (o/w)
In this types of emulsion oil is dispersed phase & water is
continuous phase
o/w types of emulsion meant for both Internal use & External use.
Examples for internal use are Vitamin A in corn oil, liquid paraffin in
water etc.
Examples for External use are Benzyl benzonate emulsion.
Oil is dispersed phase
water is continuous pha
112. Micro Emulsion
These are clear dispersions of o/w or w/o in which the globules have
small size like as a 10nm or 0.01 µm..
Being cleared products micro emulsion are more popular now a
days.
Micro emulsions are thermodynamically stable optically transparent ,
mixtures of a biphasic oil –water system stabilized with surfactants.
113. Fine emulsion
Normally these have a milky appearance.
The globule size ranges from 0.25 to 25 µm.
114. Multiple emulsion
These are emulsion with in emulsion & designated as w/o/w or
o/w/o.
The drugs that is incorporated in the innermost phase must cross
two phase boundaries before getting absorbed.
It is generally used in oral sustained release or intramuscular
therapy.
115. Identification tests
Dilution test
Conductivity test
Dye test
Fluorescence test
Cobalt chloride test
Filter paper test
116. Dilution test
The emulsion is diluted with water, after dilution emulsion remain
stable then it is said to be o/w type of emulsion because water is in
continuous phase. If emulsion is break after dilution with water then
it is said to be w/o type of emulsion.
Add drops of water
Water distribute
Uniformly
Add drops of water
O/W Emulsion W/O Emulsion
117. Conductivity test
Conductivity test can be performed by dipping a pair of electrode
connecting with low voltage bulb & pass the current.
If bulb glows then it is said to be o/w type of emulsion because
water is in continuous phase & it is good conductor of electricity.
If bulb doesn't glow then it is said to be w/o type of emulsion
because oil is bad conductor f electricity.
Bulb glows with O/W
Emulsion
Emulsion
Bulb doesn’t glow with W/O
118. Dye test
Oil soluble Scarlet red dye is mixed with emulsion.
Place a drop of emulsion on microscopic slide cover it with cover
slip & examine under microscope.
If disperse globules appears red & ground is colourless then it said
to be o/w type of emulsion because water is present in continuous
phase.
If reserve condition occurs (If disperse globules appears colourless
& ground is red colour then it said to be w/o type of emulsion
because oil is present in continuous phase.)
Oil is dispersed
phase
Water is
continuous
phase
Water is disperse
phase
Oil is continuous
phase
119. Fluorescence test
Certain fixed oil posses the physical properties of fluorescing in the
presence of ultraviolet radiations.
If examine under microscope ground is fluorescence then it said to
be w/o type of emulsion because oil is present in continuous phase.
If examine under microscope droplet is fluorescence then it said to
be o/w type of emulsion because oil is present in disperse phase.
120. Creaming test
The direction of creaming identifies the emulsion type, if the
densities of aqueous and oil phases are known.
Water-in-oil emulsions normally cream downward as oil is usually
less dense than water.
Oil-in-water emulsions normally cream upwards.
121. Cobalt chloride test
Pour the emulsion on filter paper then it is soaked in cobalt chloride
solutions & allowed to dry turns from blue to pink.
Then this emulsion is said to be o/w type of emulsion.
This test may fail if emulsion unstable or breaks in presence of
electrolyte.
122. Filter paper test
This test is based on the fact that an o/w emulsion will spread out
rapidly when dropped onto filter paper.
In contrast, a w/o emulsion will migrate only slowly. This method
should not be used for highly viscous creams.
123. Suspension
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.
In which solid particles acts as disperse
phase where as liquid vehicle acts as
continuous phase
The external phase (suspending medium) is
generally aqueous in some instance, may
be an organic or oily liquid for non oral use.
The particle size for non oral suspension is
so important to avoid grittiness to skin.
124. Advantage of suspension
Suspension can improve chemical stability of certain drug. E.g.
Procaine penicillin
Drug in suspension exhibits higher rate of bioavailability than other
dosage forms.
Solution > Suspension > Capsule > Compressed Tablet >
Coated tablet
Duration and onset of action can be controlled. E.g. Protamine
Zinc-Insulin suspension.
Suspension can mask the unpleasant/ bitter taste of drug. E.g.
Chloramphenicol
125. Disadvantage of suspension
Physical stability , sedimentation and compaction can causes
problems.
It is difficult to formulate.
Uniform and accurate dose can not be achieved unless
suspension are packed in unit dosage form.
All suspensions are required to be shaken before measuring of
dose.
The storage of suspension may lead to changes in disperse
system especially, when there is fluctuations in temperatures.
126. Ideal qualities of good
suspension
It should settle slowly & easily re – dispersed on shaking
It should readily & evenly pour from container.
It should be chemically inert.
It should not forms hard cake.
It should prevent degradation of drug or to improve stability of
drug.
It should mask the taste of bitter of unpleasant drug.
127. Flocculated suspension
In this type, solid particles are loosely aggregates themselves,
means individual particles are come in contact with each other to
forms network like structure called as a floccules.
These flocs are light, fluffy in nature, which are held together by
weak van der waals force of attraction.
Aggregation is achieved by adding flocculating agent.
This suspension will readily sediments.
This suspension posses better physical stability but less
bioavailability as compared to deflocculated suspension due to
dissolution of floccules.
128. Deflocculated suspension
In this type of suspension, individual particle exits as a separate
entity, means particles carry a finite charges on their surface .
Hence particles approaches each other, they experience repulsive
forces. This force create a high potential barrier, which prevents a
aggregation of particles.
During storage, these suspension shows a sedimentation at slow
rate, due to that particles forms a close packing arrangement.
So that it is difficult to re dispersed on agitation & forms a cake or
claying which is hard in nature.
This type of suspension have shorter shelf life but high
bioavailability as compared to flocculated suspension.
129. Difference between flocculated & deflocculated
suspension
Flocculated Suspension Deflocculated suspension
Particles form loose aggregates & forms
network like structure.
Particle exist as separate entities.
Particles experience attractive forces. Particles experience repulsive forces.
Supernatant liquid is clear. Supernatant liquid is cloudy.
The rate of sediment is high. The rate of sediment is slow.
Sediment is rapidly formed. Sediment is slowly formed.
sediment are loosely packed, hence hard
cake is not formed.
Sediments are closely packed, hence
hard cake is formed.
The sediment is easy to redisperse on
shaking.
Sediment is difficult to redisperse on
shaking. (due to formation of hard cake)
Bioavailability is comparatively less. Bioavailability is relatively high.
The suspension is not pleasing in
appearance.
The suspension is pleasing in
appearance.
131. Semisolid dosage forms meant for external application
Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories
The suppositories are also included in this category but it is a unit
dosage forms.
Semisolid dosage forms
132.
133. Ointment
Ointment are semisolid preparation meant for application to skin
or mucous membrane.
The ointments are mainly used for their protective or emollient
properties
It may be defined as a medicament or medicaments dissolved,
suspended or emulsified in ointment base.
There is no single ointment base which possesses all the
qualities of ideal ointment base, so it become necessary to use
more than one ointment base in the preparation of ointment.
134. Qualities of ideal ointment base
It should be inert, odourless & colourless & smooth.
It should be physically & chemically stable.
It should be compatible with the skin & with incorporated
medicaments.
It should be of such consistency that it spread & soften when
applied to skin with stress.
It should not retard healing of wound.
It should produce irritation or sensitization of the skin.
135. Classification of ointment base
Oleaginous bases
Absorption bases
Emulsion bases
Water soluble bases
136. Oleaginous base
These bases consist of water soluble hydrocarbons, vegetable oils,
animal fats & wax.
The constituents of hydrocarbon bases are soft paraffin, hard
paraffin & liquid paraffin.
The vegetable oils are mainly used in ointment to lower the melting
point or to soften the bases.
These bases serve to keep the medicaments in prolonged contact
with the skin & also act as occlusive dressings. They have a low
capacity to absorb water & are used chiefly for their emollient effect.
These bases losing their importance now a days for the many
reason.
137. Disadvantages of oleaginous
bases
They are greasy.
They are sticky & are difficult to remove both from skin & clothing.
They retain body heat which may produce an uncomfortable feeling
of warmth.
They do not help in the absorption of medicaments.
138. Absorption bases
These bases are generally anhydrous substance which have the
property of absorbing considerable quantities of water but still
retaining their ointment like consistency.
The absorption bases are of two type namely as
I) Non emulsified bases
II) Water in oil emulsion
Non emulsified bases absorb water & aqueous solutions producing
w/o emulsion. E.g. Wool fat, wool alcohol, beeswax & cholesterol.
Water in oil emulsions are capable of absorbing more water & have
the properties of non- emulsified bases. E.g. hydrous wool fat (
lanoline)
139. Emulsion bases
These bases are semisolid or have cream like consistency.
Both o/w or w/o emulsions are used as a ointment base.
The o/w emulsion base is more popular now days because ease of
application will easily achieved.
The w/o type of emulsion bases are greasy & sticky.
The emulsifying ointment is prepared from emulsifying wax, white
soft paraffin & liquid paraffin.
140. Water soluble bases
These are commonly known as greaseless ointment bases.
The water soluble bases consist of water soluble ingredients such
as carbowaxes ( polyethylene glycol polymer)
The carbowaxes are water soluble, non – volatile & inert substance.
Selection of appropriate carbowaxes is depend on their molecular
weight.
141. creams
These are viscous semisolid emulsions which are meant for
external use.
Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
In case of aqueous creams the emulsions are o/w type & it is
relatively non greasy. The emulsifying waxes are anionic, cationic
& non –ionic used. Generally polysorbate, triethanolamine soap
are used as emulsifying agent.
In case of oily creams w/o type & it is relatively greasy. The
emulsifying agent such as wool fat, wool alcohols, beeswax &
calcium soap is used.
The cream should be store in collapsible tube & supplied in well
closed container to prevent evaporation & contamination.
142. pastes
Pastes are semisolid preparations intended
for external application to skin.
The pastes are generally very thick & stiff.
They do not melt at ordinary temperature &
thus forms a protective coating over the area
where they are applied.
Pastes are differ from ointment as they
contain a high proportion of finely powdered
medicaments.
They are mainly used as a antiseptic,
protective, soothing dressings.
Pastes should be stored & supplied in
containers made of materials which do not
allow absorption or diffusion of content.
143. jellies
Jellies are transparent or translucent, non greasy, semi solid
preparations mainly used for external application to skin.
These are also used for lubricating catheters, surgical gloves &
rectal thermometer.
The substance like gelatin, starch, tragacanth, sodium alginate &
cellulose derivatives are used for the formulation of jellies.
Jellies are of three types namely as
Medicated jellies
Lubricating jellies
Miscellaneous jellies
145. Introduction
With the advancement of pharmaceutical sciences, a new concept
have evolved various modern dosage forms & methods of their
administration. Some of the modern dosage forms are
Implants
Films & strips
Liposome drug carriers
Controlled drug delivery modules
Erythrocytes
Nanoparticles
prodrugs
146. Implants
These are hypodermic tablets are placed under the skin by a minor
surgery in order to release drugs over prolonged periods of time.
Now the magnetically controlled implants have been developed
which can be opened or closed at will in order to release or stop the
drug.
These implants are placed at upper thigh at a depth of 5mm.
These implants are useful in hormone therapy.
147. Films & strips
These are meant for topical application for slow release of drug over
predetermined period of time. Films & strips are more popular these
days. They are sub categorized in to following types namely as
Zero order release films
Buccal strips
Spray bandages
148. Zero order release films
These are called as laminates & meant for topical application. E.g.
Nitroglycerine laminates are prepared by mixing propylene glycol
with about 1% carbopol resin. The mixture is neutralized with NaoH
solution & then 0.1% of nitroglycerin is added. It is then placed in
polythene sheet 5*5 cm & its edges are sealed by heat. It is then
placed on pressure sensitive adhesive sheet of 5.5 * 5.5 cm so that
it can be properly adhesive to skin. Such laminates release the drug
slowly into circulation for about 12 hours.
149. Buccal strips
The buccal & sublingual tablets are now replaced with buccal strips.
These strips consist of a thin absorbent base of fabrics, filter paper
& cotton etc.
The buccal strips are prepared by immersing a long piece of fabric
made from polyamide fibers into a molten mixture of carbowaxes &
dissolved or dispersed the drug.
The fabric is then cooled & cut into small pieces.
It should be contact with buccal mucosa for about 15 min. & then
removed & discarded.
150. Spray bandage
These bandage are prepared by spraying the solution of drug in
polylactide (polymer of lactic acid anhydride)
A solution of purified lactide polymer is made in chloroform.
It is then packed in aerosol container having suitable propellant.
When these solution sprayed then it will be a comfortable bandage
which can simply washed of with warm water.
151. Liposome drug carriers
These are several carriers in our body which transport both to an
other like as enzymes, proteins etc.
These are phospholipids which can transport both hydrophilic &
hydrophobic drugs.
The large multilamellar vesicles (LMV), small unilamellar vesicles
(SUV), large unilamellar vesicles (LUV) are some of the liposome's
known today.
152. Applications
Used in diseases caused by intracellular parasites. E.g. malaria,
tuberculosis & amoebiasis.
It entrapped insulin is active orally & can be replaced by IM
administration of insulin.
It can be used to transport functional DNA/RNA molecules into cell.
It can be used to transport radio pharmaceuticals & immunological
products.
Liposomal daunomycin has longer duration of action than free
daunomycin which is used in the treatment of neoplasia.
153. Controlled drug delivery
modules
These are the device which are formed by embedding the drug
within a polymeric matrix so that it gets released slowly to the body
over a long period of time.
It will formed drug – polymer complex & may be formulated in to
tablet, capsule or any other suitable formulation.
These modules are punctured before administration with leaser
beam to make a small orifice for release of the drugs.
The drugs is released from these modules by diffusion, osmosis or
chemical reactions.
These are applied to skin, implanted subcutaneously or inserted
into various body cavities.
154. Erythrocytes
Erythrocytes are tried in order to achieve controlled release of
drugs.
The life span of erythrocytes are 120 days.
It can allow a drug to circulate in the body for long period of time
which help slow release of the drugs in to serum.
Released erythrocytes are prepared by putting them in to a
hypotonic medium. So that they can easily swollen.
The aqueous solutions of the drug is added to the medium so that
drugs gets in to erythrocytes through open pores.
When isotonicity is adjusted the erythrocytes shrink, thus
encapsulating the drug with in them. These erythrocytes may be
suspended in normal saline solutions for preparing injections.
155. Applications
Released erythrocytes of urease have been used in kidney failure to
degrade serum urea.
Released erythrocytes of asparaginase have shown good result in
asparaginase dependent leukemia.
Released erythrocytes of methotrexate & adrianycin have been tried
in cancer therapy.
Released erythrocytes of prednisolone have shown good result to
prolong the anti-inflammatory action.
156. Nanoparticles
It is based on colloidal drug delivery system.
The particles size of this system is in nanometer range (200 – 500
mm)
The system consist of a drug & carriers to deposit the drug at target
site.
The carriers used are naturally occurring macromolecules like
human serum albumin, bovine serum albumin, & other substances
like gelatin, casein & ethylcellulose.
157. Applications
Flourescein isothinocyanate (FITC) nanoparticles have been used
to incorporate cytotoxic agent into tumor cell in cancer
chemotherapy.
Nanoparticles along with biological maker like immunoglobulin can
be used to target the drugs to very specific site.
158. Prodrugs
The compound which undergo biotransformation before showing
desired pharmacological activity are called prodrugs or proagents.
Prodrugs are generally the ester or amides of parent drugs.
These are useful to improving the stability, solubility, bioavailability
of drugs, masking the unpleasant taste & odour of the parent drug &
reducing the toxicity
159. Applications
Choramphenicol palmitate, the prodrug of chloramphenicol is used
in the preparation of pediatrics suspension because it has no bitter
taste.
Procaine penicillin G & benzathine penicillin G are prodrugs of
penicillin G which shows resistance to hydrolysis as compared to
the parent drug.
Cindamycin 2- phosphate the prodrug of cindamycin has no bitter
taste of parent drug.
