Dosage forms and formulations

Introduction for Dosage forms

1. .
Introduction To Dosage
Forms
And Formulations
Varalakshmi
MSc,DCR

2. Introduction
What is the difference between a chemical and a drug?
Chemical: A substance composed of chemical elements or obtained by
chemical process (review chemistry)
Drug: An agent intended for use in the diagnosis, mitigation,
treatment, cure, or prevention of disease in man or other animals.

3. Dosage Forms
Definition:Dosage form means by which drug molecules
are delivered to sites of action within the body.
Drug substances are seldom administered alone, but
rather as a part of a formulation in combination with
one or more non medical agents that serve varied and
specialized pharmaceutical functions.

4. Pharmaceutical Ingredients
can serve several functions
solubilize
suspend
thicken
dilute
emulsify
stabilize
preserve
color
Flavor

5. Why use dosage forms?
Mechanism for the safe and convenient delivery of accurate dosage
Protection of a drug substance from destructive influences of
atmospheric oxygen or humidity
Protection from influence of gastric acid after oral administration
To mask taste of offensive drugs.

6. Why use dosage forms?
To provide liquid preparations of substances that are
either insoluble or unstable
To provide clear liquid dosage forms
To provide time-controlled release of drugs
To provide optimal topical administration

7. Why dosage forms?
To provide for the insertion of a drug into one of the
body’s orifices
Provide for placement of drugs into the blood stream
Provide for lung inhalation of drugs

8. DIFFERENT TYPES
SOLID DOSAGE FORMS
POWDERS
TABLETS
CAPSULES
SPANSULES (coated pellets in capsule)

9. SEMISOLID DOSAGE FORMS
OINTMENTS
CREAMS
PASTES
GELS
JELLIES
SUPPOSITORIES
PESSARIES

10. LIQUID DOSAGE FORMS
☺SOLUTIONS
ORAL SOLUTIONS
PARENTERALS
☺SUSPENSIONS
☺EMULSIONS

11. INHALATIONS
AEROSOLS

12. A powderis a dry, bulk solidcomposed of a large
number of very fine particles that may flow freely when
shaken or tilted.

13. A tabletis a mixture of active substances and
excipients, usually in powderform, pressed or
compacted into a solid.

14. Capsule-A small gelatinous case enclosing a dose of
medication
made both from gelatineand from plant-based gelling
substances like carrageenansand modified forms of starchand
cellulose.

15. An ointmentis a viscous semisolid
preparation used topically on a variety
of body surfaces. These include the
skinand the mucus membranesof the
eye(an eye ointment), vagina, anus,
glansand nose. An ointment may or
may not be medicated.


16. Creamsare semi-solid emulsions, that is mixtures of oil
and water.
They are divided into two types:
oil-in-water (O/W) creams which are composed of small
droplets of oil dispersed in a continuous aqueousphase,
and
water-in-oil (W/O) creams which are composed of small
droplets of water dispersed in a continuous oily phase

17. pasteis basic pharmaceutical form. It consists of fatty
base (e.g. petroleum jelly) and at least 25% solid
substance (e.g. zinc oxide).
Examples include starchpastes, toothpaste

18. Gel-colloidalsystem in which a porous
network of interconnected nanoparticles
spans the volume of a liquid medium
A suppositoryis a drug delivery system that
is inserted either into the rectum(rectal
suppository), vagina(vaginal suppository) or
urethra(urethral suppository) where it
dissolves

19. A pessaryis a small plasticor siliconemedical device or
form of pharmaceuticalpreparation which is inserted
into the vaginaor rectumand held in place by the
pelvic floormusculature

20. a solutionis a homogeneousmixture
composed of two or more substances. In
such a mixture, a soluteis dissolved in
another substance, known as a solvent.
a suspensionis a colloidal dispersion
(mixture) in which a finely-divided
species is combined with another
species, with the former being so finely
divided and mixed that it doesn't rapidly
settle out.

21. An emulsionis a mixture of two immiscible
(unblendable) substances. One substance (the dispersed
phase) is dispersedin the other (the continuous phase).

22. An inhaleror pufferis a medical
device used for delivering medication
into the body via the lungs
Medication is most commonly stored in
solution in a pressurized canister. The
canister is attached to a plastic, hand-
operated actuator.
The standard metered-dose inhaler
(MDI) on activating releases a fixed
dose of medication in aerosolform

23. Liniment, is a medicated topical preparation for application to the
skin. Preparations of this type are also called balm. less viscous
than an ointmentor cream) applied with friction.
Lotionis a liniment that is applied without friction

24. An enema(plural enemataor enemas) is the procedure
of introducing liquids into the rectumand colonvia the
anus.

25. A transdermal patchor skin patchis a medicated
adhesivepatchthat is placed on the skinto deliver a
time released doseof medication through the skin and
into the bloodstream.

26. CONSTITUENTS OF A DOSAGE FORM
DRUG
VEHICLE
PHARMACEUTICAL EXCIPIENTS

27. TABLETS
Diluents and fillers (lactose)
Binders (starch)
Antiadherents or lubricants (Mg.stearate,Ca.stearate)
Disintegrating agents (starch)
Colouring agents (amaranth solution, caramel, cupric
sulfate (blue), ferrous sulfate (red), zinc oxide (pink).
Sweetening agents (Sucrose, saccharin, aspartame)
Flavouring agents (cocoa, raspberry, orange, Cinnamon)
PHARMACEUTICAL EXCIPIENTS

28. SEMISOLID DOSAGE FORMS
–Pharmaceutical bases

29. SOLUTIONS
Solvents to dissolve the drug substances
Flavors and sweeteners
Colorants
Preservatives
Stabilizers

30. TABLETS
SOLID UNIT DOSAGE FORM OF MEDICAMENT/S WITH
SUITABLE EXCIPIENTS INTENDED FOR ORAL USE

31. ADVANTAGES:
Tablets are most widely used solid dosage forms because of following
advantages
Easy to carry
Easy to swallow
Attractive in appearance
Unpleasant taste masked by sugar coating
Unidosage accuracy
Prolonged stability
Incompatibilities of medicaments are less
Cost of production –low

32. DISADVANTAGES
Drugs of amorphous nature-cannot be compressed
Delayed action
Unconscious patients-not suitable
Swallowing difficult-children

33. ESSENTIAL QUALITIES OF
A GOOD TABLET
Accurate &uniform in weight
Drugs-uniformly distributed
Size & shape-easy administration
Not too hard-disintegration
No incompatibilities
Chemically & physically stable-storage
No breakage-transportation
No crumble-hands
Attractive in appearance
No manufacturing defects
Economical -production

34. IDEAL CHARACTERISTICS OF
EXCIPIENTS
Non toxic and acceptable to
regulatory authorities
Must be commercially available in
an acceptable grade
Cost must be low
Physiologically inert
Physically and chemically stable
Free of microorganisms
Color compatible
Must not have effect on bio-
availability

35. DILUENTS
DILUENTS/FILLERS DESIGNED TO
INCREASE THE BULK
LACTOSE
SPRAY DRIED LACTOSE
STARCH
MANNITOL
DEXTROSE
SORBITOL
MICROCRYSTALLINE CELLULOSE

36. BINDERS AND
ADHESIVES
To form granules or promote cohesive
compacts for directly compressed
tablets
Acaciaand tragacanth gums
Gelatin
Starch paste
Liquid glucose
Modified natural polymers
(Poly vinyl pyrrolidone)

37. DISINTEGRANTS
Facilitate break up or disintegration
Mechanism
Draws water in to tablet ,swelling and
causing tablet to burst apart.
Starch USPand various starch
derivatives
Modified starches are primogel and
explotab
Pregelatinized starchesare employed

38. Clays such as veegum HVand
bentonite(10%)
Ac-Di-Solis commonly used
among cellulose class.-cross
linked CMC
PVP (cross linked polymer)
DISINTEGRANTS

39. LUBRICANTS,
ANTIADHERENTS AND
GLIDANTS
Lubricants reduce friction between
tablets and dye surface during
ejection of the tablet
Antiadherents reduce sticking or
adhesion of tablets to punches
Glidantsto promote flow properties

40. Hydrocarbon oils: mineral oil
Stearic acidand its salts
Talc
Colloidal silica, talc, magnesium
stearate, starchand its
derivatives –antiadherents
Glidants:corn starch 5-
10%,colloidal silicasuch as Cab-
O-Sil ,syloid ,or aerosil in 0.25-
3% conc.

41. COLOURING AGENTS
Use of colours and dyes in tablets
Disguising of off-color drugs
Product identification
Production of a more elegant product
FD&C dyes and D&C dyes-applied
as solution in granulating agent-
and the Lake form of these dyes
A FD&C lakeis a pigment consisting
of a substratum of alumina
hydroxide on which dye is adsorbed
or precipitated

42. SWEETENING AGENTS
Limited to chewable tablets
Mannitol is 72% as sweet as
sucrose
Saccharin
Asparatame

43. FLAVOURING AGENTS
Usually limited to chewable tablets, lozenges &
effervescence tablets
Volatile oils, volatile substances & fruit flavors
Oil or water soluble liquids or dry powders
Oil soluble carriers –soya bean and other edible
oils
Water soluble carriers-water, ethanol ,
propylene glycol, glycerine and emulsifiers
Dry carriers include –maltodextrins, cornsyrup
solids, modified starches , gumarabic , salts,
sugars and whey protein.
Water soluble : less stable
Flavour range: 0.5 to 0.75

44. CAPSULE
Solid unit dosage form of medicament in which the drug(s) is
enclosed in a practically tasteless , hard or soft soluble container or
shell made up of a suitable form of gelatin

45. ADVANTAGES
Tasteless, odorless
Easily administered
Attractive in appearance
Easy to handle and carry
Economical
Drugs having unpleasant odour & taste---tasteless shell

46. DISADVANTAGES
Hygroscopic drugs
Concentrated solutions which require previous dilution

47. TYPES OF CAPSULES
HARD CAPSULES
SOFT CAPSULES

48. HARD CAPSULES
DIFFERENT SIZES
000 00 0
1
2
3
3
4
5
CAPACITY VARIES:600mg to 30mg

49. FILLING POSSIBILITY

50. DIFFERENT SHAPES
OBLONG ,OVAL & ROUND

51. SCHEDULE Y
APPENDIX-I
Data to be submitted along with the application to conduct
clinical trials / import/ manufacture of new drug for
marketing in the country .

52. 1.Introduction
2.Chemical and pharmaceutical
information
2.1Information on active ingredients
Drug information (Generic name, Chemical name or INN)

53. 2.2Physicochemical data
a.Chemical name and structure
Empirical formula
Molecular weight
b.Physical properties
Description
Solubility
Rotation
Partition coefficient
Dissociation constant

54. 2.3Analytical data
Elemental analysis
Mass spectrum
NMR spectrum
IR spectra
UV spectra
Polymorphic identification
2.4 Complete monographic
Specification include
Identification
Identity/quantification of impurities
Enantiomeric purity
Assay

55. 2.5 Validations
Assay method
Impurity estimation method
Residual solvent/other volatile impurities
2.6 Stability studies(addnldetails in app IX)
Final release specification
Reference standard characterization
Material safety data sheet

56. 2.7Data on formulation
Dosage form
Composition
Master manufacturing formula
Details of the formulation(including active ingredients)
In process control check
Finished product specification
Excipient compatibility study
Validation of the analytical method

57. Comparative evaluation with international
brand(s) or approved Indian brands,
If applicable
Pack presentation
Dissolution
Assay
Impurities
Content uniformity
pH

58. Force degradation study
Stability evaluation in market intended pack at
proposed storage conditions
Packing specifications
Process validation