Pharmaceutical Dosage Forms And Drug Delivery System

1. Reporters:
Sheila Mae Ballicud
Anne Valerie Villalon

2. • are semisolid dosage forms intended for
topical application.
• may be applied to the skin, placed on the
surface of the eye or used nasally, vaginally
and rectally.

3. • 1.partly solid; having a rigidity and viscosity
intermediate between a solid and a liquid
• Dermatological preparations intended to apply
externally on the skin to produce local or systemic
effect.

4. • is designed to deliver drug into the skin in
treating dermal disorder, with the skin as the
target organ.

5. • is designed to deliver drugs through the skin
to the general circulation for systemic effects,
with the skin not being the target organ.

6. • are semisolid preparations
intended for external
applications to the mucous
membranes.
• may be medicated or not.

7. • are generally classified by the USP into 4
groups:
1. Oleaginous bases
2. Absorption bases
3. Water-soluble bases
4. Water-removable bases

8. • Water insoluble
• Not water washable
• Can't absorb water
• Oily, occlusive, lack cosmetic appeal

9. • also termed as Hydrocarbon
bases
• an application to the skin, they
have an:
–emollient effect
–occlusive dressings; and
–protect against escape of
moisture
Examples of
Hydrocarbon bases:
• Petrolatum
• White Petrolatum
• Yellow Ointment
• White Ointment

10. • is a purified mixture of semisolid hydrocarbons
obtained from petroleum
• also known as yellow petrolatum and petroleum
jelly
• use as protectant in toenail fungus, genital rashes
(non-STD), nosebleeds, diaper rash, and chest
colds
• a commercial product is vaseline

11. • is a purified mixture of semisolid
hydrocarbons from petroleum that has been
wholly or nearly decolorized.
• the same purpose as petrolatum
• a.k.a. white petroleum jelly
• commercial product is white vaseline

12. • has the following formula for the preparation of 1000g:
- Yellow Wax 50g
- Petrolatum 950g
• Yellow wax is the purified wax obtained from the
honeycomb of the bee Apis mellifera
• heals a wound and helps to improve damaged skin
• a.k.a. simple ointment, it has a slightly greater viscosity
than plain petrolatum.

13. • differs from yellow ointment by substitution of
white wax and white petrolatum in the formula.
• used to treat extremely dry, scaly or callused
skin

14. • Water insoluble
• Not water washable
• Can absorb water
• Anhydrous
• Oily, occlusive, lack cosmetic appeal

15. • may be used as emollients
• not easily removed from the skin with water
washing since the external phase of the
emulsion is oleaginous.

16. • are of two types:
– those that permit the
incorporation of aqueous solutions in the
formation of water-in-oil emulsions. (e.g.
hydrophilic petrolatum)
– those that are water-in-oil emulsions and
permit the incorporation of additional
quantities of aqueous solutions (e.g. Lanolin)

17. • Softening and moisturizing dry, cracked, or
irritated skin
• Water-loving petrolatum
• A mixture of cholesterol, stearyl alcohol, and
white wax, in white petrolatum; used as an
absorbent ointment base and topical skin
protectant.

18. • obtained from the wool of sheep
• is a purified, wax-like substance that has
been cleaned, deodorized and decolorized.
• contains not more than 0.25% of water
• used as base in ointments

19. • oil-in-water emulsions resembling creams in
appearance
• often called water-washable bases because
the external phase of the emulsion is aqueous.
• may be diluted with water or aqueous
solution (e.g. hydrophilic ointments)

20. • water-in-oil emulsion consisting of
methylparaben, propylparaben, sodium lauryl
sulfate, propylene glycol, stearyl alcohol, white
petrolatum, and purified water; used as an
ointment base.

21. • do not contain oleaginous components.
• completely water-washable and often
referred to as greaseless
• mostly are used for the incorporation of solid
substances
• prototype example is polyethylene glycol
ointment.

22. • is a polymer of ethylene oxide and water represent
by the formula H(OCH2CH2)nOH in which
represents the average number of oxyethylene
groups.
• having an average molecular weight below 600 is
clear, colorless liquid with molecular weight
above 1000 are waxlike white materials, those
with molecular weights in between are semisolids.

23. • Desired releases rate of the drug substance from
the ointment base
• Desirability of topical or percutaneous drug
absorption
• Desirability of occlusion of moisture from the skin
• Stability of the drug in the ointment base

24. • Effect of the drug on the consistency or other
features of the ointment base
• Desire for a base easily removed by washing with
water
• Characteristics of the surface to which it is
applied

25. • STABILITY
• PENETRABILITY
• SOLVENT PROPERTY
• IRRITANT
• EASE OF APPLICATION AND
REMOVAL

26. • prepared by 2 general methods
–a. incorporation
–b. fusion
• depending primarily on the nature of the
ingredients

27. • If the components of an ointment react with metal;
hard rubber, spatulas may be used.
• The ointment is prepared by thoroughly rubbing
and working the components together on the hard
surface until the product is smooth and uniform.
• Geometric dilution is used until all portions of the
powder and base are combined thoroughly and
uniformly blended.

28. • It is often desirable to reduce the particle size
of a powder or crystalline material before
incorporation into the ointment, so it will not
be gritty.

29. • This may be done by levigating or mixing the solid
material in a vehicle in which it is insoluble to make a
smooth dispersion.
–levigating agent should be physically and
chemically compatible with the drug and base
•mineral oil for bases in which oils are the
external phase
•glycerin for bases in which water is the external
phase

30. • The amount of levigating agent used should
be about equal in volume to the solid
material.
• Mortar and pestle is used for levigation. This
allows both reduction of particle size and the
dispersion of the substance in the vehicle.
• After levigation, the dispersion is
incorporated into the oinment base by
spatulation method or with mortar and pestle

31. • Liquid substances or solutions of drugs are added
to an ointment only after due consideration of an
ointment base's capacity to accept the volume
required.
• Alcoholic solutions of small volume maybe added
quite well to Oleaginous vehicles or emulsion
bases.

32. • All or some of the components of an ointment are
combined by being melted together and cooled
with constant stirring until cogealed.
• Medicated ointments and ointment base
containing components as beeswax, paraffin,
stearyl alcohol, and high molecular weight PEG,
which do not lend themselves well to mixture by
incorporation, are prepared by fusion.

33. • Microbial content
• Minimum fill
• Packaging
• Storage
• Labeling

34. • Preparations with water tend to support microbial growth
• not require to be sterile
• Examples are methylparaben, propylparaben, phenols,
benzoic acid, sorbic acid, and quarternary ammonium
salt.
• Must be free from P.aeruginosa, S.aureus, yeast and
molds
• Strict compliance to guideliness is required

35. • Determination of the net weight or volume of the
contents of filled containers to ensure proper
contents compared with the labelled amount.

36. • Ointments and semisolids are to be place in
large mouth ointments jars or metal and
plastic tube.
• To be stored in a cool place and tightly
closed container to prevent contamination.
(room or refrigerated temperatures)
• Labels must include the type of base used.

37. • Viscosity and in vitro drug release
• Diffusion cell studies to determine the drug's
release profile from the semisolid product.

38. • Semisolid dosage preparation containing one or
more medicinal agents dissolved in either a:
–Water-in-oil emulsion
•Cold cream
–Oil-in-water
•Vanishing cream
•Contains large percentage of water, stearic
acid and other oleaginous components

39. • Are semisolid system consisting of dispersions of
small or large molecules in an aqueous liquid vehicle
rendered jellylike by the addition of a gelling agent.
• Examples of Gelling agents:
–synthetic macromolecules (carbomer 934)
–cellulose derivatives (carboxymethyl cellulose)
–natural gums (tragacanth)
• Sometimes called Jellies

40. • Single-Phase Gels - macromolecules are
uniformly distributes throughout a Liwuid with no
apparent boundaries.
• Two-Phase Gels/Magma Gels - mass consisting
of floccules of small distinct particles

41. To contain a drug substance, we use:
• Solvents - alcohol and propylene glycol
• Antimicrobial preservatives - methyl
paraben, propyl paraben and
chlorhexidinegluconate
• Stabilizers - edetate disodium

42. • Designed to deliver a drug systematically
• Accomplished by penetrating enhancers: dimethyl
sulfoxide, ethanol, ethylene glycol, glycerin, PEG,
urea, dimethyl acetamide, sodium lauryl sulphate,
spans, tweens, terpents, etc.
• Common compounded: fluroniclechitin

43. • Semisolid preparation intended for application to
the skin.
• Contain a larger proportion of solid materials
(such as 25%) than ointments and therefore are
ointments.
• Prepared in the same manner as ointments, by
desired mixing or the use of heat
• Not suited for application to hairy parts of the
body.

44. • Solid or semisolid adhesive masses spread
upon a backing material of paper, fabric,
moleskin or plastic.
• Applied to the skin to provide prolonged
contact at the site.

45. • are plastic masses containing gelatin (15%), glycerin (40%),
water (35%) and an added medicina substance (10%) ZnO
• They are prepared by:
–softening the gelatin in the water for about 10 minutes,
heating on a steam bath until gelatin is dissolved
–Adding the medicinal substance mixed with the glycerin
–Allowing the mixture to cool with stirring until congealed
• Applied to the skin for long-term residence

46. • Topical Dermatological
Product
– are packaged in either jars, tubes, or
syringes whereas opthalmic, nasal,
vaginal and rectal semisolid products
are almost always packaged in tubes or
syringes.

47. • Are filled on small scale in the pharmacy by
carefully transferring the weighed amount of
ointment into the jar with a spatula.

48. • Are filled from the open back end of the tube,
opposite from the cap end.
• Can also be filled using a “Caulking gun” system
where the semisolid is filled into the chamber and
the product is delivered into the tube.

49. • Can be filled either by drawing the semisolid
into the barrel using the plunger, or by
removing the plunger and filling through the
back end of the syringe.

50. • used for topical application to the perianal area
and for insertion within the anal canal.
• used to treat local conditions
–anorectal pruritus
–inflammation; and
–pain and discomfort associated with
hemorrhoids

51. • vaginal surface is lined with squamous epithelium
produced by various underlying glands
• used to treat vulvovaginal infections
–vaginitis
–conditions of endometrial atrophy
–contraception with spermatocidal agents

52. • Semisolid dosage forms - to deliver a
drug to the surface of the skin or to be
absorbed into the surface of the skin.