Topicals

Question 1

State at least FOUR types of ointment bases.

Answer 1

Four from hydrocarbon, fats and fixed oils, silicone, absorption,
emulsifying and water-soluble.

Question 2

For TWO ointment bases, write a suitable formulation.

Answer 2

Paraffin Ointment BP – HP(3%), WSP(90%), White Beeswax (2%),
(hydrocarbon base) cetostearyl alcohol (5%).
Simple Ointment BP – Wool fat (5%), HP (5%), cetostearyl alcohol (5%),
(absorption base) yellow or WSP (85%).
Emulsifying Ointment BP – emulsifying wax*(30%),WSP (50%),LP (20%)
(emulsifying bases) *cetostearyl alcohol/sodium lauryl sulphate
(Anionic Emulsifying Wax BP)
Macrogol Ointment BP – PEG 4000 (40%), PEG 400 (60%).
(water-soluble base)

Question 3

Describe the mechanism by which ointments emolliate the skin.

Answer 3

Ointments soften or melt at body temperature, forming an occlusive film
on the surface of the skin. This prevents transepidermal water loss
causing the skin to hydrate.

Question 4

What is the functions of skin?

Answer 4

protection from pollution, temperature, humidity & radiation.

a protection for internal organs.
- a limiter for the passage of chemicals.
- a stabiliser for blood pressure & temperature.
- a mediator of heat, cold, touch and pain.
- expresses the emotions of fear,anger, embarrassment, and anxiety.
- an indicator of human characteristics such as colour, hair, odour & texture.

Question 5

What are the three main regions of skin?

Answer 5

Epidermis, Dermis, Subcutaneous tissue

Question 6

Features of the epidermis

Answer 6

multilayered - thickness varies - palms and soles 0.8mm and eyelids are 6 micrometres

Stratum corneum is the dead , dense and impermeable surface layer

Swells several-fold in water (maceration)

Question 7

Features of the Dermis

Answer 7

3-5cm thick
Matrix of connective tissue woven from fibrous proteins (collagen, elastin and reticulin)
nerves, blood vessels and lymphatics traverse the matric and skin appendages pierce it

Question 8

What are the different skin appendages?

Answer 8

Eccrine sweat glands
apocrine Sweat glands
Sebacious glands
Hair follicles

Question 9

What are skin appendages?

Answer 9

The skin appendages include sweat glands, nails, and the pilosebaceous unit of the skin, comprised of the hair shaft, hair follicle, sebaceous gland, and arrector pili muscle — these appendages derive from a down growth of the epidermis beginning in the third month of fetal life.2

Question 10

What are eccrine sweat glands?

Answer 10

Produce sweat of pH 4.0-6.8
Secrete drugs,protein, antibodies and antigens
AID HEAT CONTROL

Question 11

What are Apocrine sweat glands?

Answer 11

Develop at the pilosebacious follicle
Milky or oily secretion contain proteins, lipids, lipoproteins and saccharides
surface bacteria metabolise this (initially) odourless liquid to produce body smells

Question 12

What are sebacious glands?

Answer 12

Sebacious glands open into hair follicles
they produce sebum from cell disintegration
contain glycerides, fatty acids, cholesterol and its esters, wax esters and squalene

Question 13

What are hair follicles?

Answer 13

Develop over all skin except lips, palms and soles

Question 14

What is the problem and treatment for the Stratum Corneum? adv and disadv treatment

give eamples of non proprietary and proprietary

Answer 14

To hydrate the horny layer
To stimulate ‘sloughing’ (keratosis) or exfoliation
Emollients are used because
- Sooth, smooth and hydrate the skin.
- Indicated for all dry or scaling disorders
- As the effects are short-lived, they are applied frequently
- Useful in dry and eczematous disorders.
- Have limited use in the treatment of psoriasis

Non-proprietary: Aqueous Cream BP, White Soft Paraffin BP,
Liquid and White Soft Paraffin Ointment NPF,
Emulsifying Ointment BP, urea* etc.

Proprietary: Neutrogena™, Cetroben™, Ultrabase™, *Neutraplus™

Question 15

What is the treatment for hyperhydrosis of sweat glands?

Answer 15

Reduce hyperhydrosis of the sweat glands

eg with antiperspirants containing aluminium salts - aluminium chloride hexahydrate 20% alcohol solution (Anhydrol Forte™)

Question 16

Treatment of acne

Answer 16

Treatment of acne (mild to moderate)

eg  topical exfolients such as salicylic acid, benzoyl peroxide,
      tretinoin (retinoic acid), isotretinoin and azelaic acid.
      - Brevoxil™ is an aqueous cream containing benzoyl peroxide 4%.

      topical antibiotics containing erythromycin and clindomycin.

Question 17

Treatment of fungal diseases?

Answer 17

Treatment of fungal diseases (localised)

eg dermatophytoses of the scalp, body, groin, hand, foot or nail.
- topical imidazoles include clotrimazole, econazole, miconazole, keroconazole and sulconazole (also effective against Candidiasis).

Question 18

Treatment of male pattern baldness

Answer 18

Treatment of male pattern baldness

eg  Finasteride™, Minoxidil™

Question 19

Treatment of conditions with the epidermus/ dermus

Answer 19

efficient delivery of drug to the receptor
use of ‘pro-drug’ (release active when at target receptor)
Antiinflammatories - steroidal and non-steroidal (NSAIDs). Non-proprietary: Ketoprofen gel, Piroxicam gel. Proprietary: Oruvail™ gel, Feldene™ gel, Fenbid™ (ibuprofen), Voltarol™(diclofenac).

Anaesthetics - relief of local pain (*can cause hypersensitivity). Benzocaine, amethocaine, lignocain.

Antipruritics*- alleviate itching of pruritis in eczema. Calamine (often ineffective), Eurax™(crotamiton), Xepin™ (doxepin hydrochloride 5%).

Antihistamines* - Effective against insect bites & stings (not eczema). Anthisan™(mepyramine), Wasp-Eze™ (antazoline).

UV (PUVA) and - The psoralens/with UV-light mitigate psoriasis.
light (PDT) therapies - Aminolaevulinic acid/with light treats skin cancer.

Question 20

How to formulate a liquid?

Answer 20

Simple soaks/baths

-  an active ingredient in aqueous solution
    or suspension.

-  gums and gelling agents may vary the consistency.

-  Oilatum™ emollient bath additive deposits
    a layer of liquid paraffin/wool alcohols
    on stratum corneum. 

-  Oilatum™ Plus contains benzalkonium chloride
   and triclosan as parasiticides/antiseptics.

Question 21

Formulation of ointments?

Answer 21

Greasy, semisolid preparations

-  hydrocarbon bases act as emollients and inc hydration of the stratum cornea. Liquid and soft paraffins (VASELINE Vicks VAPOUR RB, WHITE SOFT PARAFFIN AND PETROLEUM JELLY.

-  fats and fixed oil bases  non volatile plant/animal origin

-  silicone bases , water

-  absorption bases, water and oil emulsions fatty and water compounds readily absorb water

-  emulsifying bases - water and oil emulsions - surfactants with fatty alcohols sitosterol high HLB.

-  water-soluble bases. non greasy easily removed from skin oil and water emulsions

Question 22

Formulation of liniments and lotions

Answer 22

Liniments
- alcoholic or oily solutions or emulsions.

• do not apply to broken skin. (alcohol will sting)
• massaged into the skin as counterirritants.
• can contain methyl salicylate or camphor. (essential oils)

Lotions

-  aqueous solutions/suspensions.

-  evaporation of water/alcohol cools & soothes 		   	    the skin. takes away heat from skin

-  can be dilute O/W emulsions. lotions

Question 23

Formulation of oily creams?

Answer 23

Oily creams

contain a W/O emulsifying agent

wool fat, wool alcohols, fatty acid sorbitan esters
and their salts (eg calcium).

Question 24

Formulation of aqueous creams?

Answer 24

Aqueous creams

• contain an O/W emulsifying agent
• emulsifying waxes/alkali salts of fatty acids
• polyethylene glycol derivatives of sorbitan esters.

Question 25

Give an example of solid/semi-solid, what is it used for? PASTE

Answer 25

Zinc and salicylic acid paste BP (Lassar’s Paste) is a
non-proprietary paste for the treatment of hyperkeratotic skin disorders, warts and calluses, scalp conditions and fungal nail infections.

Contains: zinc oxide (24%), salicylic acid (2%),
starch (24%), white soft paraffin (50%).

Zinc oxide - a mild astringent and topical protectant with some antisceptic action

salicylic acid - exfolient

starch - binder and thickening agent

white soft paraffn - emollient

Question 26

Give an example of solid/semi-solid, what is it used for? OINTMENT

Answer 26

Emulsifying Ointment BP is a mixture of emulsifying wax – cetostearyl alcohol/sodium lauryl sulphate - (30%),
white soft paraffin (50%) and liquid paraffin (20%).
It is readily miscible in water and forms an ‘emulsifying base’
for many topical preparations. On its own, it is indicated for
all dry or scaling disorders.

cetostearyl alcohol: emollient/ emulsifier/viscosity enhancer.

sodium lauryl sulphate: anionic surfactant/wetting agent skin penetrant/emulsifying agent.

white soft paraffin: emollient

liquid paraffin : emollient