TOPIC SUPPLY WORK MECHANISM

General pharmacokinetics

Topical pharmacokinetic preparations generally describe the course of active ingredients in

certain concentrations applied to the skin and then absorbed into the skin layer, then
distributed systemically. This mechanism is important to understand to help choose topical
preparations to be used in therapy. The travel of topical preparations after application to the
skin is illustrated in the following picture:

In general, topical preparations after application are passed through three compartments,
namely: the surface of the skin, the stratum corneum, and healthy tissue. The stratum
corneum can act as a reservoir for the vehikulum where a number of elements in the drug are
still in contact with the surface of the skin but have not penetrated but cannot be removed by
rubbing or being erased by clothing.

The topical vehiculate element can undergo evaporation, then the active substance binds to
the skipped layer as in the epidermis, dermis. Under certain conditions the drug preparations
can carry active ingredients through the hypodermis. Meanwhile, the active ingredient in
topical preparations will be absorbed by the vascular skin of the dermis and hypodermis.
Pathway for topical preparation

Penetration of topical preparations passes through several types of paths as shown in the
following figure:

When topical preparations are applied to the skin, 3 interactions occur:

1. Solute vehicle interaction: the interaction of active ingredients dissolved in the vehicle.
Ideally the active substance dissolved in the vehicle remains stable and easily released. This
interaction already exists in the preparation.

2. Vehicle skin interaction: an inter-action vehicle with the skin. At the beginning of the
application of the skin reservoir function to the vehicle.

3. Solute Skin interaction: interaction of dissolved active ingredients with the skin (lag phase,
rising phase, falling phase).

a. Transepidermal penetration

Transepidermal penetration can be intra-lullular and intracellular. Intercellular penetration is

the dominant pathway, the drug will penetrate the stratum corneum through the intercellular
space in the lipid layer that surrounds the corneocyte cell. Diffusion can occur in the protein
lipid matrix of the stratum corneum. After successfully penetrating the drug stratum corneum
will penetrate the epidermal layer as soon as it is underneath, until it finally diffuses into the
capillary vessels.
Intracellular penetration occurs through fusion of drugs through the stratum wall of
corneocytes cells that die and also across the lipid matrix of the start corneum protein, then
passing it to cells in the lower layers to the capillaries below the basal epidermis and diffuses
into capillary.

b. Transfollicular penetration

Follicular penetration analysis appears after in vivo experiments. The experiment showed that
small molecules such as caffeine can penetrate not only through corneum cells, but also
through the follicular route. The drug diffuses through the cracks of the hair follicles and also
the sebaceous glands to then diffuse into the capillaries.

General absorption of topical preparations

When a preparation is applied to the skin, absorption will go through several phases:

a. Phase lag

This period is when the preparation is applied and has not passed through the stratum
corneum, so that at this time no active ingredient in the blood vessels has been found.

b. Rising phase

This phase begins when some preparations penetrate the stratum corneum, then enter the
dermal capillary, so that it can be found in blood vessels.

c. Falling phase

This phase is the release phase of the active ingredient from the surface of the skin and can be
carried to the capillary dermis.

The absorption of topical preparations is generally influenced by various factors:

1. The active ingredients mixed in certain carriers must blend into the surface of the skin in
sufficient concentration.

2. The concentration of the active ingredient is an important factor, the amount of drug
absorbed percutaneously perunit surface area each time period, increasing as compared with
the increase in drug concentration in a carrier.
3. The use of medicinal ingredients on a wider surface will increase the amount of the drug
absorbed.

4. Absorption of active ingredients will increase if the carrier easily spreads to the surface of
the skin.

5. Whether there is a wrapper or the like when the preparation is applied. In general, rubbing
the preparation will increase the amount of active ingredients absorbed.

7. Percutaneous absorption will be greater if topical preparations are used on skin with a thin
horn layer.

8. In general, the longer the preparation attaches to the skin, the more likely it is to be
absorbed.

In intact skin, the main way of penetrating preparations through the epidermal layer, is better
than through hair follicles or sweat glands, because the surface area of follicles and sweat
glands is smaller than the skin area that does not contain these anatomical elements. The
stratum corneum as a keratin web will act as a semi-permeable membrane, and drug
molecules are etched by passive diffusion.

Working mechanism of topical preparations

Some differences in mechanism of action are due to the components of preparations that are
fat-soluble and soluble in water.

1. Liquid

When applied to the surface of the skin, the dominant effect of fluid will play softening
because of the diffusion of the liquid into the foreign period found on the skin surface; a
small portion will experience evaporation.

Compared to solution, the penetration of the tura is much stronger. However, tingtura
preparations have rarely been used because the effects affect the skin. Dosage forms that have
existed include tingtura iodi and tingtura spiritosa.

2. Powder of Oxydum zincicum

as a component of powder it works to absorb water, thus giving a cooling effect. The talcum
component has considerable adhesive power and slip power.
Powder can not penetrate the skin layer because of its composition consisting of solid
particles, so it is used as a cover for the surface of the skin, preventing and reducing the shift
in the intertriginous area.

3. Ointment

Ointment with hydrocarbon base material such as vaseline, stays for a long time on the
surface of the skin and then penetrates. Therefore the hydrocarbon-based ointment is used as
a cover.

The ointment is made from absorbent ointment (abdominal ointment) works mainly to
accelerate penetration because of its large water component.

The base of the ointment that can be washed with water and the base of the salve dissolves in
water is able to penetrate far into the hypodermis so that it is widely used in conditions that
require deep penetration.

4. Penetration Cream

W / O cream is much stronger than O / W because oil components make the dosage form last
long above the skin surface and can penetrate the skin layer even further. However, the W / O
cream is less co-smoked because the old oil component remains above the skin surface. O /
W creams have better cooling power than W / O creams, while W / O emollient power is
greater than O / W.

5. Pasta

Paste-shaped preparations penetrate the skin layer. This dosage form is more protective as it
does not melt at body temperature. Milled pasta when applied over the lesion is able to
absorb wet lesions such as serum.

6. Powder shake

The working mechanism of powder shake is more important on the surface of the skin. The
addition of liquid and glycerin components aims to make the powder component stick to the
surface of the skin for a long time and the effect of the active substance can be maximal.
7. Cooling paste

Slightly different from pasta, adding a liquid component makes it easier to penetrate into the
skin layer, but the sticky shape makes the preparation uncomfortable to use and has rarely
been used.

8. Penetration Gel

the gel can penetrate the hypodermic layer so that it is widely used in conditions that require
penetration such as analgesic gel preparations. The diffusion route of the transfiterular gel
path is also good, due to the ability of the gel to form an absorption layer.