3 - Topical Products Flashcards by Karlo Sison

Dosage form designed to deliver drug

INTO the skin

treating dermal disorders with the

SKIN as the TARGET ORGAN

Topical Product

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Dosage form desinged to deliver the drug

THROUGH THE SKIN

(percutaneous absorption)

to the general circulation for SYSTEMIC EFFECTS

skin is NOT the target organ

TRANSDERMAL PRODUCT

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Type of Ointment BASE?

Hydrocarbon non-polar compound

Remain on skin for a long period, protect against loss of moisture

Emollients + Occlusive

OLEAGINOUS Base

Most HydroPHOBIC

Petrolatum / Yellow+White Ointment

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Type of Ointment BASE

HydroPHOBIC Compounds + W/O Surfactant

Allows small quantities of aqeueous solutions to be incorporated into the ointment base

similar to oleaginous base, but NOT as occlusive

Absorption Base

(Emulsion Base)

2nd MOST hydroPHOBIC

HydroPhilic petrolatum

Aquaphor/base

Lanolin

Polysorb

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Type of Ointment BASE

Hydrophobic Compunds + W/O Surfactants + Water

Permits small quanitities of aqueous solution to be added to intment base

forms a W/O Emulsion

Absorption Base + WATER

(W/O Base)

3rd most HydroPHOBIC

Eucerin

W/O Products

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Type of Ointment BASE

HydroPHOBIC compounds + Water + O/W Surfactant

O/W Emulsion

easily washed from skin

Water-Removable Base aka Water-washable

(O/W Base)

2nd most HydroPhilic

Dermabase + Vanicream

HydroPhilic ointment

contains stearyl alcohol + white protolatum

EMULSIFIED in water + sodium lauryl sulfate

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Type of Ointment BASE

Polethylene Glycols

NO hydroPHOBIC Ingredients = greaseless

Soften with addition of water

WATER SOLUBLE

least Hydrophilic

PEG Ointment

Polybase

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Type of Ointment BASE

Methycellulose / Carbomer Dispersions

HIGH 95% of Water

Aqueous Bases

MOST HydroPhilic

Methylcellulose

Carbomer Gels

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All the different types of OINTMENT BASE

Categorization

In order of HydroPhobicity

Oleaginous

Absorption

Absorption + Water (W/O Base)

Water-Soluble

Water-Removable (O/W Base)

Aqueous / HydroPhilic Base

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Applied to DRY and SCALY SKIN

Ointment

HydroPHOBIC

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Product applied to WEEPING or OOZING surfaces

Cream

HydroPhilic

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Methods to Prepare

OINTMENTS

INCORPORATION

Trituration -> Levigation in glycerin or mineral oil

Unguator - elecctric equipment / heated vessel

or mortar and pestle

FUSION

Melting + Mixing

use lowest temp

may include emulsification

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In the order of what?

Water > Glycol > Petrolatum

INCREASING

POLARITY

Water >

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What type of Topical Dosage form?

HydroPHOBIC Base

W/O emulsion w/ water

water evaps after cream is applied leaving hydrophobic residue

Phamaceutical OINTMENTS

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What type of Topical Dosage form?

Either O/W Emulsion or W/O Emulsion

Other Water-washable base or Water-soluble base (glycol)

Pharmaceutical CREAMS

Topical Skin products

Rectal

Vaginal

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What type of Topical Dosage form?

HydroPhilic dispersions in an aqueous vehicle

–> jelly-like by addition of a gelling agent

Carbomers / Cellulosics

Organogels (hydroPHOBIC)

GELS

What type of Topical Dosage form?

Stiff SemiSolid preperation containing a

HIGH PERCENTAGE of Solids ~25%

Fxn: Protectant + Absorbent of secretions

PASTES

Lassar’s Plain Zinc Paste

(25% zinc oxide and 25% starch in white petrolatum

What type of Topical Dosage form?

Solid OR Semisolid Masses spread on PAPER or other backing

PROLONGED contact w/ skin

can be used to remove CORNS

PLASTER

Salicylic Acid (10-40%) Plaster

used to remove CORNS

What type of Topical Dosage form?

Gelatin + Glycerin + Water + medicament

GlyceroGELATINS

Zing Gelatin Boot

to form a Pressure Bandage

Additional Requirements for

OTHALMIC Ointments / Gels

STERILITY

may require ASEPTIC processing, if can not be Terminally sterilized

Metal Particles

Micronized Solid Particles <1um

Typical Formulation of Topical Products

SIMPLEST IS BEST

DRUG

LEVIGATING AGENT (wetting agent)

BASE (what Dr. Prescribes

if needed : pH buffer / preservative / penertraition enhancer

Type of Lotion

Cream Base + Water

HydroPhilic Lotion

Non-viscous liquid for application to skin, base is either ointment or cream

Type of Lotion

Ointment Bases + Mineral Oil

HydroPHOBIC Lotion

Non-viscous liquid for application to skin, base is either ointment or cream

Preperation of LOTIONS

Prep the lotion base
Incorporate drug (mortar + pestle or electrical unguator)
1. Tituration -> Levigation
Dissolution in solvent (water or alcohol)
Pulverization by intervention
1. let alchol evap
Geometric Dilution

**Types of STICKS & how they are made** Stick = hardened ointment or cream base for skin application

**HARD STICK** = use **Moistening Base** ***Soft Stick = use Melting base*** **_FUSION_** - Melt ingredients --\> pour in MOLDS

**Agent** that **INCREASES skin permeability** by **reversibly damaging / altering** the physicochemical nature of the **_Stratum Corneum_** to reduce its **diffusional resistance**

**_PERCUTANEOUS ABSORPTION ENHANCERS_** **Azone** / **Ethanol** Diemthyl Formamide / Sulfoxide **Sodium lauryl Sulfate** **PEG / Propylene Glycol**

Agent which uses these MECHANISMS: **INCREASED Hydration of _Stratum Corneum_** and/or Change in **structure of lipids/lipoproteins** in **intercellular channels** through **solvent action or denaturation**

**PERCUTANEOUS ABSORPTION ENHANCERS**

**Iontophoresis** Deliver CHARGED compound by means of an ELECTRIC FIELD **Sonophoresis** High Frequency ULTRASOUND

*Other methods of* **Percutaneous Absorption Enhanncement**

**Factors Affecting Percutaneous Absorption** **Transdermal Patches** **(Transdermal Drug delivery Systems = TDDS)**

* **Concentration** related to SIZE/Concentration of TDDS * **Partitioning** @ site of application * **Molecular Weight** * 100-800, prefer **\<400** * BOTH **aqueous / lipid soluble** * **Hydration** * favors absorption * **Stratum Corneum** = horny layer * **Contact Time**

_One of 2 basic designs of Transdermal Patches_ ## Footnote **Drug dissolved in POLYMER MATRIX** *sustained release*

**MONOLITHIC** **TDDS**

_One of 2 basic designs of Transdermal Patches_ **Drug in RESERVOIR** **MECHANICAL sustained release**

**Membrane Controlled** additional membrane in dosage form controls the drug release

**Disadvantages of Transdermal Patches**

**LIMITED DRUGS** **MW limitation \<400**, 100-800 **Dermatitis on site of patch**

**ADVANTAGES of TDDS** **transdermal patches**

AVOID **GI Absorption problems** AVOID **First-pass metabolism** **non-invasive** / can use when **vomitting/diarrhea** **Extended therapy** / **easy to terminate** easy identification

**Scopolamine** **Nitroglycerin** **Nicotine** **Estradiol / Contraceptives** **Testosterone** **Oxybutinin**

Examples of ## Footnote **TDDS PRODUCTS**

Affect of **Wet / Moist skin** on **TDDS**

**ENHANCE DRUG RELEASE**

**Affect of OILY SKIN** **on TDDS**

**Impede ADHESION of patch to skin**

**TDDS Counseling**

Use only on **recomended site & ROTATE** Apply to **clean/dry skin**, free of **hair** do not use *skin lotion* **DO NOT CUT OR ALTER SIZE** hold in place for **10 sec** for adherence

**Levigating Agent** **that makes the Dosage form HydroPHOBIC** Drug + Levigating Agent + Base

**MINERAL OIL**

**Levigating Agent** **that makes the Dosage form HydroPhilic** Drug + Levigating Agent + Base

**GLYCERIN**