3 - Topical Products Flashcards

1
Q

Dosage form designed to deliver drug

INTO the skin

treating dermal disorders with the

SKIN as the TARGET ORGAN

A

Topical Product

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2
Q

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

A

TRANSDERMAL PRODUCT

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3
Q

Type of Ointment BASE?

Hydrocarbon non-polar compound

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

Emollients + Occlusive

A

OLEAGINOUS Base

Most HydroPHOBIC

Petrolatum / Yellow+White Ointment

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4
Q

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

A

Absorption Base

(Emulsion Base)

2nd MOST hydroPHOBIC

HydroPhilic petrolatum

Aquaphor/base

Lanolin

Polysorb

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5
Q

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

A

Absorption Base + WATER

(W/O Base)

3rd most HydroPHOBIC

Eucerin

W/O Products

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6
Q

Type of ​Ointment BASE

HydroPHOBIC compounds + Water + O/W Surfactant

O/W Emulsion

easily washed from skin

A

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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7
Q

Type of ​Ointment BASE

Polethylene Glycols

NO hydroPHOBIC Ingredients = greaseless

Soften with addition of water

A

WATER SOLUBLE

least Hydrophilic

PEG Ointment

Polybase

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8
Q

Type of ​Ointment BASE

Methycellulose / Carbomer Dispersions

HIGH 95% of Water

A

Aqueous Bases

MOST HydroPhilic

Methylcellulose

Carbomer Gels

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9
Q

All the different types of OINTMENT BASE

Categorization

In order of HydroPhobicity

A

Oleaginous

Absorption

Absorption + Water (W/O Base)

Water-Soluble

Water-Removable (O/W Base)

Aqueous / HydroPhilic Base

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10
Q

Applied to DRY and SCALY SKIN

A

Ointment

HydroPHOBIC

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11
Q

Product applied to WEEPING or OOZING surfaces

A

Cream

HydroPhilic

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12
Q

Methods to Prepare

OINTMENTS

A

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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13
Q

In the order of what?

Water > Glycol > Petrolatum

A

INCREASING

POLARITY

Water >

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14
Q

What type of Topical Dosage form?

HydroPHOBIC Base

W/O emulsion w/ water

water evaps after cream is applied leaving hydrophobic residue

A

Phamaceutical OINTMENTS

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15
Q

What type of Topical Dosage form?

Either O/W Emulsion or W/O Emulsion

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

A

Pharmaceutical CREAMS

Topical Skin products

Rectal

Vaginal

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16
Q

What type of Topical Dosage form?

HydroPhilic dispersions in an aqueous vehicle

–> jelly-like by addition of a gelling agent

Carbomers / Cellulosics

Organogels (hydroPHOBIC)

A

GELS

17
Q

What type of Topical Dosage form?

Stiff SemiSolid preperation containing a

HIGH PERCENTAGE of Solids ~25%

Fxn: Protectant + Absorbent of secretions

A

PASTES

Lassar’s Plain Zinc Paste

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

18
Q

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

A

PLASTER

Salicylic Acid (10-40%) Plaster

used to remove CORNS

19
Q

What type of Topical Dosage form?

Gelatin + Glycerin + Water + medicament

A

GlyceroGELATINS

Zing Gelatin Boot

to form a Pressure Bandage

20
Q

Additional Requirements for

OTHALMIC Ointments / Gels

A

STERILITY

may require ASEPTIC processing, if can not be Terminally sterilized

Metal Particles

Micronized Solid Particles <1um

21
Q

Typical Formulation of Topical Products

3

A

SIMPLEST IS BEST

DRUG

LEVIGATING AGENT (wetting agent)

BASE (what Dr. Prescribes

if needed : pH buffer / preservative / penertraition enhancer

22
Q

Type of Lotion

Cream Base + Water

A

HydroPhilic Lotion

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

23
Q

Type of Lotion

Ointment Bases + Mineral Oil

A

HydroPHOBIC Lotion

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

24
Q

Preperation of LOTIONS

A
  1. Prep the lotion base
  2. Incorporate drug (mortar + pestle or electrical unguator)
    1. Tituration -> Levigation
  3. Dissolution in solvent (water or alcohol)
  4. Pulverization by intervention
    1. let alchol evap
  5. Geometric Dilution
25
Q

Types of STICKS & how they are made

Stick = hardened ointment or cream base for skin application

A

HARD STICK = use Moistening Base

Soft Stick = use Melting base

FUSION -

Melt ingredients –> pour in MOLDS

26
Q

Agent that INCREASES skin permeability

by reversibly damaging / altering the physicochemical nature of the

Stratum Corneum

to reduce its diffusional resistance

A

PERCUTANEOUS ABSORPTION ENHANCERS

Azone / Ethanol

Diemthyl Formamide / Sulfoxide

Sodium lauryl Sulfate

PEG / Propylene Glycol

27
Q

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

A

PERCUTANEOUS ABSORPTION ENHANCERS

28
Q

Iontophoresis

Deliver CHARGED compound by means of an ELECTRIC FIELD

Sonophoresis

High Frequency ULTRASOUND

A

Other methods of

Percutaneous Absorption Enhanncement

29
Q

Factors Affecting Percutaneous Absorption

Transdermal Patches

(Transdermal Drug delivery Systems = TDDS)

A
  • 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
30
Q

One of 2 basic designs of Transdermal Patches

Drug dissolved in POLYMER MATRIX

sustained release

A

MONOLITHIC

TDDS

31
Q

One of 2 basic designs of Transdermal Patches

Drug in RESERVOIR

MECHANICAL sustained release

A

Membrane Controlled

additional membrane in dosage form controls the drug release

32
Q

Disadvantages of Transdermal Patches

A

LIMITED DRUGS

MW limitation <400, 100-800

Dermatitis on site of patch

33
Q

ADVANTAGES of TDDS

transdermal patches

A

AVOID GI Absorption problems

AVOID First-pass metabolism

non-invasive / can use when vomitting/diarrhea

Extended therapy / easy to terminate

easy identification

34
Q

Scopolamine

Nitroglycerin

Nicotine

Estradiol / Contraceptives

Testosterone

Oxybutinin

A

Examples of

TDDS PRODUCTS

35
Q

Affect of Wet / Moist skin

on TDDS

A

ENHANCE DRUG RELEASE

36
Q

Affect of OILY SKIN

on TDDS

A

Impede ADHESION of patch to skin

37
Q

TDDS Counseling

A

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

38
Q

Levigating Agent

that makes the Dosage form HydroPHOBIC

Drug + Levigating Agent + Base

A

MINERAL OIL

39
Q

Levigating Agent

that makes the Dosage form HydroPhilic

Drug + Levigating Agent + Base

A

GLYCERIN