Semi-Solid Dosage Forms and Transdermal Delivery Systems Flashcards by hello world

Types of semisolid dosage forms intended for topical application

creams, gel, and ointments

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T/F. Topical Preparations are used for both local and systemic effects.

True

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product designed to deliver drug into the skin in treating dermal disorders, with the skin as the target organ

Topical dermatological product

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product is designed to deliver drugs through the skin (percutaneous absorption) to the general circulation for systemic effects, with the skin not being the target organ

transdermal product

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Semisolid preparations intended for external to the skin or mucous membranes
+ may be medicated or not
+ unmedicated: emollient, protectant, lubricant

ointments

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Ointment bases.
+ also known as hydrocarbon bases
+ effective as occlusive dressings

Oleaginous bases

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Examples of Oleaginous bases

Petrolatum
White Petrolatum
White Ointment
Yellow Ointment

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Other names for petrolatum

Yellow petrolatum
Petroleum Jelly

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White Petrolatum

White Petroleum jelly
White soft paraffin
Vaseline

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Yellow Ointment is obtained from

APIS MELLIFERA

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2 types of Absorption bases

Anhydrous bases
w/o emulsions (emulsion bases) and permit the incorporation of small additional quantities of aqueous solutions

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bases that permit the incorporation of aqueous solutions, resulting in the formation of w/o emulsions. These absorption bases are anhydrous vehicles composed of a hydrocarbon base and an additive

Anhydrous (Absorption base) `

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Example of Absorption bases

Hydrophilic Petrolatum, Aquaphor, Aquabase, Eucerin Lanolin (Anhydrous lanolin)

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also known as water - washable base
+ o/w resembling creams
+ absorb serous discharge

Water Removable Bases

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Example of WaR base in Ointment

Hydrophilic ointment

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often referred as greaseless
do not have oleaginous components
+ example: PEG

water - soluble bases

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How to select appropriate Ointment bases?

Desired release 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
Effect, if any, 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

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Where is ointment generally applied to?

Dry, Scaly skin

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Where is cream generally applied to?

Weeping or oozing surfaces

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Where is lotion generally applied to?

Intertriginous areas

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Prep of Oint.
+ Components are mixed until uniform prep is attained
+ rubber/silicone spatula is used if drug reacts to metals

Incorporation

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What to used during incorporations

Parchment paper, Ointmnet Slab. Unguator

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Fusion

All or some of the components of an ointment are combined by being melted together and cooled with constant stirring until congealed
+ heat labile substances and any volatile substance are added last

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Compendial Requirements for Ointments

Microbial Content
Minimum Fill
Packaging (large-mouth jars, metal or plastic tubes)
Storage
Labeling

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Semisolid preparations containing one or more medicinal agents dissolved or dispersed in either a W/O emulsion or an oil-in-water emulsion or in another type of water-washable base

Pharmaceutical Creams

O/W emulsions containing large percentages of water and stearic acid or other oleaginous component; evaporation → thin residue film of stearic acid/oleaginous components

Vanishing Creams

Semisolid systems consisting of dispersions of small or large molecules in an aqueous liquid vehicle rendered jellylike by the addition of gelling agent

Gels

also known as jellies

Gels

Type of gel where macromolecules are uniformly distributed throughout a liquid with no apparent boundaries between the dispersed macromolecules and the liquid

Single phase gel

Type of gel where a gel mass consisting of floccules of small distinct particles. Often referred to as Magmas.

Two phase gels

* Semisolid preparations intended for application to the skin. * Generally contain larger proportion of solid material (25%) than ointments→ stiffer * Not suited for application to hairy parts of the body

Pastes

Example and other name for that paste

Zinc Oxide Paste (Lassar's Plain Zinc Paste)

Solid/semisolid adhesive masses spread upon a backing material of paper, fabric, moleskin or plastic + applied to skin to provide prolong contact at site

Plasters

Example of Plasters

Salicylic Acid Plasters

Components of glycerogelatins

Gelatin (15%) Glycerin (40%) Water (35%) Medicinal Substances (10%)

Glycerogelatins are melted before application. It is applied by a brush. How long is applied in the skin?

For a long time

Example of Glycerogelatins

Zinc glycerogelatin

Where is zinc glycerogelatin used for?

varicose ulcers

Package. Made of clear or opaque glass or plastic. Some are colored green, amber, or blue

Ointment Jars

Used for light-sensitive products, are porcelain white, dark green or amber

Opaque Jars

Made of aluminum or plastic (HDPE or LDPE or a blend of PP, PET) + for opthalmic, nasal, vaginal , rectal products

Ointment tubes

Examples of Gelling agents

CMC, HPMC, carbomers, tragacanth

facilitate the passage of therapeutic quantities of drug substances thru the skin and into the general circulation for their systemic effects

Transdermal Drug Delivery System

First transdermal system

Scopolamine patch

Types of TDDS

Microneedles Iontophoresis Sonophoresis Electroporation Transdermal Patches Absorption Enhancers

What skin layer behaves as a semipermeable membrane and drug moleceules can penetrate through passive diffusion?

Stratum Corneum

Percentage of Protein and Water in SC

40% protein 40% water

Factors affecting drug movement across percutaneous skin layer

drug concentration in the vehicle aqueous solubility oil–water partition coefficient between the stratum corneum and the product's vehicle conditions of the skin

Transepidermal penetration

penetration through SC

Transappedegeal penetration

via appendages i.e. eccrine ducts and hair follicles

Types of transepidermal penetration

Intracellular Intercellular

Penetration Sites for Percutaneous Absorption

* Between the cells of stratum corneum * Through the walls of the hair follicles * Through sweat glands * Through sebaceous glands * Through cells of stratum corneum

Factors Affecting PA

Drug Formulation Patient Factor Miscellaneous Factor

Increases skin permeability by reversibly damaging or altering the physicochemical nature of the SC to reduce its diffusional resistance

Chemical Enhancers

How do chemical enhancers alter physicochemical nature of SC?

hydration, structural change, or denaturation of SC

Types of Chemical Enhancers

Acetone azone ethanol oleic acid dimethylsulfoxide propylene glycol glycerin PEG urea dimethylacetamide sodium lauryl sulfate poloxamers Spans Tweens lecithin terpenes

delivery of a charged chemical compound across the skin membrane using an electrical field

Iontophoresis

also known as high frequency ultrasound

Sonophoresis

used where the semisolid dosage form is placed on a membrane → drug is released from the dosage form and passes through the membrane into the receptor solution where it is sampled and analyzed for content

Franz diffusion cell

the drug matrix layer composed of polymeric material in which the drug is dispersed is found between the backing and frontal layer

Monolithic systems

designed to contain a drug reservoir, or pouch, usually in liquid or gel form; a rate-controlling membrane; and backing, adhesive, and protecting layers

Membrane controlled TS

Transdermal Scopolamine

Transderm Scop

Transdermal Clonidine

Catapres

Transdermal Nicotine

NicoDerm CQ

Transdermal Estradiol

Estraderm

Transdermal NTG

Deponit

Transdermal Testosterone

Testoderm

Transdermal Contraceptive System

Norelgestromin, ethinyl astradiol

Trandermal Methylphenidate

tx ADHD

Lidocaine patch (for pain associated with postherpetic neuralgia

patches

Solid DFs designated to be inserted under the skin of special injections or by surgery to provide continuous long drug therapy thru slow release of medication

Subdermal implants

Implant protection from pregnancy

Norplant system of levonorgestrel implants

It consists of a drug that is impregnated into a flexible, durable woven fabric or extruded synthetic material that is coated with an adhesive agent.

Tapes

Animals tested in Percutaneous Absorption Models (in Vivo)

Weaning Pig, Rhesus Monkey, Hairless Mouse or Rat

What to verify and quantify first in PA Models (in vivo)?

Cutaneous bioavailability Systemic bioavailability

Drug diffusion in PA Models in vitro is determined through

Periodic sampling assay of the drug content in receptor solution

Matrix that controls the rate at which the drug is released

Polymer Matrix in Monolithic Systems