Phamaceutics Exam 2 Material

Hard Gelatin Capsules

Two-piece solid dosage forms consisting of a longer body and shorter cap prefabricated from gelatin, sugar, and water; contains 13% to 16% moisture and minimal to no plasticizer; filled with dry powders, granules, pellets, or non-aqueous pastes

Soft Gelatin Capsules

Single-piece, hermetically sealed elastic capsules containing high concentrations of plasticizers (glycerin, sorbitol) along with gelatin; formed, filled, and sealed simultaneously in a rotary die process; holds liquids, suspensions, or dry powders

Plasticizers in Capsules

Substances such as glycerin or polyhydric alcohols (sorbitol) added to gelatin formulations to impart flexibility, pliability, and elasticity to soft gelatin capsule shells

Hard Capsule Sizes

Standardized human sizing numbering from 000 (largest volume, ~1.4 mL) down to 5 (smallest volume, ~0.13 mL)

Hard Capsule Moisture Content

Official moisture content of 13% to 16%; if stored below this range shells become brittle and fracture, whereas excessive humidity softens shells and causes collapse

Soft Gelatin Incompatible Fills

Formulations with water content exceeding 5%, liquids that easily migrate through the gelatin shell, and low-molecular-weight water-soluble organic compounds such as alcohols, ketones, amines, and esters

Punch Method

An extemporaneous compounding technique for hard gelatin capsules where triturated powder is placed on a tile to 1/3 to 1/2 the capsule body depth and the empty body is repeatedly pressed downward into the powder bed until filled

Capsule-within-a-Capsule

An extemporaneous compounding approach used to physically isolate incompatible active ingredients or excipients by placing the sensitive drug in a small capsule (size 4 or 5) and enclosing it within a larger capsule; the inner capsule must not be visible through the outer shell

Pastes in Hard Capsules

Preparation of pasty masses intended for gastric disintegration inside hard capsules using an absorption vehicle like lanolin or an absorbent diluent like kaolin

Compressed Tablets (C.T.)

Standard uncoated oral solid dosage forms prepared by high-pressure mechanical compaction of granular powder formulations

Multiple Compressed Tablets (M.C.T.)

Tablets subjected to more than one compression cycle to create layered tablets or a tablet-within-a-tablet; used to physically separate chemically incompatible substances and to stage drug release rates over time

Sugar-Coated Tablets (S.C.T.)

Compressed tablets surrounded by a thick, sweet, colored sucrose barrier that effectively masks bitter tastes and odors but increases tablet weight and bulk by up to 50%

Film-Coated Tablets (F.C.T.)

Compressed tablets coated with a thin polymer barrier (e.g., hydroxypropyl methylcellulose) that protects against humidity and masks taste without adding significant weight or bulk

Enteric-Coated Tablets (E.C.T.)

Tablets coated with acid-resistant polymers (e.g., cellulose acetate phthalate) that remain intact in gastric acid (pH 1-2) and dissolve in alkaline intestinal fluid (pH > 6); protects acid-labile drugs and shields gastric mucosa from irritation

Sublingual Tablets

Flat, fast-dissolving tablets placed under the tongue for rapid drug absorption across the thin, highly vascular sublingual mucosa directly into systemic circulation, completely bypassing gastric acid and hepatic first-pass metabolism

Buccal Tablets

Tablets placed in the cheek pouch designed to erode slowly for transmucosal absorption; formulated with a bland taste (flavorants are avoided) to prevent stimulating salivation and premature swallowing

Effervescent Tablets

Tablets compressed from effervescent salts (sodium bicarbonate, citric acid, tartaric acid) that release carbon dioxide (CO2) when dropped into water, accelerating drug dissolution and gastric emptying

Vaginal Tablets (Inserts)

Ovoid or bullet-shaped compressed tablets inserted via an applicator to treat localized infections, particularly vulvovaginal candidiasis (e.g., Nystatin Vaginal Tablets)

Pellet Capsules vs Single-Unit Tablets

Single-unit non-disintegrating tablets depend on Phase III migrating motor complexes and have erratic gastric emptying delayed by 4-10+ hours with food; multi-particulate pellet capsules disperse into hundreds of small beads (< 2 mm) that empty continuously through the pylorus regardless of meals

Physiological Modulators of Gastric Emptying

Biological variables that significantly alter gastric motility, emptying time, and GI transit of solid dosage forms, including pregnancy, heavy physical exercise, and the menstrual cycle

Weight Variation Test

A USP compendial test determining net fill weight consistency across dosage units; used primarily for high-potency drugs where active ingredient forms the bulk of the formulation

Content Uniformity Test

A mandatory USP test for coated or uncoated capsules/tablets containing low doses of active drug (< 25 mg or < 25% by weight); requires individual units to assay between 85% and 115% of labeled potency

Air Displacement Agents

Inert gases such as nitrogen and carbon dioxide used to displace atmospheric oxygen from the headspace of hermetically sealed containers to prevent oxidative drug degradation

FD&C Red No. 20

An official certified synthetic pharmaceutical colorant used to impart color to capsules and compressed tablets

Percutaneous Absorption

The passage of topically applied substances from outside the skin across epidermal layers into the microcirculation of the dermis for systemic uptake

Stratum Corneum

The outermost 10-15 µm horny skin layer composed of 15 to 25 layers of dead, keratinized corneocytes embedded in a lipid-rich extracellular matrix (40% protein, 40% water, 20% lipid); the primary rate-limiting barrier in transdermal delivery

Viable Epidermis

The living, cellular layer (~100 µm thick) located directly beneath the stratum corneum that is completely avascular

Dermis

The 3-5 mm connective tissue layer containing capillary loops and venules; the skin layer closest to the microvascular blood supply where systemic transdermal absorption occurs

Transcellular Route

Percutaneous penetration pathway directly through corneocyte cells, favored primarily by nonpolar, lipophilic drugs

Paracellular Route

Percutaneous penetration pathway winding between cells through intercellular lipid matrices, favored primarily by polar, hydrophilic drugs

Transappendageal Route

Percutaneous shunt pathway bypassing the stratum corneum via hair follicles, sebaceous glands, and sweat gland pores

Stratum Corneum Hydration

The swelling of corneocytes and alteration of intercellular lipid packing caused by water retention; dramatically increases percutaneous penetration flux and is enhanced by occlusive patch backings

Stratum Corneum Thickness

Anatomical barrier factor inversely proportional to percutaneous absorption rate; thin skin (postauricular behind ear) permits high absorption, whereas calloused skin (palms, soles) severely restricts penetration

Skin Barrier Integrity

The physical condition of the stratum corneum; abrasions, cuts, burns, or dermatological disease states (e.g., psoriasis, eczema) disrupt barrier function and cause erratic, elevated drug influx

Cutaneous Vascularity

Dermal microvascular blood flow that clears diffused drug molecules into systemic circulation, maintaining a steep concentration gradient across the skin

Age and Percutaneous Absorption

Premature infants and neonates have underdeveloped, thinner stratum corneum layers and higher surface-area-to-weight ratios, elevating absorption and toxicity risk; geriatric skin has reduced hydration and blood flow

Melanocytes in TDDS

Skin pigmentation and melanocyte density do NOT alter or influence percutaneous absorption rates or TDDS efficacy

Ideal TDDS Physicochemical Properties

Small molecular weight (between 100 and 800 Da), high pharmacological potency (requiring low daily doses in mg or µg), and a balanced partition coefficient (both lipid and aqueous solubility)

Chemical Penetration Enhancers

Substances that reversibly reduce stratum corneum diffusional resistance by increasing skin hydration and altering intercellular lipid/protein fluidity (e.g., DMSO, Azone, ethanol, propylene glycol, PEG)

Dimethylsulfoxide (DMSO)

A chemical penetration enhancer requiring relatively high concentrations (> 60%) to alter lipid fluidity and protein structure to boost percutaneous absorption

Iontophoresis

An active physical TDDS technology applying a small direct electric current through an electrode to drive charged, ionized drug molecules across the skin via electromigration and electroosmosis (e.g., dexamethasone)

Sonophoresis

An active physical TDDS technology using high-frequency ultrasound to create acoustic cavitation in keratinocytes; delivers unionized drugs and does NOT generally require chemical enhancers (e.g., hydrocortisone, salicylic acid)

Monolithic (Matrix) TDDS

Transdermal patch design where the drug is dissolved or dispersed directly within a polymeric matrix/adhesive layer sandwiched between a backing and peel strip; polymer matrix controls release (e.g., Nitro-Dur)

Membrane-Controlled (Reservoir) TDDS

Transdermal patch design containing a distinct liquid or gel drug reservoir pouch bounded by a rate-controlling semipermeable membrane, delivering zero-order release (e.g., Transderm-Scōp, Transderm-Nitro)

Rate-Limiting Step in TDDS

The slower process between device release and skin penetration controls absorption; if membrane release is slower than skin absorption, the membrane is rate-limiting; if membrane release is faster than skin absorption, the skin is rate-limiting

Cutting Reservoir Patches Hazard

Membrane-controlled reservoir patches must NEVER be cut or damaged, as puncturing the reservoir pouch causes catastrophic, potentially fatal dose dumping of the liquid drug

Transderm-Scōp

The first FDA-approved transdermal patch (1979); a membrane-controlled system delivering 1.5 mg scopolamine over 3 days (72 hours) applied behind the ear (postauricular) for motion sickness

Transderm-Nitro

A membrane-controlled reservoir nitroglycerin patch delivering 0.2, 0.4, or 0.6 mg/hr applied to the chest or upper arm/shoulder for 24 hours for angina prevention; removed at night to prevent nitrate tolerance

Nitro-Dur

A monolithic (matrix) nitroglycerin patch delivering 0.1 to 0.8 mg/hr applied to the chest or upper arm/shoulder for 24-hour angina prophylaxis

Transdermal Nicotine

Daily monolithic transdermal patches delivering 7 to 22 mg/day applied to the arm or upper torso for smoking cessation, maintaining sustained plasma levels to prevent withdrawal

Estraderm (Transdermal Estradiol)

A transdermal system delivering 0.05 or 0.1 mg/day applied to the lower stomach area below the waistline (strictly avoiding the breasts) on a 3-weeks-on, 1-week-off regimen for postmenopausal symptoms

Duragesic (Fentanyl TDDS)

A 72-hour transdermal patch delivering 25 to 100 µg/hr applied to the arm, chest, or flat back; indicated ONLY for severe chronic pain in opioid-tolerant patients and strictly contraindicated in acute/PRN pain

Oleaginous (Hydrocarbon) Bases

Anhydrous, hydrophobic, greasy ointment bases that are insoluble in water, not water-washable, and cannot absorb water; provide an emollient effect, act as occlusive dressings, and prevent moisture loss (e.g., Petrolatum, White Ointment)

Petrolatum, USP

A purified mixture of semisolid hydrocarbons derived from petroleum that melts between 38°C and 60°C; serves as an occlusive protectant and emollient base; the decolorized variety is White Petrolatum, USP

Absorption Bases (Type I & II)

Oleaginous, water-insoluble, non-washable bases capable of absorbing water; Type I is anhydrous and absorbs water to form W/O emulsions (Hydrophilic Petrolatum/Aquaphor); Type II is already a W/O emulsion capable of absorbing additional water (Lanolin)

Hydrophilic Petrolatum

An official Type I anhydrous absorption base containing white petrolatum, white wax, stearyl alcohol, and cholesterol; permits incorporation of aqueous solutions into hydrocarbon bases (Aquaphor)

Lanolin, USP

A Type II absorption base obtained from sheep wool containing no more than 0.25% water; acts as a semisolid vehicle capable of absorbing water and forming pastes inside capsules

Water-Removable Bases

Oil-in-water (O/W) emulsions resembling creams with an aqueous continuous phase; easily washed from skin and clothing with water, non-greasy, dilutable with water, and capable of absorbing serous discharge (e.g., Hydrophilic Ointment)

Hydrophilic Ointment, USP

An official water-removable O/W base containing sodium lauryl sulfate (emulsifying agent), methylparaben, propylparaben, propylene glycol, stearyl alcohol, white petrolatum, and purified water

Water-Soluble Bases

Greaseless ointment bases composed entirely of water-soluble components without oleaginous substances; completely water-washable, soften upon addition of water, and used primarily for incorporating solid dry drugs (e.g., PEG Ointment)

Polyethylene Glycol (PEG) Ointment, NF

An official water-soluble, greaseless base prepared by blending PEG 3350 (solid) and PEG 400 (liquid)

Clinical Base Selection

Ointments are applied to dry, scaly, chronic lesions for emollient occlusion; Creams (O/W) are applied to weeping/oozing surfaces to absorb discharge; Lotions are applied to hairy or intertriginous friction areas (armpits, groin)

Spatula Selection in Compounding

Stainless steel spatulas are standard for incorporating ingredients on an ointment slab; a rubber or hard plastic spatula MUST be used when incorporating substances that react with or discolor metal (e.g., iodine)

Levigation Rule

The process of reducing powder particle size by grinding with a small volume of insoluble liquid; use mineral oil when oil is the external phase, and use glycerin or propylene glycol when water is the external phase

Liquid Incorporation into Hydrocarbon Bases

Aqueous solutions cannot be mixed directly into hydrophobic hydrocarbon bases; they must first be incorporated into a minimum quantity of an absorption base (e.g., Aquaphor) and then blended into the hydrocarbon vehicle

Fusion Method for Ointments

Compounding process where components are melted together and cooled with continuous stirring until congealed; materials with highest melting points are melted first, and heat-sensitive/volatile agents are added last at lowest temperatures

Gels & Carbomer 940

Semisolid dispersions of organic polymers in an aqueous vehicle; a high-molecular-weight polyacrylic acid polymer (0.5%-2.0%) neutralized with base to yield clear, highly viscous aqueous gels

Magmas

A specific category of two-phase gel systems consisting of a loose, high-volume structural network of small inorganic floccules (e.g., Bentonite Magma) exhibiting thixotropy

Pastes

Thick, stiff semisolid preparations containing a high proportion of solid materials (~25%, e.g., Zinc Oxide Paste); used to absorb serous secretions and stay firmly adhering in place without softening

Plasters

Solid or semisolid adhesive masses spread upon a fabric, plastic, or paper backing for prolonged skin contact; medicated plasters contain keratolytics (10% to 40% salicylic acid) for removing foot corns

Glycerogelatins (Unna's Boot)

Topical protective masses formulated with 15% gelatin, 40% glycerin, 35% water, and 10% zinc oxide; melted, applied with a brush, and bandaged for long-term treatment of varicose leg ulcers

Corneal Simple Diffusion

The major route of ocular drug transport through the eye; secondary pathways include the conjunctiva and sclera

Ophthalmic Ointment Sterility

Ophthalmic semisolids must meet USP sterility standards and metal particle limits; because terminal heat degrades bases, they are prepared aseptically and preserved with agents like methylparaben, propylparaben, or benzalkonium chloride

Ophthalmic Packaging Restriction

Ophthalmic preparations must be packaged exclusively in sterile collapsible tubes with narrow applicator tips or dropper bottles, and must NEVER be packaged in wide-mouth jars

Nasal Ointments & Gels

Formulations applied for local action (decongestants) or systemic peptide/protein delivery across the richly vascularized ciliated nasal mucosa

Dermatologic Patient Counseling

Counsel patients to wash and dry the area, apply only a thin film (1-3 mg/cm²), leave the area uncovered unless directed, wash hands thoroughly after use, and review therapeutic goals and treatment outcomes

Disperse System

A heterogeneous, two-phase system where particulate matter (dispersed / internal phase) is distributed throughout a continuous dispersion medium (external phase)

Suspension

A two-phase disperse system of finely divided insoluble solid drug particles uniformly dispersed throughout a liquid medium in which the drug exhibits minimum solubility

Emulsion

A two-phase disperse system in which one liquid is dispersed throughout another immiscible liquid in the form of microscopic droplets (O/W or W/O)

Stokes' Law Equation

dx/dt = [d² (ρi - ρe) g] / (18 η); defines sedimentation velocity (dx/dt) where d is particle diameter, ρi is particle density, ρe is vehicle density, g is gravity, and η is continuous phase viscosity

Stokes' Law Viscosity Relationship

Continuous phase vehicle viscosity (η) sits in the denominator; increasing viscosity slows particle settling, whereas decreasing viscosity INCREASES the rate of particle settling

Controlled Flocculation vs Deflocculation

Deflocculated particles settle slowly but pack into an irreversible, dense hard cake; floccules are loose, high-volume structural aggregates that settle faster but prevent caking and resuspend easily upon agitation

Emulsifying Agents (Surfactants)

Amphiphilic compounds possessing both hydrophilic and lipophilic groups that reduce interfacial tension, form mechanical interfacial films, and impart repulsive charges to prevent droplet coalescence

Surface Tension Theory

The emulsification theory proposing that surfactants lower interfacial tension between immiscible phases, reducing the repulsive work required to break liquids into small globules

Oriented-Wedge Theory

The emulsification theory stating that monomolecular surfactant layers orient at droplet interfaces based on molecular geometry and HLB value; the phase with which the surfactant interacts more favorably becomes the external continuous phase

Interfacial Film Theory

The emulsification theory stating that multimolecular hydrocolloid films (e.g., acacia) surround dispersed droplets to form a tough mechanical barrier that physically prevents coalescence

Hydrophile-Lipophile Balance (HLB)

A 1 to 20 scale measuring surfactant amphiphilic balance; low HLB values (3 to 6) indicate lipophilic surfactants that form W/O emulsions, whereas high HLB values (8 to 18) indicate hydrophilic surfactants that form O/W emulsions

Phase Localization in Emulsions

An active drug dissolves in the emulsion phase with which it shares solubility; in a W/O emulsion, a water-soluble drug (e.g., Ampicillin) is solubilized exclusively inside the internal aqueous droplets

Emulsifier Selection Criteria

An ideal emulsifying agent must be nontoxic, stable, chemically compatible with ingredients, and possess relatively little odor, taste, or color so as not to spoil formulation palatability

Cetomacrogol

An official non-ionic surfactant used as an emulsifying agent to produce and stabilize dispersions

Potassium Phosphate, Monobasic

An official pharmaceutical buffering agent used to resist changes in pH upon dilution or addition of acids/bases

Bentonite

An official natural aluminum silicate suspending and viscosity-increasing agent; hydrates in water to form thixotropic inorganic lattices (Bentonite Magma) to avoid sedimentation

Adult Rectal Suppositories

Bullet- or torpedo-shaped tapered suppositories measuring ~32 mm (1.5 inches) long and weighing approximately 2 grams when prepared with a cocoa butter base

Pediatric Rectal Suppositories

Narrow pencil-shaped suppositories measuring ~16-20 mm long and weighing approximately 1 gram (half the adult weight) when formulated with cocoa butter

Vaginal Suppositories (Pessaries)

Globular, oviform (egg-shaped), or cone-shaped solid inserts weighing approximately 5 grams with cocoa butter; modern clinical practice frequently uses compressed ovoid tablets

Urethral Suppositories (Bougies)

Slender pencil-shaped units measuring 100-150 mm long (4 g) for males and 50-60 mm long (2 g) for females; used for localized conditions such as erectile dysfunction (MUSE alprostadil single-use pellet)

Advantages of Rectal Drug Delivery

Bypasses gastric acid degradation and enzymatic breakdown, prevents gastric mucosal irritation (e.g., NSAIDs), and provides an effective alternative during severe nausea/vomiting, unconsciousness, or pediatric aversion

Hepatic First-Pass Bypass in Rectal Delivery

Lower and middle hemorrhoidal veins drain directly into systemic circulation (inferior vena cava), allowing approximately 50% of a rectally absorbed drug dose to bypass hepatic portal clearance

Rectal Physiological Factors

Absorption is markedly superior in a vacant rectum (feces physically blocks mucosal contact); rectal fluid volume is small (2-3 mL), neutral (pH ~7.0-7.4), and lacks buffer capacity, meaning rectal tissue does not alter drug ionization

Partition Coefficient Rule in Suppositories

Lipophilic drugs placed in oleaginous cocoa butter bases partition into aqueous rectal fluids very slowly; therefore, to achieve rapid release and systemic action, the ionized (water-soluble salt) form of the drug is preferred