Routes of Drug Administration and Dosage Formulations Created

Routes of Drug Administration and Dosage Formulations Created by Jennifer Majeske, Mineral Area College

� Differentiate between the terms route of administration, dosage form, and drug delivery system. � Explain the properties of oral, topical, and parenteral dosage forms. � Identify inactive ingredients and the various coatings of tablets and their functions. � Differentiate between a suspension and an emulsion liquid dosage form. � Identify dosage formulations utilizing the transmucosal route of administration. Created by Jennifer Majeske, Mineral Area College

� Define the emulsion characteristics of topical products such as ointments, creams, lotions, and gels. � Explain the advantages and disadvantages of oral, topical, and parenteral dosage formulations. � Discuss the importance of syringe selection for a diabetic patient. � Contrast the advantages and disadvantages for insulin in multi-dose vials and prefilled insulin syringes. Created by Jennifer Majeske, Mineral Area College

� Understand the stability and expiration dates of insulin at room and refrigerated temperatures. � Demonstrate correct techniques for administration of eyedrops, eardrops, metered-dose inhalers, and various parenteral injections. � Differentiate among enteric-coated, sustained-release, and extended-release dosage formulations. Created by Jennifer Majeske, Mineral Area College

� There exists many pharmacological agents with a variety dosage forms available to customize patient treatment. � Pharmaceutics – the study of the release characteristics of various dosage forms or drug formulations. � Medications can be taken: orally, inhaled, injected, inserted, applied to the skin, and each route affects the drugs’ onset and duration of action. � Pharmacokinetics – the study of how drugs are absorbed, distributed, metabolized, and eliminated. Created by Jennifer Majeske, Mineral Area College

� Route of administration – a way to get a drug into or onto the body. � What are the major routes of administration? � Dosage form – the physical manifestation of a drug – such as a tablet, capsule, suspension, ointment, cream, patch or injection – that is designed to deliver the medication by one or more routes of administration. � Systemic effect – the series of steps to get a drug into the bloodstream to exert its therapeutic effect. Created by Jennifer Majeske, Mineral Area College

� Delayed systemic effect: �Tablets, capsules, and oral liquids � Immediate �Parenteral systemic effect: injections, IV bolus and infusions � Localized effect – when a drug exerts its pharmacological action at or near the site of administration. �Drugs administered by the transmucosal, topical and inhalation route �Example: eardrop in the ear Created by Jennifer Majeske, Mineral Area College

� Oral route of administration – medication administered for absorption along the gastrointestinal (GI) tract into the systemic circulation. � Oral can also refer to applying medication to the mouth. � The abbreviation po – from the Latin term per os, meaning “by mouth”, is used to indicate the oral route of medication on a prescription. Created by Jennifer Majeske, Mineral Area College

� Tablets, capsules, solutions, suspensions, syrups and elixirs. � Tablets and capsules are the two most common types and are inexpensive to manufacturer. � The active ingredient in many tablets, capsules and suspensions are sometimes powders or granules. � Drugs available in salt forms add shelf life to the product and/or to affect the release characteristics of the drug. Created by Jennifer Majeske, Mineral Area College

� Tablet – a solid dosage form produced by compression. � Tablets contain one or more active ingredient along with inert or inactive ingredients (excipients). � Tablets are available in a variety of shapes, sizes, surface markings and coatings. Created by Jennifer Majeske, Mineral Area College

� Tablets can be designed to be easy to swallow, mask taste or exert an immediate pharmacological effect. � Compression tablets are the most inexpensive and common dosage form. �Acetaminophen (Tylenol) � Multiple compression tablet (MCT) is made by multiple compression cycles and is a tablet on top of a tablet or a tablet within a tablet. � Caplet – a hybrid of a capsule and tablet; shaped like a tablet, coated like a capsule. Created by Jennifer Majeske, Mineral Area College

� Most compression tablets are not coated. � Coatings improve flavor, appearance, or ease of swallowing. � Sugar-coated tablet (SCT) – contains an outside layer of sugar that protects the medication and improves appearance and flavor. � Sugar coating makes tablets larger and heavier thus more difficult to swallow. � Film-coated tablet (FCT) – contains a thin outer layer of a polymer that can either be soluble or insoluble. � Film coating are colored for an attractive appearance; taste-masking benefits can be lost if crushed. Created by Jennifer Majeske, Mineral Area College

� Most tablets are designed to be swallowed whole and dissolve in the GI tract. �Chewable tablet – contains a base that is flavored and/or colored. It is designed to be chewed (masticated) and absorbed quickly for slightly faster onset. �Oral disintegrating tablet (ODT) – designed to melt in your mouth. ODT’s are useful for pediatric and geriatric patients who may have difficulty swallowing or for patients with nausea. Created by Jennifer Majeske, Mineral Area College

� The active ingredient of a capsule is in the form of a granular powder (liquid gel) enclosed by a gelatin shell. � The body and cap may be sealed to prevent tampering. � Diluent – pharmacologically inert filler used in capsules. � Some capsule formulations are designed to provide better absorption of drugs, with less side effects. � Some medications that come in capsule form are substitutable with a tablet, others are not. Created by Jennifer Majeske, Mineral Area College

� Powders and effervescent salts are used less frequently by patients, but offer some advantages over tablets and capsules. � Powders – preparations in the form of fine particles. �Goody’s headache powders � Effervescent salts – granules or coarse powders containing one or more medicinal agents, as well as some combination of sodium bicarbonate with citric acid, tartaric acid or sodium bisphosphate. �Alka-Seltzer Created by Jennifer Majeske, Mineral Area College

� Liquids – consist of one or more active ingredient in a liquid vehicle such as a solution or suspension. � Most liquids are commercially available as solutions (elixirs and syrups), suspensions or emulsions. Created by Jennifer Majeske, Mineral Area College

� Solution – a liquid in which the active ingredients are completely dissolved in a liquid vehicle. � Solutions can be classified as aqueous, alcoholic, or hydroalcoholic. � Solvent – the vehicle that makes up the greater part of the solution. � Solute – the ingredient dissolved in a solution. Created by Jennifer Majeske, Mineral Area College

� Solutions are often classified by their ingredients; elixirs and syrups are the most common dosage forms of solutions. � Elixir – a clear, sweetened, flavored solution containing water and ethanol. � Syrup – an aqueous solution thickened with a large amount of sugar – sucrose – or sugar substitute. � Syrups can contain additional flavors, colors or aromatics. � Most pediatric formulations are syrups or elixirs. Created by Jennifer Majeske, Mineral Area College

� Aromatic water – a solution of water containing oils or other substitutes that have a pungent, and usually pleasing smell. � Extract – potent dosage form derived from plant or animal sources which most or all of the solvent has evaporated to produce a powder, an ointment like form, or a solid. � Fluidextract – a liquid dosage form prepared by extraction from plant sources and commonly used in the formulation of syrups. � Tincture – alcoholic or hydroalcoholic solution of extractions from plants. � Spirit – alcoholic or hydroalcoholic solution containing volatile, aromatic ingredients. Created by Jennifer Majeske, Mineral Area College

� Suspension – the state of a substance when its solid particles are mixed with but undissolved in a liquid. � Dispersion – the medication is simply dispersed or distributed throughout the vehicle, creating an incomplete mixture of solid and liquid. � Suspensions contain inactive ingredients such as colorings, flavorings and coatings. � Some suspensions are commercially available, others come in the form of powders that must be reconstituted prior to dispensing. Created by Jennifer Majeske, Mineral Area College

� Emulsion – another type of dispersion; a mixture of two immiscible or unblendable substances. � What is an example of an emulsion? � Emulsions contain an emulsifying agent that renders the emulsion stable and less prone to separate. Created by Jennifer Majeske, Mineral Area College

� Colloid – a mixture having physical properties between those of a solution and a fine suspension. � Magma – or milk like liquid, is an example of a dispersion containing ultrafine colloidal particles that remain distinct in a two-phase system. � Microemulsion – another type of colloidal dispersion; a liquid that is dispersed in another. Created by Jennifer Majeske, Mineral Area College

� What are some common advantages and disadvantages to administering a drug using the oral route? � Tablets � Capsules � Liquids Created by Jennifer Majeske, Mineral Area College

� Patients should be counseled by the pharmacist what drinks and foods to take or not take with medications. � Patients should be counseled by the pharmacist on behaviors to avoid while taking medications. � Auxiliary labels are affixed to drug containers to ensure that patients are taking medications in the correct manner. � Patients should be reminded of proper storage conditions. Created by Jennifer Majeske, Mineral Area College

� Oral syringe – measures and delivers oral liquid medications to pediatric patients. � This type of syringe is a calibrated device consisting of a plunger and cannula, and is used without a needle to administer medications to the mouth. � Oral syringes can be used to slowly administer liquid medications. � Very small doses (less than 1 m. L) can be administered with a tuberculin syringe (without a needle). Created by Jennifer Majeske, Mineral Area College

� Manufacturers often provide a medication cup for OTC liquids. � These are plastic cups that contain specific dose demarcations in different units of measure. � Droppers offer the ability to deliver the correct dosage of smaller volumes of medication. � Dropper – contains a small squeezable bulb at one end a hollow glass or plastic tube with a tapering point. � Viscosity – the thickness and flow characteristics of fluids. Created by Jennifer Majeske, Mineral Area College

� Transmucosal route of administration – allows the drug to be absorbed through or across the “sieve-like” or permeable mucous membranes of the mouth, eyes, ears, nose, rectum, vagina and urethra. � What advantages are there to using a transmucosal route of administration? � Transmucosal dosage forms include: tablets, gum, and lozenges (sublingual); ointments, solutions, suspensions, and sprays (eyes, ears, and nose); suppositories and solutions (rectum, urethra, and vagina). Created by Jennifer Majeske, Mineral Area College

� Sublingual route of administration – sub meaning “under” and lingua meaning “tongue”; the tablet is placed under the tongue, where it is rapidly absorbed by blood vessels. Created by Jennifer Majeske, Mineral Area College

� Buccal route of administration – a drug absorbed by the blood vessels in the lining of the mouth. � What are some examples of drugs administered via this route? � Lozenge – troche, solid dosage form containing active ingredients and flavorings, that are dissolved in the mouth. Created by Jennifer Majeske, Mineral Area College

� All can be delivered to a specific site with a minimum of systemic side effects. � Irrigating solution – a solution for cleansing or bathing an area of the body, can be used both topically as well as instilled. � Ophthalmics �Ocular route of administration – application of a drug into the eye. �Conjunctival route of administration – the application of a drug to the conjunctival mucosa. Created by Jennifer Majeske, Mineral Area College

� Otics �Otic route of administration – the application of a drug into the ear canal. �Eardrops can never be used in the eye, but eyedrops can be used in the ear. � Nasal sprays/solutions �Intranasal route of administration – the application of a drug into the passages of the nasal cavity. �Spray – a dosage form that consists of a container having a valve assembly unit, when activated, emits a fine dispersion of liquid. Created by Jennifer Majeske, Mineral Area College

� Suppository – an example of a semisolid dosage form that is created from an inactive ingredient and formulated to melt at body temperature and release an active drug. Created by Jennifer Majeske, Mineral Area College

� Rectal suppositories/solutions �Rectal route of administration – used to deliver drugs into the rectum. �Enema – a water-based solution administered rectally for cleansing or evacuating the bowel before a GI procedure. � Vaginal suppositories/solutions �Vaginal route of administration – the application of any drug within the vagina. � Urethral suppositories/solutions �Urethral route of administration – the application of a drug within the urethra. Created by Jennifer Majeske, Mineral Area College

� Sublingual medications �Advantage: rapid onset �Disadvantage: short duration � Buccal medications �Advantage: faster onset �Disadvantage: “dose dumping” � Ophthalmics, otics, and nasal sprays/solutions �Advantage: fast onset �Disadvantage: Created by Jennifer Majeske, Mineral Area College

� Suppositories and Solutions � Rectal suppositories/solutions �Advantage: used in both old and young �Disadvantage: patient inconvenience � Vaginal suppositories/solutions �Advantage: self-treatment �Disadvantage: Created by Jennifer Majeske, Mineral Area College

� Sublingual medications – storage requirements; nitroglycerin. � Buccal medications – chewing differences between regular gum and nicotine gum � Ophthalmics, otics, and nasal sprays/solutions �Ophthalmics – administered at or near room temperature; Fig. 4. 2 �Otic – store at room temperature; Fig. 4. 3 �Nasal medications – used for relief of nasal congestion or prevention of allergy symptoms Created by Jennifer Majeske, Mineral Area College

� Suppositories and solutions – certain preparatory steps and administrative techniques �Rectal medications – proper storage and administration �Vaginal medications – use medication for prescribed time period; Table 4. 4 Proper Technique for Administration of Vaginal Medications, pg. 126 Created by Jennifer Majeske, Mineral Area College

� Topical route of administration – application of a drug directly to the surface of the skin; exert local effects; side effects are minimal. � Ointments, pastes, and plasters �Ointment – a dosage form that is a water-in-oil (W/O) emulsion – a formulation that contains a small amount of water dispersed in oil. �Liniment – a medicated topical preparation �Paste – like an ointment that contains more solid materials, creating a dense consistency. �Plaster – a solid or semisolid that adheres to the body and contains backing material such as paper, cotton, linen, silk, moleskin, or plastic. Created by Jennifer Majeske, Mineral Area College

� Creams, lotions, and gels � Cream – an oil-in-water (O/W) emulsion – a small amount of oil dispersed in water. � Lotion – another O/W emulsion for topical application. � Gel – contains solid particles in a liquid, but the particles are fine or ultrafine. � Jelly – a gel that contains a higher portion of water in combination with a drub substance and a thickening agent. � Glycerogelatin – a topical preparation made with gelatin, glycerin, water, and medicinal substances. � Colloid – a mixture with physical properties that fall between a solution and a fine suspension. � Irrigating solutions – douche, is often reconstituted from a powder and introduced into the vaginal cavity for local cleansing. Created by Jennifer Majeske, Mineral Area College

� Major advantage of topicals is they have a fast onset of action with relatively few systemic side effects. � Ointments �Advantage: especially good for extremely dry areas of skin �Disadvantage: appearance and greasy residue � Creams, lotions and gels �Advantage: apply more smoothly to the skin and leave a very thin film �Disadvantage: Created by Jennifer Majeske, Mineral Area College

� Ointments – risk of increased absorption; careful application of topical medications; nitroglycerin; corticosteroid ointments. � Creams, lotions, and gels – specific precautions that patients should follow during application. Created by Jennifer Majeske, Mineral Area College

� Inhalation route of administration – the application of a drug through inhalation into the lungs, typically through the mouth. � Inhalation Dosage Forms: � Aerosols and MDIs �Aerosol – a spray in a pressurized metered-dose container that contains a propellant �Metered-dose inhaler (MDI) – a handheld, propellant-driven device, an MDI provides a specific measured amount of medication with compressed gas. Created by Jennifer Majeske, Mineral Area College

� Sterile Solutions and Nebulizers �Nebulizer – atomizing machine that delivers medication as a mist � Volatile Medications and Vaporizers �Used to deliver moisture to the air for relief of cold systems � Micronized Inhalers Powders and Nonaerosolized �Breath-activated powder for inhalation to avoid propellants �Administers a higher concentration of drug as a micronized powder into the lungs Created by Jennifer Majeske, Mineral Area College

� Major advantage of inhalation dosage forms is the rapid onset of action, which is only second to the IV route of administration. � Major disadvantage is poor inhalation technique, with all MDIs; higher risk of side effects with larger amounts of medication. Created by Jennifer Majeske, Mineral Area College

� The more immediate-acting drug when using multiple MDIs should be used first, followed by the second 5 -10 minutes later. � Table 4. 5 Proper Technique for Administration of an MDI, pg. 132 � Spacer device – the medication is released into a “storage chamber” where it can be more easily inhaled by the patient. � The patient should be sure to rinse their mouth after administration of an MDI to prevent an oral fungal infection. Created by Jennifer Majeske, Mineral Area College

� Parenteral solution – a sterile or microbial-free solution (w/ or w/o medication) that is administered via a hollow needle or catheter inserted through one or more layers of skin. � Parenteral comes from the Greek roots para meaning “beside” and enteron meaning “intestine. ” � This route bypasses – or goes “beside” rather than through – the alimentary canal or GI tract. � Parenteral route of administration – the injection of any drug or fluid into the bloodstream, muscle, or skin. Created by Jennifer Majeske, Mineral Area College

� IV Route – one of the more common parenteral routes of drug and fluid administration. �Intravenous (IV) infusion – a method for delivering a large amount of fluid and/or high concentration of medication directly into the bloodstream over a prolonged period and at a slow, steady rate. � IM Route – used to administer antibiotics, narcotics, medications for migraine headaches…and vaccines. �Injection – administration of a parenteral medication into the bloodstream, muscle or skin Created by Jennifer Majeske, Mineral Area College

� Subcutaneous route – administer medications below the skin into the subcutaneous tissue. � What are some common medications administered subcutaneously? � ID route – used for diagnostic and allergy skin testing, local anesthesia, and various diagnostic tests and immunizations. � What ID administrations mentioned in your text? Created by Jennifer Majeske, Mineral Area College

� The parenteral route is used for medications that contain molecules that are unstable, to large for absorption, or broken down to quickly in the stomach or liver. � IV route – preferred route of administration in an emergency situation; rapid action to control and treat symptoms. � IV bolus injection – administration of a drug all at once. � IV infusion – continuous amount of needed medication over a given period. Created by Jennifer Majeske, Mineral Area College

� Pyrogens – fever-producing by-products of microbial metabolism. � Embolism – blockage of a vessel. � Phlebitis – a severe painful reaction at the injection site. � IM route – offers a more convenient way to deliver injectable medications; slower onset than IV administration; duration of action is much longer, making it more practical for use outside of a hospital setting; unpredictable rate of absorption. Created by Jennifer Majeske, Mineral Area College

� Parenteral preparations contain ingredients that are dissolved or reconstituted with solutions. � Most parenteral preparations are made up of ingredients place in a sterile water medium. � Administration of IV, IM, subcutaneous or ID must be sterile because they introduce medication directly into the body. � Only trained professionals and healthcare providers are legally allowed to give parenteral injections. Created by Jennifer Majeske, Mineral Area College

� Parenteral injections are administered via a syringe and/or needle. � Syringe – a calibrated device used to accurately draw up, measure, and deliver medication to a patient through a needle. � Common syringes � Insulin syringe � Tuberculin syringe Cannula – bore area inside the syringe � Hypodermic syringe � Needle – attached to the tip of a syringe and is used to either draw fluid into or push fluid out of the syringe; the larger the gauge the smaller the opening. Created by Jennifer Majeske, Mineral Area College

� IV Route – IV medications can be administered via two routes: IV bolus and IV infusions. � Patient-controlled analgesia (PCA) infusion device – a programmable machine that delivers a small amount of painkillers upon patient demand. Created by Jennifer Majeske, Mineral Area College

IM Route – IM injection doesn’t work as fast as an IV injection infusion, but the pharmacological effect will last longer. � Subcutaneous Route – injections typically administered on the outside of the upper arm, top of the thigh, or lower portion of each side of the abdomen. � Created by Jennifer Majeske, Mineral Area College

� Administration of Insulin – most commonly used medication that is administered subcutaneously is insulin. � Insulin Product Selection – syringe size, needle length and needle gauge. Insulin vials are 10 m. L (containing 1, 000 units of insulin); prefilled syringes contain 3 m. L. � Insulin vials – Syringes sizes 0. 3 m. L, 0. 5 m. L, 1 m. L; size is determined by dose of insulin; insulin vials should never be shaken. � Insulin Pens – a portable device in which the prescribed dose of medication is “dialed up” to administer insulin. Created by Jennifer Majeske, Mineral Area College

� What are some of the advantages of the insulin pens? Disadvantages? � Storage of insulin – insulin must be protected against extreme temperatures. Open vials and pens can be stored at room temperature and discarded after one month. Unopened vials and pens should remain refrigerated. � Insulin Coverage for Insulin Supplies – insurance companies require a prescription for coverage of diabetic supplies. � ID Route – ID injections are given into the capillary-rich skin layer just below the epidermis. Created by Jennifer Majeske, Mineral Area College

� Drug delivery system – a design feature of a dosage form that modifies the release of a drug by one or more pharmacokinetic parameters of the drug. � Improved efficacy and safety is a result of formulating medications based on the pharmacokinetic process. � Tablets or capsules have coatings to delay release and protect the stomach or extend their release. � Transdermal patches release medication slowly over a certain period of time. � Vaginal rings and intrauterine devices are inserted vaginally to prevent pregnancy. Created by Jennifer Majeske, Mineral Area College

� Most tablets and capsules are “immediaterelease, ” the medication is designed to activated or released shortly after the drug is taken. � Alphabet of release formulations: DR, CD, XR, SR, XT, and XL. � Delayed-release (DR) formulations – have a special coating designed to delay absorption of the medication and to resist breakdown by acidic gastric fluids. �Enteric-coated formulation. tablet (ECT) – delay-release Created by Jennifer Majeske, Mineral Area College

� Extended-release (XL) formulations – allow a reduced frequency of dosing as compared with immediate-release medications. �Sustained-release (SR) formulations: two doses every 8 -12 hours. �Controlled-release (CR) formulations: one dose Created by Jennifer Majeske, Mineral Area College

� New drug delivery systems employ scientific and biotechnologic processes to design medications to produce long-term effects. � Matrix-controlled release formulations – a reservoir-controlled release utilizing an osmotic pressure principle or an ion exchange resin. � Oxy. Contin (matrix-controlled release) � Tussionex (ion exchange resin) � Wax matrix systems – the drug is embedded in a polymer matrix, release takes place by partitioning of the drug into the polymer matrix and surrounding medium. Created by Jennifer Majeske, Mineral Area College

� Osmotic pressure system – the drug is delivered to the body by slowly being “pushed out” into the bloodstream. � Target drug delivery systems – a drug is “carried” by a liposome, and released at a targeted organ site; increasing availability in the near future. Created by Jennifer Majeske, Mineral Area College

� Transdermal dosage form – designed to deliver a drug contained within a patch or disk to the bloodstream via absorption through the skin. � Therapeutic uses – effects last 24 hours to 1 week. � Administration – transdermal patches should be applied to a relatively hair-free area; localized heat speeds up the movement from the patch into the body. Created by Jennifer Majeske, Mineral Area College

� Vaginal ring delivery system and intrauterine device continually deliver hormones to a female’s reproductive tract. � Nuva. Ring � Intrauterine device (IUD) – another way to prevent conception via a drug delivery device. Created by Jennifer Majeske, Mineral Area College

This workforce solution was funded by a grant awarded by the U. S. Department of Labor’s Employment and Training Administration. The solution was created by the grantee and does not necessarily reflect the official position of the U. S. Department of Labor. The Department of Labor makes not guarantees, warranties, or assurances of any kind, express or implied, with respect to such information, including any information on linked sites and including, but not limited to, accuracy of the information or tis completeness, timeliness, usefulness, adequacy, continued availability, or ownership. This work by Mineral Area College is licensed under the Creative Commons Attribution 4. 0 International License. Created by Jennifer Majeske, Mineral Area College

� Picture on slide 15 � Capsule � Picture on slide 24 � Female � Picture by Pixabay is licensed under CC BY lips by Pixabay is licensed under CC BY on slide 29 � Human head anatomy with external and internal carotid arteries by Patrick J. Lynch licensed under CC BY � Picture on slide 33 � Suppository � Picture by Eric Schulz licensed under CC BY on slide 64 � Vaginal ring by Victor byckttor licensed under CC BY Created by Jennifer Majeske, Mineral Area College