Introductory to Pharmacy PC701 Chapter 1 PDF

Introductory to Pharmacy PC701 Chapter 1 Dr. Rana Sammour Pharmaceutical Dosage Forms Definition: It is a combination of a drug entity and excipients (additives) in a form suitable for administration via the appropriate route. Example: Tablets are a solid dosage form administered orally. ...

Introductory to Pharmacy PC701 Chapter 1 Dr. Rana Sammour Pharmaceutical Dosage Forms Definition: It is a combination of a drug entity and excipients (additives) in a form suitable for administration via the appropriate route. Example: Tablets are a solid dosage form administered orally.  According to their physical state (shape) Types of the Pharmaceutical Dosage Forms According to the route of administration Types of Pharmaceutical Dosage Forms A. According to their physical state (shape) Solid dosage forms. Liquid dosage form. Semisolid dosage form. Gaseous dosage form 1. Solid dosage forms: Powder: Homogeneous mixtures of dry finely divided drug or chemicals intended for internal or external use. 1. Solid dosage forms: Granules :  Granules are consisting of solid, dry aggregates of powder particles often supplied in single-dose sachets. 1. Solid dosage forms: Tablets:  A hard, compressed medication in round, oval or square shape. 1. Solid dosage forms: Capsule :  Solid dosage form in which the drug is enclosed within a hard or soft gelatin shell. 1. Solid dosage forms: Spansules  Capsules that are filled with granules that dissolve at different rates. 1. Solid dosage forms: Caplet :  A caplet is a tablet that is shaped like a capsule, but smooth-sided like a tablet. 1. Solid dosage forms: Lozenges :  Hard, oval, or discoid solid dosage forms with a drug contained in a flavored sugar base. 1. Solid dosage forms: Effervescent tablets :  They are a solid dosage form designed to dissolve in water, releasing carbon dioxide in the process. This reaction creates a fizzy solution that contains the dissolved medication, which is then consumed as a liquid.  1. Solid dosage forms: Pastilles :  They are solid medicated preparations designed to dissolve slowly in the mouth.  They are softer than lozenges. 1. Solid dosage forms: Chewable tablets :  They are solid dosage forms designed to be chewed and broken down in the mouth before swallowing, rather than being swallowed whole. 1. Solid dosage forms: Orally Disintegrating Tablets (ODTs) :  They are a solid dosage form designed to dissolve or disintegrate rapidly in the mouth, typically within seconds, without the need for water. 1. Solid dosage forms: Modified-Release Tablets or Capsules :  They are designed to release the active ingredient(s) of the medication at a specific rate, location, or over a particular period of time, rather than immediately after administration. 1. Solid dosage forms: Transdermal patch A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. https://puzzel.org/en/crossword/play?p=-O5vy1KTo-BoWFjcSzbT 2. Liquid dosage forms: Solutions: Solution is a one homogenous phase, prepared by dissolving one or more solutes in a solvent. 2. Liquid dosage forms: Syrup: A syrup is a concentrated, viscous, and sweet liquid preparation that typically contains one or more active ingredients dissolved in water. 2. Liquid dosage forms: Emulsions: Emulsion is a dispersion system consisting of two immiscible liquids, cloudy appearance, either oil in water (O/W) or water in oil (W/O). 2. Liquid dosage forms: Suspensions: Suspension is a dispersion system where solid particles are dispersed in liquid phase. 3. Semisolid dosage forms: Gels: Thin, transparent or translucent, non- greasy preparation for external application. 3. Semisolid dosage forms: Creams: Cream is a topical preparation that consists of a mixture of water and oil phases, with the drug dispersed or dissolved in either phase. 3. Semisolid dosage forms: Ointments: Ointment is a semisolid dosage form with the oleaginous (hydrocarbon), water-soluble or emulsifying base. Oleaginous (hydrocabon) base: Petrolatum (Vaseline – white, yellow). Water-soluble base: Polyethylen glycol (PEG) ointment.  3. Semisolid dosage forms: Pastes:  Paste is a semisolid dispersion system, where a solid particles > 25%, e.g. ZnO, are dispersed in ointments – mostly oleaginous (Petrolatum). 3. Semisolid dosage forms: Suppositories: They are designed for insertion into body orifices, where they dissolve, melt, or soften at body temperature to release their active ingredients. They are commonly used for rectal, vaginal, or urethral administration. 3. Semisolid dosage forms: Pessaries  Pessaries (vaginal suppositories)  PEGs or glycerinated gelatin are often used as base.  Their administration needs applicator. 4. Gaseous dosage forms:  A gaseous dosage form refers to a medication that is administered in the form of gas or vapor. These dosage forms are typically used for inhalation therapy, where the drug is delivered directly to the respiratory system. Common examples include anesthetic gases like nitrous oxide and inhalers that deliver medication in the form of a fine mist, such as those used for asthma. Types of Pharmaceutical Dosage Forms A. According to the route of administration Systemic administration. Local administration. a) Dosage forms for Systemic administration It is a route of administration for medication, nutrition, or other substances into the circulatory system, affecting the entire body.  Route Dosage form Oral Powder, effervescent granules, tablets, capsules, syrups, drops. a) Dosage Rectal Enemas, suppositories forms for Parenteral Intravenous (I.V.), intramuscular (I.M.), systemic intraperitoneal (IP), subcutaneous (S.C.). administration Sublingual Tablets, spray. Transdermal Gel, patches. b) Dosage forms for Local administration The delivery of medication or treatment directly to the specific site or area where the therapeutic effect is needed, rather than into the systemic circulation (which would affect the entire body).  Route Dosage form Skin Ointment, cream, lotion, jells, shampoos(antidandruff ). b) Dosage Intravaginal Pessaries, creams, douches, foams. forms for Ophthalmic Drops, ointments. systemic administration Intranasal Drops, spray, ointment. Enteral or peroral Sublingual/Buccal Percutaneous (skin topical) Pulmonary (inhalation) Ophthalmic (ocular) Rectal Intravaginal Intra-nasal Parenteral ROUTES OF DRUG ADMINISTRATION  Enteral or peroral or oral: ROUTES OF DRUG ADMINISTRATION Administration to or by way of the mouth.  Buccal: ROUTES OF DRUG Administration ADMINISTRATION directed toward the cheek.  Sublingual: ROUTES OF DRUG Administration ADMINISTRATION beneath the tongue.  Topical (Cutaneous) ROUTES OF DRUG ADMINISTRATION Administration on the surface of the skin   Percutaneous Transdermal Administration ROUTES OF DRUG through the dermal ADMINISTRATION layer of the skin to the systemic circulation.   Intranasal Administration into ROUTES OF DRUG the nose. ADMINISTRATION   Ophthalmic (ocular) ROUTES OF DRUG ADMINISTRATION Administration into the eye.  Rectal ROUTES OF DRUG Administration into ADMINISTRATION the rectum.  Intravaginal ROUTES OF DRUG Administration into ADMINISTRATION the vagina.  Auricular (Otic) ROUTES OF DRUG Administration into ADMINISTRATION the ear.  Pulmonary (Inhalation) ROUTES OF DRUG Administration within ADMINISTRATION the lungs or its bronchi.  Parenteral route of drug administration: ROUTES OF DRUG ADMINISTRATION Administration by injection, infusion, or implantation.  Intra-arterial ROUTES OF DRUG Administration within ADMINISTRATION an artery.  Intra-articular ROUTES OF DRUG Administration within ADMINISTRATION a joint.  Intracardiac ROUTES OF DRUG Administration into ADMINISTRATION the heart.  Intracerebral ROUTES OF DRUG Administration into ADMINISTRATION the cerebrum.  Intravenous (I.V.) ROUTES OF DRUG Administration into a ADMINISTRATION vein.  Subcutaneous (S.C.) ROUTES OF DRUG Administration ADMINISTRATION beneath the skin; hypodermic.  Intramuscular (I.M.) ROUTES OF DRUG ADMINISTRATION Administration within a muscle.  Intradermal (I.D.) ROUTES OF DRUG ADMINISTRATION Administration within the dermis. Drug (API) & Excipients   Drug, active pharmaceutical ingredient (API), is a chemical compound which has certain pharmacological effect and used in diagnosis, treatment or prevention of diseases (prophylaxis). DRUG (API)  Generally, drugs are chemical compounds not administered to patients as such, but they are combined as part of a formulation with one or more non therapeutic (inert) agents known as excipients or additives.  API handling can be difficult or impossible (e.g. low doses, mg and µg ). DRUG (API) Accurate drug dosing can be difficult or Direct clinical impossible. use of the Some API can benefit from reducing the exposure to the environmental factors (light, active drug moisture…). substances, as API can be degraded at the site of administration (e.g., low pH in stomach). they are, is API may cause local irritations or injury when rare they are present at high concentrations at the site of administration. API can have unpleasant organoleptic qualities (taste, smell, etc.….).  Natural Products Sources of Drugs Synthetic drugs Semi-synthetic drugs Sources of Drugs 1. Natural Products: (a) Plants-drug  Drug is found in plant parts: roots, leaves stems, etc.  Examples: caffeine, morphine. Sources of Drugs 1. Natural Products: (b) Animals  Examples are beef/pork insulin (for diabetes mellitus). Sources of Drugs 1. Natural Products: (c) Mineral sources  Found in natural resources such as petroleum.  Examples: mineral oil (oral laxative). Sources of Drugs  1. Natural Products:  (d) Molds and yeast  Some drugs are isolated and purified from molds  e.g. Penicillin-G from green Penicillium notatum molds. Sources of Drugs 2. Synthetic drugs: Chemically synthesized moieties. Examples: acetaminophen (paracetamol). 3. Semi-synthetic drugs: Chemically modified natural products. Examples: Ampicillin (semisynthetic penicillins).  Definition: An excipient is a pharmacologically inactive substance formulated alongside the active pharmaceutical ingredient of a medication. EXCIPIENTS Purposes served by excipients: (ADDITIVES)  Provide bulk to the formulation.  Facilitate drug absorption or solubility and other pharmacokinetic considerations.  Aid in handling of “API” during manufacturing.  Provide stability and prevent from denaturation.  Ideal properties of excipients:  Chemically stable,  Pharmacologically inert, EXCIPIENTS  Easily for handling, (ADDITIVES)  Acceptable with regards to organoleptic characteristics,  Cost effective,  Non-toxic,  Non-reactive.  Various types of interactions that an excipient can undergo are termed as: EXCIPIENTS Drug-Excipient interactions, (ADDITIVES) Excipient-Excipient interactions, Package-Excipient interactions. Excipients Excipient category Function in formulation Examples of excipient Used in Solid Diluents Fillers: makes up the Lactose Dosage bulk of solid unit dosage Dextrose Forms forms when drug itself is inadequate to produce the bulk.  Excipient Function in formulation Examples of category excipient Excipients Binders and Impart cohesive qualities to Acacia Used in Solid Adhesives powdered material. Gelatin Dosage Forms Improves free flow qualities by formulation of granules.  Excipient Function in Examples of category formulation excipient Excipients Lubricants Reduce inter-particular Magnesium Used in Solid friction, prevent stearate adhesion of tablet Dosage material to the surface Forms of dies and punches facilitate easy ejection of tablet from die cavity. Excipients Excipient Function in Examples of Used in Solid category formulation excipient Dosage Glidants Added in dry state prior Corn starch Forms compression, it reduces friction between particles. Therefore, it improves flow characteristics of powder mixture.  Excipient Function in Examples of category formulation excipient Excipients Disintegrants Facilitate breakup or Starches Used in Solid disintegration administration after Dosage Coloring agents Impart aesthetic Dyes (must be Forms appearance form and for to dosage product approved and certified by F.D.A) identification.  Excipient Function in Examples of Excipients category formulation excipient Used in Solid Flavors Mask unpleasant flavors Dosage taste syrups Forms Sweeteners Impart sweet taste Mannitol to the formulation Excipients Excipient Function in formulation Examples of category excipient Used in Solid Coating Protect tablet ingredients Hydroxy propylmethyl Dosage materials from deterioration by cellulose (HPMC) moisture, help swallowing Forms unpleasant tasting tablets.  Excipient Function in formulation Examples of category excipient Excipients Solvents Dissolving solute/Active Water alcohol pharmaceutical ingredient. Used in Liquid Dosage Forms Co-solvents Increase the solubility of solute Ethanol Glycerin in water  Excipient Function in Examples category formulation Buffers Maintain pH of the Phosphate Excipients buffers formulation. Used in Liquid Dosage Forms Antimicrobial Prevent microbial growth in Benzyl alcohol formulations. preservatives Control oxidation. Ascorbic acid Antioxidants  Excipient Function in Examples category formulation Excipients Prevent sedimentation, Hydroxyethyl Thickening Used in Liquid modify viscosity. cellulose agents Dosage Forms Humectants Retard evaporation of Glycerol aqueous vehicles from dosage forms.  Excipient Function in formulation Examples category Excipients Emulsifying Promotes and Tween maintains the Used in Liquid agents dispersion of finely Dosage Forms subdivided particles of liquid in vehicles where it is immiscible.  Excipient Function in Examples category formulation Sweetening agents Impart sweetness Sucrose Saccharin Excipients Aspartame Used in Liquid Dosage Forms Colors Impart color Amaranth Flavors Impart flavor Aromatic waters Syrup  Excipient Function in formulation Examples category Gelling Increase the viscosity of a Carboxy methyl Excipients agents substance. cellulose (CMC) Used in Form gels. Semisolid Emollients Softens the skin or soothes Glycerin irritated skin or mucous Dosage Forms membranes. Suppository Used to form base for Cocoa butter bases dissolving active ingredient.  Excipient Function in formulation Examples category Stiffening Increases thickness or White soft Excipients agent hardness of preparations, paraffin Used in usually an ointment. Semisolid Dosage Forms Levigating An intervening agent used Mineral oil to reduce the particle size Agent of a powder by grinding, usually in a mortar.