Workshop 2 Pharmaceutical Forms PDF

Workshop 2 Pharmaceutical Forms Vittoria Carrabs PhD aa 2024/2025 III Medicine  GENERIC DRUGS 2. DOSAGE FORMS 3. ROUTES OF ADMINISTRATION 4. SYMBOLS AND ABBREVIATIONS 1. GENERIC DRUGS Medicine substant that...

Workshop 2 Pharmaceutical Forms Vittoria Carrabs PhD aa 2024/2025 III Medicine  GENERIC DRUGS 2. DOSAGE FORMS 3. ROUTES OF ADMINISTRATION 4. SYMBOLS AND ABBREVIATIONS 1. GENERIC DRUGS Medicine substant that solubilize change color of flavor dilute or suspende it API (Active Pharmaceutical Excipients Ingredients) INACTIVE pharmaceutical ingredients The purpose of using excipients is to: solubilize stabilize suspend preserve thicken color dilute flavor emulsify 1. GENERIC DRUGS Bioavailability (BA): the rate* and extent* to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action. * Rate: How rapidly does the drug get from its site of administration, to the general circulation * Extent: How much of the administered dose enters the general circulation 1. GENERIC DRUGS Figure. Summary of Bioavailability Definitions PHARMACEUTICAL EQUIVALENT: All acetylsalicylic acid tablets of a particular dose PHARMACEUTICAL ALTERNATIVE tetracycline hydrochloride, 250 mg capsules vs. tetracycline phosphate complex, 250 mg capsules quinidine sulfate, 200 mg tablets vs. quinidine sulfate, 200 mg capsules. Amoxicillin, 500 mg capsules vs. Amoxicillin, 250 mg sachet  1. GENERIC DRUGS REFERENCE PRODUCT GENERIC DRUG (INN*) ✓ Identified by the Regulatory ✓Drug product which is identical or Authorities as “Designated bioequivalent to Brand/ Reference Reference Product” drug in: ✓ Usually the Global Innovator’s Active ingredient (s) Route of administration Product Dosage form ✓Protected by a patent Strength ✓Marketed under manufacturers Indications brand name Safety ✓ Clinical efficacy and safety profile ✓May have different: Inactive ingredients is well documented in extensive trials Colour ✓ All generics must be clinically Shape Bioequivalent to it ✓ Almost half of drugs in market have need to know the allergy for the change of excipient Generics (E.F.G.) * Each International Nonproprietary Name (INN) is a unique name that is globally recognized and is public property. A nonproprietary name is also known as a generic name. 1. GENERIC DRUGS Two drug products are considered BIOEQUIVALENTS if they exhibit similar pharmacokinetic profiles in terms of how the drug is absorbed into the body, specifically: Rate of absorption: This refers to how quickly the drug reaches its maximum concentration in the bloodstream after administration. It's measured by Cmax (the maximum plasma concentration). Extent of absorption: This refers to the total amount of the drug that enters the bloodstream. It's measured by the AUC (Area Under the Curve), which represents the drug concentration over time. Bioequivalent drugs are expected to have the same efficacy and safety profile when used interchangeably. This is a key factor in the approval of generic drugs, ensuring that they perform similarly to the original reference product. How to administer? 1. GENERIC DRUGS DOSAGE FORMS 3. ROUTES OF ADMINISTRATION 4. SYMBOLS AND ABBREVIATIONS 2. DOSAGE FORMS They are classified according to: Route of administration Physical form Oral Solid Topical Semisolid Rectal Liquid Parenteral Vaginal Inhaled Ophthalmic Otic 2. DOSAGE FORMS 2.1. SOLID dosage forms: Powder Granule Capsule Tablet Suppository Pessaries Implants (pellets) 2. DOSAGE FORMS Powder: a mixture of dry, finely divided drugs 2.1. SOLID dosage forms: Types of Powders ✓ Dusting powders: External use talc and zinc stearate ✓ Effervescent powders ✓ Insufflations (Inhalers) Internal use ✓ Dentifrice ✓ Oral powders 2. DOSAGE FORMS 2.1. SOLID dosage forms: Granule: a small particle or grain.  Granulation is the process of particle size enlargement of homogeneously mixed powder ingredients. 2. DOSAGE FORMS 2.1. SOLID dosage forms: Capsule: a medication in a gelatin container Advantage: mask the unpleasant taste, good stability and BA Disadvantages: swallowing problems Specific Types of Capsules 1. Hard capsules: used for dry, powdered ingredients 2. Soft capsules, used for oils Gastro-resistant capsules 3. Controlled-release capsules Modified-release capsules steroids : large time 2. DOSAGE FORMS 2.1. SOLID dosage forms: Tablet: a hard, compressed medication in round, oval or square shape. Pill: small, round solid dosage forms Advantages: Precision dosing and extended shelf life Disadvantages: Limited use in patients who can not swallow, BA problems. 2. DOSAGE FORMS 2.1. SOLID dosage forms: Tablets ✓ Uncoated tablets: ✓ Coated tablets: A coating may be applied to: 1. mask the unpleasant tastes, odor 2. Improve the appearance 3. protect the active ingredient from air, moisture, light 2. DOSAGE FORMS 2.1. SOLID dosage forms: Tablets ✓ Delayed-release tablet: releases the drug at a time other than promptly after administration (e.g., enteric-coated tablets) ✓ Sublingual and buccal tablets: Advantages: - Rapid absorption (e.g., vasodilators) → Quick onset of action. between gum - to avoid: and cheek under the tongue - acid and enzymatic environment of the (buccal) (sublingual) stomach [4 h disintegration time] [2 min disintegration time] - drug metabolizing enzymes of the liver - first pass effect 2. DOSAGE FORMS 2.1. SOLID dosage forms: Tablet ✓Multilayer tablet: several different granulations compressed on top of each other to form a single tablet. use: - incompatible drug substances - release of drugs at different times intervals ✓Chewable tablets: they are disintegrated smoothly in the mouth, either with or without actual chewing use: - administration to children (e.g., vitamins) - patients with difficulty swallowing children 2. DOSAGE FORMS 2.1. SOLID dosage forms: Tablet ✓Effervescent tablet: uncoated tablets that contain acid substances and carbonates or bicarbonates which release carbon dioxide when dissolve in water. ✓Lozenge: A small, medicated candy intended to be dissolved slowly in the mouth to lubricate irritated tissues of the throat. 2. DOSAGE FORMS 2.1. SOLID dosage forms: Suppository: a solid dosage form intended for insertion into body orifices where they melt, soften, or dissolve at body temperature. Rectal suppositories: mechanical (laxatives), local (anesthetics) or systemic actions Advantages: used to promote evacuation of bowel. avoid any gastrointestinal irritation. can be used in unconscious patients. avoid first-pass metabolism (systemic absorption). people suffering from severe nausea or vomiting. 2. DOSAGE FORMS 2.1. SOLID dosage forms: Vaginal suppositories or Pessaries: These are meant for introduction into vagina for local action. Common ingredients for inclusion in pessaries include: antiseptics contraceptive agents local action local anesthetics various therapeutic agents to treat infections molded pessaries compressed pessaries (vaginal tablet) vaginal capsule (Ovule) 2. DOSAGE FORMS 2.2. SEMISOLID dosage forms: Ointment Paste Cream Gel 2. DOSAGE FORMS 2.2. SEMISOLID dosage forms: not cream Ointment: a semi-solid greasy preparation meant for application to skin, rectum or nasal mucosa. The base is usually anhydrous and immiscible with skin secretions. Uses: - Emollient - Application for active ingredients to the skin - More occlusive than cream 2. DOSAGE FORMS 2.2. SEMISOLID dosage forms: Paste: they are basically ointments into which a high percentage of insoluble solid has been added. They are generally very thick and stiff. - good protective barrier over the skin Examples: - Triamcinolone acetonide dental paste - Zinc oxide paste 2. DOSAGE FORMS 2.2. SEMISOLID dosage forms: Cream: a viscous semisolid emulsion system that is mixtures of oil and water. Miscible with the skin secretion. Two types: A-oil-in-water (aqueous cream): small droplets of oil dispersed in a continuous aqueous phase. B-water-in-oil (oily cream): small droplets of water dispersed in a continuous oily phase. 2. DOSAGE FORMS 2.2. SEMISOLID dosage forms: Gel (Jelly): semisolid system in which a liquid phase is constrained within a 3-D polymeric matrix having a high portion of water. Uses: medication or lubrication. 2. DOSAGE FORMS 2.3. LIQUID dosage forms: Solution Suspension Emulsion Syrup Elixir Liniments Injection  2. DOSAGE FORMS 2.3. LIQUID dosage forms: Solution, Suspension and Emulsion: a- solution: one or more APIs completely dissolved in a solvent or mixture of mutually miscible solvents b- suspension: solid particles dispersed throughout a liquid phase in which the particles are not soluble  extemporaneous suspension: prepared in time to be administered. Administration of poorly water soluble active ingredients. c- emulsion: stabilized oil-in-water dispersions, either or both phases of which may contain dissolved solids miscellar water 2. DOSAGE FORMS 2.3. LIQUID dosage forms: Advantages: - Rapid release of active ingredients: high speed BA. - More easy and comfortable dosage (tablespoons, drops) - Particularly of choice in children Drawbacks: - A higher microbiological contamination (addition of preservatives) - Lower stability of the active ingredient 2. DOSAGE FORMS 2.3. LIQUID dosage forms: Syrup: saturated sugar solution Elixir: sweetened hydroalcoholic solution Liniments: alcoholic or oily liquid dosage forms intended for application to the skin generally by rubbing for skin 2. DOSAGE FORMS 2.3. LIQUID dosage forms: oil or water Injection: A solution, emulsion (O/W) or suspension prepared in a sterile and pyrogen-free vehicle, which is intended to be administered parenterally: emulsion suspension solution possible - intravenous - intramuscular The most common - subcutaneous 1. GENERIC DRUGS 2. DOSAGE FORMS ROUTES OF ADMINISTRATION 4. SYMBOLS AND ABBREVIATIONS 3. ROUTES OF ADMINISTRATION CLASSIFICATION SYSTEMIC LOCAL Epidermal Intranasal Inhalation Parenteral Conjunctival Transdermal Mucosal-throat Enteral Inhalation Vaginal (digestive tract) Injections Intravenous Mouth Oral (swallow) Intramuscular Ear Sublingual Subcutaneous Otic Buccal Intra-arterial Rectal Intra-articular Intrathecal Intradermal Intramammary 3. ROUTES OF ADMINISTRATION Factors to be considered: 1. properties of the drug 2. onset of action required 3. convenience 4. cost 3. ROUTES OF ADMINISTRATION ENTERAL ROUTES 3.1. Oral route (po)  Onset of action: 30 minutes Advantages: - safest route Dosage forms - most convenient Capsules, tablets, syrup, emulsion, etc. - economical Disadvantages: - slow-onset of action - GI irritation - dosage absorbed is erratic - inactivation in the liver 3. ROUTES OF ADMINISTRATION When to Avoid Giving Drugs Orally? If the drug causes nausea and vomiting If the patient is currently vomiting emisis If the patient is unwilling or unable to swallow (e.g., child, mentally handicapped, unconscious) If the drug is destroyed by digestive enzymes (e.g., insulin) If the drug is not absorbed through the gastric mucosa (e.g., aminoglycosides) local anesthetic If the drug is rapidly degraded (e.g., lidocaine) 3. ROUTES OF ADMINISTRATION ENTERAL ROUTES 3.2. Sublingual route Drugs:  Onset of action: minutes - Nitrates: angina attacks - Calcium-channel blockers: hypertensive Advantages: emergencies - rapid onset of action - Opioids: intense pain - avoid first pass effect - Benzodiazepines: anxiety attack Dosage forms: Tablets and aerosols 3. ROUTES OF ADMINISTRATION ENTERAL ROUTES 3.3. Rectal administration  Onset of action: faster onset, higher bioavailability, shorter peak, and shorter duration than the oral route Advantages: - can be used with infants, unconscious or vomiting patients - partially avoids first-pass elimination Disadvantages: - absorption is erratic unpredictable Dosage forms: Suppositories and enemas  3. ROUTES OF ADMINISTRATION ENTERAL ROUTES 3.3. Rectal administration Enema: a liquid-drug solution Uses: - Laxative: - Local action: Crohn's disease treatment - Systemic action (colonic absorption): status epilepticus treatment in children (microenemas Diazepam) 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES EXTRAVASCULAR 3.4. Parenteral administration Intradermal (ID) (into skin) Intraperitoneal (IP) (peritoneal cavity) INTRAVASCULAR Intrathecal (IT) (cerebrospinal fluids) Intravenous (IV) (into veins; Epidural (into the epidural space) urgency) Intramuscular (IM) (into skeletal Intra-arterial (IA) (into arteries) muscle) Intracardiac (IC) (into the heart Subcutaneous (SC) muscles or ventricles; emergency) (into subcutaneous tissue) Intra-articular (synovial fluids) 100% Bioavailavility 100% of absorption  3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.4. Parenteral administration Subcutaneous hgher liposolubility Drugs administered by SC route are absorbed more slowly than IM injections. A volume of 0.5 to 1 mL is used for subcut injection. Intramuscular Drugs that are irritating to subcut tissue can be given by IM injection. Drugs given by this route are absorbed more rapidly than drugs given by the SC route (rich blood supply in the muscle). A larger volume (1 to 3 mL) can be given at one site. 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.4. Parenteral administration Intravenous Drug action occurs almost immediately. Drugs administered by the IV route may be given: Slowly, over 1 or more min Rapidly (IV push) By piggyback/syringe pump infusions Into an existing IV line (the IV port) Into an intermittent venous access device called a heparin or saline lock By being added to an IV solution and allowed to infuse into the vein over a longer period 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.4. Inhalation  Site: Inspiration mouth/nose Rapid access to  Advantages: circulation - large surface area - thin membranes separate alveoli from circulation - high blood flow Rapid onset of action  Uses: - Local action: asthma and COPD treatment - Systemic action: general anesthesia Dosage forms: - Aerosols sprays - Nebulizers 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.5. Transdermal  Site: absorption of drug through skin  Advantages: - Stable blood levels (controlled drug delivery system) - No first pass metabolism - Long duration of action Dosage forms: - Transdermal patch 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.6. Topical administration (top.)  Onset of action: minutes Local action TOPICAL ROUTES ▪ Dermatologic ▪ Ophthalmic ▪ Otic ▪ Nasal ▪ Dental and throat ▪ Vaginal Dosage forms: Lotion, Cream, Liniment, Ointment, etc 3. ROUTES OF ADMINISTRATION TOPICAL ROUTES 3.7. Ophthalmic route (o.u.)  Site: directly into the eye (conjunctival sac)  Local action Dosage forms: Cream, Ointment or Liquid drop (ophthalmic preparations are sterile and often refrigerated for storage) Place medication in the conjunctival sac. Do not instill the medication directly onto the cornea. 3. ROUTES OF ADMINISTRATION PARENTERAL ROUTES 3.8. Auricular route (a.u.)  Administration to or by way of the ear.  The drug action is mostly topical/local. Dosage forms: Sterile drops and solutions 1. COMMON DOSAGE FORMS 2. GENERIC DRUGS 3. ROUTES OF ADMINISTRATION SYMBOLS AND ABBREVIATIONS 4. SYMBOLS AND ABBREVIATIONS Products which must be stored between 2-8° C° Products which have a shelf life less than 5 years. EFP, OTC Products available without medical prescription Prescription-only products Hospital use / Diagnosis performed in hospital; It requires specialist H / DH prescription and inspection visa TLD Products available on a renewable prescription ECM Specialist supervision Narcotic medicinal products Psychotropic substances included in the Annex II of the Convention on psychotropic substances of 1971 For psychotropic substances in Schedules I, II and IV in the Annex I of the Convention on psychotropic substances of 1971 4. SYMBOLS AND ABBREVIATIONS Products which may reduce the ability to drive or operate machines Products which may produce photosensitivity International symbol established by the UNE-73302 (1991) indicative of radioactivity Symbol of oxidizing medical gas Symbol of flammable medical gas