Drug Delivery Systems & Dosage Forms PDF

om il. c DRUG DELIVERY SYSTEMS m a @ g & DOSAGE FORMS 92 4 PREPARED BY: KARL KIRBY 2 Z. COSTALES,...

om il. c DRUG DELIVERY SYSTEMS m a @ g & DOSAGE FORMS 92 4 PREPARED BY: KARL KIRBY 2 Z. COSTALES, RPH a li m l a. s h i l sh a Where Degrees Become Legacies.  OUTLINE om l. c mai @ g 92 2 I. Introduction II. Solid Dosage Forms m 4 li sa III. Liquid Dosage Forms a. ill IV. Semi-solid Dosage Forms a h sh Write lesson or topic here Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a. sa ill ah I. INTRODUCTION s h A. DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail An agent intended for use in the ____________, ____________, ___________, m ______________ and _____________ of disease in man or animals. g Article recognized in official pharmacopeias and formularies, including homeopathic @ 2 pharmacopeias, or any documentary supplement to any of them, which are recognized and 9 adopted by the FDA. 2 It refers to the component which produces the pharmacologic activity. 4 m AKA: _____________, _______________, ______________ _______________ li sa Inactive ingredient present in a dosage form that typically constitutes the largest portion.. It typically improves the aesthetic appearance or the stability of the product. ill a Examples: Vehicle, suspending agents, lubricants, binders a h sh INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail The _________, by which drugs are delivered to their site of action. g m 2 @ The _________ ___________ used to deliver medication to site-specific area. 9 Formulations which provide a therapeutic amount of drug to the proper site in the body 2 4 promptly and maintain the desired drug concentration products that allow the uniform m release and targeting of drugs into the body. li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail The _________, by which drugs are delivered to their site of action. g m 2 @ The _________ ___________ used to deliver medication to site-specific area. 9 Formulations which provide a therapeutic amount of drug to the proper site in the body 2 4 promptly and maintain the desired drug concentration products that allow the uniform m release and targeting of drugs into the body. li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail Formulation containing a specific quantity of active ingredient(s) in combination with one m or more excipients. @ g It provides a mechanism for the safe and convenient delivery of the drugs. It allows for the concealment of offensive taste and the protection from the environment. 92 Examples: Tablet, capsule, injectables 4 2 The finished dosage form that contains the active ingredient, generally, but NOT m NECESSARILY, in association with one or more other ingredients. li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail A prototype chemical compound that has a fundamental desired biologic or pharmacologic m activity. g A compound that requires metabolic transformation after administration to produce the @ 2 desired pharmacologically active compound. 2 9 m 4 li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES ail A rare disease or condition that affects fewer than 200,000 people in the United States. m Examples: Chronic Lymphocytic Leukemia, Gaucher Disease, Cystic Fibrosis g A drug or biologic product for the diagnosis, treatment, or prevention of a rare disease or @ 2 condition. 2 9 m 4 li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  A. DEFINITION OF TERMS om. c TERM NOTES A dosage form with no active ingredient. ail m “I shall please” g Similar to placebo, but it has a negative effect or it can cause harm. @ 2 “I shall harm” 2 9 m 4 li a. sa h ill sh a INTRODUCTION | DEFINITION OF TERMS Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill ah I. INTRODUCTION s h B. SKINCARE Where Degrees Become Legacies.  B. SKINCARE om. c TERM NOTES ail Any substance or preparation intended to be placed in contact with the m External parts of the human body (epidermis, hair, nails, lips, genitals) Teeth Mucus membrane of the oral cavity @ g 92 With a view exclusively or mainly to: C_____ P_________ 4 2 li m C_________ ______ ____________ sa C_________ ______ ______ a. P_________ ill K__________ _____ __ ____ ________ h Regulated as drugs: a sh Mouthwash Diaper ointments Anti-perspirants INTRODUCTION | Skincare Where Degrees Become Legacies.  B. SKINCARE om. c TERM NOTES ail A photoprotective topical product that protects against sunburn and prevent skin cancer m by scattering UV-A (___________) and UV-B (_____________) @ g Its level of protection is measured by SPF or SUN PROTECTION FACTOR It is defined by the ratio of the dose of energy required to produce a Minimum 92 Erythemal Dose (MED) on protected skin over UNprotected skin 4 2 SPF = exposure time to produce erythema (protected) / exposure time to produce li m erythema (unprotected) a. sa Example: SPF 10 means its protection can last ten times longer than without ill sunscreen. a h sh ACTIVE INGREDIENTS: Organic: p-Aminobenzoic acid, Cinnamates, Salicylates, Anthranilates, Camphor, Benzophenones, Dibenzoylmethanes, Octocrylene Inorganic: Zinc oxide, Titanium dioxide INTRODUCTION | Skincare Where Degrees Become Legacies.  B. SKINCARE om. c TERM NOTES Reddens the skin through vasodilation to relieve pain ail Helpful for oily skin g m Causes the constriction of body tissues to stop bleeding or tighten pores. 2 @ Similar to astringents, but it is more helpful for dry skin Relieves itching 2 9 m 4 Produces a superficial irritation in one part of the body to relieve irritation in another li sa Makes the skin soft and pliable a. Prevents the escape of water from the skin h ill Prevents drying of the dosage form sh a INTRODUCTION | Skincare Where Degrees Become Legacies.  OUTLINE om l. c mai @ g 2 I. Introduction II. Solid Dosage Forms 2 9 A. Powders m 4 li sa B. Granules a. ill C. Capsules h D. Tablets sh a Write lesson or topic here Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill II. SOLIDahDOSAGE FORMS s A. POWDERS h Where Degrees Become Legacies.  A. POWDERS om. c NOTES DEFINITION Mixture of finely divided particles in dry form ail m It may be used internally (e.g. oral powders) or externally (e.g. topical powders) @ g Use of medicated powders is limited → preparation of other dosage forms is more common. Compression into tablets or encapsulation into capsules 92 Dissolved or suspended in a solvent or vehicle 2 Incorporated in semisolid bases 4 m PROS Rapid onset of action li sa Readily adjustable dose. Dry and devoid of moisture ill a More stable compared to liquid preparations h CONS Inaccuracy of dose sh a Not easily wetted Poor flowability Inconvenient Some are hygroscopic, deliquescent, or efflorescent SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c i. BULK POWDERS m ai g For non-potent drugs @ Dispensed in large quantities Non-individual dosing 92 2 Packaging: Wide-mouth plastic or glass bottles, sifter cans, aerosol EXAMPLES NOTES m 4 li sa Dissolved in liquids (e.g. water or infant formulas) or taken with soft food. Used if patients have difficulty swallowing other solid dosage forms ill a CONS: unpleasant taste, extensive first-pass effect h Examples: a Local effect: Laxatives sh Systemic: Analgesics SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c i. BULK POWDERS m ai g Powder for cleaning teeth @ Abrasive, anti-cariogenic 2 Examples: Toothpaste powders (especially those containing fluoride) 9 Has no systemic toxicity 4 2 Locally applied into the skin by sifter-top containers li m Examples: Talc, cornstarch, Canesten (clotrimoxazole) a. sa h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c i. BULK POWDERS m ai g Administered with the aid of dry powder inhalers (DPIs) @ Examples: Relenza (Zanamivir) From coarsely powdered herbs 92 4 2 Dilutions of potent powdered drugs m 1:10 ratio li a. sa h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c i. BULK POWDERS m ai g Applied into body cavities (i.e. vagina) @ Dissolved in warm water, with a pH of 3.5-5 Examples: Massengill powders 92 4 2 Introduced into body cavities with an insufflator or puffer Powder is placed into the vessel and the rubber bulb is squeezed to releasethe drug particles. li m sa It must pass through a mesh #100 a. It also uses Polyox, an ethylene oxide polymer that is a moisture-activated adherent. This ill forms a viscous, muco-adhesive gel that allows for long-term drug delivery. a h CONS: Inaccurate dosing sh SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c ii. DIVIDED POWDERS m ai g AKA chartulae, Individualized Powders, Paper Tabbing @ For potent drugs (but this may also be used for non-potent drugs) Dispensed in small quantities 92 2 Individual dosing Preparation m 4 li 1. Potent: Weighing each dose separately before enfolding in paper sa 2. Non-Potent: Block-and-divide method a. hill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c ii. DIVIDED POWDERS m ai g PAPER NOTES BOND PAPER NO moisture resistance 2 @ 9 Opaque, used for pharmaceutical elegance :> VEGETABLE 4 LIMITED moisture resistance 2 m SEMI-opaque, Thin i PARCHMENT GLASSINE sa l LIMITED moisture resistance. TRANSPARENT, Glazed a ill WAXED Waterproof paper a h TRANSPARENT sh SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 1. Types of Powders l. c SITUATION USE THIS: m ai Hygroscopic or deliquescent powder Waxed @ g Only a limited barrier against moisture is necessary 92 Glassine, Vegetable parchment Volatile 4 2Waxed, Glassine li m Waxed Paper is typically double wrapped and then wrapped again in bond paper for aesthetic appeal. a. sa h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 2. Classification of Powders l. c m ai *For Chemicals @ g 2 Description Sieve No. Limit Coarse 2 9 NMT 60% thru No. 40 Moderately Coarse m 4 NMT 60% thru No. 60 li sa Fine No Limit Very Fine a. h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 2. Classification of Powders l. c m ai *For Crude Drugs @ g 2 Description Sieve No. Limit Very Coarse 2 9 NMT 20% thru No. 60 Coarse m 4 NMT 40% thru No. 60 li sa Moderately Coarse NMT 20% thru No. 80 Fine a. NMT 20% thru No. 100 Very Fine h ill No Limit sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 2. Classification of Powders l. c m ai *Summary @ g 2 Description Crude Drugs Chemicals Very Coarse 2 9 Coarse m 4 li sa Moderately Coarse Fine a. Very Fine h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 3. Comminution of Powders l. c Description m ai g A process of particle size reduction @ MICRONIZATION: Method of producing finer drug particles under 10 micrometers METHOD NOTES 92 4 2 This is intended to both comminute and mix m Grinding using mortar and pestle li sa MORTAR AND PESTLE NOTES ll a. Solutions, suspensions, smooth ointments, staining substances h i Preferred for simple mixing s h a Soft aggregates or crystals (with a rough inner surface) Crystalline solids (with a rougher inner surface) SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 3. Comminution of Powders l. c METHOD NOTES m ai g Use of a non-volatile non-solvent @ Forms a PASTE using a levigating agent: does NOT dissolve the active ingredient It reduces grittiness 92 2 Utilizes figure 8 track movement 4 Examples of Levigating Agents: Mineral oil, glycerin, liquid petrolatum m li Addition of a volatile solvent sa Used for gummy like particles or hard crystalline powders that do not crush or triturate a. ill easily. You intervene with the solvent, which will disappear after the goal is reached. a h Examples: Camphor + alcohol, Iodine crystals + ether sh Use of rotary cutter, hammer, or roller mills SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 4. Blending/Mixing of Powders l. c Description m ai g A process of particle size reduction @ MICRONIZATION: Method of producing finer drug particles under 10 micrometers METHOD NOTES 92 4 2 This is intended to both comminute and mix m Ratio: 1:10 li sa For non-potent substances or small quantities of powder because it can NOT achieve a. homogenous blending. ill Compression or compaction is not achievable, thus it is suitable for eutectic mixtures. h If little contact is desired, add magnesium oxide or magnesium carbonate sh a For non-potent substances Passing through sifters Results in a light, fluffy product SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  A. POWDERS om 4. Blending/Mixing of Powders l. c METHOD NOTES m ai g For potent substances @ 1:1 Ratio of diluent and powder 92 Uses a rotating chamber or a large container rotated by a motor Thorough but time-consuming 4 2 Utilized in large-scale manufacturing or if cytotoxic powders are involved. li m sa Solid-Solid Mixing: Twin Shell Blender a. Solid-Liquid Mixing: Sigma Mixer h ill sh a SOLID DOSAGE FORMS | Powders Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill II. SOLIDahDOSAGE FORMS s B. GRANULES h Where Degrees Become Legacies.  B. GRANULES om. c NOTES DEFINITION Prepared agglomerates of smaller particles of powder ail m Passed through size 4-12 mesh Irregularly shaped but it may be spherical @ g 2 PROS Prevents segregation of the constituents of the powder Improves flowability 2 9 4 Improves compaction (due to outer binder-rich layer) m More stable & more easily wetted li sa Less prone to caking or hardening TYPES OF a. Good Granules: Pass through #20 but not #40 ill GRANULES Fine Granules: Pass through #40 a h IDEAL RATIO: 90% Good and 10% Fine sh Too Many Good → Voids Too Many Fines → Interparticulate friction SOLID DOSAGE FORMS | Granules Where Degrees Become Legacies.  B. GRANULES om. c EXAMPLE NOTES EFFERVESCENT Citric acid: Tartaric acid: NaHCO3 ail m GRANULATED 1:2:3.4 SALTS Citric acid only: @ g 2 Tartaric acid only: Prepared by: 2 9 4 Dry/Fusion Method: molecules of water of citric acid acts as a binding agent m li Wet Method: water added to alcohol acts as a moistening agent a. sa h ill sh a SOLID DOSAGE FORMS | Granules Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill II. SOLIDahDOSAGE FORMS s C. CAPSULES h Where Degrees Become Legacies.  C. CAPSULES om. c NOTES DEFINITION ail Solid dosage forms in which medicinal agents and/or excipients are encapsulated in a small m shell of gelatin GELATIN @ g Obtained by the partial hydrolysis of collagen obtained from the skin, white connective 2 tissues, and bones of animals. Properties: 2 9 4 Insoluble but it softens in cold water through the absorption of water up to 10 times its m weight of water li Soluble in hot water and warm gastric fluid → This means it is easily dissolved,. sa digested, and absorbed. ill a ALTERNATIVES TO Indicated for religious or dietary restrictions h GELATIN Examples: Vegetable capsules (Vegetel), HPMC, Hard starch capsules, Gulaman (From sh seaweeds) a SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  C. CAPSULES om 1. Types of Gelatin l. c GELATIN A m ai GELATIN B g Pork Skin Bones, Animal Skin Acidic hydrolysis 2 @ Basic hydrolysis Isoelectric point: 9 2 9 Isoelectric point: 4.7 QC TEST NOTES m 4 li sa BLOOM Weight in grams needed by a specific plunger to depress the gel without breaking STRENGTH a. Measures the strength of gelatin h ill HGC: 200 to 250 g sh a SGC: 150 g SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  C. CAPSULES om 2. Capsule Sizes l. c ai Size Capacity (mL) Easier Version gm 000 1.4 1.4 @ 00 0.95 1.0 92 0 0.68 0.7 42 1 0.5 0.5 im 2 0.37 0.4 sa l 3 0.30 0.3 a. ill 4 0.21 0.2 h 5 0.13 0.1 sh a SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  C. CAPSULES om 3. Types of Capsules l. c i. HARD GELATIN CAPSULES m ai g AKA Hard-shell capsules, Two-piece, Dry-filled COMPONENTS Gelatin + Sugar + Water → Capsule Shell 2 @ 9 0.15% Sulfur Dioxide → Anti-oxidant FD&C or D%C Dyes → Colorants 4 Titanium dioxide → Opaquant 2 13-16% li m sa MOISTURE. CONTENT If too dry → brittle, crumble ill a If too moist → tacky, distorted, and looses rigidity h STORAGE 21-25 degree Celsius CONDITIONS PARTS sh a 31-50% relative humidity Cap: shorter, wider Body: taller, narrower SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  C. CAPSULES om 3. Types of Capsules l. c i. HARD GELATIN CAPSULES mai @ g 92 42 lim a.sa hill sh a SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  C. CAPSULES om 3. Types of Capsules l. c ii. SOFT GELATIN CAPSULES m ai g AKA Soft-Shell Capsules, Softgel, One-piece Capsule COMPONENTS Gelatin 2 @ 9 Plasticizer (Glycerin, Polyhydric alcohol (Sorbitol)) → renders felexibility 4 Titanium dioxide → Opaquant 2 Methylparaben or Propylparaben → Preservative 6-10% li m sa MOISTURE. CONTENT STORAGE ill a 21-25 degree Celsius h CONDITIONS 31-50% relative humidity USES sh a Water-Immisible volatile and nonvolatile liquids Fat-soluble drugs and vitamins SOLID DOSAGE FORMS | Capsules Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill II. SOLIDahDOSAGE FORMS D. TABLETS s h Where Degrees Become Legacies.  D. TABLETS om. c NOTES DEFINITION ail Solid dosage forms usually prepared with the aid of suitable pharmaceutical excipients. m Prepared primarily by compression or molding. g They may be scored or grooved that allows them to be easily broken into two or more parts. @ 2 PROS Low manufacturing cost, easy to package and ship 9 Precision and low content variability 2 4 Easy to swallow m Most stable of all oral dosage forms li sa CONS Some drugs are incompressible. Some drugs are sensitive to humidity and air a h ill sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c i. MOLDED TABLETS (SOFT TABLETS) m ai g Small, cylindrical tablets containing small amounts of usually potent drugs (10%) @ They must be readily and completely soluble in water 92 They are also soft and designed for rapid dispersion. 2 Examples: NTG Tablets 4 Used by physicians in extemporaneous preparations of parenteral solutions. m li No longer available, replaced by prefabricated injectables sa Problem: Sterility Issues a. ill Used by pharmacists in extemporaneous preparations of parenteral solutions. AKA: compounding tablets a h They contained large amounts of highly potent drugs. sh SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c ii. COMPRESSED TABLETS (HARD TABLETS) m ai g Underwent only 1 compression 2 @ 9 Underwent 2 or more compressions Types: 4 2 Multiple-Layer Tablet: Initial compaction of 1 drug followed by another compaction li m Compression-Coated Tablet: A core of 1 drug is covered with a shell of another drug. sa Used if: a. Active ingredients are incompatible ill Mask the bitter taste a h Drug is irritating to the stomach sh SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c ii. COMPRESSED TABLETS (HARD TABLETS) m ai g Big tablets, with a creamy base, meant to be chewed and subsequently swallowed @ For patients who cannot swallow 2 Diluents: Mannitol, Xylitol (sugar-free alternative) → has a negative heat of solution 9 2 Examples: Multivitamins, Antacids (Kremil-S) 4 Designed to be absorbed in the buccal pouch m Lasts for 4 hours li sa Small, flat, and oval a. ill Designed to be placed under the tongue Lasts for 2-3 minutes (uses Superdisintegrants) a h Examples: Nitroglycerin sh Releases carbon dioxide when exposed in water AKA vaginal inserts Uses a plastic inserter device SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c ii. COMPRESSED TABLETS (HARD TABLETS) m ai g AKA vaginal inserts @ Uses a plastic inserter device 2 Moisten with water and then push the plunger 9 2 Disc-shaped solid dosage forms containing a medicinal agent and generally a flavoring 4 m substance in a hard candy or sugar base. li Example: Dichlorobenzyl alcohol + Amylmetacresol (Strepsils) a. sa Compressed Lozenges (Taladafil) ll Molded Lozenges (cough drops, Scott’s Vitamin C) h i a Lozenges on sticks (Fentanyl (ACTIQ)) s h SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c ii. COMPRESSED TABLETS (HARD TABLETS) m ai g Implanted under the skin by a trocar or cannula inserted to provide sustained release of @ the drug that lasts up to weeks and months Examples: 92 2 Levonorgestrel: contraceptive (5 years) 4 Goserelin/Leuprolide acetate: treatment for prostate Cancer (1 year) m li LARGE tablets intended for veterinary use for LARGE ANIMALS. sa Licked by animals a h ill sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c ii. COMPRESSED TABLETS (HARD TABLETS) m ai g Utilizes a water-soluble and quickly dissolving sucrose solution as a coating @ Masks offensive taste or objectionable odor 2 CONS: May add 50% to the weight & bulk of the uncoated tablet 9 4 2 Coating with a thin layer of a polymer forming a skin-like film PROS: More durable, less bulky, less time consuming li m Designed to dissolve in alkaline/basic pH to release medication in the small intestine. sa Utilizes Shellac, HPMCP, Polyvinylacetate phthalate, CAP a h ill sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c iii. MODIFIED-RELEASE TABLETS m ai g Disintegrates and releases their medication with NO special rate-controlling medication @ This is the point of comparison for other modified-release tablets. 92 Liquefies in the tongue within 15 seconds or 1 minute leaving an easy to swallow residue 2 Examples: Anti-psychotics (Risperidone), Antiemetics, Clarinex (Loratidine) 4 m Releases drug other than the time it was administered li It may be time-based or environment-based. sa AKA Bimodal Release a ill Two-layer tablets where one layer is immediately released while the other layer is released h later as a second dose or in an extended manner. sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c iii. MODIFIED-RELEASE TABLETS m ai g drug release directed towards isolating or concentrating a drug in a body region, tissue, or @ site for absorption or for drug action. 2 Colonic Tablets: Delivers drug into the colon without dilution in other regions of GIT, 9 2 such as Mesalamine and its metabolite 5-ASA for ulcerative colitis 4 Gastroretentive Tablets: aka Floating Tablets with low density that remain in the m li stomach (PUD Drugs) sa It releases drug slowly so that plasma concentration is maintained at therapeutic level for a. ill 8-12 hours. ZERO-ORDER kinetics a h Maintains a plateau and may be transdermal, oral, or others sh FIRST-ORDER kinetics Releases drug gradually and may only be oral SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c mai @ g 92 42 lim a.sa hill sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c iv. Other Types of Tablets m ai g Small round solid dosage form intended to be administered orally Very small pills 2 @ Tapered at one end 2 9 4 Made by Eli Lily i Tapered at both ends l m sa Capsules containing granules, coated w/ materials of slow dissolving rate a. h ill sh a SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  D. TABLETS om 1. Types of Tablets l. c iv. Other Types of Tablets m ai g AKA Monoliths @ Drug is homogenously dispersed in a rate-controlling medium 9 A TABLET in the shape of capsules 2 Osmotic- 4 2 Consists of a drug an osmotically active substance that allows drugs to move out an orifice i m Controlled Release through osmosis. Oral Drug Delivery sa l. System (OROS) ill a a h sh SOLID DOSAGE FORMS | Tablets Where Degrees Become Legacies.  om l. c mai @ g 92 42 lim a.sa ill ah III. LIQUIDS s h A. SOLUTIONS Where Degrees Become Legacies.  A. SOLUTIONS om. c NOTES DEFINITION ail Liquid preparations that contain 1 or more chemical substances dissolved in a suitable m solvent or mixture of mutually miscible solvents SOLUTE + SOLVENT = SOLUTION @ g 92 2 mL to dissolve 1g V 4 Very Soluble m li sa F Freely Soluble So a. Soluble ill Spa Sparingly Soluble a h Sli Slightly Soluble sh VSS PI Very Slightly Soluble Practically Insoluble LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 1. Vehicles of Solutions l. c i. Aqueous Vehicles m ai g Obtained by distillation, reverse-osmosis, and ion-exchange @ Total Solids: NMT __ ppm pH of 5-7 92 2 For finished and prescription products 4 Obtained by distillation and reverse-osmosis m Pyrogen-free li sa Solvent for parental solutions a. ill Basically, WFI + Sterilization Packaged in single-dose containers of NMT 1000 mL a h sh Basically, SWFI + 0.2% benzyl alcohol Packaged in multiple-dose containers of NMT 30 mL Causes gasping syndrome in neonates LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 1. Vehicles of Solutions l. c i. Aqueous Vehicles m ai g Basically, SWFI but used in humidifiers 2 @ 9 Basically, SWFI but used in cleaning and washing 4 2 li m a. sa h ill sh a LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 1. Vehicles of Solutions l. c ii. Non-Aqueous Vehicles m ai g Dissolves water-insoluble substances @ Used with co-solvents (glycerin) due to low dielectric constant Self-preserving at 10% 92 4 2 m < 6 years old 0.5% li sa 6 to 12 years old 5% a. > 12 years old 10% ill AKA Glycerol a h Miscible with water and ethanol sh Humectant, Emollient, Preservative, Viscosity Enhancer LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 1. Vehicles of Solutions l. c ii. Non-Aqueous Vehicles mai g Substitute for glycerin 2@ 9 Se Co 42 m Cot Pe li a.sa h ill sh a LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c i. Aqueous Solutions m ai g AKA Medicated waters @ Clear, aqueous solutions saturated with volatile oils or other aromatic or other volatile substances 92 2 Use: Perfumed Vehicle 4 Storage: Tight, Light-resistant bottles m i Instability: Salting out sa l Dilution of concentrated acids with purified water a. ill Example: Diluted HCl for achlorhydria w/w%: concentrated acids a h w/v%: diluted acids (10% except acetic acid (6%)) sh LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c i. Aqueous Solutions m ai g Astringents: Ca(OH)2 @ Anti-infectives: 3% Hydrogen peroxide 92 Aqueous solutions directed against a part or into a body cavity for cleaning and antiseptic action 4 2 Dispensed as tablets or powders to be diluted with water li AKA rectal injections m. sa Use: (1) evacuation of bowel; (2) retention in the intestine (nutritive, medicated, a ill diagnostic) a h sh LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c i. Aqueous Solutions m ai g Used by swishing the liquid in the oral cavity @ Mouth cleanser, treatment of oral mucus membrane 92 Contains antiseptic, antibiotics, and/or anesthetics for the treatment of the pharynx and 4 Example: Betadine for sore throat2 nasopharynx by expelling air from the lungs thru the gargle, held in throat and spit out li m Prepared from fresh ripe fruit a. sa h ill sh a LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c ii. Sweet and Viscid Aqueous Solutions m ai @ g 92 2 Simple Syrup: 85% w/v of sucrose SYRUP USE Specific Gravity: 1.313 m 4 Orange and Cherry Acidic medium i l Self preserving at 65% w/w or 85% w/v sa Low solvent capacity Cocoa Bitter a. Raspberry Sour and Salty ill Glycyrrhiza B-complex vitamins a h Acacia Urea sh Eriodictyon Ora Sweet Alkaloids Compounding LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c ii. Sweet and Viscid Aqueous Solutions m ai g Viscous oral liquid that contain 1 or more active ingredients dissolved in a suitable base that @ generally contains a higher concentration of sugar or other sugars 92 Thick liquid preparations allied to syrups but used as base 4 2 Thick, viscid adhesive liquids made of dispersing gum in water m Suspending Agents: Acacia, Tragacanth li sa Class of gels with a structural matrix containing a higher concentration of water. Examples: Lubricants, Nonoxynol-9 a h ill sh a LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c ii. Sweet and Viscid Aqueous Solutions m ai g Occlusive, protectant, applied over bandages 2 @ 2 9 m 4 li a. sa h ill sh a LIQUID DOSAGE FORMS | Solutions Where Degrees Become Legacies.  A. SOLUTIONS om 2. Types of Solutions l. c iii. Non-Aqueous Solutions m ai @ g 92 AKA Galenicals 4 2 Concentrated preparations of crude drugs obtained by using selective solvents li m Syrupy consistency, without removing the solvent sa Semiliquid extracts a. Pilular extracts Plastic consistency, with removing NEARLY ALL solvent ill Powdered extracts Dry, with removing ALL solvent