PHARMA-Drug forms


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PHARMA-Drug forms

  1. 1. Drug Forms andDrug Delivery System 1
  2. 2. Before FDA approval• Rx company must clearly state in what form or forms the drug will be manufactured• Rx company must clearly state what routes of administration are determined safe and effective 2
  3. 3. Classification According to its physical properties– Gaseous dosage forms– Liquid dosage forms– Semisolid dosage forms– Solid dosage forms 3
  4. 4. 4
  5. 5. Classification According to its physical properties• Gases – Gases • medicinal gases • inhalation/volatile anaesthetics (vaporised before administration by inhalation) – Aerodispersions of solid particles • (e.g., inhalation antiasthmatics) • liquid particles (inhalation antiasthmatics or sprays) 5
  6. 6. Classification According to its physical properties• Liquid dosage forms 1. Solutions • one homogenous phase, prepared by dissolving one or more solutes in a solvent • never need to be mixed • drug fully dissolved 2. Emulsions • a dispersion system consisting of two immiscible liquids • o/w or w/o • cloudy appearance 3. Suspensions o • w in liquid phase solid particles(undissolved) are dispersed • Not intended for systemic administration of drugs with high potency 6
  7. 7. Types of Solutions• Elixirs – alcohol & water base with added sugar & flavoring – Taken orally – Ex. Antihistaminic elixirs• Syrups – sugar, 1 water soluble active ingredient & flavoring thicker• Tinctures – alcohol & water base used topically – a solution that has alcohol as the solvent. 7
  8. 8. Liquid Sprays• Water & alcohol base• pump or aerosol spray• some dispensed as foams 8
  9. 9. Suspensions• Contain fine, undissolved particles of a drug suspended in a liquid base• Important to always shake before use• gel-suspended in a thicken water medium- does not have to be shaken 9
  10. 10. Classification According to its physical properties• Semisolid dosage forms – Unshaped (without specific physical shape) 1. Gels • A semisolid systems • solid, jelly-like material that can have properties ranging from soft and weak to hard and tough • a liquid phase is constrained within a 3D cross-linked matrix. 10
  11. 11. • Semisolid dosage forms – Unshaped (without specific physical shape) 2. Creams – semisolid emulsion systems (o/w, w/o) containing more water. • o/w creams – more comfortable and cosmetically acceptable as they are less greasy and more easily water washable • w/o creams – accommodate and release better lipophilic API, moisturizing, Cold creams Hydrocortisone cream 11
  12. 12. • Semisolid dosage forms – Unshaped (without specific physical shape) 3. Ointments – Semisolid emulsion of oil and water- main ingredient oil – Oleaginous (hydrocabon) base: Petrolatum (Vaseline – white, yellow) 12
  13. 13. Classification According to its physical properties• Semisolid dosage forms – Shaped 1. Suppositories • different shapes Glycerin suppositories • Melting/dissolving at body temperature • Oleaginous (cacao butter, adeps neutralis) or aqueous (glycerinated gelatine) • Types: – Rectal – Vaginal – urethral 13
  14. 14. • Solid suppository is melted within the ampula recti, API is dissolved and is absorbed• It can gets into the systemic circulation (Middle & inferior haemorrhoidal veins Iliac vein inferior vena cava – bypassing liver there is no first pass effect)• It can pass through portal circulation: via Superior haemorrhoidal veins Inferior mesenteric vein Hepatic portal Liver (First Pass effect can take place). It becomes to be more important when supp. is position too high in rectum.• Storage: cool place! 14
  15. 15. 1. Suppositories (for rectal administration)• Preferred: – when drug is destroyed in GI tract – + vomiting – unconscious, – difficulty swallowing• Major disadvantages: 1. Inconvenient. 2. Rectal absorption of most drugs is frequently erratic and unpredictable. 3. Some suppositories "leak" or are expelled after insertion. 15
  16. 16. Rectal suppositories are commonly used for:1. Laxative purposes = glycerin or bisacodyl2. Tx of hemorrhoids by delivering a moisturizer or vasoconstrictor3. Delivery of many other systemically-acting medications Glycerin suppositories = promethazine or aspirin4. General medical administration purposes: – the substance crosses the rectal mucosa into the bloodstream; – Ex: paracetamol(acetaminophen), diclofenac, opiates, and eucalyptol suppositories. paracetamol 16
  17. 17. 17
  18. 18. 2. Pessaries (vaginal suppositories) – Tx gynecological ailment (candidiasis) – Inserted in vaginal tract – Globular, oviform or cone-shaped – Weigh between 3-5 g – Instruction: • quickly dip supp in water before insertion. • Wear sanitary napkin to protect nightwear and linens – Purpose: • contraceptives • feminine hygiene antiseptics • bacterial antibiotics • to restore the vaginal mucosa. 18
  19. 19. Advantages of vaginal suppositories:1. there is less drug degradation compared to oral administration2. The dose can be retrieved if necessary3. There is the potential of long term drug absorption with various intrauterine devices (IUDs). 19
  20. 20. 3. Urethral suppositories – Alprostadil = tx severe erectile dysfunction – Diminished since dev’t of oral impotence medications. 20
  21. 21. Classification according to its physical properties• Solid dosage forms – Unshaped (without specific shape) - powders for external/internal use – Shaped - Tablets - Capsules - Transdermal patches 21
  22. 22. Classification according to the route of administration• Dosage forms – for systemic administration • p.o. • s.l. and buc. • rectal • parenteral • transdermal • inhalation – for local administration • Topical (on the skin or mucosa) – Into/onto - the eye, nose, ear - the oral cavity - the vagina, rectum - the skin • Local parenteral (viz Parenteral above) 22
  23. 23. Pharmaceutical dosage forms for systemic administration• Generations of dosage forms – 1st gen. – conventional (unmodified) release of API – 2nd gen. – controlled release of API (CR) – 3rd gen. – targeted distribution drug delivery systems 23
  24. 24. Conventional vs. controlled release dosage forms• I. Gen. – Disintegration of the dosage form and dissolution of API is spontaneous process; – drug absorption and distribution is based only on physico-chemical properties of API• II. Gen. – The release of API is under control of the drug delivery system (temporal control) – Advantages: – Avoids fluctuations of plasma drug concentration better safety and efficacy – Decreased frequency of drug administration (often once daily admin) better compliance – Can be much more economical (better cost-effectiveness) 24
  25. 25. Tablets• Drug form which contains dried powdered active drug• Contains binders and fillers to provide bulk and proper size• Many different types of tablets 1. Conventional = can be divided 2. Coated = not to be divided 25
  26. 26. • Sustained release (SR) – release of the initial API dose & further prolonged release• Controlled release (CR) – properly controlled release of API• Pulsatile release – Rapidly released after a certain period of time on the basis of time-controlled disintegration mechanism 26
  27. 27. 27
  28. 28. Chewable Tablet• Solid dosage containing API with or without suitable diluents that is intended to be chewed• Producing pleasant tasting residue in the mouth• Easily swallowed, no after-taste 28
  29. 29. Scored Tablets• Indented line running across the top• Can easily be broken into two pieces with a knife to produce two doses 29
  30. 30. Dispersible Tablet (Tablet for Suspension)• intended to be placed in liquid prior to administration. 30
  31. 31. Effervescent Tablets– not a final dosage form– Containing mixtures of acids (citric acid/tartaric acid) and sodium bicarbonate– Which release carbon dioxide when dissolved in water– Intended to be dissolved or dispersed in water before administration • Rapid absorption rapid on-set of action • Avoids potential tablet adhesion to mucosa and local irritation 31
  32. 32. Enteric Tablets• Delayed release dosage form• Covered with a special coating that resists stomach acid• but dissolves in the alkaline environment in small intestines• stable at the highly acidic pH• breaks down rapidly at a less acidic pH• Coatings made of: – Fatty acids, Waxes – Shellac, Plastics – Plant fibers 32
  33. 33. • Coated (not to be divided) Advantages: – To mask unpleasant taste or smell of API – To avoid of adhesion in esophagus (to facilitate swallowing and/or avoid release of API and local adverse rxns) – To ensure drug stability – To provide enterosolvent coating • To overcome – possible degradation of API in the stomach and possible local irritation/adverse reactions in the stomach 33
  34. 34. Caplets- Tablets• Coated tablets in the shape of a capsule• Easier to swallow 34
  35. 35. Lozenges- Tablets• Formed with a harden base of sugar , water and flavorings• never swallow• dissolve slowly in mouth• Containing 1 or more API• Intended to dissolve/disintegrate slowly in the mouth 35
  36. 36. Capsule• Comes in two varieties• generally easier to swallow 36
  37. 37. Soft gelatin- Capsule• Manufactured in one piece in which the drug is in a liquid form inside the soft shell 37
  38. 38. Hard shell- Capsule• Manufactured in two pieces that fit together and hold the drug which is in a powder or granular form 38
  39. 39. Transdermal Patches• Consist of a multi-layered disk of a drug reservoir, a porous membrane and a adhesive layer to it to the skin 39
  40. 40. Pellet/Bead Gentamicin implantable pellet• Drug can be implanted in the body in the form of a pellet or bead that slowly releases into tissue 40
  41. 41. Parenteral Drugs• Drugs administered other than the alimentary canal 1. Inhalation • Drugs administered by nasal/oral-respi route • Nebulizers, aerosols – Forms of Inhalation 1. Gaseous/volatile drugs 2. Suspended tiny droplets in aerosols 3. Inhaler/puffer (to the lungs) 4. Nebulizer (mist inhaled into lungs) 41
  42. 42. Advantages of Inhalation:1. Pulmonary administration offers large surface alveolar area for diffusion of drug into pulmonary circulation.2. Rapid entry of drug to the blood stream3. Direct application of drug to the bronchial tree and alveolar tissues4. Fastest method, 7-10 secs for the drug to reach the brain5. User can titrate (regulate) the amount of drug they are receiving. 42
  43. 43. Disadvantage of Inhalation:1. Difficult to administer, some have difficulty in using inhalers2. Particles are trapped in the cilia and mucus in the respiratory tract3. Drugs may serve as irritant to alveoli and respiratory tract4. Unpredictable amount of drugs delivered to the lungs5. Most addictive route of administration as it hits the brain so quickly.6. Difficulties in regulating the exact amount of dosage. 43
  44. 44. 2. Injection• Drug is administered by means of a syringe puncturing the body• Administered in – Vein = IV – Muscle = IM – Subcutaneous = SC 44
  45. 45. Forms of Injection:1. Liquid for injection IV (vein)2. Liquid for intra-arterially (Arteries)3. Liquid for subcutaneous (directly beneath the skin)4. Liquid for intramuscular (within large muscles)5. Liquid for intrathecal (within the sheath or at the spinal subarachnoid space) 45
  46. 46. Advantages of Injection1. Outcome can be predicted in a short period of time2. Reach the target sites rapidly3. Drugs given intra-arterially are used to localize drugs into certain tissues with few exposure of drug to other tissues.4. Effective for administration of radio opaque dyes for diagnostic purposes.5. Effects seen within few minutes.6. Convenience in 1 time administration that has a long acting effect (ex. Depo-Provera, a birth control shot that works for 3 months) 46
  47. 47. Disadvantages of Injections:1. self-administration may be difficult with most of the injection routes2. High risk for addiction due to the quick onset of action of most injectable drugs.3. Risk of HIV and other infectious diseases transmission if needles are accidentally shared.4. most dangerous route of administration because the drug is not screened by the body’s natural defenses, placing the client at risk of developing hepatitis, abscesses, and infections from undissolved particles or additive/contaminants.5. Risk of air boluses (bubbles) which can be fatal may occur during drug administration especially when drugs are not prepared properly.6. Need for observing strict asepsis as this provide a port entry for microbes that can cause infection 47
  48. 48. 3. Topical/Dermatologic – Drugs applied to the surface of the skin/mucous membrane 1. Iontophoresis • Use electric current to drive the ionized form of medications through the skin 2. Phonophoresis • Use ultrasound waves as driving force to propel drug through the dermis. 48
  49. 49. Forms of Topical/Dermatologic Drugs1. Ointments2. Creams3. Gel4. Paste5. Powder6. Liniment (muscular stiffness/pain)7. Lotion8. Transdermal patch9. epicutaneous 49
  50. 50. Advantages:1. Applied directly to skin/membranes to treat itself2. Bypasses systemic absorption3. Direct action4. Easy to apply5. Safe and effective method of administering medications6. Provides a slow, controlled release of the drugs into the body7. Effective in maintaining plasma levels at constant levels for prolonged period of time. 50
  51. 51. Disadvantages:1. Poorly absorbed systemically through epidermis and are not intended for systemic tx.2. Some drugs applied to the mucous membranes are also absorbed to some degree that may cause adverse effects.3. Drugs that cannot penetrate the skin will unlikely be an effective agent administered by this route.4. Drugs that are easily degraded by the enzymes present in the skin will cause failure of the drug to meet its therapeutic effects. 51
  52. 52. 4. Instillation & irrigationsInstillation – Administered in drop form or – Administered into the body cavity by means of catheter and stays in place after administration.Irrigation – Administering drugs that stays for a while and are removed minutes after it is administered. 52
  53. 53. 1. Opthalmic Administration – Eye medications Eye drops • Saline-containing liquid • Used as vector to administer medication in the eye • May contain steroids or topical anesthetics Advantage: • Direct contact on the target site Disadvantages: • Intolerance to bright light • Excess use may discourage the eyes to produce tears naturally = increase dependence on drugs 53
  54. 54. Eye Drops or Eye Ointment 54
  55. 55. 2. Otic administration – Ear drops (antibiotics & steroids for otitis externa) Advantage: • Has direct contact to affected site Disadvantage: • Client has to be kept in position for 2-3 min to facilitate drops to reach the affected area • Head tilted slightly toward the unaffected side 55
  56. 56. Ear Drops 56
  57. 57. 3. Nasal administration – Intransal route (into the nose) – Ex decongestant nasal sprays. Advantage: • Direct contact to affected site Disadvantage: • Client may become uncomfortable when asked to maintain position (head tilted backward) for 5 mins after instillation of drops 57
  58. 58. 4. Vaginal administration – Vaginal, ex: • Topical estrogens • Antibacterial – Advantage: • Direct contact to affected site. – Disadvantage: • May cause severe vaginal wall irritation 58
  59. 59. 5. Rectal administration – Advantages: • Direct contact • Ease in application – Disadvantages: • Vaginal and rectal suppositories melts easily even before application. 59
  60. 60. HAND OUTS 60