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147 Cards in this Set
- Front
- Back
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What are the 5 advantages solid dosage forms have over liquids?
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5 advantages
1. active and inactive ingredients in the solid form are most stable 2. more easily packaged, transported, administered, and stored than liquids 3. accurate and easier dosing with individual units 4. easier taste masking than liquids 5. easier design of controlled release products |
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Definition of powder
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intimate mixtures of dry, finely divided drugs and/or chemicals that may be intended for internal (Oral) or external (Topical) use
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What are 2 other names for powder dosage forms that are applied to the skin for local effect?
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topical bulk powders
dusting powders |
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What are 2 powder dosage forms applied to the skin and used as antiinfectives?
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bacitracin zinc
polymyxin B sulfate |
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What is the powder dosage form applied to the skin and used as an antifungal?
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tolnaftate
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Name 4 bulk powders used for internal use. These all must be nonpotent drugs.
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antacid powders (sodium bicarbonate)
bulk laxative powders (Metamucil) douche powders (Massengill Powder) Brewer's Yeast powder containing B-complex vitamins |
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Blended powders may be dispensed as divided powders, also known as what?
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chartulae
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With powders, particle size influences what 5 factors?
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5 factors
1. rate of dissolution and bioavailability; the smaller the particle size, the larger the surface area and the faster the rate of dissolution 2. dose-to-dose uniformity by uniform distribution of active drug 3. wide distribution of particle sizes tend to stratify suspended particles, which leads to inaccurate dosing 4. penetrability of particles into the respiratory tract 5. nongrittiness of solid particles in dermal ointments, creams, and ophthalmic preparations |
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What are the 6 methods of particle size analysis?
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1. sieving
2. microscopy 3. sedimentation rate 4. light diffraction or light scattering 5. laser holography 6. cascade impaction |
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What are 3 methods of powder particle size reduction?
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1. trituration
2. levigation 3. pulverization by intervention |
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Define trituration
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the pharmacist utilizes a mortar and pestle for reducing particle sizes
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In trituration, what would be used to make finer particles?
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A mortar with a rough surface like Wedgewood or porcelain, as opposed to one with a smooth surface like glass
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Define levigation
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The pharmacist uses levigation to form a paste (ointment) by reducing the particle size and grittiness of powders with the aid of a suitable liquid (levigating agent)
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Define pulverization by intervention
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Waxy materials or hard crystals are not easily crushed into fine powder with simple trituration. The addition of a minimum volume of a second agent (alcohol) helps reduce particle size and then the agent is removed from the final product
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What are the 5 mthods of blending powders?
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1. geometric dilution
2. spatulation 3. sifting 4. trituration 5. tumbling |
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Noyes-Whitney equation
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dC/dt = KS(Cs-C)
dC/dt = change of concentration with time K = the dissolution rate constant S = surface area of the solid particle Cs = solubility of the drug C = concentration of the drug in solution at time t |
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Describe the method of geometric dilution.
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This is the general method of blending powders with a mortar and pestle. The ingredient present in the smallest quantity or the potent drug is placed in a mortar and approximately equal volume of the diluents is added and triturated thoroughly. A second portion of diluents in a volume equal to the mixture is added and triturated. Continue this process until all diluents are used.
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Describe the process of spatulation.
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A method of blending powders by using a spatula on a sheet of paper or an ointment tile. It is not good for large quantities of powders or powders containing potent drugs. It is suited to the mixing of solid substances that form eutectic mixtures (or liquefy).
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Which blending technique is not suitable for large quantities of powders?
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spatulation
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Which blending techniques (2) are not suitable for powders containing potent drugs?
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spatulation
sifting |
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Which blending technique is most suitable to the mixing of solid substances that form eutectic mixtures or liquefy?
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spatulation
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Describe the process of sifting.
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a method by which powders pass through sieves or sifters (as with flour in baking)
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When blending powders via trituration, what type of mortar is generally preferred?
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glass
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Describe the process of tumbling.
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a method in which the powder is enclosed in a rotating container (motorized) and tumbled; widely employed in industry (V-blenders, ribbon blenders, double conical bleners)
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What are granules?
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prepared agglomerates of smaller particles of powder that fall within the 4 to 12 sieve size range
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Are granules good for making tablets? Why or why not?
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yes, because they flow well
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Describe the stability in of granules in different environments.
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They are more stable in moist environments and more easily wetted by liquids than fluffy powders. Often preferred for dry porducts to be reconstituted into solutions or suspensions
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Describe the 2 Wet methods for preparing granules.
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The powders are moistened to form paste-like mass, which passes through a screen of the mesh xize followed by drying. Another type is that powder particles are placed in a fluidized bed and dispersed and suspended while a liquid is sprayed on them
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Describe the 2 Dry methods for preparing granules.
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The dry powder is passed through a roller compactor to form densified sheets or forms followed by mechanical granulation. Another type is that large tablets or slugs are made by compressing powder followed by crushing them into the desired particle size.
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What are effervescent granulated salts?
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Granules containing a drug and usually a mixture of sodium bicarbonate, citric acid, and tartaric acid. Upon contact with water, sodium bicarbonate reacts with citric acid or tartaric acid to liberate carbon dioxide (effervescent)
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Define capsule
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solid dosage form in which drug substances are enclosed with a small shell of gelatin or other suitable substances (HPMC)
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How are most hard shell capsules made?
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Out of gelatin, which is obtained by the partial hydrolysis of collagen of the skin, white connective tissue, and bones of animals, along with sugar and water. Gelatin is not soluble in cold water but is soluble in hot water.
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What is gelatin soluble in?
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hot water, but not cold water
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How much water is contained in hard gelatin capsules?
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10-15%
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What is added to capsules to make them opaque?
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titanium dioxide
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What can cause hard gelatin capsules to lose their rigidity and be brittle?
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high humidity or extreme dryness
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What is the size range for gelatin capsules?
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000 (largest) to 5 (smallest), larger can be made for large animals
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Name 4 inactive ingredients that can be put into capsules.
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1. diluents (filler)
2. lubricant (glidant) 3. surfactant 4. disintegrating agent |
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What are diluents?
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Substances that may be added to the formulation to ensure the proper capsule volume
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Give 4 example of diluents.
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1. lactose
2. microcrystalline cellulose 3. sodium carboxymethyl cellulose 4. starch |
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What is the purpose of lubricant?
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to help free-flow of powders into the capsule fill from the hopper
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Give 5 examples of lubricants.
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1. magnesium stearate
2. calcium stearate 3. stearic acid 4. talc 5. fumed silicon dioxide |
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What is the purpose of surfactants in hard shell capsules?
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When water-insoluble excipients (lubricants) or poorly soluble drugs are present in the formulation, the addition of surfactant (sodium lauryl sulfate) facilitates wetting of the content of the capsule.
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What is the major rule when selecting a capsule size?
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choose the smallest size that will produce a filled capsule with no void space
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What 3 steps should be taken when filling capsules to determine the uniformity of the capsules?
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1. take 10 capsules and weigh them individually
2. calculate a relative standard deviation (RSD) 3. the percentage of labeled drug amount should be 85-115% and RSD should be less than 6% |
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What is the major advantage of hard shell capsules?
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fewer excipients than tablet dosage forms
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Name 4 advantages of hard shell capsules that apply to patients.
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1. elegant
2. tasteless 3. compact 4. easy administration |
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Name 4 advantages of hard shell capsules that apply to scientists.
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1. tasteless
2. single or combination of drugs 3. useful for clinical trial 4. good bioavailability |
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Name 6 disadvantages of hard capsules?
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1. not suitable for soluble salts
2. not suitable for hydroscopic drugs 3. not suitable for deliquescent drugs 4. not suitable for effervescent drugs 5. potential for tampering 6. can't be used for drugs solubilized by gelatin |
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What ingredients are used in soft shell capsules?
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the key material is gelatin but glycerin and/or polyhydric alcohol (sorbitol) are added to render the gelatin soft or elastic
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Soft gelatin capsules are filled with a variety of what 4 liquids?
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1. water-immiscible volatile and nonvolatile liquids (vegetable and aromatic oils, hydrocarbons, organic acids, esters, alcohols)
2. water-miscible, nonvolatile liquids (polyethylene glycols, nonionic surfactants (Tween series)) 3. water-miscible and relativley nonvolatile compounds (propylene glycol, isopropyl alcohol) 4. solids that are dissoloved or suspended in a suitable liquid solvent |
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Are soft geltain capsules made extemporaneously in community pharmacy settings? Why or why not?
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no, because the technology and equipment required for making soft gelatin capsules are complex
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Define tablets
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solid dosage forms containing a drug substance or substances with or without suitable pharmaceutical excipients
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Name 9 advantages of tablets
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1. patient acceptance
2. convenience 3. ease of storage and dispensing 4. easy in inventory control 5. accurate dosing 6. less susceptible to tampering 7. well established manufacturing processes 8. stability 9. can modify release characteristics |
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Name 3 disadvantages of tablets
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1. not suitable for drugs resistant to compression or susceptible to degradation by oxygen or moisture
2. dissolution-rate limited drugs 3. dose is too large - size limit for tablets |
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What is a compressed tablet?
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tablet made by exerting high pressure in compacting the powdered or granulated material
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What is a multiple compressed tablet?
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multi-layer or dry coated tablets
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What 3 purposes for multiple compressed tablets?
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1. taste masking
2. separate incompatible substances 3. desired release characteristics |
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Name 3 different forms of multiple compressed tablets that we discussed in class.
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1. tablet in tablet
2. double layer 3. triple layer |
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Give 2 example of tablet-in-tablet multiple compressed tablets.
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1. Adalat CC
2. Sular |
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Give 2 examples of double layer mulitple compressed tablets.
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1. Tylenol extended
2. Ambien CR |
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Giv 1 example of a triple layer multiple compressed tablet. Also state what all 3 layers are.
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Norgesic Forte
1. aspirin 2. caffeine 3. orphenadrine |
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Give 3 purposes for making sugar-coated tablets.
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1. protect the drug in a tablet from the environment
2. taste masking 3. permint imprinting of tablet identity |
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Give an example of a sugar-coated tablet.
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Motrin
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What is a film-coated tablet?
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a compressed tablet with a thin layer of polymeric material (water-soluble or water-insoluble); easier to produce than sugar coating
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Describe Enteric-coated tablets.
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coating is polymeric material dissolved at pH 5 or higher; methacrylic, phthalic, or succinic acid
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What is the purpose of enteric-coated tablets?
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to avoid stomach irritaion; for acid labile drugs; delivery to intestine
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Give an example of an enteric-coated tablets.
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Athrotec (diclofenac Na)
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What do enteric-coated tablets lead to?
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extended release
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What 5 things can be used to make enteric-coated tablets?
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1. CAP (cellulase acetate phthalate)
2. Eudragit L/S 3. HPMCP (hydroxy-propyl-methyl cellulose phthalate) 4. HPMCAS (hydroxy-propyl-methyl cellulose acetate succinate) 5. Kollicoat MMA |
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What are 3 advantages of buccal/sublingual tablets?
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1. avoid GI tract
2. fast acting 3. reduced nausea and vomiting |
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Give 5 examples of buccal/sublingual tablets.
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1. Progesterone (buccal)
2. Nitroglycerin (sublingual) 3. Suboxone (buprenorphine HCl) 4. Naloxone HCl 5. Fentura |
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What are lozenges/troches?
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they contain a drug and a flavoring substance intended to be dissolved slowly in the oral cavity
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Give an example of a lozenge/troche.
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hard candy (sugar and syrup)
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When would chewable tablets be used?
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for large tablet size and for children and adults who have difficulty swallowing solid dosage forms
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What are effervescent tablets?
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they release CO2 as a disintegrant to break up the tablet
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Give 2 examples of effervescent tablets.
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1. Alka-Seltzer
2. Aspirin |
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What are the characteristics of molded tablets?
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soft, soluble, and rapid dissolution
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What is the rate of instant disintegrating/dissolving tablets?
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one mintute or 10 seconds
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Give an example of an instant disintegrating/dissolving tablet.
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Claritin Reditabs
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Who would be prescribed instant disintegrating/dissolving tablets?
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pediatric and geriatric patients
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Name an instant disintegrating/dissolving tablet made by lyophilization.
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Zyprexa (olanzapine) Zydis
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Name an instant disintegrating/dissolving tablet made by soft direct compression.
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WOW-Tab
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Define diluent when it comes to excipients for tablets.
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bulking agents to make up reasonable size; must be stable physically and chemically
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Give 6 examples of diluents used as excipients for tablets.
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1. kaolin
2. lactose 3. manitol 4. starch 5. powdered sugar 6. calcium phosphate |
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Define binders when it comes to excipients for tablets.
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add cohesive properties; added as dry powder or liquid form
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Give 7 examples of binders used as excipients for tablets.
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1. cornstarch
2. glucose 3. natural gum 4. cellulose derivatives 5. gelatins 6. povidone 7. alginate derivatives |
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Define disintegrants when it comes to excipients for tablets.
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facilitate tablet disintegration by drawing water into the tablet, swelling, and causing the tablet to burst apart
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Give 7 examples of disintegrants used as excipients for tablets.
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1. cornstarch
2. potato starch 3. starch derivatives (sodium starch glycolate) 4. cellulose derivatives (Na CMC) 5. clays (Veegum, bentonite) 6. cation exchange resin 7. cross-linked polyvinyl pyrrolidine |
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Define lubricants/antiadherents/glidants when it comes to excipients for tablets.
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reduce friction between the walls of the tablet and the alls of the die cavity; reduce sticking the tablet powder or granule to the punch faces or the die walls; reduce friction among the particles to promote the flow of the powder materials
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Give 3 examples of lubricants/antiadherents/glidants used as excipients for tablets.
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1. talc
2. Mg stearate 3. Ca stearate |
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Define colors/dyes when is comes to excipients for tablets.
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disguise off-color drugs; used for product identification; more elegant products
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Give 3 examples of colors/dyes used as excipients for tablets.
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1. FD&C dyes
2. D&C dyes 3. lakes |
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Define flavoring agents/sweeteners when it comes to excipients for tablets.
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used only for chewable tablets or tablets intended to dissolve in the mouth
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Define adsorbents when it comes to excipients for tablets.
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capable of holding quantities of liquid in an apparently dry state
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Give 4 examples of adsorbents used as excipients for tablets.
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1. magnesium oxide
2. magnesium carbonate 3. bentonite 4. silicon dioxide |
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Describe the wet granulation method of tablet preparation.
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dampening or wet massing of a tablet powder mixture with liquid adhesives followed by wet screening or granulation
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What are the 2 advantages of the wet granulation method of tablet preparation?
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1. most reliable
2. highest probability of meeting the requirements for making a successful tablet |
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What are the 4 disadvantages of the wet granulation method of tablet preparation?
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1. need to prepare a uniform granulation
2. labor intensive 3. time consuming 4. cannot use water sensitive drugs |
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Describe the dry granulation method of tablet preparation.
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process of preparing a tablet mixture without a wet binder or moisture; a slug is formed and then compressed
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What are the 2 advantages of the dry granulation method of tablet preparation?
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1. useful for water and heat sensitive drugs
2. fewer steps |
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What is the 1 disadvantage of the dry granulation method of tablet preparation?
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1. requires drugs or excipients with cohesive properties
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Define the direct compression method of tablet preparation.
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no granulation involved in the process; becoming a desired method due to availiability of excipients which enable this process to be carried out
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What are the 6 advantages of the direct compression method of tablet preparation?
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1. can prepare a tablet from powdered mixture without granulation
2. faster 3. useful for crystalline drugs 4. useful for large dose drugs 5. useful for moisture sensitive drugs 6. limited number of excipients - optimal bioavailability |
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What are the 3 disadvantages of the direct compression method of tablet preparation?
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1. requires materials which can be directly compressed
2. drugs/excipients must have good flow properties 3. can get non-uniform tablets |
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Define the fluid bed granulation method of tablet preparation.
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becoming a commonly used method because of convenience and availability of equipment; requires only one piece of machinery that mixes all the powders and granules on a bed of air
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What are the 8 steps of wet granulation?
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1. grinding
2. blending 3. adding liquid 4. pelleting 5. drying 6. screening 7. add excipients 8. compression |
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What are the 7 steps of dry granulation?
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1. grinding
2. blending 3. pelleting 4. crushing pellets 5. screening 6. add excipients 7. compression |
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What are the 2 advantages of sugar coating a tablet?
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1. high glossy appearance
2. elegant; attractive |
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What are the 7 disadvantages of sugar coating a tablet?
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1. children think its candy
2. skilled method 3. 3-5 days per batch 4. costly space and equipment 5. microbial growth and contamination 6. hydroscopic 7. substantial weight gain up to 50% |
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What characteristics does sugar coating allow a tablet to have?
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waterproofing/sealing coating
subcoating smoothing and final rounding finishing and coloring imprinting polishing |
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What are the 8 advantages of film coating a tablet?
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1. add only 10-20 ug
2. no need to seal tablets 3. easily automated 4. short time period 5. noncarolic 6. flexible 7 not complex process 8. not susceptible for microbial contamination |
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What are the 2 disadvantages of flim coating a tablet?
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1. use of solvents and effect on worker safety and environment
2. cannot hide tablet appearance |
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What are the 2 types of film coating?
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1. aqueous
2. nonaqueous |
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What are the 2 methods of film coating?
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1. spray pan coating
2. air suspension coating |
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Film coating for tablets usually include what 4 things?
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1. film formers or polymer
2. alloying substances (pore former) 3. plasticizers 4. opaquants and colorants |
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How does the hardness of a tablet relate to how quickly it dissolves?
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the harder the tablet, the slower it dissolves
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Define friability.
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the tablet's tendency to crumble by allowing it to roll and fall in the rotating tumbling apparatus
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What is the maximum disintegrating time for uncoated USP tablets?
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30 minutes
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How quickly should buccal tablets dissolve?
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4 minutes
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How quickly should enteric-coated tablets disintegrate?
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no disintegration after 1 hour in gastric fluid, should disintegrate in intestinal fluid in 2 hours plus specified time
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What are the 5 advantages of modified release dosage forms?
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1. reduce problems with patient compliance
2. reduce the fluctuation of drug blood level 3. reduce dosing frequency 4. reduce local or systemic side effects 5. reduce overall health care costs |
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What are the 5 disadvantages of modified release dosage forms?
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1. dose dumping
2. less accurate dose adjustment 3. increased potential for first-pass metabolism 4. dependence on residence time in GI tract 5. delay onset |
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What are the 5 drug candidates suited for modified release products?
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1. neither very slow nor very fast rates of absorption and excretion
2. uniform absorption from the GI tract 3. small dose (less than 500 mg drug) 4. wide therapeutic index 5. chronic disease condition |
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What is a monolithic matrix system made up of?
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a drug dispersed homogeneously throughout an inert polymer matrix; drug in the outside layer exposed to the aqueous solution is disolved and diffuses out of the matrix; this process continues with the interface between the aqueous solution and the solid drug moving toward the interior
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What are the 2 advantages of monolithic matrix controlled systems?
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1. easier to produce than reservoir devices
2. can deilver high molecular-weight compounds |
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What are the 2 disadvantages of monolithic matrix controlled systems?
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1. cannot obtain zero-order release
2. removal of remaining matrix is necessary for implanted systems |
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Describe a bioerodible/biodegradable matrix system.
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never dependent on dissolution only or diffusion only; as the polymer dissolves, the diffusion pathlength for the drug may change; zero-order release can occur only if surface erosion occurs and surface area does not change with time; does not result in a ghost matrix
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What are the 2 advantages of a bioerodible/biodegradable matrix system?
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1. same as monolithic
2. removal from implant sites is not necessary |
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What are the 2 disadvantages of a bioerodible/biodegradable matrix system?
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1. difficult to control kinetics owing to multiple processes or release
2. potential toxicity of degraded polymer |
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Describe a reservoir controlled system.
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characterized by a core of drug, the reservoir, surrounded by a polymeric membrane
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What are the 2 advantages of a reservoir controlled system?
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1. zero-order delivery is possible
2. release rate variable with polymer type and thickness |
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What are the 3 disadvantages of a reservoir controlled system?
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1. bad for high-molecular weight compounds
2. cost 3. potential toxicity if system fails |
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Explain how ion exchange resins work.
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oral administration of resinates (drug/resin complexes) liberates the drug by an ion exhange reaction with counter ions present in the gastro-intestinal fluid
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What are the 2 advantages of ion exchange resin systems?
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1. high drug loading
2. pH independent (i.e., sulfonated resins) |
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What are the 2 disadvantages of ion exchange resin systems?
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1. no zero-order release kinetics
2. severe tailing at later stage of release |
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How do osmotically controlled systems work?
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water will flow into the tablet owing to the osmotic pressure difference; the membrane is permeable to water but not to drug
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What are the 3 advantages of osmotically controlled systems?
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1. zero-order release is obtainable
2. reformulation is not required for different drugs 3. release of drug is independent of environment of the system |
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What are the 2 disadvantages of osmotically controlled systems?
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1. systems can be very expensive
2. quality control is more extensive |
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Give 13 examples of osmotically controlled systems.
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Procardia XL, Dynacirc CR, Volmax, Accutrim, Covera HS, Glucotrol XL, Ditropan XL, Cardura XL, Effedec 24, Sudafed 24, Concerta, Envega, Viadur
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Gliadel
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parenteral; each wafer contains 192.3 mg of a biodegradable polyanhydride copolymer and 7.7 mg of carmustine; carmustine is a nitrosourea oncolytic agent; the copolymer, polifeprosan 20, is used to control the local delivery of carmustine
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Zoladex
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parenteral; D,L-lactic and glycolic acids copolymer containing goserelin acetate equivalent to 3.6-mg or 10.8-mg of goserelin; no premixing or measuring; administered subcutaneously into the upper abdominal wall either every 28 days for the 3.6-mg implant or every 12 weeks for the 10.8-mg implant
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Lupron Depot
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parenteral; microparticles containing lupronide acetate and luteinizing hormone releasing hormone in a biodegradable D,L-lactic and glycolic acids polymer; mixed with water
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Norplant
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parenteral; capsules made of Silastic silicone rubber containing progestin levonorgestrel are inserted surgically beneath the skin of the upper arm; it releases the drug up to 5 years for protection from pregnancy
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Ocusert
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ophthalmic; three-layer laminate; used to treat glaucoma; pilocarpine nitrate is dispersed in aqueous alginic acid solution
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Lacrisert
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ophthalmic; releases the drug via a controlled erosion of the hydroxypropyl cellulose rod-shaped matrix in the treatment of dry eye
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Progestasert
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intrauterine/intravaginal; progesterone is dispersed in silicone oil with an aid of BaSO4 followed by poly(vinylacetate) membrane and inserted in the intrauterine
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