540 - Drug Delivery Systems - Exam Ii - Oral Drug Delivery

Front 1

What is the excipient function of Aspartame?

Back 1

Sweetener

Front 2

What is the excipient function of Benzalkonium Halides (Cl, Br, or I)

Back 2

Antimicrobial Preservative

Front 3

What is the excipient function of Calcium Stearate?

Back 3

Lubricant

Front 4

What is the excipient function of Carbomer?

Back 4

Viscosity Increasing Agent

Front 5

What is the excipient function of Colloidal Silicon Dioxide?

Back 5

Glidant

Front 6

What is the excipient function of Corn Starch

Back 6

Diluent, Binder, Disintegrant

Front 7

What is the excipient function of Croscarmellose Sodium (Brand Name: Primellose)

Back 7

"Super Disintegrant"

Front 8

What is the excipient function of Dicalcium Phosphate?

Back 8

Diluent

Front 9

What is the excipient function of EDTA (Ethylene Diamine Tetraacetic Acid)?

Back 9

Antioxidant / Chelating Agent

Front 10

What is the excipient function of Ferric Oxide?

Back 10

Coloring Agent

Front 11

What is the excipient function of Gelatin?

Back 11

Binding Agent

Front 12

What is the excipient function of HPMC (Hydroxypropylmethylcellulose)

Back 12

Binding Agent

Front 13

What is the excipient function of Magnesium Stearate?

Back 13

Lubricant

Front 14

What are the excipient functions of Mannitol?

Back 14

Diluent, Sweetener

Front 15

What is the excipient function of Methylparaben?

Back 15

Antimicrobial Preservative

Front 16

What are the excipient functions of Microcrystalline Cellulose?

Back 16

Diluent, Compaction Aid

Front 17

What is the excipient function of Potassium Sorbate?

Back 17

Antimicrobial Preservative

Front 18

What is the excipient function of Polysorbate 80?

Back 18

Nonionic Surfactant

Front 19

What is the excipient function of Povidone?

Back 19

Binding Agent

Front 20

What is the excipient function of Propylparaben?

Back 20

Antimicrobial Preservative

Front 21

What is the excipient function of PVP?

Back 21

Binding Agent

Front 22

What is the excipient function of Sodium Benzoate?

Back 22

Antimicrobial Preservative

Front 23

What is the excipient function of Sodium Bicarbonate?

Back 23

Buffering Agent

Front 24

What is the excipient function of Sodium Lauryl Sulfate?

Back 24

Anionic Surfactant

Front 25

What is the excipient function of Sodium Saccharin?

Back 25

Sweetener

Front 26

What is the excipient function of Sodium Starch Glycolate?

Back 26

Disintegrant

Front 27

What is the excipient function of Sorbitol?

Back 27

Sweetener

Front 28

What is the excipient function of Stearic Acid?

Back 28

Lubricant

Front 29

What is the excipient function of Sucralose?

Back 29

Sweetener

Front 30

What are the excipient functions of Sucrose?

Back 30

Binding Agent, Sweetener

Front 31

What is the excipient function of Talc?

Back 31

Lubricant

Front 32

What is the excipient function of Tween 80?

Back 32

Nonionic Surfactant

Front 33

What is the excipient function of Titanium Dioxide?

Back 33

Coloring Agent

Front 34

What is the excipient function of Xanthan Gum?

Back 34

Viscosity Increasing Agent

Front 35

4. List three reasons why the oral route is the most popular for drug administration.

Back 35

1) It is the most convenient form of administration for ambulatory and conscious patients; 2) It is the most cost effective from the perspective of manufacturing, storage, and handling; and 3) It offers great flexibility in dosage regimen.

Front 36

5a. List the main compartments within the GI tract.

Back 36

The main compartments of the GI tract include the mouth, esophagus, stomach, small intestine, colon, and rectum.

Front 37

5b. Which parts of the GI tract are targeted for drug absorption?

Back 37

Parts of the GI tract commonly employed for drug absorption include the mouth (via buccal & sublingual delivery), the small intestine (most commonly targeted site), the colon (sometimes targeted), and rectum (via rectal delivery). Absorption is less significant in the stomach and essentially negligible in the esophagus.

Front 38

5c. What are some reasons that certain parts of the GI are preferred for the delivery of certain drugs?

Back 38

Buccal, sublingual, lower colon, and rectal drug deliveries bypass the liver and avoid first pass metabolism. The small intestine offers the advantage of great surface area for drug absorption. The large intestine offers the advantage of fewer digestive enzymes.

Front 39

7a. What is the difference between buccal and sublingual drug delivery?

Back 39

Buccal drug delivery is through the mucosa lining of the cheek, while sublingual drug delivery is from the mucosa under the tongue.

Front 40

7b(1). What are five advantages of buccal drug delivery?

Back 40

1) Avoidance of first pass metabolism, 2) Suitability for retentive devices that patients find acceptable, 3) Easy control and manipulation of the mucosa permeability and local environment to accommodate drug absorption, 4) Systemic delivery of drugs otherwise ineffective when delivered orally, and 5) Noninvasive delivery of potent peptide and perhaps protein drug molecules.

Front 41

7b(2) What are three disadvantages of buccal drug delivery?

Back 41

1) The inconvenience of holding the dose in the mouth, 2) The swallowed portion is essentially oral delivery and subject to first pass metabolism, and 3) Only small doses can be easily accommodated.

Front 42

8. For what reason might a patient object to the use of gelatin in the making of capsules?

Back 42

Gelatin is derived from the collagen inside animal skin and bones. Thus gelatin derived from pigs is not in accordance with Muslim halal and Jewish kosher customs, while gelatin derived from cows conflicts with Hindu customs considering the cow sacred, and gelatin derived from horses conflicts with Gypsy cultural forbidding the consumption of horses. Of course vegans and vegetarians may not accept gelatin derived from any animal source.

Front 43

10. By what mechanism do the following types of powder mixing equipment work: Drum, V-mixer, Cone, Ribbon, Fluidize, & Screw?

Back 43

Drum (Diffusive), V-mixer (Diffusive), Cone (Diffusive), Ribbon (Convective), Fluidize (Convective), and Screw (Shear)

Front 44

11. Why are hard gelatin capsules made to lock once the cap is firmly placed on the body of the capsule?

Back 44

Locking gelatin capsules ensure there is no leakage and prevent reopening of the product after filling, thus making them tamper resistant. Tamper-resistance has been a priority since the 1982 Tylenol incident in which seven people died after taking Tylenol capsules that were refilled with potassium cyanide.

Front 45

12a. What are the advantages of compressed tablets as an oral drug delivery system?

Back 45

Advantages include 1) great variety in size and shape for different dosages, 2) high speed equipment facilitates timely large-scale manufacturing at minimal costs per dose, compared to liquid preparations, 3) various options for controlling release characteristics, and 4) a coating can be used to mask an unpleasant taste, to protect the tablet ingredients during storage, or to improve the tablet appearance.

Front 46

12b. What are the disadvantages of compressed tablets as an oral drug delivery system?

Back 46

Disadvantages of include 1) dosage form inflexibility; 2) cannot be prepared extemporaneously; 3) large number of ingredients; 4) they require dissolution, which can limit bioavailability; and 5) sensitivity to moisture, oxygen, and light.

Front 47

14. What are the three basic processes for making compressed tablets? What are the major differences among these processes?

Back 47

The three basic processes for making compressed tablets are direct compression, wet granulation, and dry granulation. Direct compression involves simply pressing the blended ingredients into a tablet without prior granulation. Wet granulation utilizes a binding solution and drying, often with heat. Dry granulation most commonly involves slugging, where the powder is precompressed and the resulting “slug” is milled to produce granules. An alternative to slugging is use of a chilsonator, which compacts powder for milling with a pressure roller.

Front 48

15. What do the tablet-type acronyms CT, SCT, FCT, & ECT stand for?

Back 48

CT (compressed tablet), SCT (sugar-coated tablet), FCT (film-coated tablet), & ECT (enteric-coated tablet)

Front 49

17. What common flow problems are associated with making tablets from powders and how do they interfere with the process?

Back 49

Non-uniform flow leads to unacceptable variation in tablet weight. Uneven flow leads to segregation of active ingredients.

Front 50

19. List eight purposes for coating a tablet?

Back 50

1) Enhanced Palatability, 2) Increased Stability (vs. light, H2O, O2), 3) Enhanced Mechanical Integrity, 4) Elegant & Glossy Appearance, 5) Modified Drug Release, 6) Reduced Gastric Irritation (via EC), 7) Product Identification, 8) Separation of Incompatible Ingredients (1 in core, other in coat)

Front 51

21. What are the types of oral release patterns that can be achieved when formulating tablets and capsules?

Back 51

The, perhaps, comprehensive list of release patterns mentioned include Immediate-Release, Quick-Release, Modified-Release, Delayed-Release, Sustained-Release, Extended-Release, and Controlled-Release (Spatial and/or Temporal) as well as “Immediate / Conventional Release,” “Delayed Release / Bolus,” and “Delayed Release / Sustained.”

Front 52

22. What is an enteric tablet coating and what is the purpose of coating some tablets with them?

Back 52

An enteric tablet coating is one made of a pH-sensitive polymer that does not dissolve under acidic conditions. Enteric coatings are used to either protect the stomach from a drug or to protect a drug from the acidic conditions of the stomach.

Front 53

23. What are the incentives for utilizing sustained release technology for tablets or capsules?

Back 53

1) Increased patient compliance for drugs having short half-lives via reduced dosing frequency, 2) Sustained pharmacodynamic response to provide more effective disease treatment, 3) Reduction of side effects via lower peaks and valleys, 4) Enhanced bioavailability via targeting of the appropriate absorption window for drugs that are vulnerable to enzymatic degradation.

Front 54

24. What are three controlled drug release mechanisms for oral delivery systems?

Back 54

1) Diffusion-Controlled (from a non-degrading polymer matrix for instance), 2) Solvent-Activated Release (OROS as an example), and 3) Polymeric Degradation (drug w/i matrix freed as polymer degrades)

Front 55

25. What is an OROS?

Back 55

OROS stands for Osmotic-controlled Release Oral delivery System. Simply put, these systems hold the drug in a semipermeable membrane having one or more holes through which the drug can escape. As water flows in through the membrane, the increasing osmotic pressure forces the drug out of the holes in a sustained-release manner.

Front 56

26. Describe the three major mechanisms of polymer degradation often employed in the design of sustained release drug delivery systems.

Back 56

Mechanism A: Water-soluble polymers are made insoluble by cross-linking them together. When the cross-links are broken at some point in the body, the polymer will dissolve. Mechanism B: Water-insoluble polymers are made soluble by hydrolysis or ionization of side groups. Mechanism C: Insoluble polymers that cleave into soluble monomers.

Front 57

27. Which properties of a drug influence its passive diffusion across an intestinal membrane?

Back 57

Size, Partition Coefficient (logP), pKa (pH-Partition Theory), Concentration, and Site of Absorption

Front 58

28. When is the use of preservatives contraindicated in dosage form preparations?

Back 58

1) Dosage forms for neonates, 2) Ophthalmic solutions intended for use in eyes with nonintact corneas or for intraocular injection, and 3) Parental products having volumes greater than 50 mL.

Front 59

29. What are the properties of an ideal preservative?

Back 59

1) Effective at a low, nontoxic concentration against a wide variety of organisms; 2) Chemically stable under normal conditions of use, over a wide pH and temperature range; 3) Soluble at the required concentration; 4) Compatible with a wide variety of drugs and auxiliary agents; 5) Free of objectionable odor, taste, color, or stinging; 6) Nontoxic and nonsensitizing both internally and externally at the required concentrations; 7) Reasonable cost; 8) Unreactive (does not absorb, penetrate, or interact) with containers or closures.

Front 60

30. What are the differences between FD&C, D&C, and external D&C dyes?

Back 60

FD&C dyes may be used in foods, drugs, and cosmetics; D&C dyes are certified for use in drug and cosmetics; and external D&C dyes are restricted for use in externally applied drugs and cosmetics.

Front 61

31. What properties do patients prefer in dosage form flavors?

Back 61

1) Immediate flavor identity, 2) Rapid, full flavor development, 3) Acceptable feel to mouth, 4) Brief after taste, and 5) No undesirable sensations

Front 62

32. Which methods can be used to improve the taste of oral dosage forms?

Back 62

1) Blending Methods: the blending of flavors often yields an improved taste, 2) Masking Methods: adding a flavor and/or sweetener that has an intense, long-lasting taste can cover up the taste of the drug, 3) Physical Methods: a bad tasting drug can sometimes be rendered tasteless by using an insoluble form of the drug or by precipitating the drug in a solution by altering the pH or the solvent system of the drug preparation, 4) Chemical Methods: the drug may be complexed or a pro-drug can be made, 5) Physiological Methods: an extremely small quantity of an anesthetizing agent can be added (menthol, peppermint, & sodium phenolate) or the preparation can be stored in the refrigerator (cold reduced the intensity of disagreeable tastes and anesthetizes the taste buds)

Front 63

33. Quantify the sweetness levels of the following sweetners, relative to sugar: sorbitol, mannitol, saccharin, sodium saccharin, aspartame, stevia, splenda (sucralose)

Back 63

Sorbitol (0.5 - 0.7%), Mannitol (0.7%), Saccharin (60 mg equivalent to 30 g), Sodium Saccharin (300%), Aspartame (180%), Stevia (200%), Splenda, a.k.a. Sucralose (600%) [All relative to sugar]

Front 64

34. Which excipient ingredients are contraindicated in formulations for neonates?

Back 64

Alcohol and preservatives are "contraindicated" in formulations for neonates. Colors, flavors, and sweeteners "are not needed." Hypertonic solutions "should not be used."