Explain the Pilot plant and scale up techniques for solid dosage forms by HC12051822910


									 10 marks
1.What do you understand by controlled release and sustained release dosage forms
differentiate them write the advantages and disadvantages of the same
1. Comment on drug targeting give the detail account of various drug carriers used for
2. Explain in detail the principles involved in controlled release and sustained release
    dosage forms
3. Discuss in detail one method for the determination of pharmacokinetic parameters
    (elimination half-life absorption rate constant apparent from distribution
4. Write a note on phase-1 biotransformation reactions
5. What are pharmacokinetic models? What is the importance and utility of developing such

6. Explain the role of Pilot plant and scale up techniques in drug development and general
   factors to be considered? Explain the Pilot plant and scale up techniques for solid dosage
7. Explain in detail, the general factors to be considered in pilot plant scale up

8. Write a brief account on Targeted drug delivery systems
9. Write a brief note on liposomes
10. Define micro-encapsulation? Write method of preparation of microcapsules
11. Define slow release granulations? Write method of preparation of slow release
12. Comment on drug targeting give the detail account of various drug carriers used for
13. Define liposomes? Write in details method of preparation of liposomes
14. What is drug targeting? Explain there advantages and disadvantages of and its application
15. Explain the usefulness of compartment models in the prediction of pharmacokinetics
16. What is first pass effect and mention its role in drug absorption
17. What is the role of particle size during dissolution?
18. Explain different types of clearance
19. Explain the Noyes Whitney equation dissolution rater law
20. Write briefly on coacervation phase separation technique
22. What is the significance of Pilot plant and scale up techniques?
23. What are the advantages of herbal formulations giving its Significance?
24. Write a note on herbal formulations
25. What is process validation? Explain its salient feature and requirements
26. Write a brief account on process validation with suitable examples. Explain the design of
sustained release dosage forms
.27.For a small lipophilic drug administered orally in solution form, the rate-limiting step for
absorption is gastric-emptying. True or False? Explain your answer.
28. For a small lipophilic drug administered orally in solution form, the rate-limiting step for
absorption is gastric-emptying. True or False? Explain your answer

   29. Quick dissolving tablets, such as seen with many over-the-counter preparations (e.g.,
 benadryl and imodium) are designed to provide buccal absorption of the drug. True or false?
                                       Explain your answer
    30Name two enteral and two topical routes of administration that avoid the first pass
    31.Dipyridamole is marketed in a tablet that exhibits an absorption pattern rate-limited by
    disintegration (i.e., disintegration is the slowest step). Draw the concentration versus time
    profile for dipyridamole when a tablet is swallowed whole and the expected curve if the
    tablet was chewed before swallowing. Describe what would happen to the onset, intensity
    and duration when a tablet is chewed before swallowing versus swallowing the tablet

     32.Draw the expected concentration versus time curve for pentobarbital administered as an
     aqueous solution, an aqueous suspension, or a tablet. Which dosage form would provide
     the shortest onset? Which dosage form would provide the greatest intensity of effect?

     33.The therapeutic window for phenytoin is 10 to 20 mg/L. This means that a patient in
     whom a concentration of 8 mg/L is achieved will not clinically benefit from the drug. True
     or False? Explain the reason for your answer.

     34.Graph the relationship between molecular weight and % of drug excreted in the bile.
     35. Drug X has a half life of 4 hours and is administered as an intravenous bolus dose to
     produce a concentration of 100 mcg/ml. How long after administration of the dose of Drug
     X will the concentration drop to 25 mcg/ml?

     36. Theophylline is administered to a patient as a constant intravenous infusion at a rate of
     25 mg/hr. After 3 days of the infusion, the steady-state concentration is found to be 10
     mg/L. What is the clearance of theophylline in this patient?

      37.Drug A and B are both drugs that give rise to active metabolites and both drugs are used
      as analgesics. The active metabolite of Drug A exhibits formation rate-limited disposition,
      while the active metabolite of Drug B exhibits elimination rate-limited disposition. The
      half-life of Drug A and Drug B are found to be identical.38.Which would produce the
      longest duration of action, administration of Drug A or Drug B?
39.The average plasma concentration calculated at steady state after a large number of uniform
oral doses given with uniform dosing intervals is independent of the absorption rate constant.
True False

40.Elimination of salicylate (a weak acid) is faster when the urine pH is 4.5 compared with when
the urine pH is 8.5. True False

41..Phase II metabolism processes commonly result in metabolites that have a smaller molecular
weight than the parent drug. True False

42..Increasing the amount or percentage of lubricant in a table formulation will generally
increase the dissolution rate of the drug because of the penetrating capacity of these ingredients.
True False

43..Drugs that are extensively distributed into specific tissue regions, such as chloroquine into
the liver, tend to have quite small values for the apparent volume of distribution. (Note: This
question refers to material in Chapter 18) True False

44..When the total intrinsic liver clearance of a drug is quite high compared with liver blood flow
it may be said that the drug has flow limited clearance. True False

45.When developing a multiple dose regimen, doubling both the dosing interval and the dose
will result in the same average plasma concentration. True False

46.With just oral data it is not possible to determine separate values of V and F. True False

47.. Increasing the number of particles that make up a certain weight of drug will slow down the
overall dissolution process because there are more particles to go into solution. True False

48.. Briefly describe the intramuscular route of administration, giving advantages and
disadvantages of the method.
49..Briefly describe the parameter clearance, providing a definition, an equation suitable for
estimating this parameter, and units.

50.Define disposition, distribution, driving force of a drug?
51.What are the two major rate – limiting steps in the distribution of the drugs? Under what
circumstances they are applicable?
52. Which physicochemical properties the drug limit its distribution?
53. Name the specialized barriers for the distribution of drugs?
54. Name the three approaches by which a polar drug can be targeted to brain?

55. How are body tissues classified on the basis of perfusion rate?
56.What are the various mechanisms involved in the alternation of drug distribution
characteristics in diseased states?
  57. A protein bound drug is pharmacokinetically and pharmacodinamically inert. Explain?
58. What is the influence of protein binding and displacement interaction on the elimination half
life of a drug?
59. How do the acidic drugs like sulfonamides / NSAIDs Precipitate?
    60. Kernicterus in neonates?
    61. How does the plasma protein- drug binding influence sink conditions and
    62. Absorption of a drug from the GIT?
    63. Define bioavailability and bio equivalence?
    64 write in brief about the liposomes

    2 marks

1. Define pharmacokinetics.Two things of particular interest:

2. AUC is an indicator of what two things? Define each.

3. Define half-life.

4. Define apparent volume of distribution. Is it a physiological volume?
5. Define clearance.

6. Explain the difference between first and zero order and how to separate each graphically.
7. Define Biopharmaceutics.What 4 things are influenced by the study of Biopharmaceutics?
8. Define Pharmacodynamics.
9. What are the assumptions of compartmental modeling?

10. Define/explain Kinetic homogeneity.

11. Define Bioavailability. What 3 factors decrease it?

12. How can we verify that this data is not produced by “flip-flop” kinetics?

13. Name the six mechanisms of drug transport that we discussed in class. Which one is the
    most important mechanism? Which are energy-dependent? Which ones are saturable?
14. What is the effect on rate of diffusion if surface area available for exchange increases? ^/↓
    What about a thicker membrane? Increases/Decreases
    A more lipophilic drug? Increases/Decreases
    A larger concentration gradient? Increases/Decreases
15. Which transport mechanism is the only one by which a drug NOT in solution could be
16. Where within the GI tract is the optimal site for the absorption of drugs?
17. In terms of oral absorption, what is an “absorption window” and “residence time?”
18. Name the four things we discussed that affect GI transit time.
19. How can a highly lipophilic drug molecule bypass the portal vein, but still be absorbed when
    given orally?
20. What is the purpose of finding the pH solubility and pH stability profile for a drug?
21. If the size of drug particles is reduced, what effect does this have on dissolution (assume
    Noyes-Whitney dissolution behavior)?

22. List the three advantages and three disadvantages of extended release dosage forms.

23. In the one-compartment extravascular model (first order absorption/first order elimination),
    is it theoretically possible for the intercept of the residual line to exceed the intercept of the
    extrapolated line? Why/why not?
24. Regarding dissolution, why is polymorphism a problem?

25. Why is a highly lipophilic drug both good and bad for oral absorption?

26. What are characteristics of a successful extended release drug product?
27. If other parameters are held constant, what effect does increasing ka have on tmax &

28. Distribution of drugs in the body depends primarily on what two things?

29. Briefly, explain the difference between “flow-limited” & “permeability-limited”

30. Can hepatic clearance be greater than blood flow? Explain.

31. Can intrinsic clearance and/or free intrinsic clearance be greater than blood flow?

32. Explain the difference between bioavailability and bioequivalence. What extra
    information do we need to demonstrate bioequivalence? When is it important to
    demonstrate bioequivalence?

33. Generally speaking, which drug should have a larger volume of distribution, a
    lipophilic or hydrophilic one?

34. Give three reasons that we discussed that could explain a large volume of
35. If other factors are held constant and the free fraction of drug in the plasma (fu) is
    increased, what will the effect be on the Vd?
36. What if the free fraction of drug in the tissues (fu,t) is increased?

37. If clearance is held constant and volume is increased, will half-life be affected? If so,

38. In a multicompartment model, which estimate of volume of distribution is the most

39. What is the relationship between a single dose peak concentration and a steady state
    peak concentration? Does the same relationship exist with the trough concentrations?

40. The degree of accumulation depends on the relationship between what two variables?

41. Define steady state. The eventual steady state concentration depends on what
42. In what cases will the use of the Css average equation be most useful clinically?

43. If a drug cleared solely by the liver is a low extraction ratio drug, and there is a
    doubling in the free fraction of the drug, what will be the effect on volume of
    distribution, clearance, and half-life? What if it was a high extraction ratio drug?
44. What three factors must be the similar and within that range to consider two
    medications bioequivalent? When is it important?
45. True or False. Only bound drug produces a pharmacological effect.
46. When is calculating the absolute and relative bioavailabilities important?

47. How long until steady state is achieved?
48. In intermittent IV infusion, which will give the highest peak and highest trough?
        a. Small doses given more often
        b. Large doses given less often
49. As the length of the intermittent IV infusion approaches the dosing interval it takes on
the characteristics of being essentially
50. When is protein binding really important?
51. What is normal liver blood flow?
52. What is superimposablity?

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