PHYSICOCHEMICAL PROPERTIES

Question 1

bioavailability depends on

Answer 1

route of administration

Question 2

the fraction of the dose of a drug that is found in general circulation

Answer 2

bioavailability

Question 3

LIPINSKI’S RULE OF FIVES

molecular mass

Answer 3

less than 500

Question 4

LIPINSKI’S RULE OF FIVES

calculated value of log P

Answer 4

less than 5

Question 5

LIPINSKI’S RULE OF FIVES

hydrogen bond acceptor groups

Answer 5

less than 10

Question 6

LIPINSKI’S RULE OF FIVES

hydrogen bond donor groups

Answer 6

less than five

Question 7

it is desirable that leads and analogues have a balance between their ____ and their ____

Answer 7

water solubility & lipophilicity

Question 8

the lipophilicty of a compound is often represented by the ____ of that compound in a defined solvent system

Answer 8

partition coefficient

Question 9

base/standard partition coefficient

Answer 9

octanol

Question 10

• Developed to optimize the development of an oral dosage form taking into consideration two rate-limiting factors, drug permeability and drug dissolution, the latter of which is related to drug solubility.
• Divided into four (4 classes)

Answer 10

Biopharmaceutical Classification System

Question 11

are well absorbed and are affected by a limited set of interactions that alter drug absorption
* Ex: Acetaminophen, Metoprolol

Answer 11

Class I

Question 12

dissolution rate limits drug absorption
* Absorption of this class of drugs is often enhanced in proportion to the fat content of the co administered meal.
* Example: Griseofulvin, Digoxin

Answer 12

Class II

Question 13

an antifungal drug that should be taken w high fat meal

Answer 13

Griseofulvin

Question 14

permeation is the rate-limiting step in the absorption from IR dosage forms.
Examples: Acyclovir, Chloramphenicol

Answer 14

Class III

Question 15

undesirable for good oral drug absorption Examples: Furosemide and Paclitaxel

Answer 15

Class IV

Question 16

determines the drug’s ability to bind to receptors and other target sites

Answer 16

structure of the drug

Question 17

is the formation, either temporary or permanent, of chemical bonds between the drug or analogue with the receptor

Answer 17

binding

Question 18

• used to treat cancer
• owes its action to the strong covalent bonds it forms with DNA
• dialkylating agent

Answer 18

Melphalan

Question 19

For a drug to be effective, it must be stable long enough after administration for sufficient quantities of it to reach its target site.

Answer 19

stability after administration

Question 20

The main method of increasing drug stability in the biological system is to prepare a more stable analogue pharmacological activity.

Answer 20

structure modificaiton

Question 21

Complexing with ____ is used to improve both the
stability and solubility of thalidomide, which is used to inhibit rejection of bone marrow transplants in the treatment of leukaemia.

Answer 21

hydroxypropyl-b-cyclodextrin

Question 22

active form of cyclophosphamide

Answer 22

phosphoramidate mustard

Question 23

• time taken for a drug’s pharmacological activity to decline to an unacceptable level
• no universal specification
• However, 10% decomposition is often taken as an acceptable limit provided that the decomposition products are not toxic.

Answer 23

Shelf life