Pharm Formulation and Delivery Systems

Question 1

Area of study concerned with the formulation, manufacturing, stability, and effectiveness of dosage forms

Answer 1

Pharmaceutics

Question 2

• The study of the relationship between the physical, chemical, and biological properties of a drug substance, dosage form and drug action
• The study of the physicochemical factors of drug dosage forms that influence the rate and extent of systemic drug absorption

Answer 2

Biopharmaceutics

Question 3

The aim is to adjust the delivery of the drug substance to the site of action to provide optimal therapeutic activity

Answer 3

Biopharmaceutics

Question 4

Importance of drug delivery

Answer 4

• must be present at site of action for adequate time

- more than 50% of developed drugs fail because they can not be silvered to target

Question 5

Two approaches to achieve efficient drug discovery

Answer 5

• via a suitable drug delivery system/dosage form

- via a drug modification

Question 6

Components of Pharmaceutical Dosage Forms

Answer 6

• Drug substance (API)
• Pharmaceutical ingredients (non-medicinal)

   Product: Drug Substance + Excipients

Question 7

Name at least 5 Pharmaceutic Ingredients

Answer 7

Binders, disintegrates, diluents, fillers, lubricants, flavors, compression aids, colorants, preservatives, glidants, suspending/dispersing agents, sweeteners, film coatings, printing inks

Question 8

Purpose of Dosage Forms

Answer 8

To provide:
Consistent accurate administration
Convenient administration
A palatable form for administration
Controlled-release of drug
To protect:
The substance from environmentally-induced degradation

Question 9

Purpose of Pharmaceutic ingredients

Answer 9

Impose patient acceptability and product stability, optimize production processes, enable product identification

Question 10

In typical tablet formula Latino, what is the % composition of the API?

Answer 10

The desired dose

There is also diluents/fillers, binders, disintegrates, surfactants, lubricants/gildants

Question 11

Preformulation considerations

Answer 11

The physicochemical characteristics of the drug, target site for drug, intended therapeutic use, age of target population, compatibility

Question 12

Biopharmaceutical Classification System

Answer 12

See/draw figure on Slide 19

Question 13

• process by which a solid of only fair solubility enters solution
• time for drug substance to dissolve in fluid at absorption site

Answer 13

Dissolution rate

Question 14

Dissolution Rate

Answer 14

dM/DT=DS/h (Cs-C)

dC/dt=DS/Vh (Cs-C)

A solid particle with surface area S 9cm20 dispersed in a solvent of volume V is surrounded by a stagnant layer of thickness h (cm)
Diffusion coefficient (cm2/sec)
M is the mass of solute dissolved in time t

Notes-Whitney equation

dM/DT=DS/h (Cs-C)

dC/dt=DS/Vh (Cs-C)

A solid

Question 15

Dosage forms with drug released features based on time, course or location that are designed to accomplish therapeutic or convenience objectives not achieved with immediate-release forms

Answer 15

Modified Release

• Delayed release
• Extended (sustained) release
• Controlled release systems

Question 16

Designed to release the drug at a time other than immediately after administration

Answer 16

Delayed release (enteric-coated)

Question 17

Defined as those that allow a reduction in dosing frequency compared with a conventional dosage form

Answer 17

Extended (sustained) release

Look over slides 26-28

Question 18

Include a component that can be engineered to regulate essential characteristic and have a duration longer than a day

Answer 18

Controlled release systems

Question 19

Type A and B Gelatins

Answer 19

Type A:
      Acid processing of pork skins
      Plasiticity and Clarity
      pI 7.0-9.0
Type B:
      Alkali processing of bones and animal skins
      Firmness but is hazy
       pI: 4.8-5.0

Usually mixture of A and B is used

Question 20

Physicochemical properties of gelatin

Answer 20

Bloom strength
-Empirical measure of gel strength
-measured in Blood telomeres
Viscosity

Question 21

Why is gelatin ideal material?

Answer 21

Swells but is insoluble in cold water
Has the ability to form a thermally reversible gel
Has excellent film-forming properties
Freely soluble in the stomach secretions
As a protein, is digested to amino acids

Question 22

Characteristics of Enteric-coated Tabs

Answer 22

• Form of delayed-release
• Designed to pass unchanged through stomach
• Tablet disintegration in intestine allowing drug dissolution and absorption
• Sow to have substantially higher absorption in intestine when stomach is by-passed
• Unstable in gastric pH
• irritating in gastric mucosa

Question 23

Tablet Additives (list at least 6)

Answer 23

• Diluents (fillers, bulking agents)
• Binders or Adhesives
• Lubricants and Antiadherents
• Disintegrants
• Colorants
• Flavoring Agents and Sweeteners
• Wetting Agents