Pharmaceutics II Exam II: Solids Dosage Forms and Drug Delivery Systems

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Transit time for food through the digestive tract: Mouth

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1 minute

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Transit time for food through the digestive tract: Esophagus

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4-8 seconds

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44 Terms

1

Transit time for food through the digestive tract: Mouth

1 minute

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2

Transit time for food through the digestive tract: Esophagus

4-8 seconds

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3

Transit time for food through the digestive tract: stomach

2-4 hours

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4

Transit time for food through the digestive tract: small intestine

3-5 hours

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5

Transit time for food through the digestive tract: Colon

10 hours to several days

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6

Modified oral dosage forms are pharmaceutical formulations that are designed to alter the ____, ____, and/or _____ of drug release in the gastrointestinal (GI) tract.

rate, time, location

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7

Unlike immediate-release (IR) forms, modified-release (MR) systems offer controlled drug delivery, improving the therapeutic ______ and patient _______.

outcome, experience

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8

Modified dosage forms aim to deliver the (minimum/maximum) amount of drug necessary to the site of action to produce the desired therapeutic response

maximum

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9

Modified dosage forms aim to deliver the drug at an optimal rate to ______ the beneficial response and _______ unnecessary drug exposure (minimize side effects)

maximize, minimize

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10

Some other modified- release dosage forms and drug delivery systems are also described, including ______, _______, ________, and _______ products

ocular, parenteral, subdermal, and vaginal

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11

Drugs that are long lasting and only require a once a day oral dose are formulated in the conventional manner in __________ dosage forms

immediate release

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12

Some drugs are inherently long lasting and require only once-a-day oral dosing to maintain adequate drug ________ and desired ________

plasma levels, therapeutic effect

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13

What is the half life of drugs that are rapidly cleared by the body and require multiple doses per day?

t1/2= 30 min

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14

Multiple daily dosing is inconvenient for the patient and can result in __________, _________, and _______ with the regimen

missed doses, made-up doses, and noncompliance

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15

When conventional immediate-release dosage forms are taken on schedule and more than once daily, they cause sequential therapeutic blood level ____ and _____ (troughs) associated with the taking of each dose

peaks, valleys

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16

What does SR/ER mean? Are they the same thing?

Sustained release, Extended release, YES they are the same

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17

What are 3 benefits of patients using SR/ER?

- Reduced dosing frequency. Increase patient compliance especially for chronic diseases (e.g., hypertension, diabetes)

- Maintaining therapeutic levels

- Reduced side effects

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18

Delayed release (DR)/ Enteric coated (EC) are drugs that delay drug release until it reaches a specific part of the _______

GI tract, typically the intestine

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19

Why are DR/EC used?

- Bypass the stomach: protects the drugs that are unstable or degraded by gastric fluid

- Protect the stomach lining: NSAIDs, aspirin irritates the stomach

- Targeted release: release drug in a specific part of the GI tract for better absorption or achieve local effect (e.g., treatment of Crohn's disease, ulcerative colitis)

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20

__________: To release a drug after a specific period (not location-specific), often for"chronotherapy" (delivery of drugs based on biological rhythms)

Time controlled release systems

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21

What is the rationale for using time controlled release systems?

Circadian Rhythm Synchronization: Some diseases (e.g., asthma, rheumatoid arthritis, and hypertension) exhibit time-dependent symptoms.Releasing a drug at a specific time of day can increase its effectiveness

Nighttime Effectiveness: Drugs that need to act during the night (like antihypertensives) can be designed to release several hours after ingestion

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22

What is an example of time controlled release systems?

Verapamil: taken at bed time, reduce nighttime blood pressure spikes

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23

_______: increase gastric retention time for drugs that are absorbed primarily in the stomach or upper intestine

Gastro Retentive systems

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24

What is the rationale for Gastro-retentive systems?

- Prolonged Gastric Retention: Increases the residence time of the drug in the stomach, which is beneficial for drugs that have a narrow absorption window(only absorbed in the upper GI tract).

- Improved Absorption: Drugs with low solubility at high pH (e.g., basic drugs)benefit from a longer stay in the acidic gastric environment.

- Localized Action: Drugs intended to act locally in the stomach (e.g., fortreating H. pylori infection) are released at the site of action

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25

What are examples of gastro retentive systems?

- Gebapentin ER

- Metformin GR

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26

What is the rationale for colon targeted drugs?

- Treatment of colon-specific diseases

- Avoid systemic absorption

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27

What are examples of Colon-targeted drugs?

- Mesalamin for ulcerative colitis

- Prenisolon colon-targeted for inflammation in Crohn's disease.

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28

For zero order kinetics there is a ______ amount of remain/release

constant

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29

For 1st order kinetics there is a constant _______ of drug remain/release

fraction

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30

What is the release kinetics to plasma concentration profile?

Dosage form -> drug release -> Drug solution -> Drug absorption -> In circulation

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31

Examples of immediate release systems include:

-Capsules

-Injections

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32

Examples of first order release systems:

-Implantable devices

-Hydrogels

-Polymeric particles

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33

Examples of zero order release systems?

-Osmotic pumps

-Actuated pumps

-Microchips

-Intravaginal rings

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34

Which equation is associated with the first order kinetic?

Noyes Whitney

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35

With the first order kinetic ______ is limited and there is no change in the _____ of the dosage form so the ______ remains constant

diffusion, shape, surface area

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36

First order kinetic: Erosion

There (is/is not) a change in the shape of the dosage form

Is

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37

What equation is used for the First order kinetic with Erosin

Hixson-Crowell

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38

What are examples of drugs/things with there mechanism of release by erosion?

Hard candy/lollipop

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39

First order kinetic: Erosion and Diffusion

_____ model is used

Higuchi

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40

Simplest and most widely used. It describes the release of drugs from solid matrices where drug release is dependent on the square root of time.

First order kinetic: Erosion and Diffusion

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41

What has a mechanism of release by erosion and diffusion?

most tablets

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42

First order kinetic: Diffusion

Noyes Whitney equation

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43

First order kinetic: Erosion

Hixson-Crowell equation

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44

First order kinetic: Erosion and Diffusion

Higuchi model/equation

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