Bioequivalence and BA: Methods and Concepts

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Questions and Answers

Which of the following is NOT a method for assessing bioavailability and bioequivalence?

In vivo pharmacodynamic comparison

In vivo measurement of active moiety

In vivo clinical trial (correct)

In vitro comparison

What is the primary purpose of a prodrug?

To reduce biotransformation of the active drug

To decrease chemical stability of the active drug

To increase first pass metabolism

To improve solubility and bioavailability of the active drug (correct)

What is the purpose of in vitro dissolution testing in bioequivalence studies?

To assess the pharmacodynamic effect of the drug

To measure the plasma level of the active drug

To evaluate the chemical stability of the drug

To replace in vivo bioequivalence studies (correct)

Which type of drug products may require additional consideration in bioequivalence studies?

All of the above Signup and view all the answers

What is the primary purpose of bioequivalence studies?

To assess the similarity in bioavailability of different drug products Signup and view all the answers

Which of the following is a factor that influences bioavailability?

All of the above Signup and view all the answers

What is an advantage of extended release products?

Reduction in healthcare cost Signup and view all the answers

What is a characteristic of targeted-release drug products?

They release the drug at or near the intended physiologic site of action Signup and view all the answers

What is an example of an orally disintegrating tablet?

Dispersed in saliva and swallowed with little or no water Signup and view all the answers

What is the primary consideration for designing MR drug products for different routes of administration?

Physiochemical, PD, and PK properties of the drug and the properties of the materials used in the dosage form Signup and view all the answers

What is a characteristic of extended release drug products?

They reduce dosage frequency by at least 2-fold Signup and view all the answers

What is a disadvantage of extended release products?

Dose dumping Signup and view all the answers

Under what conditions can an in vivo BE study of one or more lower strengths of a drug product be waived?

If the drug product is in the same dosage form but different strengths and is proportionally similar in active and inactive ingredients Signup and view all the answers

What is a characteristic of enteric coated tablets?

They are time sensitive or dependent on the environment Signup and view all the answers

What is an example of a type of MR drug product that releases a discrete portion of the drug at a time later than immediately after administration?

Delayed release drug products Signup and view all the answers

How many types of MR oral drug products are described based on drug release characteristics?

20 Signup and view all the answers

What is the main difference between controlled release and delayed release drug products?

Controlled release products release the drug promptly after administration, while delayed release products release a discrete portion of the drug at a time later than immediately after administration Signup and view all the answers

What is the purpose of a Positive Formulary?

To list therapeutically equivalent or interchangeable drug products that pharmacists may dispense Signup and view all the answers

What is required for a generic product to be assumed therapeutically equivalent?

It must be approved as safe and effective, be pharmaceutically equivalent, bioequivalent, adequately labeled, and manufactured in compliance with Current Good Manufacturing Practice regulations Signup and view all the answers

What is the name of a type of oral extended-release rate dosage form previously described?

Controlled release Signup and view all the answers

What does 'modified release' refer to in relation to oral drug products?

A type of oral dosage form that alters the timing and/or rate of release of the drug Signup and view all the answers

What is the purpose of an in vivo BE study?

To determine the bioequivalence of a drug product Signup and view all the answers

Study Notes

Methods for Assessing BA and BE

In vivo measurement of active moiety or moieties in biological fluid (PK study)
In vivo pharmacodynamic (PD) comparison
In vivo limited clinical comparison
In vitro comparison
Any approach deemed acceptable by the FDA

Factors Influencing BA

No details provided

Definition of a Prodrug

A prodrug is a chemically modified drug, usually an inactive form, to improve solubility, increase chemical stability, or increase bioavailability of the active drug by decreasing first-pass metabolism
After oral administration, the inactive prodrug is converted to the active drug generally by biotransformation or hydrolysis

Statistical Analysis for BE

No details provided

Plasma Level and Urinary Excretion Parameters to Drug BA

No details provided

Review Process for NDA and ANDA

No details provided

BE for Specific Drugs and Drug Products

Oral solution
Chewable tablets
Orally administered drugs intended for local action
BE of topical drug products for local action
Inhalation and nasal sprays for local drug action
Alcohol effects on MR drug products
Endogenous substances
Long half-life drugs
Drug products with high intrasubject variability
Drug products with complex mixtures as the active ingredients

Waivers of In Vivo BE Studies

BE studies in vitro dissolution testing may be used in lieu of in vivo BE studies for time-sensitive or environment-dependent products
Examples: Enteric coated

Types of MR Oral Drug Products

Targeted-release drug products: release drug at or near the intended physiologic site of action
Orally disintegrating tablets: disintegrate rapidly in the saliva after oral administration
Extended release drug products: dosage form releases drug over an extended period of time after administration
Delayed release drug products: dosage form releases a discrete portion/portions of drugs at a time later than immediately after administration

Advantages of Extended Release Products

Sustained therapeutic blood levels of the drug
Improved patient compliance
Reduction in adverse side effects and improvement in tolerability
Reduction in healthcare cost

Disadvantages of Extended Release Products

Dose dumping: release of more than the intended fraction or greater rate
Less flexibility in accurate dose adjustments
Less possibility for high dosage
Increased potential for first-pass clearance
Poor IVIV correlation

Generic Substitution

Positive Formulary: lists therapeutically equivalent or interchangeable drug products that pharmacists may dispense
Negative Formulary: lists drug products that are not therapeutically equivalent, and/or the interchange of which is prohibited

Therapeutic Equivalence

Therapeutic Equivalence is assumed for a generic product if:
Approved as safe and effective
Are pharmaceutically equivalent
Are bioequivalent
Adequately labeled
Manufactured in compliance with Current Good Manufacturing Practice regulations

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Description

Test your knowledge of bioequivalence and bioavailability, including methods for assessing BA and BE, regulatory differences, and key concepts like biowaivers and prodrugs. This quiz covers the fundamentals of BA and BE in pharmaceutical development.