Medicine formulations 1 wk2

Week 2

Define the term "drug" (or API).

A chemical that is used to manage a disease in humans, animals, or plants and has a physiological effect when introduced to the body.

Give examples of what blood concentrations drugs are effective in.

: Effective in blood concentrations of 0.01 to 0.1 M (ethyl alcohol) and 0.000,000,07 M (morphine).

Why are drugs typically not administered as pure chemicals?

Because of potency, bioavailability & pharmacokinetics, and stability.

What is dosage form design?

The science of the conversion of a drug into a medicine.

What is the main objective of dosage form design?

To achieve a predictable therapeutic response to a drug.

Define "excipient."

A pharmacologically inactive substance that serves as a vehicle or medium for a drug or active substance.

What are the three categories of excipients?

Preparation, patient acceptability, and function.

What is the purpose of excipients in medicines?

To facilitate making the drug into a medicine suitable for administration.

What factors impact drug specificity?

Molecular structure, receptor affinity, and formulation (targeted drug delivery).

What factors need to be considered in dosage form design?

Ability to manufacture in large scale and quality, biopharmaceutical considerations (including route of administration), physical and chemical properties of the API, and therapeutic considerations (patient factors, clinical indication).

What factors are affected by different drug delivery routes?

Absorption patterns.

What is a formulation?

A form of a medicine; a method of administering a drug.

Why is the route of drug delivery important?

the absorption pattern differs between formulations AND different administration routes.

What is bioequivalence?

Two medicines are said to be bioequivalent when they produce such similar plasma concentrations of the active ingredient that their clinical effects can be expected to be the same.

Why is bioequivalence considered?

Many generic medicines become available in the market.

How are two medicines with the same API considered bioequivalent?

If they are pharmaceutically equivalent and have similar bioavailability (pharmacokinetic data).

What pharmacokinetic parameters are considered when determining bioequivalence?

AUC (the total dose-time quantity in the plasma), Cmax (the maximum plasma concentration of drug achieved), and tmax (the time to maximum plasma concentration).

How is bioequivalence determined statistically?

By calculating the 90% confidence interval (CI) for test to reference product geometric mean ratios, with the 90% CI for the PK parameter falling within 80-125%. For drugs with a narrow therapeutic range, the 90% CI should be within 90-111%.

Give an example of a drug where bioequivalence is important.

Warfarin

Why can clinical outcomes differ even if the drug and dose are the same?

Bioequivalence can be profoundly affected by the formulation.