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5 Factors affecting drug absorption

Chemical structure


Particle size and surface area


Nature of the crystal form


Type of tablet coating and tablet matrix


Extent of ionization

CPNTE

The presence of ____ and ____ functional groups in the chemical structure of the drug affects its ____

Polar


Non polar


Absorption

How to enhance drug solubility

Alteration of the chemical structure

2 ways on how to enhance absorption rate

Reduce particle size


Increase surface area

The ability of a drug to exist in two or more crystalline forms with different arrangements in the crystal lattice

Polymorphism

Amorphous is ____ compared to crystalline

More soluble

Generic name of Insulin Lispro

Insulin semilente

Brand name of Insulin Lente

Neutral protamine of hagedorn

2 brand names of insulin ultralente

Insulin glargine


Insulin detemir

Action of insulin semilente

Fast onset of action

Action of insulin ultralente

Slow onset of action

Duration of action of insulin semilente

Short acting

Duration of action of insulin lente

Intermediate acting

Duration of action of insulin ultralente

Long acting

Form of insulin semilente

100% amorphous

Form of insulin lente

30% amorphous


70% crystalline

Form of insulin ultralente

100% crystalline

An important factor in the degree of penetration of a drug through ____ is that many drugs are ____ or ____

Membranes


Weak acids


Weak bases

An acidic drug in a basic environment is ____ and ____ to ____

Neutralized


Converted


Ionized form

3 physical factors affecting absorption

Blood flow


Contact time at absorption surface


Food

BCF

Relationship of Blood flow and absorption rate

Higher blood flow = higher absorption rate = higher blood supply

The time required for the stomach to be empty

Gastric emptying time

Degree of absorption:


Relationship of GET and absorption

Slower GET = higher absorption


Faster GET = lower absorption

Rate of Absorption:


Relationship of Food and Absorption

Delayed GET = lower absorption = higher bioavailability

The fraction of administered drug that reaches the systemic circulation

Biovailability

4 factors affecting bioavailability of drugs

FPE


Drug solubility


Chemical instability


Nature of drug formulation

FDCN

It happens when an orally administered drug is absorbed into bloodstream through GIT passes through the liver before being further distributed

FPE

3 examples of drug with first pass effect

Nitroglycerin


Lidocaine


Isoproterenol

NLI

The first pass effect ____ the drug’s ____

Decreases


Bioavailability

A drug should be ____ and ____

Partially hydrophilic


Largely lipophilic

Chemical instability of a drug ____

Decreases bioavailability

2 drugs that are chemically unstable

Penicillin G


Insulin