Drug Discovery, Formulation and Manufacturing of Medicine (wk 1)

3 categories of general considerations when de signing a dosage form

-Physioco-chemical considerations: Focus on inherent physical and chemical properties of the drug substance (solubility, particle size, pKa)-

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Biopharmaceutical considerations: how the dosage form interacts with biological systems (drug absorption, distribution, excretion) to ensure the API reaches its site of action effectively

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-Therapeutic considerations: Nature of the clinical indication, disease or illness the drug is intended for

Pharmaceutics

This is the general area of study concerned with the formulation, manufacture, stability and effectiveness of pharmaceutical dosage forms

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-conversion of drug into a medicine

Drug and other names

-The pharmacological active ingredient in a medicine

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-Medicinal agent, Active ingredient or active pharmaceutical ingredient (API)

Dosage form

-Formulated preparation or medicine-

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Physical form of a pharmaceutical formulation containing the drug and some inactive ingredients necessary to make a particular physical form

Examples of dosage forms

solutions, syrups, suspensions, tablets, capsules, ointments, creams, gels, aerosols, injections, sprays, powders and granules, inhalations, implants and emulsions

5 characteristics a dosage form must possess

-Protect drug from destructive influences O2, humidity ie : coated tablets and sealed ampoules)

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- Mask unpleasant taste or Odor of drug (flavored syrup / sugar coated capsule)

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-Administer high dosage of an insoluble drug in liquid form (suspensions)

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-provide time-controlled drug action (Controlled-release tablets, capsules, suspension)

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-Safe and convenient delivery of accurate dosage of drug

Medicines

Drug delivery systems, that are administered to the body in a safe, efficient, reproducible and convenient mannr

Pharmaceutical excipients

Components of medicinal formulations with no therapeutic effects

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-They are substances other than the active drug or pro-drug that has been included into the dosage form

Excipients

Non-medicinal agents, additives in a drug formulation providing varied and specialized pharmaceutical functions

Use of Pharmaceutical excipients

Ensures:

-optimum delivery

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,-absorption

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-release

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-Subsequent therapeutic action of the active ingredient and stability

What does an ideal excipient consist of

The ideal excipient should be inert, exerting no independent therapeutic or bio logical action of the Drug present in a dosage form

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-(Currently it has been observed that excipients have the ability to influence the rate and extent of absorption of drug substances)

Active Ingredient

Ingredient or ingredients of a pharmaceutical product responsible for its pharmacologic activity

Drug-delivery system

specialized dosage forms designed to release drugs at a constant rate for pro longed period of time. ie: Nicotine transdermal patch

List 9 routes of administration and there accompanying dosage form (bk)

bk

9 considerations when designing a drug product

-Chemical stability

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-Physical stability

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-Compatibility of drug and additives

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-Safe -

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Stable

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.-Attractive

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-Easy to administer

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- Efficacious

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- Suitable packaging

Chemical stability:

The drug should not chemically degrade or form harmful products during its shelf life

Physical stability

The dosage form should maintain its physical properties, such as appearance, consistency, and uniformity, without separating or changing

Compatibility of drug and additives

The drug and excipients should not interact in ways that reduce the drug's stability, effectiveness, or safety

Safety

Safety The formulation should be safe for the patient and should not contain harmful components at inappropriate levels

Stability

The product should remain safe, effective, and of acceptable quality throughout its intended shelf life

Attractive ness/acceptability:

should have an acceptable appearance, taste, or other characteristics that encourage patient acceptance and use

Easy to administer

The dosage form should be convenient and suitable for the intended patient, route, and method of administration.

Efficacy

The drug should deliver the active ingredient in a form and amount that produces the desired therapeutic effect

Suitable Packaging

Packaging should protect the product from factors such as moisture, light, contamination, and physical damage while maintaining its quality

Efficacy

the maximal response a drug can produce- At 100 % effect - full eradication is observed

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-they mean that 100% represents the maximum possible response, where the target being measured has been completely eliminated.

Potency

Potency is a measure of the dose that is required to produce a response.

Potency vs efficacy (bk)

Potency vs efficacy (bk)

Goal drug

An idealized theoretical drug that produces the specific therapeutic effect, is administered safely via the desired route (typically oral) at minimal dosage and frequency exhibits perfect onset and duration without side effects or residual action and is chemically stable, pharmaceutically elegant, and cost-effective to produce

Lead compound

A prototype chemical compound that has the fundamental desired biologic or pharmacologic activity -since the desired properties may not be possessed the compound's chemical structure is modified to achieve the desired effects and reduce undesired ones

Pro drug and ie

- A pharmacological inactive chemical derivative of a drug molecule that must undergo enzymatic or chemical biotransformation inside or outside the body to release the active therapeutic agent

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-Improves absorption, bioavailability or target selectivity ie: Enalapril maleate (vasotec)

Explain Enalapril maleate as a pro-drug

After oral administration the drug is bioactivated by hydrolysis to enalaprilat an ACE inhibitor to treat hypertension

Crude drug

Any unrefined natural substance derived from plant, animal, mineral, or microbial sources that has only undergone basic processes such as collection, drying, and size reduction without artificial molecular modification.