MODULE: PHARMACEUTICAL SCIENCES & PRACTICE

OF PHARMACY

CHAPTER ONE: INTRODUCTION

SEMESTER: ONE

Date of session: 23.09.24 Kenza MANSOURI

Contents:

1. Pharmaceuticals Sciences
2. Formulation
3. Dosage form design
4. Dosage form design main objectives
5. Routes of administration & dosage forms
6. Factors for various dosage form
7. Our program
Pharmaceutics:

v The word ‘pharmaceutics’ is used in pharmacy and the pharmaceutical sciences to encompass a
wide range of subject areas that are all associated with the steps to which a drug is subjected
towards the end of its development.

v It encompasses the stages that follow on from the discovery or synthesis of the drug, its isolation
and purification, and its testing for beneficial pharmacological effects and absence of serious
toxicological problems.

v Put at its simplest – pharmaceutics converts a drug into a medicine.

v The drug is the pharmacologically active ingredient in a medicine.

v Drug’ is the correct word, but alternatives are frequently used, such as ‘medicinal agent’,
‘pharmacological agent’, ‘active principle’, ‘active ingredient’, or increasingly ‘active
pharmaceutical ingredient (API)’, etc.

v Pharmaceutics is concerned with the scientific and technological aspects of the design and
manufacture of dosage forms.

v It is the most diverse of all the subject areas in the pharmaceutical sciences and encompasses:

§ an understanding of the basic physical chemistry necessary for the effective design of
dosage forms (physical pharmaceutics)

§ an understanding of relevant body systems and how drugs arrive there following
administration (biopharmaceutics)
§ the design and formulation of medicines (dosage form design)

§ the manufacture of these medicines on a small (compounding), intermediate (pilot-scale)

and large (manufacturing) scale

§ the avoidance and elimination of microorganisms in medicines (pharmaceutical

microbiology, sterilization), and

§ product performance testing (physical testing, drug release, stability testing).

v Medicines are drug-delivery systems.

v They are a means of administering drugs to the body in a safe, effective, accurate, reproducible
and convenient manner.

v ‘Ceutics’ looks at the overall considerations that must be made so that the conversion of a drug to
a medicine can take place.

v It emphasizes the fact that medicines are very rarely drugs alone but require additives (termed
excipients) to make them into dosage forms, and this in turn introduces the concept of
formulation.
v Scientific principles of dosage form design introduces some of the more important
physicochemical knowledge that is required to design and prepare dosage forms.

v The large majority of dosage forms are administered via the mouth (oral route) in the form of
solid products, such as tablets and capsules.

v This means that one of the most important stages in drug administration is the dissolution of solid
particles to form a solution in the gastrointestinal tract.

v The formulation scientist therefore needs knowledge of both liquid and solid materials, in
particular the properties of drugs in solution and the factors influencing their dissolution from solid
particles.

v Once solutions are formed, the formulation scientist must understand the properties of these
solutions.
v We will see how drug release from the dosage form and absorption of the drug into the body
across biological barriers (e.g. the epithelia of the gastrointestinal tract, airways, skin, etc.) are
strongly dependent on the properties of the drug in solution, such as the degree of ionization and
speed of diffusion of the drug molecules.

v The properties of surfaces and interfaces will also be studied. These are important to an
understanding of adsorption onto solid surfaces, and are involved in the dissolution of solid particles
and the study of disperse systems, such as colloids, suspensions and emulsions.

v Knowledge of the flow properties of liquids (whether solutions, suspensions or emulsions) and
semisolids (e.g. creams, ointments and gels) is useful in solving certain problems relating to the
manufacture, performance and stability of liquid and semisolid dosage forms.
v We will also learn about the importance of the more macroscopic properties of powders that
influence their performance during the design and manufacture of dosage forms – particle size and
its measurement, size reduction and the separation of powders with the desired size characteristics
from those of other sizes.

v Knowledge and control of the particles size of a pharmaceutical material may be vitally important.
Size will influence the dissolution rate of solid particles, which for drugs with dissolution-rate limited
absorption may affect the safety and efficacy of the drug product.

v Moreover, control of size is important in the processing of powders during the manufacture of
solid dosage forms, in the stability of dispersed systems such as suspensions, emulsions and creams,
and in ensuring the efficacy of medicinal products, for example inhaler and nasal products, and
nanomedicines amongst others.
v Another extremely important area that must be understood before a satisfactory dosage form can
be designed and manufactured is the microbiological aspects of medicines development and
production.

v It is necessary to control or eliminate living microorganisms present in the product both before
and during manufacture.

v This mainly involves avoiding (asepsis) and eliminating (sterilization) the presence (contamination)
of viable microorganisms in medicines, and preventing the growth of any microorganism which
might enter the product during storage and use of the medicine (preservation).
v It is not possible to begin to design a satisfactory dosage form without knowledge and
understanding of how drugs are absorbed into the body, the various routes that can be used for
this purpose and the fate of the drugs once they enter the body and reach their site(s) of action.

v The terms bioavailability and biopharmaceutics will be defined and explained (Biopharmaceutical
principles of drug delivery).

v The factors influencing the bioavailability of a drug and methods for its assessment will be
discussed.

v Strategies to modify the physicochemical properties of the drug or the formulation to enhance
bioavailability will also be outlined.
v This is followed by a consideration of the manner in which the frequency of drug administration
and the rate at which drug is released from a dosage form affect its concentration in the blood
plasma at any given time.

v Pharmaceutics concentrate on the preparation, administration, release and absorption of drugs

ONLY.

v It leaves to other subjects the detail of how drugs enter individual cells, how they act and how
they are metabolized and eliminated from the body.
Formulation:

v The first stage of designing and manufacturing a dosage form is known as preformulation.

v Pre-formulation involves a full understanding of the physicochemical properties of drugs and

other ingredients (excipients) in a dosage form and how they may interact.

v An early grasp of this knowledge during product development is of great use to the formulation
scientist as the data gathered in these early stages can influence strongly the design of the
future dosage form.

v Results of tests carried out at this stage of development can give a much clearer indication of the
possible (and indeed impossible) dosage forms for a new drug candidate.
v The properties of dosage forms can be modified dependent on the properties of the drug,
excipients included, the route of drug administration and specific patient needs.

v We will look into liquid dosage forms, namely solutions (drug dispersed as molecules or ions),
suspensions (drug dispersed as particles) and emulsions (one liquid phase dispersed in another,
with drug present in either phase).

v These dosage forms may be administered by a number of routes, and their formulation
requirements will vary depending on the route of administration.

v Appropriate formulation of emulsions results in more structured semisolid creams, most

frequently used for application to the skin.

v Other dosage forms applied to the skin include ointments, pastes, gels, cutaneous patches and
topical sprays.
v Whilst drugs in the solid state can be administered as simple powders, they are more usually
formulated as solid dosage forms, namely tablets (currently the most commonly encountered
solid dosage form) and capsules.

v We will look at the various stages in the processing of a powder required to manufacture tablets:
granulation (formation of drug-excipient aggregates), drying, compaction and coating.

v Tablet formulation and manufacture require inclusion of several excipients, including fillers,
disintegrants, binders, glidants, lubricants and anti-adherents.

v The strategies to modify the release of drug from solid dosage forms primarily involve the
production of monolithic matrix systems or the use of a rate-controlling membrane.
v For all dosage forms, drug must be released at an appropriate rate at the appropriate site for drug
absorption and/or drug action to occur.

v This is particularly pertinent for solid oral dosage forms, which must permit dissolution of drug at
an appropriate rate and at an appropriate site within the gastrointestinal tract.

v Bioavailability (i.e. the amount of drug that is absorbed into the bloodstream) may be limited by
the rate of drug dissolution, whilst the pH range in the gastrointestinal tract (pH 1–8) may
adversely affect the absorption of ionizable drugs.

v Consequently, dissolution testing is a key development and quality control test and is considered
in detail here.
v Once the product is demonstrated to be of appropriate quality for patient use, and following
approval by regulatory authorities, the pharmaceutical technologist passes the product on to
another aspect of pharmacy – the interface with the patient, i.e. dispensing and pharmacy
practice.
Scope of pharmaceutics:

• Pharmaceutical formulation
• Pharmaceutical manufacturing
• Pharmaceutical technology
• Physical pharmacy
• Microbiology
• Packaging
• Pharmaceutical jurisprudence
Formulation:

Active Pharmaceutical
Ingredient (API)
+ Excipients/Additives/Non
drug components

Pharmaceutical Dosage
Forms
Active Ingredients:

- Drugs are rarely alone in the dosage form

- Excipients, non active ingredients will be added to the API
- E.g. AspirinR 300mg soluble tablets
- It contains 300mg of acetylsalicylic acid
- Excipients to make it to 4g total mass
- API = 12.5% (m/m)
- Dosage form is soluble tablets
 API= active pharmaceutical ingredient
It is responsible for the beneficial health effect of the patient.

Excipient= non medicinal agent

Its uses are :
• thicken
• stabilize
• flavour
• suspend
• dilute
• preserve
• efficacious
• emulsify
• colour
• appealing
It is necessary to formulate the drug to provide the physiochemical characteristics required for the
desired application.
Dosage form

There are various physical different forms:

solid: - tablets
- caplets
- capsules
- lozenges

Liquid: - sirop
- solution
- emulsion

Semi-liquid: - gels
- crems
- ointments
v However, to know whether to formulate a drug as a solid, liquid, or semi-solid formulation, a
formulation scientist conducts preformulation studies.

v Such studies help to evaluate the physical, chemical, and mechanical properties of the drug
substance, its stability, and interaction with other chemical ingredients.
Dosage form design main objective:

Reproducible

Efficient Safe

Stable
attractive
Easy to
take
Routes of administration & Dosage forms
Factors for various dosage form:

These can be broadly grouped into three categories:

I. Biopharmaceutical considerations, including factors affecting the absorption of the drug
substance from different administration routes;
II. Drug factors, such as the physical and chemical properties of the drug substance;
III. Therapeutic considerations, including consideration of the clinical indication to be treated and
patient factors.

High-quality and efficacious medicines will be formulated and prepared only when all these factors
are considered and related to each other. This is the underlying principle of dosage form design.
Pharmaceutical Sciences Program:

v Some history
v Introduction to pharmacy law
v Different pharmacists role
v Drug development
v The physical and biochemical background needed for drug formulations development
v Drug dosage form design

v The objectives of the course are to provide the physicochemical, technological and regulatory
forms for pharmaceutical administration: liquids, suspensions, emulsions, solutions, semi- solids
and solids.

v Mainly lectures & 4 workshops (graded).