DRUG

FORMULATION
AND
DEVELOPMENT
Prepared by:
M.Sc. Rasha Abu Thawabeh
The Drug Development Process
Drug
Formulation
Basic
Principles of dosage form design

Drug Chemical Administration

Formulation form of the Route
drug

01 02 03
What is Drug Formulation
Drug formulation consists of various
inactive substances, also known as
excipients, with the active
pharmaceutical ingredient (API), also
known as the drug substance, to
produce a final product for patients.
Role of Excipients in Formulations
• Drugs are rarely administered as pure chemical substances alone and are almost
given as formulated preparations or medicines. These can range from relatively
simple solutions to complex drug delivery systems through the use of appropriate
additives or excipients in the formulations.

• The excipients provide varied and specialized pharmaceutical functions. It is the

formulation additives that solubilize, suspend, thicken, preserve, emulsify, modify
dissolution, increase the compactibility and improve the flavour
Chemical form of the drug
 Importance of Drug Formulation and
Development in the Pharmaceutical Industry
• Drug formulation and development play a crucial role in ensuring the safety, efficacy,
and quality of pharmaceutical products.

• It involves converting a drug compound into a usable form, such as tablets, injections, or
topical products.

• The process includes identifying the most effective delivery methods, stabilizing the drug,
and ensuring it meets regulatory standards.

• It bridges the gap between laboratory research and patient care, ensuring that new drugs
can be safely and effectively administered.
 The Drug Development Process

Step 1 Step 2 Step 3 Step 4 Step 5

Discovery & FDA Post-Market
Preclinical Research Clinical Research FDA Review
Development Safety Monitoring
 Discovery
Typically, researchers discover new drugs through:

New insights Identifying Unexpected

New
into a disease treatments for effects of
process diseases. treatments technologies
 Development
Once researchers identify a promising compound for development, they conduct experiments to
gather information on:

How it is absorbed, Side effects or

01 distributed, metabolized,
and excreted
05 adverse events

Its potential benefits How it affects

02 and mechanisms of
action.
06 different groups of
people

How it interacts with

03 The best dosage
07 other drugs
treatments.
and

Its effectiveness as
The best way to
04 give the drug 08 compared
similar drugs.
with
 The Drug Development Process

Step 1 Step 2 Step 3 Step 4 Step 5

Discovery & FDA Post-Market
Preclinical Research Clinical Research FDA Review
Development Safety Monitoring
 Step 2: Preclinical Research
• Before testing a drug in people, researchers must find out whether it
has the potential to cause serious harm, also called toxicity.
The two types of preclinical research are:

in in
vitro vivo
Step 2: Preclinical Research

• FDA requires researchers to use good laboratory practices (GLP), defined in medical

product development regulations, for preclinical laboratory studies. The GLP

regulations are found in 21 CFR Part 58.1: Good Laboratory Practice for Nonclinical

Laboratory Studies. These regulations set the minimum basic requirements for:
 Facilities

Personnel Equipment

Study Study Written

Conduct Reports Protocols

Operating Quality
Procedures Assurance
 The Drug Development Process

Step 1 Step 2 Step 3 Step 4 Step 5

Discovery & FDA Post-Market
Preclinical Research Clinical Research FDA Review
Development Safety Monitoring
Step 3: Clinical Research
“Clinical research” refers to studies, or trials, that are done in people. As the developers design the
clinical study, they will consider what they want to accomplish for each of the different Clinical
Research Phases and begin the Investigational New Drug Process (IND).

Designing Clinical Trials

Clinical Research Phase

Studies The Investigational New
Drug Process

Asking for FDA Assistance

FDA IND Review Team

Approval
1. Designing Clinical Trials

Researchers design clinical trials to answer specific research questions

related to a medical product.

These trials follow a specific study plan, called a protocol, that is

developed by the researcher or manufacturer.

Before a clinical trial begins, researchers review prior information about the drug to develop research
questions and objectives. Then, they decide:

01 03 05 07

How the drug will be How the data

Who qualifies How long the
given to patients and will be reviewed
to participate study will last
at what dosage? and analyzed
How many Data Collection
people will Control group?
and Timing?
be part of
the study

02 04 06
 2.Clinical Research Phase Studies

01 02 03 04 05

Study Participants: Study Participants: Study Participants: Study Participants:

20 to 100 Several hundred 300 to 3,000 Several thousand
Length of Study: Length of Study: Length of Study: Length of Study:
Several months months – 2 years 1 to 4 years {open}
Purpose: Purpose: Purpose: Purpose:
Safety and dosage Efficacy and S.E Efficacy and Safety & Efficacy
monitoring of A.R
70% of drugs 33% of drugs
move to the next move to the next 25-30% of drugs
phase phase move to the next
phase
 3. The Investigational New Drug Process
In the IND application, developers must include:

Clinical protocols for Data from any prior human

studies to be conducted research

01 03 05

02 04

Animal study data and Information about the

Manufacturing information
toxicity investigator
 4. Asking for FDA Assistance

Drug developers are free to ask for help from FDA at any point in the drug
development process, including:

A. Pre-IND application, to review FDA guidance documents and get answers to

questions that may help enhance their research

B. After Phase 2, to obtain guidance on the design of large Phase 3 studies

C. Any time during the process, to obtain an assessment of the IND application
 5. FDA IND Review Team

Project Manager Medical Officer Statistician Pharmacologist

evaluate protocols
is the primary contact Reviews all clinical Reviews
and safety and
for the sponsor. study information preclinical studies
efficacy data.

Pharmakineticist Chemist Microbiologist

assess response
Focuses on the Evaluates a drug’s across different
drug’s ADME chemical compounds classes of microbes.
 6. Approval
The FDA review team has 30 days to review the original IND submission.
The process protects volunteers who participate in clinical trials from unreasonable and
significant risk in clinical trials.

FDA responds to IND applications in one of two ways:

1. Approval to begin clinical trials.
2. Clinical hold to delay or stop the investigation.

FDA can place a clinical hold for specific reasons, including:

i. Participants are exposed to unreasonable or significant risk.
ii. Investigators are not qualified.
iii. Materials for the volunteer participants are misleading.
iv. The IND application does not include enough information about the trial’s risks.
Step 4: FDA Review

Once FDA receives an NDA, the review team decides if it is complete. If

it is not complete, the review team can refuse to file the NDA. If it is

complete, the review team has 6 to 10 months to make a decision on

whether to approve the drug

Step 5: FDA Post-Market Safety Monitoring

Even though clinical trials provide important information on a drug’s efficacy and safety, it

is impossible to have complete information about the safety of a drug at the time of

approval. Therefore, the true picture of a product’s safety actually evolves over the months

and even years that make up a product’s lifetime in the marketplace. FDA reviews reports of

problems with prescription and over-the-counter drugs, and can decide to add cautions to

the dosage or usage information, as well as other measures for more serious issues.
Manufacturing Considerations
 Manufacturing Considerations

2
1 3

GMP (Good Role of equipment Common

Manufacturing in formulation challenges in
Practice) (mixers, manufacturing
compliance. granulators,
coating machines).
Future Trends
in Drug
Formulation
Future Trends in Drug Formulation

01 02 03

Personalized Nanotechnology Sustainability in

Medicine. in drug delivery formulation
Personalized medicine is an
emerging practice of
medicine that uses an
individual's genetic profile to
guide decisions made in
regard to the prevention,
diagnosis, and treatment of
disease.
Nanomaterials (NMs) synthesized from natural sources have

been attracting greater attention, due to their intrinsic

advantages including biocompatibility, stimuli-responsive

property, nontoxicity, cost-effectiveness, and non-

immunogenic characteristics in the biological environment.

Biocompatibility is necessary for treating a disease safely

without any adverse effects. Some components in DDS

respond to the physiological environment, such as pH,

temperature, and functional group at the target, which

facilitates targeted drug release. NM-based DDS is being

applied for treating cancer, arthritis, cardiovascular diseases,

and dermal and ophthalmic diseases.

Principles of sustainability applicable in drug discovery

01 Medical Needs

Artificial intelligence and big data 02

Biomarkers and bioinformatics to

03 support precision medicine

Risk and decision-taking models 04

05 Cost-Effective