Unit 4 Substance Discovery And Product Development

1. To ask about drug discovery and drug development. 2. To get familiar with using passive voice in writing scientific articles or experimental instructions. 3. To describe some dosage forms. Research Development (R D) Research + Testing chemical compounds + Finding substance which has beneficial effect on a targeted disease Development + Carrying forward scientific discoveries made during the research process + Producing a marketable drug

Lesson : Substance discovery and product development

Objectives

1 To ask about drug discovery and drug

development

2 To get familiar with using passive voice in

writing scientific articles or experimental instructions

3 To describe some dosage forms

Research & Development (R & D)

3

Research

Testing chemical compounds

Finding substance which has beneficial effect on a targeted

disease

Development

Carrying forward scientific discoveries made during the research process

Producing a marketable drug

Match each phonetic spelling to one of the words

Match each of the following concepts with its definition

1 an analysis of disease _ is an experiment conducted to identify the

chemical makeup or characteristics of a particular sample

2 an analytical testing _ are the manners in which drug substances are

presented in the market

3 a clinical trial _ is the science of detection, assessment,

understanding and prevention of side effects which allows us to understand more about the risks and benefits of a medicine

4 dosage forms _ is aimed at finding the efficacy target of a drug

5 drug safety _ is a research performed in people that are aimed

at evaluating a medical, surgical, or behavioral intervention

6 drug discovery _ is the process by which new

candidate medications are discovered

7 target identification _ is an organized, proactive approach to health care

for members of a population designed to prevent the development of specific diseases

Language Focus: Passive voice

S + to be + PP

Used to show interest in the person or object that experiences an action rather than the person or object that performs the action

Example:

Mr Hieu teaches the class of D20

=> The class of D20 is taught by Mr Hieu

Give examples of passive voice

Sentence: Chính quyền đã cung cấp 3 gói thuốc cho những người ở nhà trong thời gian họ tự cách ly

Translate: The authority provided three packs of medicine to people staying at home during the quarantine

Passive voice: Three packs of medicine were provided by the authority

to people staying at home during the quarantine

Give examples of passive voice

Sentence: Các nhà hảo tâm đã từ thiện lương thực và thực phẩm đến người dân địa phương

Translate: The benefactors have donated food and clothes to the local people

Passive voice: Food and clothes have been donated by the benefactors

to the local people

Point out sentences written in the passive voice

The syntheses of compounds (which are) reported in this paper

are outlined in Figure 8 and described in details in Information S1 In the first step, 2,4-diamino-5-cyanopyrimidine (1) was

prepared according to the method (which was) reported by

Huber [30], by condensing guanidine nitrate with

ethoxymethylenemalononitrile in ethanol in the presence of a

significant amount of sodium ethoxide, to form the free

guanidine base The cyano group was reduced using Raney

nickel as catalyst and 98% formic acid as solvent [31]

[Skedelj V, Arsovska E, Tomasic ́ T, Kroflic A, Hodnik V, et al (2012)

6-Arylpyrido[2,3-d]pyrimidines as Novel ATP-Competitive Inhibitors of Bacterial D- Alanine:D-Alanine

Ligase PLoS ONE 7(8): e39922 doi:10.1371/journal.pone.0039922]

Rewrite the experimental instruction in passive voice

Weigh 6 g of p-aminophenol and

transfer thoroughly to a 100 ml

cleaned and dried conical flask Add

to the flask 6.5 ml of acetic

anhydride and 3-4 drops of

concentrated sulfuric acid carefully

The contents of the flask may be

mixed thoroughly Warm the

mixture on a water-bath previously

maintained at 600C for about 20-25

min with constant stirring Allow

the contents of the flask to attain

room temperature, and pour it

directly into a beaker having 100 ml

of cold water and stir it vigorously

6 g of p-aminophenol is weighed

and transferred thoroughly to a 100

ml cleaned and dried conical flask

6.5 ml of acetic anhydride and 3-4 drops of concentrated sulfuric acid are carefully added to the flask The contents of the flask may be mixed thoroughly The mixture is warmed

on a water-bath (that was) previously maintained at 600C for about 20-25 min with constant stirring The contents of the flask are allowed to attain room temperature, and (are) poured directly into a beaker having 100 ml

of cold water and (are) stirred vigorously

What is the meeting about, and what needs to be discussed?

 Breakthrough in the search for NCE for Mensapatch TM development, ideas

for new substance and further development

What kind of product is Mensamint TM?

 A new lozenge form of the product Mensadent TM to stimulate brain

activity and thinking power

What do patients have to do to obtain it?

 Get a prescription from a physician

What are the dosage form of this product?

 Lozenges (for adult patients) and chewing gum (for young patients)

Are there any known side effects?

 Yes, there are loss of sleep, increased blood pressure, heart palpitations and headaches

Answer the following questions

How many patients were surveyed in all?

 Nearly 2000 (patients were surveyed in all)

Were more male or female patients interviewed?

 (More) Male (patients were interviewed than female ones)

What kind of dosage form is most preferred by the patients surveyed?

 Capsules (preferred by 32% of the patients surveyed)

What kind of side effects were experienced by the least number of patients?

 Dizziness, vomitting and diarrohea (were experienced by the least number

of patients)

What chronic health conditions did most patients have?

 Bronchitis and asthma (are chronic health conditions that most patients had)

Answer the following questions

Classification of dosage form

16

Physical state

Route of administration

Site of application

aerosol

/ˈeərəsɒl/

• a container with a liquid that is administered in spray form

drop

/drɒp/

• a very small amount of liquid that form a round shape

inhaler

/ɪnˈheɪlə(r)/

• a small device with medicine to breathe in through the mouth

liniment

/ˈlɪnəmənt/

• an oily liquid to rub

on painful body parts

to reduce pain

ointment

/ˈɔɪntmənt/

• a smooth, thick substance to rub on the skin for healing

patch

/pætʃ/ • a medication on material or cloth placed on the skin

pill

/pɪl/ • a small, round piece of medicine to be swallowed without chewing

syrup

/ˈsɪrəp/

• a sweet, liquid medicine taken with a spoon or cup

Fill in the gaps in the following sentences with the words from

the box

dosage – drops – patch – pills – suppository – syrup – tablets

1 Calculating the correct ……… for some patients isn’t always easy

2 Children and older people often have trouble swallowing lagre ……… or

………

3 Wearing a ……… may create problems for people with skin allergies

4 Some medications are available in liquid form, such as ……… or ………

5 We often use a ……… to administer medication to babies or other patients who are

not able to take drugs orally

NCE – New chemical entity

NCE is a molecule developed by the innovator company in the early drug discovery stage, which after undergoing clinical trials could translate into a drug that could be a treatment for some disease

Drug discovery and development:

questions often asked

What kind of formulation could we

develop?

What is the toxicity of this NCE?

What about using other forms? What about the bioavailability of this

NCE?

Are tablets, capsules, or drops possible? When can we start the first in-man study?

What about the dosage for these forms? Do we have the technology to make

patches?

Listen to the conversation about an R & D meeting

What participants query about the new chemical substance?

kind of formulation that could be developed from the NCE?

the bioavailability of the NCE?

the toxicity of the substance?

kind of time frame for the first in-man study?

could the new dosage form be made with current technology?

Opinions: asking and giving

Asking for opinions What do you think ….?

What’s your opinion on …?

What’s your view of …?

Avoiding/Withholding opinions I would rather not say …

I’m sorry I cannot comment on … I’m affaid I’m not in the position to answer that

Giving opinions I think/feel …

In my opinion, … From my point of view, …

Giving strong opinions I firmly believe …

I feel very strongly that … I’m sure/certain/convinced …

Give examples of asking and giving opinions

Put one of the vocabulary items from the box into the

sentences below

chemist – dosage form – formulation – in-man study – prescription - toxicology

1 A specialist or expert in the scientific field of chemistry is called a ………

2 Using the right ……… …… is especially important when giving medicine to

children, because they often have problems swallowing pills

3 The science of poisons, including their source, chemical composition, action, tests,

and even their antidotes, is what we call ………

chemist

dosage form

toxicology

Put one of the vocabulary items from the box into the

sentences below

4 If a drug or medicine is not available ‘over-the-counter’, it is normally means that

a ……… from a physician is needed to obtain it from a pharmacy

5 Chemists and pharmacologists are also interested in how the medicine is

administered, so they often ask about its ………

6 Before drugs or medicines can be made available to the public, they have to be

tested on human beings We call this an ………

Read the answers below and write your own version of the questions (You may consult the conversation of the R & D meeting or the questions often asked about the topic of drug

discovery and development)

1 ………

It is already available in lozenge and chewing gum form, but we hope to develop a time-release patch in the near future

2 ………

We will have to test the bioavailability to be able to calculate dosages for

non-intravenous routes of drug administration for this NCE

What kind of fomulation could we develop from this NCE

What is the bioavailability of this NCE

Is there some information available on the toxicity of the substance

Are we in the position to make this new dosage form with our current

technology

What kind of time frame are we talking about for the first in-man study

Listen to the conversation between Janet, a chemist, and Brian, a pharmacologist about the brainstorming meeting

Decide if the statements are true (T) or false (F)?

1 The side-effects research for the product is not finished yet

2 There are other dosage forms which work better than the patch form

3 It will only take a few months to further develop the patch form

4 Cream, ointment, and suppository forms would also be possible for this

Talking about time periods

a bit more time We’ll need a bit more time

still running We are still running tests to find out what kinds of side effects are possible

in about (+ time period) We should be able to come up with an answer in about four weeks

from … to … Developing a patch would take anything from six months to a couple of years

We don’t have the technology perfected yet

Read the article about different classes of drugs

What are the advantages of providing drugs and medications by presciption, BTC and

OTC?

How are drugs and medications made available in your country?

Should patients have the right to obtain drugs and medications online from other countries?