2. CONTENTS
Introduction
History
Structure of Carvedilol
Properties of Carvedilol
Uses of Carvedilol
How its‟s works ??
Why Carvedilol is preferred ??
Common Side Effects
Manufacturing Process
SHE Considerations
Price aspect
Market Demand Vs. Supply
3. INTRODUCTION
Carvedilol also known as Coreg
Used commonly in the treatment of CHF
or Congestive Heart failure or high blood
pressure
Carvedilol is a nonselective beta
blocker/alpha-1 blocker indicated in the
treatment of mild to severe congestive
heart failure (CHF)
4. HISTORY
Carvedilol was discovered by Robert R.
Ruffolo
The discovery and development of
carvedilol encountered an adverse
regulatory climate, skepticism by the
cardiology community and hesitance by
the company, and in the early 1990s
The fate of the drug was uncertain
5. Robert R Ruffolo was President of Research and
Development for Wyeth Pharmaceuticals, and
corporate Senior Vice President of Wyeth from 2001
to 2008
Robert R Ruffolo
7. The trade name of Carvedilol is known as Coreg
This tablet is oval in shape and white colored
It contains differing concentrations
of Carvedilol namely in 3.125, 6.25, 12.5 and 25 m
dosages.
Molecular Formula: C 24 H 26 N 2 O 4
Carvedilol in tablet form
8. PROPERTIES OF “CARVEDILOL”
These active pharmaceutical ingredients can
be dissolved in water, intestinal fluids or
gastric fluids
Carvedilol should be taken with food
9. USES OF “CARVEDILOL”
Carvedilol is used for treating high blood
pressure and congestive heart failure.
It is also used after a heart attack to improve
the chance of survival if your heart is not
pumping well
To treat a certain type of irregular heartbeat
Carvedilol also helps to relax blood
vessels, reduces the need for oxygen in the
body, and helping the heart beat more
regularly and efficiently
10. HOW IT WORKS ??
Most norepinephrine reactants will activate
nerve endings, which control heart muscle
movements
Carvedilol drug works by blocking the binding
of the norepinephrine to these receptors
This way, the heart rhythm slows down and
the pumping force of the heart muscles is also
reduced
11. WHY “CARVEDILOL” IS PREFERRED??
Carvedilol does not worsen existing heart
failure symptoms like some other drugs do
Compared to other drugs, which work in a
similar fashion, Carvedilol does not have
much inotropic effects or inverse agonist
effects
However, there is no scientific evidence to
support the fact that Carvedilol is more
preferred compared to other beta blocking
drugs
12. COMMON SIDE EFFECTS:
The most common side effects include:
Dizziness
Fatigue
Hypotension
Diarrhea
Weight gain
13. SIDE EFFECTS IF YOU DISCONTINUE THE
CONSUMPTION OF „CARVEDILOL‟
Sharp chest pain
Irregular heartbeat
Sometimes heart attack
14. MANUFACTURING PROCESS OF
“CARVEDILOL”
The manufacture of products based on small molecule Active Pharmaceutical Ingredients
(API) remains critical to global healthcare
The manufacturing landscape is also full of
challenges and opportunities
This is due to emerging international markets
and rapidly evolving
social, economic, regulatory and
environmental expectations
15. SIFTING
Sift Carvedilol through , Lactose
monohydrate and Ferric Oxide
through the above sifted Carvedilol
and Lactose monohydrate it is
sifted with Ferric Oxide through
Lactose monohydrate and
Microcrystalline Cellulose.
16. DRY MIXING
Load the above sifted material in Rapid mixer
granulator and mix for 10 minutes with
impeller slow speed.
GRANULATING
Add binder solution over dry mix material in a
period of 10 minutes at impeller slow speed
and mix the content in Rapid Mixer Granulator
at impeller slow speed.
17. DRYING
Air dry the wet mass for 10 minutes and
dry at inlet temperature to reach NMT
80°C, dry the granules till loss on drying
reaches to not more than 105°C.
18. SIFTING AND MILLING
Sift the dried granules and mill
retentions through multimill using 1mm
screen at medium speed and knives
forward configuration. Sifting of extra
granular Materials; Sift Silica Colloidal
Anhydrous and Magnesium Stearate.
19. BLENDING AND LUBRICATION
Mix the materials of dried granules with Silica
Colloidal Anhydrous in Octagonal Blender for
15 minutes. Add Magnesium Stearate to the
above materials in Octagonal Blender for 5
minutes.
23. SAFETY CONSIDERATION
Reduce direct skin contact, reduce exposure via
inhalation; and minimize the possibility of chemicals
being brought home on workers‟ clothing
As with all potentially hazardous
exposures, protective measures should include:
engineering controls (e.g., barriers and
containments, laboratory hoods, glove boxes, and
worker isolation);
Administrative controls; personal protective
equipment (e.g., respirators, gloves and lab coats)
Training
24. HEALTH CONSIDERATION
Hazardous exposure to workers may occur
through inhalation of dust created during:
hand manipulation
operation of a tablet encapsulation machine
by performing sieving and granulation
operations
25. PRICE ASPECT OF THIS PROCESS
Chronic heart failure (CHF) is now recognized as a
major and escalating public health problem.
The costs of this syndrome, both in economic and
personal terms, are considerable.
The prevalence of CHF is 1–2% and appears to be
increasing, in part because of ageing of the
population.
60 tablets of carvedilol of 25mg would be $4.00
26. MARKET DEMAND VS. SUPPLY
Manufacture and market Carvedilol Tablets, 3.125
mg, 6.25 mg, 12.5, and 25 mg. The Office of Generic
Drugs, U.S. Food and Drug Administration, has
determined the Ranbaxy formulations to be
bioequivalent and have the same therapeutic effect
as that of the reference listed drug Coreg®
Tablets, 3.125 mg, 6.25 mg, 12.5 mg, and 25
mg, respectively.
Total annual market sales for Carvedilol Tablets were
$1.6 billion (IMS – MAT: June 2007).
