api ingredients

VINOTHARAN NAIR(1000024)SANGIDHA JAGATHEESAN(1000013)

ACTIVE PHARMACEUTICAL

INGREDIENTS“CARVEDILOL”

IntroductionHistoryStructure of CarvedilolProperties of CarvedilolUses of CarvedilolHow its’s works ??Why Carvedilol is preferred ??Common Side EffectsManufacturing ProcessSHE ConsiderationsPrice aspectMarket Demand Vs. Supply

CONTENTS

Carvedilol also known as CoregUsed 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)

INTRODUCTION

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

HISTORY

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

STRUCTURE OF “CARVEDILOL”

3D view2D view

The trade name of Carvedilol is known as Coreg

This tablet is oval in shape and white coloredIt contains differing concentrations

of Carvedilol namely in 3.125, 6.25, 12.5 and 25 m dosages.

Molecular Formula: C24H26N2O4 

Carvedilol in tablet form

These active pharmaceutical ingredients can be dissolved in water, intestinal fluids or gastric fluids

Carvedilol should be taken with food

PROPERTIES 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 effi ciently

USES OF “CARVEDILOL”

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

HOW IT WORKS ??

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

WHY “CARVEDILOL” IS PREFERRED??

The most common side effects include:DizzinessFatigueHypotensionDiarrheaWeight gain

COMMON SIDE EFFECTS:

Sharp chest painIrregular heartbeatSometimes heart attack

SIDE EFFECTS IF YOU DISCONTINUE THE CONSUMPTION 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

MANUFACTURING PROCESS OF “CARVEDILOL”

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.

SIFTING

Load the above sifted material in Rapid mixer granulator and mix for 10 minutes with impeller slow speed.

DRY MIXING

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.

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.

DRYING

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.

SIFTING AND MILLING

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.

BLENDING AND LUBRICATION

THE PROCESS

FLOWCHART

RAPID MIXER GRANULATOR

SHE 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

SAFETY CONSIDERATION

Hazardous exposure to workers may occur through inhalation of dust created during:hand manipulationoperation of a tablet encapsulation

machineby performing sieving and granulation

operations

HEALTH CONSIDERATION

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

PRICE ASPECT OF THIS PROCESS

Manufacture and market Carvedilol Tablets, 3.125 mg, 6.25 mg, 12.5, and 25 mg. The Offi ce 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).

MARKET DEMAND VS. SUPPLY

THANK YOU

http://eurjhf.oxfordjournals.org/content/3/3/283.fullhttp://www.goodrx.com/coreg/pricehttp://www.aafp.org/afp/1998/1101/p1627.htmlhttp://

www.ranbaxy.com/ranbaxy-gains-us-fda-approval-to-manufacture-and-market-carvedilol-tablets-in-the-us-market

http://en.wikipedia.org/wiki/Norepinephrine/

REFERENCES