İon Exchange in Pharmaceutical

7/31/2019 on Exchange in Pharmaceutical

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Ion Exchange in

Pharmaceutical Industry

Prepared by ; Mine KK - 05070008943

Submitted to : Prof.Dr. Nalan KABAY

Ege University / Chemical Engineering

Department

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Contents

General properties of ion exchange resins in

Pharmaceutical Industry ,

Usage area in Pharmaceutical Industry.

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Ion exchange resins are cross-linked, waterinsoluble, polymer-carrying,ionizable functional

groups.[1]

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Ion exchange resins have been used for many

years inpharmaceutical formulations. Their uses

have large range .[2]

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Properties of pharmaceutical grade ion exchange [2]

fine , free-flowing powders,

particle size of 25-150 microns,

contain functional groups capable of exchanging

ions and/or ionic groups,

insoluble in all solvents , all pH levels,

not adsorbed by the body, do not have a defined moleculer weight,

be non-toxic and very safe.

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It is important to

recognize that this is areversible reaction, the

equlibrium position of

which will depend on the

environment n which thedrug and ion exchange

resin are found.[2]

Drugs can be loaded onto the resins by an exchanging

reaction , and hence, a drug-resin complex (drug resinate) is

formed.[1]Following figure shows are the equlibrium reactionbetween an anion exchange resin and drug molecule.[3]


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Factors controlling the equlibrium

constant include the following[2] ;

Moleculer weight,

pKa of drug and resin, Solvent,

Solubility,

Temperature,

Hydrophobicity

Concentration ofcompeting ions

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Physical Properties of Resinates ;

o fine, free- flowing powders,

o particle size similar to the starting polymer,

o contain the active pharmaceutical ingredient

in salt form,

o do not have a melting point.

The loaded resin is often reffered to as a resinate . The

typical properties of resinates are shown in following . The properties

are very similar to those the original ion exchange resin.[2]


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The performance of resinate is governed by several factors

such as[3];o pH and temperature of drug solution,

o Molecular weight and charge ,intensity of the drug and ionexchange resin,

o Geometry,

o Mixing speed,o Ionic strength of the drug solution,

o Degree of cross linking and particle size of the ionexchange resin,

o The nature of the solvent,

o Contact time between the drug species and the ionexchange resin.


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Ion exchange resins are used in the

pharmaceuticals, not only for catalyzing certain reactions

but also for isolating and purifying pharmaceutical active

ingredients.

Three ion exchange resins are used as active ingredients ;

o Polystyrene sulfonate

o Colestipol

o

Cholestramine [4]

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Polystyrene Sulfonate ; is strongly acidicion exchange resin and is used to treat

hyperkalemia.[4]The kidneys continuously remove potassium .When kidney function is failing, it may benecessary to remove potassium from the intestinaltract by artificial means. This can be achieved byusing Polystyrene Sulphonates, in either the sodium

or calcium form.As the resins pass through theintestinal tract they exchange the sodium orcalcium on the resin for potassium. The adsorbedpotassium cannot pass into the blood and continuesthrough the body without being released .Introduced into clinical use in the early 1950s,

such resins are now widely used in the treatment ofacute and chronic hyperkalaemia, in addition tocontrolling serum potassium levels in patientsundergoing renal dialysis.[5]

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Polystyrene Sulphonates inSodium Form


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Cholestyramine ; is a strongly basic ionexchange resin and is used to treat

hypercholesterolemia.

Cholestyramine is a bile acid sequestransts, which

binds bile in the gastrointestinal to prevent its

reabsorption. It is a strongion exchange resin, which

means that it can exchange its chloride anions with

anionic bile acids in the gastrointestinal tract and bind

them strongly in the resin matrix. The functional

group of the anion exchange resin is a quaternary

ammonium group attached to an inert styrene-

divinylbenzene copolymer.

Cholestyramine removes bile acids from the

body by forming insoluble complexes with bile acids

in the intestine, which are then excreted in the feces.

When bile acids are excreted, plasma cholesterol is

converted to bile acid to normalize bile acid levels.

This conversion of cholesterol into bile acids lowers

plasma cholesterol concentrations.[4]

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Colestipol ; is a weakly basic ionexchange resin and is also used to treathypercholesterolemia.

Colestipol is a vile acidsequestransts used to lowerblood cholestrol, specifically low

density lipoprotein (LDL).Likecholestyramine, colestipol works in thegut by trapping bile acids andpreventing them from being reabsorbed.This leads to decreased enterohepaticrecirculation of bile acids, increased

synthesis of new bile acids by the liverfrom cholesterol, decreased livercholesterol, increased LDLreceptor expression, and decreasingLDL in blood.[4]

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Ion exchange resins are also used as excipients

in pharmaceutical formulations such as tablets, capsules

and suspensions. In these uses the ion exchange resin

can have several different functions[4] ;

Taste masking

Sustained and controlled release

Tablet disintegration

Improving the chemical stability of the activeingredients.

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Taste Masking ;The scope of Ion exchange resins for masking the undesirabletaste of pharmaceuticals is unlimited.Since the drug resin

complex is insoluble, it has virtually no taste, so that even bitterdrugs lose their taste when converted into a drug resinate withproper selection of ion exchange resins. The drug resinate can

be made sufficiently stable so that it does not break down in themouth and so that the patient does not taste the drug when it isswallowed. However, when the drug resinates come in contactwith gastrointestinal fluid, usually the acid of the stomach, thecomplex is broken down quickly and completely.[3]

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Sustained and controlled release;

Sustained release formulations ensure that drug is releasedcontinuously into the body at a slower, but steady rate. The

release of drugs from ion exchange resins depends upon a

aeries of ionic reactions between various body fluids and the

drug-resin complex. The rate of release of drug can be

controled by varying the particle size, degree of crosslinkingand the chemistry of resin. The release profile can almost be

tailor made to suit a particular application.[6]

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Tablet Disintegrat ;Ion exchange resins, because of their excellent swelling

property when immersed in water, can be used as a tablet

disintegrating agent. [7]

Resins although insoluble, have great affinity for water andhence, act as disintegrant.[1]

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The rate of permeation of water and subsequent swelling is

very fast and cuts down the disintegrating time.

Ion exchange resins do not have adhesive tendency onhydration ; hence tablets disintegrate evenly without lumps.

Ion exchange resin is effective in low concentration as a

disintegrant.

After incorporation of ion exchange resins, the hardness of

the tablets increases. [3]

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The advantages of ion exchange resins overconventional disintegratiing agents include :


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Drug stabilization ;

The drug resinate is frequently more stable than the

original drug. Vitamin B12 has a shelf-life of only a few

months, but the resinate is stable for more than two years.

Another example is nicotine; it discolors quickly on exposure to

air and light, but the resinate, used in nicotine chewing gums

and lozenges, is much more stable. [7]

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I try to explain ;

Generally properties of resin and resinate ,

Usage area of Pharmaceutical ion exchange

resins.

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I hope it is clear and concise !


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REFERENCES

1. Mahore J. G, Wadher K. J. ,Umerkar M. J, Bhoyar P.K., IONEXCHANGE RESINS: PHARMACEUTICAL APPLICATIONS ANDRECENT ADVANCEMENT , Volume 1 ,Issue 2 ,March-April 2010 ,Article 002

2. Dr. L. HUGHES ,New Uses of Ion Exchange Resins in PharmaceuticalFormulation , Rohm and Haas Research LaboratoriesSpring House

3. Sunil K. Bajpai , Manjula Bajpai , Sutanjay Saxena , Ion Exchange andSolvent Extraction,,A series Advances,Volume 16,Ion Exchange Resins inDrug Delivery ,2007

4. http://en.wikipedia.org/wiki/Ion-exchange_resin#Pharmaceuticals (lastupdate : 25.04.2012)

5. http://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhpr

oducts9_10_08.pdf(last update :02.05.2012)6. http://www.thermax-usa.com/tulsion/pharmaceutical-applications-

#startOfPageId51(last update : 25.04.2012 )

7. http://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdf

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http://en.wikipedia.org/wiki/Ion-exchange_resinhttp://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhproducts9_10_08.pdfhttp://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhproducts9_10_08.pdfhttp://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdfhttp://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdfhttp://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdfhttp://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdfhttp://fabad.org/fabad.org/pdf/volum32/issue2/91-100.pdfhttp://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.thermax-usa.com/tulsion/pharmaceutical-applications-http://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhproducts9_10_08.pdfhttp://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhproducts9_10_08.pdfhttp://www.purolite.com/customized/uploads/pdfs/AppGuide_ActivePhproducts9_10_08.pdfhttp://en.wikipedia.org/wiki/Ion-exchange_resinhttp://en.wikipedia.org/wiki/Ion-exchange_resinhttp://en.wikipedia.org/wiki/Ion-exchange_resin


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İon Exchange in Pharmaceutical