SKP SKP PharmaPharmaNigeria LimitedNigeria Limited

TO BE DELIVERED BYTO BE DELIVERED BY

OKE, MUSHAFAU OKE, MUSHAFAU ADEBAYOADEBAYO

WELCOMES YOU TO THIS CLINICAL PRESENTATION

SCIENCE OF SCIENCE OF CHELATIONCHELATION

ADVANCE IN DRUG DELIVERY

DRUG DELIVERYDRUG DELIVERY

Drug deliveryDrug delivery is is the method or the method or process of process of administering a administering a pharmaceuticalpharmaceutical compound to compound to achieve a achieve a therapeutic effecttherapeutic effect in in humanshumans or or animalsanimals. .

DRUG DELIVERYDRUG DELIVERY

Drug delivery technologies are Drug delivery technologies are patent protected formulation patent protected formulation technologies that modifytechnologies that modify drug release profile drug release profile absorption, distribution and elimination absorption, distribution and elimination

for the benefit of improvingfor the benefit of improving product efficacy and safety, product efficacy and safety, as well as patient convenience and as well as patient convenience and

compliance. compliance.

ESSENCE OF DRUG ESSENCE OF DRUG DELIVERYDELIVERY

How much How much vitamin/mineral did you vitamin/mineral did you take? take?

How much did your body How much did your body absorb? absorb?

Efficient mineral/drug Efficient mineral/drug delivery is not about delivery is not about how much of a how much of a mineral/drug you take, mineral/drug you take, it’s a question of how it’s a question of how much your body absorbs. much your body absorbs.

PROBLEMS ASSOCIATED PROBLEMS ASSOCIATED WITH INORGANIC MINERALS WITH INORGANIC MINERALS

INTAKEINTAKE1.1. Low bioavailability:- Low bioavailability:- The effective absorption of inorganic minerals is The effective absorption of inorganic minerals is

generally less than 10% (Fouad, 1976). generally less than 10% (Fouad, 1976). For a mineral to be absorbed in the small intestine, it For a mineral to be absorbed in the small intestine, it

has to be soluble in the luminal fluid of the small has to be soluble in the luminal fluid of the small intestine and present itself as a singular molecule or an intestine and present itself as a singular molecule or an ionic entity. ionic entity.

Most inorganic metals ions are soluble in an acidic Most inorganic metals ions are soluble in an acidic medium but not in a medium with a pH value greater medium but not in a medium with a pH value greater than 7.0. than 7.0.

Therefore, at the pH of the small intestinal fluid below Therefore, at the pH of the small intestinal fluid below the duodenum which is in the range of 7.0-7.2, the the duodenum which is in the range of 7.0-7.2, the minerals tend to form insoluble hydroxides, a gelatinous minerals tend to form insoluble hydroxides, a gelatinous magma type of precipitation, thereby rendering the magma type of precipitation, thereby rendering the metals non-absorbable (Fang metals non-absorbable (Fang et. al., 1982et. al., 1982))..

PROBLEMS ASSOCIATED PROBLEMS ASSOCIATED WITH INORGANIC MINERALS WITH INORGANIC MINERALS

INTAKEINTAKE2.2. Gastrointestinal disturbances such as Gastrointestinal disturbances such as

constipation and diarrhea. constipation and diarrhea.

3.3. Malabsorption of other nutrients due to the Malabsorption of other nutrients due to the coating of magma on the mucous membrane coating of magma on the mucous membrane of the small intestine. of the small intestine.

4.4. Formation of insoluble complexes with Formation of insoluble complexes with various substances present in foodstuffs various substances present in foodstuffs such as carbonates, phytates, phosphates, such as carbonates, phytates, phosphates, and oxalates. and oxalates.

5.5. Decrease vitamin bioavailabilty and stability.Decrease vitamin bioavailabilty and stability.

WAY FORWARDWAY FORWARD One way to circumvent or prevent the One way to circumvent or prevent the

problems associated with the oral problems associated with the oral administration of inorganic minerals is administration of inorganic minerals is to use to use metal chelates metal chelates oror organic organic minerals.minerals.

A well-prepared metal chelate would A well-prepared metal chelate would resist the attack of anions such as resist the attack of anions such as hydroxides, phosphates, carbonates, hydroxides, phosphates, carbonates, oxalates or phytates, thus keeping the oxalates or phytates, thus keeping the minerals in a soluble and readily minerals in a soluble and readily absorbable form in the small intestine. absorbable form in the small intestine.

WAY FORWARDWAY FORWARD Organic minerals:- e.g. metal proteinates, Organic minerals:- e.g. metal proteinates,

sequestered minerals, EDTA chelates and sequestered minerals, EDTA chelates and methionine complexes. These forms of methionine complexes. These forms of organic minerals contain less mineral organic minerals contain less mineral potency than inorganics, and are more potency than inorganics, and are more expensive per unit of elemental mineral. expensive per unit of elemental mineral. Some organic minerals are complexed by Some organic minerals are complexed by such strong bonds that they cannot be such strong bonds that they cannot be broken by the animal’s enzymes. Other broken by the animal’s enzymes. Other bonds are so weak that they dissociate bonds are so weak that they dissociate prior to absorption.prior to absorption.

CHELATION AND CHELATION AND CHELATESCHELATES

Chelation in simple terms is the process of Chelation in simple terms is the process of attaching a central metal atom to a large molecule, attaching a central metal atom to a large molecule, called a ligand in a cyclic or ring structure through called a ligand in a cyclic or ring structure through covalent bonds. According to the American covalent bonds. According to the American Association of Feed Control Officials (AAFCO), Association of Feed Control Officials (AAFCO),

“ “Metal proteinate is defined as the product Metal proteinate is defined as the product resulting from the chelation of a soluble salt with resulting from the chelation of a soluble salt with amino acid and/or partially hydrolysed protein.”amino acid and/or partially hydrolysed protein.”

““Metal Amino Acid Chelate is defined as the Metal Amino Acid Chelate is defined as the product resulting from the reaction of a metal ion product resulting from the reaction of a metal ion from a soluble metal salt with amino acids with a from a soluble metal salt with amino acids with a mole ratio of one metal to one to three moles of mole ratio of one metal to one to three moles of amino acids to form coordinate covalent bonds.” amino acids to form coordinate covalent bonds.” (AAFCO, 1987)(AAFCO, 1987)

Amino Acid Chelated Amino Acid Chelated MineralMineral

DEFICIENCIES OF DEFICIENCIES OF POPULAR METAL POPULAR METAL

CHELATESCHELATES Several metal chelates are presently in Several metal chelates are presently in

the market; however many of the so-the market; however many of the so-called “metal chelates” are found to be called “metal chelates” are found to be simple physical mixtures of inorganic simple physical mixtures of inorganic metal salts with ligands such as amino metal salts with ligands such as amino acids, hydrolysed proteins, acids, hydrolysed proteins, monosaccharides, polysaccharides or monosaccharides, polysaccharides or other organic compounds. Most of these other organic compounds. Most of these metal preparations are physical mixtures metal preparations are physical mixtures or weak chelates at best and have dubious or weak chelates at best and have dubious advantages over the inorganic metal salts. advantages over the inorganic metal salts.

ADVANTAGES OF AMINO ADVANTAGES OF AMINO ACID CHELATESACID CHELATES

Increased mineral bioavailability: - they are Increased mineral bioavailability: - they are able to resist the attack of anions thus able to resist the attack of anions thus keeping the mineral in a soluble and readily keeping the mineral in a soluble and readily absorbable form in the small intestine.absorbable form in the small intestine.

Decreased gastrointestinal tract side effects.Decreased gastrointestinal tract side effects. Increased bioavailablility of vitamins due to Increased bioavailablility of vitamins due to

decreased mineral adsorption with vitamins. decreased mineral adsorption with vitamins. Increase vitamin’s antioxidant effect:- by Increase vitamin’s antioxidant effect:- by

decreasing vitamin’s oxidation by minerals. decreasing vitamin’s oxidation by minerals.

ADVANTAGES OF AMINO ADVANTAGES OF AMINO ACID CHELATESACID CHELATES

All trace minerals in the body are All trace minerals in the body are transported by either protein transported by either protein polypeptides or amino acid carrier polypeptides or amino acid carrier systems. systems.

Chelates have ability to cross placental Chelates have ability to cross placental barriers to feed the foetus (Jensen, N., barriers to feed the foetus (Jensen, N., 1979).1979).

At pH 7.5-10.0, amino acid chelates have At pH 7.5-10.0, amino acid chelates have higher stability constant and biological higher stability constant and biological life: - the charts below show the life: - the charts below show the comparison of our amino acid chelates for comparison of our amino acid chelates for Cu and Fe with the inorganic sulphates. Cu and Fe with the inorganic sulphates.

ADVANTAGES OF AMINO ADVANTAGES OF AMINO ACID CHELATESACID CHELATES

In a study conducted by Fang In a study conducted by Fang et. alet. al..(1982) and Scholmerich (1982) and Scholmerich et. alet. al.(1987) .(1987) on man and rats, the amino acid on man and rats, the amino acid chelate, zinc-histidine was absorbed chelate, zinc-histidine was absorbed three times greater than zinc sulphate. three times greater than zinc sulphate.

In another study, the inorganic CuSO4 In another study, the inorganic CuSO4 and FeSO4 both precipitate out at and FeSO4 both precipitate out at about pH 6, which is below the normal about pH 6, which is below the normal physiological pH of the small intestine physiological pH of the small intestine of pH 7.2. of pH 7.2.

ADVANTAGES OF AMINO ADVANTAGES OF AMINO ACID CHELATESACID CHELATES

This indicates that a large portion of This indicates that a large portion of most inorganic metal salts will most inorganic metal salts will precipitate out in the small intestine and precipitate out in the small intestine and become non-absorbable.become non-absorbable.

This explains why the bioavailabilities of This explains why the bioavailabilities of some of these inorganic minerals are less some of these inorganic minerals are less than 10% after the oral administration. than 10% after the oral administration.

Some people advocate compensation by Some people advocate compensation by using an excess amount of the inorganic using an excess amount of the inorganic salts because of their inexpensive costs. salts because of their inexpensive costs. This however, greatly enhances the This however, greatly enhances the potential side effects.potential side effects.

AMINO ACID CHELATESAMINO ACID CHELATES

AMINO ACID CHELATESAMINO ACID CHELATES

AMINO ACID CHELATESAMINO ACID CHELATES

AMINO ACID CHELATESAMINO ACID CHELATES

Source: AMT Labs, 2008

SKP PRODUCTS ARE SKP PRODUCTS ARE PREPARED WITH THE POWER PREPARED WITH THE POWER

OF CHELATIONOF CHELATION Our metal proteinates are advanced forms Our metal proteinates are advanced forms

of chelates with bonds between the metals of chelates with bonds between the metals and the ligands of proper strength. and the ligands of proper strength.

The resulting product is resistant to The resulting product is resistant to hydroxide ion attack- the metal will not hydroxide ion attack- the metal will not precipitate until the pH is higher than 10.5. precipitate until the pH is higher than 10.5.

Therefore, it is assured that the metals in Therefore, it is assured that the metals in our metal proteinates will remain soluble in our metal proteinates will remain soluble in the small intestine for subsequent the small intestine for subsequent absorption into the body to serve their absorption into the body to serve their intended physiological action. intended physiological action.

SKP PRODUCTS ARE SKP PRODUCTS ARE PREPARED WITH THE POWER PREPARED WITH THE POWER

OF CHELATIONOF CHELATION

Efficient mineral delivery is not Efficient mineral delivery is not about how much of a mineral you about how much of a mineral you take, it is a question of how much take, it is a question of how much your body absorbs. your body absorbs.

Amino acid chelated minerals by Amino acid chelated minerals by SKP have the highest bioavailalbility.SKP have the highest bioavailalbility.

Prof. Fang of SK Pharmaceuticals, Prof. Fang of SK Pharmaceuticals, Texas, USA owns the patent of Texas, USA owns the patent of amino acid chelated minerals.amino acid chelated minerals.

CalciferCalciferComprehensive Iron and Calcium Comprehensive Iron and Calcium

formula forformula for

Anemia and Bone healthAnemia and Bone health

CALCIFERCALCIFER HVP Chelated Calcium 20% 300 mg HVP Chelated Calcium 20% 300 mg Calcium Carbonate 270 mg Calcium Carbonate 270 mg Magnesium Oxide 100 mg Magnesium Oxide 100 mg Calcium Ascorbate 50 mg Calcium Ascorbate 50 mg HVP Chelated Iron 10% 30 mg HVP Chelated Iron 10% 30 mg Vitamin E 15 UI Vitamin E 15 UI Magnesium Stearate 9 mg Magnesium Stearate 9 mg Manganese Sulfate 5 mg Manganese Sulfate 5 mg Copper Sulfate 2.5 mg Copper Sulfate 2.5 mg Vitamin BVitamin B1212 1% 1 mg 1% 1 mg Folic Acid 10% 0.8 mg Folic Acid 10% 0.8 mg Vitamin DVitamin D3 3 10 mcg 10 mcg Silicon Dioxide 10 mg Silicon Dioxide 10 mg

Active Ingredients

CALCIFERCALCIFER

Comprehensive formula for both AComprehensive formula for both Anemianemia and and Bone Health. Bone Health.

Support iron and calcium in one capsule.Support iron and calcium in one capsule. Provides 100% of amino acid chelated iron, Provides 100% of amino acid chelated iron,

calcium and other minerals with hcalcium and other minerals with higher igher bioavailability than inorganic minerals. bioavailability than inorganic minerals.

100% soluble iron and calcium in the small 100% soluble iron and calcium in the small intestine, ready to be absorbed.intestine, ready to be absorbed.

No Side Effects Commonly Seen in Other No Side Effects Commonly Seen in Other Products.Products.

Protect Vitamins from Being Destroyed.Protect Vitamins from Being Destroyed.

Key Features

CALCIFERCALCIFERSuggested usersSuggested users Teenage girlsTeenage girls Adult women at childbearing ageAdult women at childbearing age Pregnant womenPregnant women Women and men with anaemia Women and men with anaemia

DirectionsDirections Take 1 to 2 capsules once a day.Take 1 to 2 capsules once a day.

CALCIFERCALCIFER Economic/Market AdvantageEconomic/Market Advantage

Combines all the minerals needed by Combines all the minerals needed by pregnant women and anaemics into a pregnant women and anaemics into a single dose.single dose.

Takes care of blood and bone at the same Takes care of blood and bone at the same time.time.

Most affordable in that category.Most affordable in that category. Easy compliance due to convenient Easy compliance due to convenient

dosage.dosage. American product at an affordable price.American product at an affordable price.

OsteoforteOsteoforteSupport healthy Support healthy

bones bones

from 9 to 90from 9 to 90

OSTEOFORTEOSTEOFORTE

Vitamin D3 40 IU Vitamin D3 40 IU

Calcium (amino acid chelate) 154.6 mg Calcium (amino acid chelate) 154.6 mg Phosphorus 18.9 mg Phosphorus 18.9 mg

Magnesium (amino acid chelate) 6.8 mg Magnesium (amino acid chelate) 6.8 mg

Manganese (amino acid chelate) 2.0 mg Manganese (amino acid chelate) 2.0 mg

Copper (amino acid chlate) 0.2 mg Copper (amino acid chlate) 0.2 mg

22% 22% Zinc (oxide) 8.0 mg Zinc (oxide) 8.0 mg

84% 84%

Active Ingredients

OSTEOFORTEOSTEOFORTE

Comprehensive formula for supporting Comprehensive formula for supporting bone health bone health

Amino Acid Chelated calcium, Amino Acid Chelated calcium, magnesium, manganese, and copper with magnesium, manganese, and copper with hhigher bioavailability than inorganic igher bioavailability than inorganic minerals minerals

Vitamin D3 – maintain serum calcium and Vitamin D3 – maintain serum calcium and phosphorus concentration, reduce bone phosphorus concentration, reduce bone fracturefracture

No Side Effects Commonly Seen in Other No Side Effects Commonly Seen in Other ProductsProducts

Protect Vitamins from Being DestroyedProtect Vitamins from Being Destroyed

Key Features

OSTEOFORTEOSTEOFORTE

Suggested usersSuggested users Children (above 5)Children (above 5) Teenage boys and girls Teenage boys and girls Adult, men and womenAdult, men and women SeniorsSeniors Lactose intolerance Lactose intolerance VegetariansVegetarians Osteoporosis Osteoporosis Directions Directions Take 1 to 2 capsules once a day.Take 1 to 2 capsules once a day.

OSTEOFORTEOSTEOFORTE

Economic/Market AdvantageEconomic/Market Advantage Takes care of bone faster than Takes care of bone faster than

inorganic preparations.inorganic preparations. Most affordable in that category.Most affordable in that category. Easy compliance due to convenient Easy compliance due to convenient

dosage.dosage. American product at an affordable American product at an affordable

price.price.

Glucotin DSGlucotin DSThe leading choice of The leading choice of

nutritional support for nutritional support for joint structure and joint structure and

functionfunction

GLUCOTIN DSGLUCOTIN DS

Glucosamine sulphate Glucosamine sulphate 375mg 375mg

Chondroitin sulphate Chondroitin sulphate 100mg 100mg

Vit D3 Vit D3 4mg (40 I.U.)4mg (40 I.U.)

Amino acid chelated calcium Amino acid chelated calcium 300mg 300mg

Active Ingredients

Directions

Take one capsule by mouth 1-2 times a day with a meal

GLUCOTIN DSGLUCOTIN DS Glucosamine Glucosamine

Helps maintain healthy joints and Helps maintain healthy joints and reduce cartilage wear.reduce cartilage wear.

Chondroitin Chondroitin

Play an important role in the Play an important role in the lubrication and nutrition of the joint. lubrication and nutrition of the joint. Vital for structure and function of Vital for structure and function of cartilagecartilage

GLUCOTIN DSGLUCOTIN DS Glucosamine and Chondroitin are two Glucosamine and Chondroitin are two

molecules that make up the type of cartilage molecules that make up the type of cartilage found within joint. Inside the joint, cartilage found within joint. Inside the joint, cartilage undergoes a constant process of breakdown undergoes a constant process of breakdown and repair. However to be properly repaired, and repair. However to be properly repaired, the building blocks of cartilage must be the building blocks of cartilage must be present and available. The theory behind present and available. The theory behind using the Glucosamine and Chondroitin joint using the Glucosamine and Chondroitin joint supplements is that more of the cartilage supplements is that more of the cartilage building blocks will be available for cartilage building blocks will be available for cartilage repair.repair.

How Glucosamine and How Glucosamine and Chondroitin WorkChondroitin Work

For over two decades Glucosamine and For over two decades Glucosamine and Chondroitin have been widely used in the Chondroitin have been widely used in the treatment of Osteoarthritis, which is a treatment of Osteoarthritis, which is a condition that causes problems of wearing out condition that causes problems of wearing out of the normal smooth cartilage surface of the of the normal smooth cartilage surface of the joints. Often called wear-and-tear arthritis, joints. Often called wear-and-tear arthritis, including joint pain, swelling and deformity.including joint pain, swelling and deformity.

Clinical studies indicated that Glucosamine Clinical studies indicated that Glucosamine and Chondroitin substantially reduce joint and Chondroitin substantially reduce joint pain inflamation without NSAIDS which might pain inflamation without NSAIDS which might cause serious side effects such as G.I. cause serious side effects such as G.I. complaints and bleeding. complaints and bleeding.

REFERENCES REFERENCES A.A.F.C.O. 1987. “Official Publication of American A.A.F.C.O. 1987. “Official Publication of American

Association of Feed Control Officials” Section 57.23.Association of Feed Control Officials” Section 57.23. AMT Labs Inc., U.S.A. 2008.AMT Labs Inc., U.S.A. 2008. Fang, S.M., Burton, S.A. and Peterson, R.V. 1982. Fang, S.M., Burton, S.A. and Peterson, R.V. 1982.

“Bioavailability of zinc: Effect of amino acid “Bioavailability of zinc: Effect of amino acid chelation”. chelation”. Chelated Mineral Nutrition in Plants, Chelated Mineral Nutrition in Plants, Animals and Man.Animals and Man. Charles C. Thomas. Publisher, Charles C. Thomas. Publisher, Springfield, IL pp. 134-151.Springfield, IL pp. 134-151.

Fouad, M.T. 1976. “Chelation and chelated Fouad, M.T. 1976. “Chelation and chelated minerals” minerals” J. Appl. Nutr. J. Appl. Nutr. 28:6.28:6.

Jensen, N. 1979. “Amino acid chelates: their Jensen, N. 1979. “Amino acid chelates: their mechanisms of action and key aspects of mechanisms of action and key aspects of preparations” preparations” J. Appl. Nutr. J. Appl. Nutr. 31: 25-6.31: 25-6.

Thank YouThank You

for listeningfor listening